Ciprofloxacin - instructions for use. Antibiotic Ciprofloxacin: principle of action, form of release and pharmacological parameters Can ciprofloxacin be given to children

Keywords: fluoroquinolones, ciprofloxacin, newborn, quinolone arthropathy, pediatrics

Despite great progress in the development of highly effective antibacterial drugs, treatment severe forms bacterial infections, especially with the localization of the process, which is difficult for the drug, still remains one of the most difficult problems of infectious pathology. This issue is especially difficult for pediatric practice.

Not all antibacterial drugs meet the requirements necessary for pediatrics - low toxicity and good tolerability. At the same time, the lack of a therapeutic effect in the treatment of known antimicrobial agents (more often due to the problem of drug resistance) forces the pediatrician in some cases, usually for health reasons, to turn to drugs that are limited for use in children and adolescents. Therefore, a detailed study and detailed information on the toxicological properties of such drugs, the experience of their clinical use in adult patients, an analysis of the frequency and nature of possible adverse reactions, as well as a generalization of the clinical data obtained in world clinical practice when using such drugs in children are necessary. This knowledge is especially important when it comes to drugs with proven high therapeutic efficacy in adult patients, with good tolerance.

Fluoroquinolones, introduced into clinical practice in the early 1980s, are highly effective broad-spectrum antibacterial drugs with optimal pharmacokinetic properties and good tolerability in adult patients. A high degree of bioavailability allows treatment in most cases with oral administration of drugs. Currently, fluoroquinolones are considered as a serious alternative to traditional highly active broad-spectrum antibiotics.

Ciprofloxacin, synthesized in 1983 by Bayer specialists, belongs to one of the most active drugs of the fluoroquinolone group and has been used in wide clinical practice for almost 15 years, including the period of multicenter studies during clinical approbation. For wide medical use, ciprofloxacin was approved in 1987, in 1989 it was registered and approved for use in Armenia.

Ciprofloxacin acquired the greatest importance in the treatment of severe generalized forms of bacterial infections caused mainly by strains of gram-negative bacteria and staphylococci with acquired resistance to antimicrobial drugs of other groups, including strains with multiple resistance. The peculiarity of the pharmacokinetics of ciprofloxacin and good tolerance by patients, combined with high activity against aerobic pathogenic and opportunistic bacteria and a number of other microorganisms, determined wide indications for its use in adult patients. It is very important that the drug is available in dosage forms both for oral and parenteral use.

Ciprofloxacin is a fluoroquinolone with the highest activity against most aerobic gram-negative bacteria, including pathogens of severe generalized infectious processes.

Ciprofloxacin - a drug with a bactericidal type of action, is characterized (as well as other fluorinated and non-fluorinated quinolones) by a mechanism of action on a microbial cell, fundamentally different from the mechanism of action of antimicrobial agents of other chemical groups, including antibiotics. This determines the activity of ciprofloxacin against strains of bacteria resistant to other antimicrobial agents. The drug provides a long-term post-antibiotic effect, and when acting at subinhibitory concentrations, it causes a disruption in the normal function of the microbial cell. The drug is active against microorganisms, which are characterized by intracellular localization in an infected organism.

The characteristics of the antimicrobial spectrum of ciprofloxacin, its pharmacokinetic parameters in comparison with other fluoroquinolones and the scope of the drug, depending on the etiology and localization of the process in adult patients, are presented in Table. 1-3.

Table 1

In vitro activity of ciprofloxacin (range, mg/l) in comparison with other fluoroquinolones against “problematic” pathogens of pyoinflammatory processes

* For some strains 128 mg/l.

According to reviews

table 2

The degree of penetration of ciprofloxacin into body fluids, tissues and cells (% of the concentration in the blood, for cells intra/extracellular concentrations) *

*Based on reviews

Table 3

Features of the pharmacokinetics of ciprofloxacin in normal and impaired renal function in comparison with other fluoroquinolones

*Dose adjustment required; ** with liver failure - up to 352, dose adjustment is necessary. Based on reviews

One of the complex issues for clinical practice is the age restrictions on the use of ciprofloxacin and other fluoroquinolones. These limitations are based on experimental data: fluoroquinolones and non-fluorinated drugs of the quinolone class interfere with the development of cartilage tissue in the supporting joints in immature animals of some species at a certain stage of cartilage formation.

Until 1987-1988 fluoroquinolones, including ciprofloxacin, were used only in adult patients. Over the past 10 years, despite contraindications, considerable experience has been accumulated in the use of fluoroquinolones in pediatric practice, and the largest number of clinical observations (more than 2000 sick children) concerns the use of ciprofloxacin in pediatrics for health reasons. Obviously, the question of the possibility of using ciprofloxacin in children requires special discussion at the present time.

The problem of the use of fluoroquinolones in pediatrics has received much attention in the last 5 years. This is reflected in a series of individual clinical publications and summarized in a number of detailed reviews. In 1994, a special symposium was held in France on the use of both fluorinated and non-fluorinated quinolones in pediatrics.

The question of the use of ciprofloxacin and other fluoroquinolones in pediatrics involves several aspects:

• experimental data, on the basis of which restrictions were introduced on the use of fluoroquinolones in children;
• the results of the use of fluoroquinolones in pediatric practice for health reasons and the analysis of specific clinical observations in terms of effectiveness and possible adverse reactions, primarily arthrotoxicity;
• study of possible mechanisms of cartilage tissue damage under the influence of fluoroquinolones;
• validity of the existing age limits for the use of fluoroquinolones in pediatrics.

Detailed information on all these issues will allow, on the one hand, to avoid the unjustified use of ciprofloxacin in pediatric practice, on the other hand (subject to a thorough analysis of the ineffectiveness of previous therapy) - to make the right decision on the possibility of prescribing ciprofloxacin for health reasons, taking into account the sensitivity of the infectious agent to fluoroquinolones.

Ciprofloxacin is a low-toxic fluoroquinolone. In the experiment, the toxicological properties of the drug when administered orally, intravenously, intraperitoneally in acute, subacute (4 weeks) and chronic (3-6 months, 21 months and 2 years) experiments on mice, rats, rabbits, dogs and monkeys were studied in detail. dose range. In experiments on mice, rats, rabbits, the effect of ciprofloxacin on reproductive function was studied. In a long-term experiment (up to 2 years) when feeding the drug to mice and rats with food, the possibility of a carcinogenic effect of ciprofloxacin was studied. In special test systems, in cell culture, in biochemical studies, a possible mutagenic effect, effect on GABA receptors, and effect on bone marrow cells were evaluated.

It has been shown that ciprofloxacin is well tolerated by animals, including in chronic experiments when used at doses significantly higher than therapeutic doses for humans. Ciprofloxacin does not have hepatotoxic, nephrotoxic and ototoxic toxic action and does not negatively affect the hematopoietic system, does not show mutagenic activity, carcinogenic effects, does not affect reproductive function in experiments on females and males.

Based on the toxicological properties and features of the mechanism of action of fluorinated and non-fluorinated quinolones, special studies have studied in detail the effect of ciprofloxacin on the growth and development of articular cartilage tissue in immature animals, as well as the possibility of a nephrotoxic effect when using high doses of the drug, the effect of ciprofloxacin on the lens tissue, the retina of the eye and on the function of the central nervous system.

Different animal species have shown varying degrees of sensitivity and tolerance to fluorinated and non-fluorinated quinolones. The most sensitive were puppies of dogs of any breeds, which developed irreversible damage to the cartilage tissue in the supporting joints, rats were much less sensitive, then rabbits, pigs; monkeys and mice were practically insensitive.

Ciprofloxacin has a damaging effect on the development of cartilage tissue in the supporting joints in immature rats and puppies of dogs of various breeds. When the drug was administered at a daily dose of 200 mg for two weeks, all puppies aged 10-16 weeks developed cartilage lesions in the knee joints, and when administered at a dose of 100 mg/kg per day, these changes developed only in one puppy out of four. In a three-week experiment, joint damage was recorded in the dose range of 30-100 mg/kg. Immature rats were significantly less sensitive to the effect of ciprofloxacin on cartilage: only one rat out of 20 after a dose of 500 mg / kg (which is 30-35 times the daily dose for humans) showed an arthrotoxic effect, and lower doses did not cause cartilage damage at all .

Cartilage damage in experimental animals is expressed in the formation of blisters, erosions and disruption of the normal development of chondrocytes. Under the action of high doses of the drug and the development of severe lesions, the process is irreversible. In joints with a reduced load (including when applying an immobilizing bandage), changes in cartilage tissue were significantly less pronounced than in control non-immobilized joints.

In the cell culture of cartilage tissue of the mouse embryo, a slight damaging effect of ciprofloxacin was noted only when exposed to a high concentration of the drug - 100 mg/l, which significantly exceeds the therapeutic level of ciprofloxacin in the blood and tissues.

So far, the mechanisms that cause damage to cartilage tissue during a certain period of growth are not clear enough and require study. It is assumed that at certain stages of development of cartilage tissue, fluoroquinolones can inhibit the biosynthesis of mitochondrial DNA in chondrocytes, since the effect was enhanced by the combined action of quinolones on these cells in combination with DNA inhibitors. It is also suggested that fluoroquinolones can form chelate complexes with divalent zinc and magnesium ions necessary for the normal formation and development of chondrocytes.

Zinc ions, in particular, are necessary for the normal function of enzymes associated with the synthesis of peptidoglycan in the cartilage. The high sensitivity of puppy cartilage chondrocytes to the action of ciprofloxacin may be associated with the action of high concentrations of the drug, due to the very slow elimination of ciprofloxacin from tissues in this animal species: the half-life of the drug from the tissue fluid after a single administration of ciprofloxacin to dogs was, depending on the dose, 20.08 and 17.78 hours, and from the blood - 4.65 and 3.95 hours. In immature dogs, when food containing magnesium salts is excluded from the diet, the same changes in cartilage can develop as with the introduction of high doses of fluoroquinolones.

In experiments on mature animals, ciprofloxacin does not cause damage to cartilage tissue in the joints.

The question is being discussed: is cartilage damage the result of a direct effect on cartilage tissue or is it an indirect process as a result of the general toxic effect of drugs of this group.

There are no published data showing or confirming cartilage tissue damage in adult patients or in children with the use of ciprofloxacin or other fluoroquinolones. Studies conducted using nuclear magnetic resonance did not find a negative effect of ciprofloxacin on the structure of articular cartilage in adults and children with cystic fibrosis treated with ciprofloxacin for the treatment of infection of the lower respiratory tract.

It is interesting to note that non-fluorinated quinolones (Negram, Gramurin, Pallin, and others) in puppies show a higher level of arthrotoxicity than fluoroquinolones. Even before the fact of cartilage damage was established, these drugs were widely used in pediatrics, including in young children. Over a long period of time (since 1962), there have been no cases of severe, especially irreversible, damage to cartilage tissue, both during therapy and according to follow-up data.

In an experiment on rats, it was shown that with an alkaline reaction of urine, ciprofloxacin crystals may precipitate in the form of complexes with magnesium salts and protein. Ciprofloxacin crystals did not form at pH 7 and below.

In experiments on monkeys with prolonged administration (6 months) of ciprofloxacin in daily doses up to 20 mg/kg, no development of cataracts was found in animals. There was also no accumulation of ciprofloxacin in the lens tissue. In experiments on dogs and cats, the drug did not cause changes in the retina.

The experiment has shown that ciprofloxacin is an inhibitor of GABA receptors, and this effect is enhanced in the presence of non-steroidal anti-inflammatory drugs. This must be taken into account in clinical practice, especially in patients with a tendency to convulsive reactions.

Only when using high doses of ciprofloxacin (150 mg/kg three times a day for 11 days) in experiments on mice, a short-term reversible suppressive effect of the drug on hematopoiesis was noted. The authors consider ciprofloxacin safe for the treatment and prevention of infection in patients with diseases of the blood system.

Thus, arthrotoxicity of fluoroquinolones was observed only under experimental conditions. Damage to cartilage tissue in immature animals with the introduction of non-fluorinated quinolones - nalidixic (Negram), oxolinic (Gramurin), pipemidic (Pallin) acids - was established 15 years after the introduction of the first non-fluorinated quinolone (Negram) into clinical practice, i.e. in 1977. By this time, a fairly large positive clinical experience with the use of these drugs both in adult patients and in pediatrics had been accumulated.

The use of ciprofloxacin in children and adolescents

Starting from 1988-1989. in the literature from year to year the number of publications on the successful use of ciprofloxacin in children is increasing. After the discovery of the arthropathic effect of ciprofloxacin in immature animals, controlled studies of the therapeutic effect of this drug in children have not been conducted. Ciprofloxacin (as well as some other fluoroquinolones) was considered for pediatric use only as a drug for use in severe infections in case of failure of previous therapy. Doctors - specialists in various fields of pediatrics - prescribed ciprofloxacin in their practice, as a rule, for health reasons, in the absence of the effect of traditional treatment. antimicrobials, including highly active broad-spectrum antibiotics.

The main characteristics of ciprofloxacin, which attract pediatricians in these cases and ensure high therapeutic efficacy of the drug, are as follows:

• a wide antibacterial spectrum, including such microorganisms as Pseudomonas aeruginosa, Pseudomonas spp., Acinclobacter spp., Klebsiella spp., Serratia spp. and multiresistant strains of staphylococci;
• high concentration level and good diffusion in tissues, including bronchial secretion, cerebrospinal fluid;
• high bioavailability of the drug when administered orally, which is essential in the treatment of severe chronic processes and in cases where parenteral administration is not possible;
• good tolerability and low frequency of adverse reactions (according to the results wide application drug in adults).

Ciprofloxacin, for health reasons, with the ineffectiveness of previous standard therapy, was used in newborns, including premature babies, in children of the first year of life, aged 2-10 years, and in adolescents.

Indications for the use of the drug were severe forms of bacterial infection caused mainly by gram-negative aerobic flora, mainly multi-resistant strains of bacteria, including multi-resistant strains of Enterobacter cloacae, Klebsiella pneumonia, Pseudomonas aeruginosa, Serratia marcescens. The isolated gram-negative microorganisms were resistant to semi-synthetic penicillins, III generation cephalosporins, aminoglycosides, but showed selective high sensitivity to ciprofloxacin.

Ciprofloxacin has been used to treat septic processes, bacteremia, intestinal infections, various forms of respiratory tract infection in children with cystic fibrosis.

In fact, the drug is included in the list of the most important drugs indicated in the treatment of infection in patients with cystic fibrosis. The ability to use ciprofloxacin orally is in this case an important advantage in comparison with parenteral antibiotics.

According to the literature, the therapeutic efficacy of ciprofloxacin in pediatric practice has been confirmed in the treatment of septicemia, purulent bacterial meningitis, severe forms of aspiration pneumonia, and purulent respiratory infections in patients with cystic fibrosis.

The drug was used intravenously and orally in daily doses from 7-9.5 mg/kg to 25-40 mg/kg, usually in two doses with an interval of 12 hours. The duration of treatment varied widely: from 1-3 to 10-46 days, in isolated cases longer courses of treatment were used. In newborns, the drug was used intravenously; in older children, various routes of administration were used, including sequential intravenous and then oral therapy.

In the treatment of various purulent-septic diseases and intestinal infections, the effectiveness of ciprofloxacin turned out to be high, and the authors, who described groups of patients from 3-17 patients, rarely (no more than 1 case per group) state the absence of a therapeutic effect of the drug.

The main results of the use of ciprofloxacin in children and adolescents, according to the literature, are summarized in tables 4 and 5.

Table 4

The use of ciprofloxacin in children (doses of 15-40 mg / kg per day, orally or intravenously; duration of treatment - according to clinical indicators and the results of bacteriological studies)

* Summarized according to reviews; **; *** Hart C et al., 1992, op.

Table 5

Results of the use of fluoroquinolones in children with generalized forms of bacterial infection*

* Summarized based on publications

It is of interest to analyze some clinical materials.

The successful use of ciprofloxacin in 97 children with various pathologies (severe malnutrition, sickle cell anemia, malaria, schistosomiasis, tuberculosis, HIV infection and AIDS) complicated by salmonella infection is reported. Salmonellosis proceeded in the form of a generalized form with diagnosed bacteremia and in the form of infectious arthritis or osteomyelitis. The drug was administered at a daily dose of 10 mg/kg in two doses, the duration of treatment was on average 9.3 days, and for joint infections - up to 6 weeks. Among the pathogens were various representatives of Salmonella: S. typhi, S. typhimurium, S. enteritidis and some others. Complete recovery, according to clinical and bacteriological data, was achieved in 88% of children with bacteriologically confirmed bacteremia. In all patients with Salmonella infection of the joints or bones, recovery was achieved with good tolerance to long-term courses of treatment (from 27 to 42 days). There were no marked changes in the articular system. Only in one child on the 20th day of observation, pain and swelling in the area of ​​the knee joint were noted after exercise (long transition). One child had pruritus, 30 children had transient abnormalities of varying degrees in laboratory parameters (bilirubin, alkaline phosphatase, alanine aminotransferase), which, given the severity of the underlying pathology, cannot be fully attributed to the drug.

The successful use of ciprofloxacin in otorhinolaryngological practice in the treatment of chronic purulent otitis media, most often etiologically associated with multiresistant strains of Pseudomonas aeruginosa, is reported. Thus, in 28 children aged 1 to 10 years and in 40 children aged 1 to 14 years with such a pathology, a course of treatment with ciprofloxacin showed high therapeutic efficacy and the absence of arthropathy and arthralgia.

For the treatment of 28 children and adolescents aged 19 days to 15 years with severe forms of generalized purulent infection, caused in most cases by P. aeruginosa or K. pneumoniae, intravenous ciprofloxacin was used with the ineffectiveness of previous antimicrobial therapy or intolerance to antibiotics. The authors indicate that the drug was prescribed for health reasons. The therapeutic effect was obtained in 507 children. The drug was well tolerated by patients: adverse reactions in the form of mild pain in the abdomen were noted only in one patient.

There are reports of the use of ciprofloxacin in two children in cases of extrapulmonary mycobacteriosis caused by multiresistant strains of Mycobacterium avium and Mycobacterium tuberculosis.

Ciprofloxacin is used in pediatric practice for the purpose of prevention and, mainly, for the treatment infectious complications in patients with neutropenia and oncological diseases, as well as for the prevention of infection in cases of bone marrow transplantation. The drug was used in 17 children at a daily dose of 20 mg/kg (up to 800 mg per day) in combination with standard drugs (polymyxin, clotrimoxazole, fluconazole) to prevent infection during bone marrow transplantation. Ciprofloxacin was prescribed 14 days before transplantation (decontamination regimen) and then continued therapy until bone marrow engraftment. Good tolerability of the applied schemes is noted, arthralgia was observed in two cases, there were no deaths associated with the occurrence of a bacterial infection. Ciprofloxacin is considered possible drug in the decontamination system in the preparation of children for bone marrow transplantation, as well as in the treatment of infections of the skin, soft tissues, lower respiratory tract, septicemia, both in cases with a bacteriologically unconfirmed diagnosis, and in cases of infection caused by gram-negative flora, with unsuccessful previous therapy with beta-lactam in combination with aminoglycosides.

Experience with ciprofloxacin in high-risk neonates

An analysis of literature data summarizing more than 2,000 clinical observations on the use of fluoroquinolones in children (including successful use in severe infections in newborns) showed the validity of prescribing these drugs to children for health reasons, a high clinical effect and the absence of serious side effects.

Thus, ciprofloxacin was used in 10 premature newborns with severe pulmonary pathology after unsuccessful standard therapy with third-generation cephalosporins, imipenem, and aminoglycosides. Of the 10 children, 7 premature babies had unilateral pneumonia, 2 had bilateral lung damage, and 1 child had lung atelectasis. The developed infection in 9 observations was caused by P. aeruginosa, and 8 strains were resistant to imipenem. 4 children had a mixed infection: Pseudomonas aeruginosa in combination with Klebsiella pneumonia (a strain sensitive to imipenem), with Serratia marcescens (a strain resistant to cephalosporins and imipenem) or Staphylococcus aureus (multidrug resistant strain). In one child, the infection was caused by Mycoplasma pneumonia; It should be noted that this was the first observation of the use of ciprofloxacin for mycoplasmal infection in pediatric practice. All children were on artificial lung ventilation. Ciprofloxacin was administered intravenously (30-minute infusion) at daily doses of 15 to 40 mg/kg, with an average dose of 20 mg/kg. The course of treatment was 7-10 days. To increase the effectiveness of ciprofloxacin against gram-negative flora, it was used in conjunction with amikacin (7.5 mg/kg every 12 hours). After the inclusion of ciprofloxacin in the treatment regimen, the therapeutic effect was obtained in 8 children, including according to the data microbiological research. In two cases (a child with lung atelectasis and a child with bilateral pneumonia), a fatal outcome occurred due to severe functional impairment. respiratory system, hemorrhage and bleeding disorders. In recovered children, according to clinical and radiological studies, there were no disorders and changes in the development of the skeletal system, the presence of arthropathies or an increase in the volume of the joints. The authors emphasize the effectiveness of ciprofloxacin in the treatment of pneumonia caused by mycoplasma.

In another observation, ciprofloxacin, also for health reasons, was used in 5 preterm infants aged 8 to 80 days for the treatment of purulent meningitis caused in three cases by Escherichia coli, in one by Enterobacter cloacae and in the other by Pseudomonas aeruginosa. The developed infection was resistant to cephalosporin therapy in combination with aminoglycosides (cefotaxime + amikacin, cefotaxime 4-netilmicin, cefotaxime + gentamicin and ceftazidime + amikacin + ticarcillin), as well as to imipenem in combination with netilmicin. Ciprofloxacin after unsuccessful previous therapy was prescribed in daily doses of 10 to 20-30 mg/kg for 10-43 days. In 3 children, ciprofloxacin was used sequentially: when the condition improved after intravenous therapy (from 15 to 25 days), they switched to the use of the drug orally. Higher doses (30 mg/kg per day) were prescribed during oral therapy. In 4 children, recovery was observed; the fifth child also had a therapeutic effect, but there was a recurrence of the infection; recovery was achieved after re-appointment of ciprofloxacin. The subsequent control within 9 months did not reveal any deviations from the norm in the development of the child.

Recently, publications have appeared in the literature about long-term observations (catamnesis) of the growth and development of children who received fluoroquinolones in the neonatal period. In particular, detailed remote observation of such newborns was carried out for 42 months by authors from Turkey. According to vital indications, 9 newborns received ciprofloxacin at a dose of 20 mg/kg per day in the neonatal period due to sepsis caused by bacterial flora resistant to other antibacterial drugs. For objective evaluation and comparison, other 9 patients with the same medical history (birth weight and gestational age) were selected who were treated with cefotaxime (control group 1). Control group 2 consisted of 9 healthy children with the same parameters. Dynamic observation for 3.5 years (42 months) did not reveal any significant differences in the rate of growth and development of children in the comparison groups. In the group of children treated with ciprofloxacin, no pathology of the osteoarticular system was noted. The authors conclude that ciprofloxacin can be used in newborns for health reasons, with sepsis caused by multidrug-resistant microorganisms.

The data detailed above also allowed us, according to vital indications, subject to the selective sensitivity of the isolated microflora to ciprofloxacin and in the absence of the effect of previous antibiotic therapy (3rd generation cephalosporins, aminoglycosides), to use the fluoroquinolone drug ciprofloxacin in the treatment of newborns.

Cyprobay (ciprofloxacin, Bayer, Germany) was used in the treatment of 51 sick children in the neonatal intensive care unit of the Children's City Clinical Hospital No. N.F. Filatov (Moscow). Indications for the appointment of cyprobay were severe pneumonia and/or septic condition in critically ill neonates on artificial lung ventilation, in cases where traditional antibiotic therapy failed. All these children belonged to the high-risk group of newborns, the progression of the infectious process in which is dangerous and can lead to death. Thus, ciprofloxacin was administered to these patients for health reasons.

Of the total number of patients treated with cyprobay, 44 (88%) had varying degrees of prematurity (mean gestational age 32.6 ± 0.7 weeks). Body weight at admission ranged from 800 to 4300 g and averaged 2250 ± 140 g. Newborns were on artificial lung ventilation from 2 to 41 days (average 16.0 ± 1.3 days). In 46 (92%) patients, pneumonia developed on the background of asphyxia, respiratory distress syndrome, or meconium aspiration. Of the comorbidities, birth trauma was most frequently noted, including intraventricular hemorrhages of the II-IV degree — in 12 patients (24%). All children were under microbiological monitoring.

A positive decision on the appointment of cyprobay was made in case of deterioration of the patient's condition associated with the progression of the infectious process, taking into account the data of bacteriological examination (sowing of a smear from the mucous membranes of the pharynx and tracheobronchial discharge). Tsiprobay was prescribed in those cases when the drugs traditionally used in the department (aminoglycosides, cephalosporins of the II and III generation) were ineffective against the microflora of the patient, and the isolated microorganisms showed selectively high sensitivity only to ciprofloxacin.

Cyprobay was always used after previous courses of antibiotic therapy, on average 11.5 ± 0.8 days after the patient was admitted to the department.

All patients were prescribed cyprobay parenterally (intravenously), the daily dose was divided into two doses. Doses ranged from 18 to 40 mg/kg (average 27.6 ± 0.6 mg/kg) were used. The duration of therapy averaged 5.6 ± 0.4 days (from 3 to 11 days).

In 39 sick children out of 51 (76%), against the background of the use of cyprobay, there was a pronounced positive dynamics in the course of the infectious process, both in clinical and microbiological parameters; the children were soon transferred to independent breathing and then nursed in other departments.

At the time of writing this work, 5 out of 39 children who received cyprobay during the neonatal period were able to conduct a follow-up examination. Children at the age of 1 year were examined by a neonatologist and a pediatric orthopedist. All examined children corresponded to the age norm in terms of physical development and neurological status, no deviations from the osteoarticular system were found. Work on the collection of follow-up data is ongoing.

Of the 51 children, 12 (23.5%) died. The analysis of the causes of deaths in the study group of newborns who were under observation in connection with the use of cyprobay is summarized in Table. 6. One deep premature baby(gestational age 26 weeks, weight 800 g) received cyprobay for 12 days. There was a pronounced positive trend both in terms of the clinical picture and in terms of bacteriological parameters. At the time of the appointment of cyprobay, the patient had a pronounced picture of bilateral progressive pneumonia, while Serratia liquefaciens was sown in large quantities from the washings of the trachea. By the 3rd day of using cyprobay, Serratia liquefaciens was eliminated from the trachea. During 12 days of cyprobay administration, the tracheal contents remained sterile. This patient, who had been on a ventilator since birth, died from acute pulmonary hemorrhage. Three patients died from the consequences of a massive intraventricular hemorrhage during childbirth, three - as a result of a generalized viral infection (laboratory confirmed), one child - due to a generalized candidal infection, one - from progressive intrauterine cirrhosis of the liver, one - as a result of the progression of hydrocephalus. It is extremely important to note that none of the 12 dead newborns had bacterial infectious complications as direct causes of death. Given that ciprofloxacin was prescribed in the most severe cases, in the absence of the effect of other antibiotics, with the isolation of multi-resistant microflora, the mortality rates (12 out of 51, i.e. 23.5%) should be considered low for this group of patients. It is also important to emphasize that none of the three victims had a purulent-inflammatory or septic process recorded in the pathoanatomical diagnosis.

Table 6

Mortality in high-risk newborns depending on ciprofloxacin therapy

The study revealed the high efficiency of cyprobay in the treatment of serious infections caused by multidrug-resistant gram-negative microflora in preterm infants on artificial lung ventilation. None of the children treated with cyprobay had negative side effects during the period of taking the drug. According to our data, the optimal dose of cyprobay in children should be considered 20-30 mg/kg per day. This is consistent with the above literature data.

Possible dosages of ciprofloxacin when using the drug in children according to vital indications

Given the absence of any official indications of the possible dosages of fluoroquinolones in children, in practice, the decision on this issue remained in each case for clinicians.

Data on dosages of ciprofloxacin in pediatrics are summarized in Table. 7. Case reports of pefloxacin use in childhood indicate dosages of 12 to 30 mg/kg intravenously 2 times a day with an average of 20 mg/kg per day. Most often in childhood, ciprofloxacin is used from fluoroquinolones, and, as can be seen from Table. 7, its doses are quite variable. It is interesting to note that in adult patients, the average daily doses of ciprofloxacin are lower than in children, and are approximately 1-10 mg / kg when taken orally in approximately 40% of patients, 11-20 mg / kg in half, and more than 16% in only 16%. 20 mg/kg. According to V. Chysky, R. Hullman, the average daily dose of ciprofloxacin in children is 25.5 mg/kg orally and 7.0 mg/kg intravenously. The average duration of treatment with ciprofloxacin in adult patients is also lower (85% up to 14 days) than in children (23 days). Obviously, this is due to the selectively severe pathology in which the pediatric clinician makes a choice in favor of prescribing a fluoroquinolone to a child. In the literature, there are also reports of cases of excessive deviation from the average dosages, in particular, the use of ciprofloxacin in a 9-year-old child at a dose of 76.9 mg / kg intravenously for 5 days, at which the concentration of the drug in the blood serum was 43 μg / ml. This case is of interest

Table 7

Therapeutic doses of ciprofloxacin used in pediatrics

from the point of view of good tolerance even when using super-high doses, however, it should be considered unjustified to prescribe fluoroquinolones, including ciprofloxacin, in such high doses to children.

Tolerability and adverse reactions when using ciprofloxacin in children

When using ciprofloxacin in children, the attention of clinicians is drawn primarily to the tolerability of the drug and adverse reactions, especially from the articular and skeletal systems.

Of the undesirable effects, the most common are disorders of the gastrointestinal tract (nausea, vomiting, abdominal pain, less often - diarrhea), sometimes symptoms of the central nervous system (dizziness, headache, anxiety), skin-allergic reactions, including photosensitivity . Usually these symptoms are mild or moderate and most often do not cause discontinuation of therapy. In the group of metabolic disorders, mainly cases of a transient increase in the activity of liver enzymes are summarized. V. Chysky et al. the analysis of the results of a multicenter study on the use of ciprofloxacin in children on a sufficiently large clinical material according to the standard method is given (Table 8).

Table 8

The frequency of adverse events when using ciprofloxacin in children *

* Summarized by V.Chysky and R.Hullman; T.Rubio , U.Yu. Smirnova and others, Beloborodova N.V. and etc.

When registering cases of arthralgia in children, most authors note that this symptom cannot be directly associated with the action of ciprofloxacin (or other fluoroquinolones). In patients with purulent-inflammatory diseases of various etiologies and in children with intestinal infections, reactions from the joints are practically not observed. The described rare cases of arthralgia mainly concern children suffering from cystic fibrosis with a long history of the disease; in this group of children, joint pain may occasionally occur spontaneously and without treatment with fluoroquinolones.

Clinical observations in children with cystic fibrosis show that when using ciprofloxacin, transient arthralgia was observed in 1-1.3% of cases. An analysis of 10 publications, given in a detailed review of the tolerance of fluoroquinolones in children, shows that the incidence of arthralgia with the use of these drugs in 1522 children was on average 3.5%, and in 1308 children who received ciprofloxacin, on average 3.2%.

In children with other forms of bacterial infections, when treated with fluoroquinolones, including ciprofloxacin, transient arthralgia was observed in no more than 1% of cases (0.4% on average).

In comparative clinical studies using the method of nuclear magnetic resonance and fluoroscopy data in sick children with cystic fibrosis who received ciprofloxacin, no changes in cartilage tissue were found that could be associated with the negative effect of the drug. However, monitoring of possible changes in the cartilage tissue and reactions from the joints, of course, should be continued. Long-term monitoring of the state of the osteoarticular system in children treated with ciprofloxacin is very important. It should be pointed out that the mechanism of development of arthralgia and arthropathy under the action of quinolones and fluoroquinolones has not yet received an exhaustive explanation. French researchers, based on extended toxicological experiments, believe that model experiments on dogs and rats are not adequate to transfer these results to humans.

In comparative studies that included 75 children (age from 6 months to 15 years) with cystic fibrosis, the use of ciprofloxacin did not reveal arthropathies both during the administration of the drug and according to follow-up data. Histological studies of cartilage tissue, in cases of lethal outcomes, did not differ in structure from cartilage tissue in the control group of patients who did not receive ciprofloxacin. No accumulation of fluorine in cartilage tissue was found.

The nature of possible adverse reactions that can be observed in children from 1 year and older and in adolescents under 17 years of age with ciprofloxacin therapy is presented in Table. 9 indicating their possible relationship with the action of fluoroquinolone. In children treated with ciprofloxacin and other fluoroquinolones, no convulsive reactions were noted, including the use of ciprofloxacin in patients with meningitis.

Table 9

The nature and frequency of adverse reactions when using ciprofloxacin in 205 children and adolescents (from 1 to 17 years old) with cystic fibrosis after 580 courses of treatment

Proper adherence to the patient's regimen during treatment (complete exclusion of sun exposure and UV exposure) is a necessary guarantee against the development of photodermatosis.

It is known that during treatment with antibacterial drugs, the development of superinfection of various etiologies is possible. When using fluoroquinolones, the most likely candidates for the role of microorganisms - causative agents of secondary infection are, apparently, enterococci and other gram-positive cocci resistant to fluoroquinolones, as well as some strains of P. aeruginosa and C. albicans.

Thus, the appointment of ciprofloxacin to a child with a clinical picture of a progressive infection caused by a gram-negative flora (peritonitis, meningitis, sepsis), despite previous intensive therapy with third-generation cephalosporins (ceftriaxone, cefotaxime or ceftazidime) and aminoglycosides (netilmicin, amikacin, gentamicin) should be considered microbiologically justified. ), in case of isolation of a pathogen sensitive to fluoroquinolones.

Most often, such situations occur in hospital conditions with a long stay of a patient in a hospital, especially in intensive care units, or when a seriously ill patient is admitted from another hospital due to treatment failure. With suspicion and microbiological confirmation of the leading role in the infectious process of multiresistant “problem” gram-negative bacteria (Pseudomonas spp., Serratia spp., Klebsiella spp., Enterobacter spp.), ciprofloxacin with a high probability can be a truly life-saving drug.

Received 12/17/10

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Tradename: Ciprofloxacin-Teva

International non-proprietary name:

ciprofloxacin

Dosage form:

coated tablets film sheath

Composition
1 tablet contains:
active substance ciprofloxacin 250.0/500.0 mg (ciprofloxacin hydrochloride monohydrate 291.1/582.2 mg);
excipients: microcrystalline cellulose 36.65 / 73.30 mg, povidone K-30 18.75 / 37.50 mg, croscarmellose sodium 21.00 / 42.00 mg, colloidal silicon dioxide 3.75 / 7.50 mg, magnesium stearate 3.75/7.50 mg;
shell Opadray white Y-1-7000H: hypromellose 3.125/6.250 mg, titanium dioxide 1.5625/3.1250 mg, macrogol-400 0.3125/0.6250 mg.

Description
Tablets 250 mg: white, round, biconvex, film-coated tablets, debossed with "CIP 250" and scored on one side. The cross section shows two layers. The kernel is white to yellowish white.
Tablets 500 mg: white, film-coated capsule-shaped tablets, debossed with "CIP 500" and scored on one side. The cross section shows two layers. The kernel is white to yellowish white.

Pharmacotherapeutic group:

antimicrobial agent - fluoroquinolone

ATC Code: J01MA02

Pharmacological properties
Pharmacodynamics.
A broad-spectrum antimicrobial agent of the fluoroquinolone group. It suppresses topoisomerases II (bacterial DNA gyrase) and IV, responsible for the process of supercoiling of chromosomal DNA around nuclear RNA, which is necessary for reading genetic information), disrupts DNA synthesis, growth and division of bacteria, causes pronounced morphological changes and rapid death of the bacterial cell. It acts bactericidal on gram-negative organisms during the period of rest and division (because it affects not only DNA gyrase, but also causes lysis of the cell wall), on gram-positive microorganisms - only during the period of division.
Low toxicity to macroorganism cells is explained by the absence of DNA gyrase in them. While taking ciprofloxacin, there is no parallel development of resistance to other antibiotics that do not belong to the group of gyrase inhibitors, which makes it highly effective against bacteria that are resistant, for example, to aminoglycosides, penicillins, cephalosporins, tetracyclines and other antibiotics. The effectiveness of ciprofloxacin depends largely on the relationship between pharmacokinetic (PK) and pharmacodynamic (PD) parameters - between the maximum concentration in blood serum (Cmax) / minimum inhibitory concentration (MIC) and between the area under the concentration-time curve (AUC) / IPC. Resistance develops slowly and gradually ("multi-stage" type). There is no cross-resistance with other fluoroquinolones. The basis for the formation of resistance to ciprofloxacin are gene mutations (amino acid substitutions) in the region of the "quinolone pocket" - the site of the polypeptide chain of topoisomerases II and IV, in which they should bind to ciprofloxacin. Another possible mechanism of resistance is associated with mutations in the gene that encodes membrane proteins involved in the active ejection (efflux) of ciprofloxacin from the cell and / or a decrease in the permeability of the cell membrane for ciprofloxacin. Usually, single mutations lead to a slight (2-4 times) increase in BMD. A high level of resistance is usually associated with two or more mutations in one or more genes.

Susceptibility to ciprofloxacin in vitro
The most sensitive microorganisms

Gram-positive aerobic microorganisms: Bacillus anthracis, Staphylococcus aureus (including methicillin-sensitive strains), Staphylococcus saprophytics, Streptococcus spp. Gram-negative aerobic microorganisms: Aeromonas spp., Brucella spp., Citrobacter koseri, Francisella tularensi, Haemophilus ducreyi, Haemophilus influenzae, Legionella spp, Moraxella catarrhalis, Pasteurella spp, Neisseria meningitidis, Salmonella spp., Shigella spp., Vibrio spp., Yersiniapestis. Anaerobic microorganisms: Mobiluncus spp. Other microorganisms:
Microorganisms with varying degrees of sensitivity to ciprofloxacin Gram-positive aerobic microorganisms: Enterococcus faecalis, Streptococcus pneumoniae. Gram-negative aerobic microorganisms: Acinetobacter baumannii, Burkholderia cepacia, Campylobacter jejuni, Citrobacter freundii, Enterobacter aerogenes, Enterobacter cloacae, Escherichia coli, Klebsiella oxytoca, Klebsiella pneumoniae, Morganella morganii, Neisseria gonorrhoeae, Proteus mirabilis, Proteus vulgaris Pseudomonas fluorescens, Serratia marcescens, Streptococcus pneumoniae.
Resistant microorganisms Gram-positive aerobic microorganisms: Actinomyces spp., Enterococus faecium, Staphylococcus spp. (methicillin-resistant strains). Gram-negative aerobic microorganisms: Burkholderia cepacia, Listeria monocytogenes Nocardia asteroids, Stenotrophomonas maltophilia. Anaerobic microorganisms (with the exception of Mobiluncus spp., Peptostreptococcus spp., Propionibacterium acnes). Other microorganisms: Bacteroides fragilis, Clostridium difficile, Mycoplasma genitalium, Treponema pallidum, Ureaplasma urealyticum. Pharmacokinetics
Absorption. Following oral administration, ciprofloxacin is predominantly absorbed into the duodenum and upper jejunum. Cmax is achieved 60-90 minutes after ingestion. After taking a single dose of 250 mg or 500 mg Cmax is approximately 0.8-2.0 mg/l and 1.5-2.9 mg/l, respectively. Absolute bioavailability is approximately 70-80%; Cmax and AUC values ​​increase in proportion to the dose taken.
Eating (with the exception of dairy products) slows down the absorption, but does not change the Cmax and bioavailability of ciprofloxacin.
Distribution. The equilibrium volume of distribution (Vd) of ciprofloxacin is 2-3.5 l/kg. Large Vd is associated with high tissue penetration of ciprofloxacin. Since ciprofloxacin binds to blood proteins to a small extent (20-30%) and is present in the blood plasma in a non-ionized form, almost the entire dose taken can freely penetrate into the extravascular space. As a result, the concentration of ciprofloxacin in some body fluids and tissues may exceed its concentration in the blood. The content in tissues is 2-12 times higher than in plasma. Therapeutic concentrations are achieved in saliva, tonsils, liver, gallbladder, bile, intestines, organs abdominal cavity and small pelvis, uterus, seminal fluid, prostate tissue, endometrium, fallopian tubes and ovaries, kidneys and urinary organs, lung tissue, bronchial secretion, paranasal sinuses, bone tissue, muscles, synovial fluid and articular cartilage, peritoneal fluid, skin. It penetrates into the cerebrospinal fluid in a small amount, where its concentration in non-inflamed meninges is 6-10% of that in the blood serum, and in inflamed meninges - 14-37%. Ciprofloxacin also penetrates well into eye fluid, bronchial secretion, pleura, peritoneum, lymph, breast milk, through the placenta. The concentration of ciprofloxacin in blood neutrophils is 2-7 times higher than in serum. Activity is somewhat reduced at acidic pH values.
Metabolism. Metabolized in the liver (15-30%) with the formation of inactive metabolites (desethyleneciprofloxacin (Ml), sulfocyprofloxacin (M2), oxocyprofloxacin (M3) and formylciprofloxacin (M4)). Ml, M2 and M3 are characterized by similar or lower activity compared to nalidixic acid. M4, found in the lowest concentrations, has a similar to norfloxacin antimicrobial activity.
It is a moderate inhibitor of the CYP1A2 isoenzyme.
Withdrawal. Ciprofloxacin is mostly excreted unchanged, mainly by the kidneys. Renal clearance is 3-5 ml/min/kg and total clearance is about 8-10 ml/min/kg. Transport of ciprofloxacin is carried out by glomerular and tubular secretion. Excretion of ciprofloxacin after oral administration (in % of the dose of ciprofloxacin)

The half-life (T1 / 2) of ciprofloxacin is 3-5 hours.
For moderate chronic kidney failure(creatinine clearance (CC) more than 20 ml / min), the percentage of ciprofloxacin excreted through the kidneys decreases, but cumulation in the body does not occur due to a compensatory increase in the metabolism of ciprofloxacin and excretion by the intestines. In severe renal failure (CC less than 20 ml / min), T1 / 2 increases to 12 hours and the daily dose of ciprofloxacin must be reduced by 2 times.
Childhood. The pharmacokinetics of ciprofloxacin in children with cystic fibrosis differ from the pharmacokinetics of ciprofloxacin in children without cystic fibrosis, and dosing recommendations apply only to children with cystic fibrosis. When ciprofloxacin 20 mg/kg orally is used in children with cystic fibrosis, the observed drug effect is comparable to adult patients who receive ciprofloxacin 750 mg twice a day. Indications for use
adults Respiratory tract infections. Ciprofloxacin is recommended for use in pneumonia caused by Klebsiella spp., Enterobacter spp., Proteus spp., Esherichia coli, Pseudomonas aeruginosa, Haemophilus spp., Moraxella catarrhalis, Legionela spp. and staphylococci; ENT infections (acute sinusitis, otitis media), especially if these infections are caused by gram-negative microorganisms, including Pseudomonas aeruginosa or staphylococci; eye infections; infections of the kidneys or urinary tract, including cystitis, pyelonephritis; genital infections, including adnexitis, prostatitis; complicated intra-abdominal infections (in combination with metronidazole) and uncomplicated gonorrhea; infections of the gastrointestinal tract, including diarrhea "travelers"; infections of the skin and soft tissues and skin; bone and joint infections; sepsis; infections or prevention of infections in immunosuppressed patients (patients taking antidepressants or patients with neutropenia); selective intestinal decontamination in immunocompromised patients; prevention and treatment of pulmonary anthrax (infection with Bacillus anthracis); prevention of invasive infections caused by Neisseria meningitides.
Children aged 5-17 years Acute pneumonia on the background of cystic fibrosis caused by Pseudomonas aerugenosa. Contraindications
Hypersensitivity to ciprofloxacin or other components of the drug, as well as to other antimicrobial agents from the quinolone group, including a history; simultaneous use of ciprofloxacin and tizanidine; children under 18 years of age (until the completion of the process of skeletal formation, except for the treatment of complications caused by Pseudomonas aerugenosa, in children aged 5-17 years with cystic fibrosis of the lungs); tendon diseases, including history; pregnancy; breastfeeding period. Carefully
Moderate and severe renal dysfunction (CC less than 60 ml / min), hemodialysis, peritoneal dialysis (PD), liver dysfunction, myasthenia gravis, old age; postoperative infections (limited data on efficacy and safety); prolongation of the QT interval, congenital long QT syndrome, heart disease (heart failure, myocardial infarction, bradycardia), torsades de pointes arrhythmia, glucose-6-phosphate dehydrogenase deficiency, electrolyte imbalance (eg, hypokalemia, hypomagnesemia), concomitant drug use prolonging the QT interval (including antiarrhythmic classes IA and III), simultaneous use with inhibitors of the CYP450 1A2 isoenzyme (including theophylline, methylxanthine, caffeine, duloxetine, clozapine), a history of tendon diseases associated with taking quinolones, insufficiency cerebral circulation, a history of epilepsy, diseases accompanied by organic changes in the structure of the brain, including conditions after a violation of cerebral circulation. Use during pregnancy and during breastfeeding
Ciprofloxacin is contraindicated during pregnancy.
Since ciprofloxacin is excreted in breast milk, it should not be given to nursing mothers. If it is necessary to use ciprofloxacin in the mother during lactation, feeding the child should be stopped before starting treatment. Dosage and administration
Inside, regardless of the meal, without chewing the tablet, drinking water. When used on an empty stomach, the absorption of ciprofloxacin increases. Foods high in calcium (milk, yogurt) may reduce the absorption of ciprofloxacin.
The dose of ciprofloxacin depends on the type and severity of the infection, the age, body weight of the patient and the functional state of the kidneys.
The duration of treatment depends on the severity of the disease, clinical and bacteriological response. In general, treatment should be continued for at least three days after normalization of body temperature or resolution of clinical symptoms.
adults
For mild to moderate respiratory infections

- 500 mg 2 times a day for 7-14 days.

With infection of the upper respiratory tract (acute sinusitis, otitis media)

- 500 mg 2 times a day.

The course of treatment is 10 days.

For infections of the gastrointestinal tract, including "travelers" diarrhea: diarrhea caused by Shigella spp., with the exception of Shigella dysenteriae, and empirical treatment of severe traveler's diarrhea - 500 mg 2 times a day for 1 day; diarrhea caused by Shigella dysenteriae - 500 mg 2 times a day for 3 days; typhoid fever - 500 mg 2 times a day for 5 days; diarrhea caused by Vibrio cholerae - 500 mg 2 times a day for 7 days.
Urinary tract infections, including cystitis, pyelonephritis, uncomplicated cystitis - 250-500 mg 2 times a day for 3 days; complicated cystitis and uncomplicated pyelonephritis - 500 mg 2 times a day for 7-14 days.
Infections of the genitourinary system and pelvic organs, including urethritis and cervicitis caused by Neisseria gonorrhoeae - 500 mg once a day once; prostatitis - 500 mg 2 times a day for 28 days.
Infections of soft tissues and skin caused by gram-negative microorganisms - 500 mg 2 times a day for 7-14 days.
Infections in patients with neutropenia - 500 mg 2 times a day during the entire period of neutropenia (in combination with other antibiotics).
Infections of bones and joints - 500 mg 2 times a day. The duration of treatment is not more than 3 months;
With sepsis, other generalized infectious diseases, for example, with peritonitis (in addition to antibacterial drugs that act on anaerobes), infectious diseases in patients with reduced immunity - 500 mg 2 times a day (in combination with other antibiotics) during the period necessary for treatment.
For particularly severe, life-threatening infections (especially those caused by Pseudomonas aeruginosa, Staphylococcus spp., or Streptococcus spp., such as osteomyelitis, sepsis, Streptococcus pneumoniae pneumonia, recurrent cystic fibrosis infections, severe skin and soft tissue infections, or peritonitis), the recommended dose is 750 mg twice a day.
In elderly patients, the dose depends on the severity of the disease and the state of renal function.

In patients with impaired renal function:

Patients must be closely monitored. The intervals between doses should be the same as for use in patients with normal renal function.
In patients with impaired renal function and hemodialysis
Recommended dose: 250-500 mg 1 time per day after the hemodialysis procedure.
In patients with impaired renal function and permanent outpatient PD
The recommended dose is 250-500 mg once a day after the PD procedure.
In patients with impaired liver function
Dose adjustment is not required for mild to moderate liver failure but may be necessary in severe hepatic impairment.
In patients with impaired liver and kidney function
Dose adjustment as in case of impaired renal function. Patients must be under strict supervision. In some cases, it may be necessary to determine the concentration of ciprofloxacin in plasma.
Children aged 5-17
Acute pneumonia on the background of cystic fibrosis caused by Pseudomonas aerugenosa - 20 mg / kg 2 times a day for 10-14 days. The maximum daily dose is 1.5 g.
Ciprofloxacin has not been studied in children aged 5-17 years with impaired renal and / or liver function and cystic fibrosis of the lungs, complicated by the addition of Pseudomonas aerugenosa infection. Side effect
Adverse reactions were noted in 5-14% of patients taking ciprofloxacin. Most frequent side effects are nausea, vomiting and skin rash.
The incidence of side effects is classified according to the recommendations World Organization health care: very often - at least 10%; often - not less than 1%, but less than 10%; infrequently - not less than 0.1%, but less than 1%; rarely - not less than 0.01%, but less than 0.1%; very rarely - less than 0.01%, including isolated cases.
Infections and invasions: infrequently - fungal superinfection, candidiasis (including the oral cavity, vaginal candidiasis, candidiasis of the gastrointestinal tract (GIT)).
From the side digestive system: often - nausea, diarrhea, vomiting, indigestion, loss of appetite, flatulence, abdominal pain; rarely - dysphagia, pancreatitis, hepatitis, jaundice, including cholestatic, liver necrosis, in isolated cases leading to life-threatening liver failure; very rarely, antibiotic-associated pseudomembranous colitis, in isolated cases, taking life-threatening forms.
From the nervous system: often - dizziness, headache, agitation, tremor; infrequently - insomnia, taste perversion (reversible, disappears after the abolition of ciprofloxacin); rarely - hallucinations, paresthesia (peripheral paralgesia), "nightmare" dreams, depression, convulsions, hypesthesia, drowsiness, exacerbation of symptoms of myasthenia gravis, confusion, disorientation, peripheral neuropathy, polyneuropathy; very rarely - grand mal seizures, gait disturbance, psychosis (in the development of which patients can harm themselves), increased intracranial pressure, ataxia, hyperesthesia, muscular hypertension, impaired sense of smell, loss of smell (usually disappears after discontinuation of ciprofloxacin), migraine , anxiety, loss of taste sensations.
On the part of the organ of vision: very rarely - visual impairment, double vision, impaired color perception.
On the part of the organ of hearing and balance: very rarely - tinnitus, temporary deafness (especially with frequent use of ciprofloxacin).
From the musculoskeletal system: infrequently - pain in the joints; rarely - muscle pain, joint swelling, pain in the extremities, back pain, increased muscle tone, muscle weakness, exacerbation of symptoms of myasthenia gravis; very rarely - convulsive muscle contraction, inflammation of the tendon (mainly the Achilles tendon, including tenosynovitis), partial or complete rupture of the tendon (mainly the Achilles tendon).
From the side of the cardiovascular system: infrequently - a feeling of palpitations; rarely - tachycardia, vasodilation, fainting, flushing of blood to the face, lowering blood pressure (BP); very rarely - tachycardia, vasculitis (petechial, hemorrhagic bullae, papules, scab-like formations), arrhythmia, pirouette-type arrhythmia, prolongation of the QTc interval, (mainly in patients with other risk factors for prolongation of the QTc interval).
From the respiratory system: infrequently - pulmonary embolism, pulmonary edema, hemoptysis, hiccups, shortness of breath, nosebleeds; rarely - shortness of breath.
From the side of the blood system and hematopoietic organs: often - eosinophilia; infrequently - leukopenia, neutropenia, anemia, granulocytopenia, thrombocytopenia; rarely - leukocytosis, thrombocytosis; very rarely - hemolytic anemia, agranulocytosis, pancytopenia (life-threatening), depression of bone marrow function (life-threatening).
From the urinary system: rarely - acute renal failure, hematuria, crystalluria, interstitial nephritis.
Allergic reactions: often - skin rash; infrequently - itching, spotty-nodular rash, urticaria; rarely - photosensitivity, erythema multiforme, erythema nodosum, swelling of the face; very rarely - anaphylactoid reactions, laryngeal edema, Steven-Johnson syndrome, Lyell's syndrome, petechiae, anaphylactic shock, serum sickness, angioedema.
Laboratory data: infrequently - increased activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase, hyperbilirubinemia, increased blood urea concentration; rarely - changes in prothrombin, hyperglycemia; very rarely - increased activity of amylase, lipase.
Other: infrequently - general weakness, sweating, drug fever; rarely - chest pain, peripheral edema. Overdose
Symptoms: dizziness, tremor, headache, fatigue, seizures, hallucinations, prolongation of the QTc interval, gastrointestinal disorders, liver and kidney dysfunction, crystalluria, hematuria.
Treatment: induction of vomiting or gastric lavage, taking activated carbon, antacids containing calcium and magnesium, to reduce the absorption of ciprofloxacin, symptomatic therapy. The patient must be under close medical supervision. Kidney function should be constantly monitored. Ciprofloxacin with hemodialysis or peritoneal dialysis is excreted in small quantities (less than 10%). Maintaining an adequate water regime minimizes the risk of crystalluria. Interaction with other drugs
It is possible to increase the concentration of theophylline (and other xanthines, such as caffeine) in the blood serum and prolong the half-life. As a result, the risk of unwanted effects caused by theophylline may increase. During treatment with ciprofloxacin, more frequent monitoring of theophylline and caffeine levels in the blood serum is recommended.
Ciprofloxacin inhibits the CYP1A2 isoenzyme, and this may cause an increase in plasma concentrations of concomitantly taken drugs that are metabolized by the CYP1A2 isoenzyme.
Significant changes in the pharmacokinetic parameters of tizanidine, including an increase in AUC, T1 / 2, Cmax, an increase in oral bioavailability, and a decrease in plasma clearance were observed with simultaneous use with ciprofloxacin. This pharmacokinetic interaction can lead to serious adverse events. A clinically significant decrease in blood pressure (both systolic and diastolic blood pressure decreases), drowsiness was observed with the simultaneous use of ciprofloxacin and a single dose of 4 mg tizanidine. In this regard, the simultaneous use of tizanidine with ciprofloxacin is contraindicated. In patients receiving concomitantly with ciprofloxacin any other drugs that are a substrate for the CYP1A2 isoenzyme, care must be taken to prevent the occurrence of symptoms of an overdose of these drugs. Plasma concentrations of these drugs should be determined periodically, especially when theophylline is used.
The absorption of ciprofloxacin is slowed down by the simultaneous use of iron, zinc, sucralfate or antacids and drugs with high buffering activity containing magnesium, aluminum or calcium. This also applies to sucralfate, antiviral drugs containing buffered didanosine, oral nutrition solutions. Also, this effect is observed when eating large amounts of dairy products (milk or liquid dairy products such as yogurt). Thus, ciprofloxacin should be taken either 1-2 hours before or 4 hours after taking the above substances. These restrictions do not apply to H2-histamine receptor blockers.
Simultaneous use of very high doses of quinolones and some non-steroidal anti-inflammatory drugs (except acetylsalicylic acid) may lead to seizures.
With simultaneous use with uricosuric drugs, excretion slows down by 50% and the plasma concentration of ciprofloxacin increases. With the simultaneous use of cyclosporine and ciprofloxacin, a transient increase in creatinine concentration is observed. Such patients should regularly check the concentration of creatinine in the blood.
Ciprofloxacin, like other quinolones, may enhance the effect of anticoagulant agents - coumarin derivatives, including warfarin. With the simultaneous use of these drugs, prothrombin time (PT) or other appropriate coagulation tests should be monitored. If necessary, the dose of warfarin should be adequately adjusted.
With the simultaneous use of ciprofloxacin and glibenclamide, the effect of glibenclamide may be enhanced.
Probenecid inhibits the excretion of ciprofloxacin by the kidneys, leading to an increase in the concentration of ciprofloxacin.
Metoclopramide accelerates the absorption of ciprofloxacin. The maximum concentration of ciprofloxacin is reached in more than a short time. The bioavailability of ciprofloxacin does not change.
With the simultaneous use of ciprofloxacin or phenytoin, both an increase and a decrease in the concentration of phenytoin in plasma are possible, therefore it is recommended to control its concentration.
The simultaneous use of ciprofloxacin and mexiletin may lead to an increase in the concentration of mexiletin.
The concomitant use of opioid premedication drugs (eg, papaveretum) or opioid premedication drugs with anticholinergic premedication drugs (atropine or hyoscine) with ciprofloxacin is not used due to a decrease in plasma concentrations of ciprofloxacin.
The simultaneous use of ciprofloxacin and benzodiazepines does not affect the concentration of ciprofloxacin in plasma. However, in connection with reports of a decrease in clearance and an increase in T1 / 2 of diazepam with the simultaneous use of ciprofloxacin and diazepam and, in some cases, with the simultaneous use of ciprofloxacin and midazolam, it is recommended to monitor the effectiveness of treatment with benzodiazepines.
With the simultaneous use of ropinirole with ciprofloxacin, there is a possibility of an increase in the concentration of ropinirole, which may be accompanied by an increased risk of adverse reactions. In the case of simultaneous use, more careful monitoring of therapy with ropinirole is necessary.
It has been reported clinically meaningful interactions between ciprofloxacin and didanosine.
With the simultaneous use of ciprofloxacin and methotrexate, renal tubular transport is suppressed, potentially leading to an increase in plasma concentrations of methotrexate, which may increase the risk of toxic reactions associated with methotrexate. Therefore, it is necessary to monitor the condition of patients in the treatment of methotrexate and the simultaneous administration of ciprofloxacin.
With simultaneous use with omeprazole, there may be a slight decrease in the maximum concentration of the drug in plasma and a decrease in AUC.
In clinical studies, it has been shown that the simultaneous use of duloxetine and potent inhibitors of the CYP1A2 isoenzyme (such as fluvoxamine) can lead to an increase in the AUC and Cmax of duloxetine. Despite the lack of clinical data on a possible interaction with ciprofloxacin, it is possible to foresee the possibility of such an interaction with the simultaneous use of ciprofloxacin and duloxetine.
In a study on healthy volunteers, it was found that the simultaneous use of drugs containing lidocaine and ciprofloxacin, a moderate inhibitor of the CYP1A2 isoenzyme, leads to a decrease in the clearance of lidocaine by 22% when administered intravenously. Despite the good tolerability of lidocaine, with simultaneous use with ciprofloxacin, side effects may increase due to the interaction.
With the simultaneous use of clozapine and ciprofloxacin at a dose of 250 mg for 7 days, an increase in serum concentrations of clozapine and N-desmethylclozapine by 29% and 31%, respectively, was observed. The patient's condition should be monitored and, if necessary, the dosage regimen of clozapine should be adjusted during its simultaneous use with ciprofloxacin and for a short time after completion of combination therapy. special instructions
In patients with epilepsy or other central nervous system (CNS) disorders (eg, seizures, a history of seizures, reduced cerebral blood flow, changes in brain structure, or after a stroke), ciprofloxacin should only be used if the benefit of such use outweighs the possible risk because the possibility of CNS side effects puts these patients at increased risk.
Undesirable effects on the central nervous system may occur after the first use of ciprofloxacin. Depression or psychosis can in some cases lead to self-harm. In the event of such reactions, treatment with ciprofloxacin should be interrupted immediately.
Ciprofloxacin is not the drug of choice for suspected or established pneumonia caused by Streptococcus pneumoniae.
Cases of crystalluria associated with the use of ciprofloxacin have been reported. Patients receiving ciprofloxacin should be adequately hydrated. Excessive alkalinization of urine should be avoided.
Pseudomembranous colitis is a special form of enterocolitis that can develop while taking antibiotics (in most cases associated with Clostridium difficile). If severe and persistent diarrhea occurs during or after treatment, a doctor's consultation is necessary. Even if an etiological role of Clostridium difficile is suspected, ciprofloxacin should be stopped immediately and appropriate treatment instituted. Antiperistaltic drugs should not be used.
Patients with a hereditary or personal history of a defect in glucose-6-phosphate dehydrogenase are prone to hemolytic reactions when taking quinolones, so ciprofloxacin should be used with caution in such patients. Ciprofloxacin should be used with caution in patients with clinically significant hepatic or renal insufficiency.
Although ciprofloxacin rarely causes photosensitivity, prolonged exposure to direct sunlight or ultraviolet radiation should be avoided during the course of treatment.
Tendon inflammation and rupture (mainly the Achilles tendon is affected) have been described with quinolone treatment. Elderly patients and patients receiving corticosteroids were most commonly affected. If pain or inflammation occurs, treatment with ciprofloxacin should be interrupted and the affected limb should be unloaded.
If symptoms of inflammation occur in the area of ​​the Achilles tendon on one of the limbs, precautions must be taken to prevent rupture of the Achilles tendon on the other limb, i.e. treatment should aim to prevent both tendons from being torn (by using splints or supporting both heels).
Since ciprofloxacin has some activity against Mycobacterium tuberculosis, false-negative culture results may be obtained when sampling during treatment with ciprofloxacin. Ciprofloxacin should be used with caution in patients with myasthenia gravis. The use of ciprofloxacin for indications other than the treatment of pneumonia caused by Pseudomonas aerugenosa associated with cystic fibrosis in children over 5 years of age has not been sufficiently studied, and clinical experience is lacking.
The use of fluoroquinolones is associated with prolongation of the QTc interval. Ciprofloxacin belongs to a group of drugs with a low potential for this adverse event.
Caution must be exercised when using ciprofloxacin in patients at risk of torsades de pointes.
Prolonged and repeated use of ciprofloxacin may lead to superinfection with resistant bacteria or fungal infections. Influence on the ability to manage transport and other mechanisms
During treatment, one should refrain from engaging in potentially hazardous activities that require increased attention and speed of mental and motor reactions. Release form
Film-coated tablets, 250 mg and 500 mg.
10 tablets in PVC/PVDC/A1 foil blisters; 1, 2 or 10 blisters with instructions for use in a cardboard box. Storage conditions
Store at a temperature not exceeding 25°C.
Keep out of the reach of children. Best before date
3 years.
Do not use after the expiry date stated on the packaging. Terms of dispensing from pharmacies
On prescription. Legal entity in whose name the RC is issued:
Teva Pharmaceutical Enterprises Ltd., Israel.

Manufacturer:

Pharmaceutical plant Teva Private Co. Ltd., st. Pallagy 13, H-4042 Debrecen, Hungary. Claim address:
119049, Moscow, st. Shabolovka, 10, building 1.

In this article, you can read the instructions for using the drug Ciprofloxacin. Reviews of site visitors - consumers of this medication, as well as opinions of doctors of specialists on the use of Ciprofloxacin in their practice are presented. A big request to actively add your reviews about the drug: did the medicine help or not help get rid of the disease, what complications and side effects were observed, perhaps not declared by the manufacturer in the annotation. Ciprofloxacin analogues in the presence of existing structural analogues. Use for the treatment of infectious diseases of various organs and systems of the body in adults, children, as well as during pregnancy and lactation.

Ciprofloxacin- a broad-spectrum antimicrobial drug from the group of fluoroquinolones. Acts bactericidal. The drug inhibits the enzyme DNA gyrase of bacteria, as a result of which DNA replication and the synthesis of cellular proteins of bacteria are disrupted. Ciprofloxacin acts both on multiplying microorganisms and on those in the resting phase.

Ciprofloxacin is active against gram-negative and gram-positive aerobic bacteria; intracellular pathogens: Legionella pneumophila, Brucella spp., Chlamydia trachomatis, Listeria monocytogenes, Mycobacterium tuberculosis, Mycobacterium kansasii, Mycobacterium avium-intracellulare. Most methicillin-resistant staphylococci are also resistant to ciprofloxacin.

Streptococcus pneumoniae, Enterococcus faecalis are moderately sensitive to the drug.

Corynebacterium spp., Bacteroides fragilis, Pseudomonas cepacia, Pseudomonas maltophilia, Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides are resistant to the drug.

The effect of the drug against Treponema pallidum has not been studied enough.

Pharmacokinetics

Rapidly absorbed from the gastrointestinal tract. Food intake has little effect on the absorption of ciprofloxacin. Distributed in tissues and body fluids. Penetrates into the cerebrospinal fluid: the concentration of ciprofloxacin in non-inflamed meninges reaches 10%, in inflamed - up to 37%. High concentrations are reached in bile. Excreted in urine and bile.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to the drug:

• respiratory tract;
• ear, throat and nose;
• kidneys and urinary tract;
• genital organs (including gonorrhea, prostatitis);
• gynecological (including adnexitis) and postpartum infections;
• digestive system (including the oral cavity, teeth, jaws);
• gallbladder and biliary tract;
• skin, mucous membranes and soft tissues;
• musculoskeletal system;
• sepsis;
• peritonitis;
• prevention and treatment of infections in patients with reduced immunity (with immunosuppressant therapy).

For topical use:

• acute and subacute conjunctivitis;
• blepharoconjunctivitis;
• blepharitis;
• bacterial ulcers of the cornea;
• keratitis;
• keratoconjunctivitis;
• chronic dacryocystitis;
• meibomites;
• infectious lesions of the eyes after injuries or foreign bodies;
• preoperative prophylaxis in ophthalmic surgery.

Release form

Film-coated tablets 250 mg, 500 mg, 750 mg.

Drops eye and ear 0.3%.

Solution for intravenous administration(injections in ampoules for injections) 2 mg/ml.

Instructions for use and dosage

Tablets

The dose of ciprofloxacin depends on the severity of the disease, type of infection, body condition, age, body weight and kidney function of the patient.

Uncomplicated diseases of the kidneys and urinary tract - 250 mg, in complicated cases - 500 mg 2 times a day.

Diseases of the lower respiratory tract of moderate severity - 250 mg, in more severe cases - 500 mg 2 times a day.

Gynecological diseases, enteritis and colitis with severe course and high fever, prostatitis, osteomyelitis - 500 mg 2 times a day (for the treatment of banal diarrhea can be used at a dose of 250 mg 2 times a day).

The drug should be taken on an empty stomach with a sufficient amount of liquid.

Patients with severe renal impairment should be given a half dose of the drug.

The duration of treatment depends on the severity of the disease, but treatment should always be continued for at least two more days after the symptoms of the disease have disappeared. Usually the duration of treatment is 7-10 days.

The drug should be administered intravenously over 30 minutes (dose 200 mg) and 60 minutes (dose 400 mg). The solution for infusion can be combined with 0.9% sodium chloride solution, Ringer's solution, 5% and 10% dextrose (glucose) solution, 10% fructose solution, a solution containing 5% dextrose solution with 0.225% or 0.45% sodium chloride solution.

The dose of ciprofloxacin depends on the severity of the disease, type of infection, body condition, age, weight and kidney function of the patient.

A single dose is 200 mg, with severe infections - 400 mg. Frequency rate of introduction — 2 times a day; duration of treatment - 1-2 weeks, if necessary, it is possible to increase the course of treatment.

In acute gonorrhea, the drug is administered intravenously once at a dose of 100 mg.

For the prevention of postoperative infections - 30-60 minutes before surgery intravenously at a dose of 200-400 mg.

Side effect

• nausea, vomiting;
• diarrhea;
• stomach ache;
• flatulence;
• anorexia;
• dizziness;
• headache;
• increased fatigue;
• anxiety;
• tremor;
• insomnia;
• "nightmare" dreams;
• peripheral paralgesia (anomaly in the perception of pain);
• sweating;
• increased intracranial pressure;
• depression;
• hallucinations;
• violations of taste and smell;
• visual impairment (diplopia, change in color perception);
• noise in ears;
• hearing loss;
• tachycardia;
• heart rhythm disturbances;
• decrease in blood pressure;
• flushes of blood to the skin of the face;
• leukopenia, granulocytopenia, anemia, thrombocytopenia, leukocytosis, thrombocytosis, hemolytic anemia;
• hematuria (blood in the urine);
• glomerulonephritis;
• urinary retention;
• arthralgia;
• tendon ruptures;
• myalgia;
• skin itching;
• hives;
• the formation of blisters, accompanied by bleeding;
• medicinal fever;
• pinpoint hemorrhages (petechiae);
• swelling of the face or throat;
• dyspnea;
• increased photosensitivity;
• vasculitis;
• nodular erythema;
• pain and burning at the injection site;
• general weakness;
• superinfection (candidiasis, pseudomembranous colitis).

Contraindications

• deficiency of glucose-6-phosphate dehydrogenase;
• pseudomembranous colitis;
• children's age up to 18 years (until the completion of the process of skeletal formation);
• pregnancy;
• lactation period (breastfeeding).

Use during pregnancy and lactation

Ciprofloxacin is contraindicated for use during pregnancy and lactation (breastfeeding).

special instructions

If severe and prolonged diarrhea occurs during or after treatment with ciprofloxacin, the diagnosis of pseudomembranous colitis should be excluded, which requires immediate discontinuation of the drug and the appointment of appropriate treatment.

If pain occurs in the tendons or when the first signs of tendovaginitis appear, treatment should be discontinued.

During the period of treatment with Ciprofloxacin, it is necessary to provide a sufficient amount of fluid while maintaining normal diuresis.

During treatment with Ciprofloxacin, contact with direct sunlight should be avoided.

With the simultaneous intake of alcohol, the hepatotoxic effect of the drug is enhanced.

Influence on the ability to drive vehicles and control mechanisms

Patients taking Ciprofloxacin should be careful when driving a car and engaging in other potentially hazardous activities that require increased attention and speed of psychomotor reactions (especially while drinking alcohol).

drug interaction

Due to a decrease in the activity of microsomal oxidation processes in hepatocytes, ciprofloxacin increases the concentration and lengthens the half-life of theophylline and other xanthines (for example, caffeine), oral hypoglycemic drugs, indirect anticoagulants, and helps to reduce the prothrombin index.

With simultaneous use with non-steroidal anti-inflammatory drugs (with the exception of acetylsalicylic acid), the risk of convulsions increases.

Metoclopramide accelerates the absorption of ciprofloxacin, which leads to a decrease in the time to reach the maximum concentration of the latter.

Co-administration of uricosuric drugs leads to a slowdown in excretion (up to 50%) and an increase in the plasma concentration of ciprofloxacin.

When combined with other antimicrobials (beta-lactam antibiotics, aminoglycosides, clindamycin, metronidazole), synergism is usually observed. Therefore, ciprofloxacin can be successfully used in combination with azlocillin and ceftazidime in infections caused by Pseudomonas spp.; with mezlocillin, azlocillin and other beta-lactam antibiotics - for streptococcal infections; with isoxazolpenicillins and vancomycin - with staphylococcal infections; with metronidazole and clindamycin - for anaerobic infections.

Ciprofloxacin enhances the nephrotoxic effect of cyclosporine, there is also an increase in serum creatinine, so in such patients it is necessary to control this indicator 2 times a week.

When taken simultaneously, Ciprofloxacin enhances the effect of indirect anticoagulants.

Pharmaceutical interaction

The infusion solution of the drug is pharmaceutically incompatible with all infusion solutions and drugs that are physicochemically unstable in an acidic environment (pH of the ciprofloxacin infusion solution is 3.5-4.6). Do not mix the solution for intravenous administration with solutions having a pH greater than 7.

Analogues of the drug Ciprofloxacin

Structural analogues for the active substance:

• Alcipro;
• Aphenoxin;
• Basijen;
• Betaciprol;
• Vero-Ciprofloxacin;
• Zindolin 250;
• Ificipro;
• Quintor;
• Quipro;
• Liprokhin;
• Microflox;
• Oftocypro;
• Recipro;
• Sifloks;
• Tseprov;
• ciloxane;
• Tsipraz;
• Tsiprinol;
• Ciprobay;
• Cyprobid;
• Ciprobrine;
• Cyprodox;
• Ciprolaker;
• Tsiprolet;
• Ciprolon;
• Tsipromed;
• Cypropane;
• Tsiprosan;
• Cyprosin;
• Ciprosol;
• Ciprofloxabol;
• ciprofloxacin bufus;
• Ciprofloxacin-AKOS;
• Ciprofloxacin-Promed;
• Ciprofloxacin-Teva;
• Ciprofloxacin-FPO;
• Cifloxinal;
• Cifran;
• Number OD;
• Ecocyfol.

In the absence of analogues of the drug for the active substance, you can follow the links below to the diseases from which the corresponding drug helps and see the available analogues for the therapeutic effect.

pharmachologic effect

A broad-spectrum antimicrobial agent of the fluoroquinolone group. It has a bactericidal effect. Suppresses DNA gyrase and inhibits the synthesis of bacterial DNA.

Highly active against most gram-negative bacteria: Pseudomonas aeruginosa, Haemophilus influenzae, Escherichia coli, Shigella spp., Salmonella spp., Neisseria meningitidis, Neisseria gonorrhoeae.

Active against Staphylococcus spp. (including strains producing and not producing penicillinase, methicillin-resistant strains), some strains of Enterococcus spp., Campylobacter spp., Legionella spp., Mycoplasma spp., Chlamydia spp., Mycobacterium spp.

Ciprofloxacin is active against bacteria producing β-lactamase.

Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides are resistant to ciprofloxacin. The action against Treponema pallidum has not been studied enough.

Pharmacokinetics

Rapidly absorbed from the gastrointestinal tract. Bioavailability after oral administration is 70%. Food intake has little effect on the absorption of ciprofloxacin. Protein binding

is 20-40%. Distributed in tissues and body fluids. Penetrates into the cerebrospinal fluid: the concentration of ciprofloxacin in non-inflamed meninges reaches 10%, in inflamed - up to 37%. High concentrations are reached in bile. Excreted in urine and bile.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to ciprofloxacin, incl. diseases of the respiratory tract, abdominal cavity and pelvic organs, bones, joints, skin; septicemia; severe infections of the ENT organs. Treatment of postoperative infections. Prevention and treatment of infections in patients with reduced immunity.

For local use: acute and subacute conjunctivitis, blepharoconjunctivitis, blepharitis, bacterial corneal ulcers, keratitis, keratoconjunctivitis, chronic dacryocystitis, meibomitis. Infectious lesions of the eyes after injuries or foreign bodies. Preoperative prophylaxis in ophthalmic surgery.

Contraindications

Pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to ciprofloxacin and other quinolone drugs.

Dosage

Individual. Inside - 250-750 mg 2 times / day. The duration of treatment is from 7-10 days to 4 weeks.

For intravenous administration, a single dose is 200-400 mg, the frequency of administration is 2 times / day; duration of treatment - 1-2 weeks, if necessary, and more. It can be given by intravenous bolus, but drip over 30 minutes is more preferred.

When applied topically, 1-2 drops are instilled into the lower conjunctival sac of the affected eye every 1-4 hours. After the condition improves, the intervals between instillations can be increased.

Maximum daily dose for adults when taken orally is 1.5 g.

Side effects

From the digestive system: nausea, vomiting, diarrhea, abdominal pain, increased activity of hepatic transaminases, alkaline phosphatase, LDH, bilirubin, pseudomembranous colitis.

From the side of the central nervous system: headache, dizziness, fatigue, sleep disturbances, nightmares, hallucinations, fainting, visual disturbances.

From the urinary system: crystalluria, glomerulonephritis, dysuria, polyuria, albuminuria, hematuria, transient increase in serum creatinine.

From the hematopoietic system: eosinophilia, leukopenia, neutropenia, changes in platelet count.

From the side of the cardiovascular system: tachycardia, cardiac arrhythmias, arterial hypotension.

Allergic reactions: pruritus, urticaria, angioedema, Stevens-Johnson syndrome, arthralgia.

Adverse reactions associated with chemotherapeutic action: candidiasis.

Local reactions: soreness, phlebitis (with intravenous administration). When using eye drops, in some cases, mild soreness and hyperemia of the conjunctiva are possible.

Others: vasculitis.

drug interaction

With the simultaneous use of ciprofloxacin with didanosine, the absorption of ciprofloxacin is reduced due to the formation of ciprofloxacin chelators with the aluminum and magnesium buffers contained in didanosine.

With simultaneous use with warfarin, the risk of bleeding increases.

With the simultaneous use of ciprofloxacin and theophylline, it is possible to increase the concentration of theophylline in the blood plasma, increase the T1 / 2 of theophylline, which leads to an increased risk of developing toxic effects associated with theophylline.

Simultaneous administration of antacids, as well as preparations containing aluminum, zinc, iron or magnesium ions, can cause a decrease in the absorption of ciprofloxacin, so the interval between the appointment of these drugs should be at least 4 hours.

special instructions

Dosage adjustments are required in patients with impaired renal function. Use with caution in elderly patients, with atherosclerosis of cerebral vessels, cerebrovascular accidents, epilepsy, convulsive syndrome unclear etiology.

During treatment, patients should receive sufficient fluids.

In case of persistent diarrhea, ciprofloxacin should be discontinued.

With simultaneous intravenous administration of ciprofloxacin and barbiturates, monitoring of heart rate, blood pressure, ECG is necessary. In the process of treatment, it is necessary to control the concentration of urea, creatinine, and hepatic transaminases in the blood.

During the period of treatment, a decrease in reactivity is possible (especially when used simultaneously with alcohol).

Do not administer ciprofloxacin subconjunctivally or directly into the anterior chamber of the eye.

Pregnancy and lactation

Contraindicated in pregnancy, during lactation.

Ciprofloxacin crosses the placental barrier and is excreted in breast milk.

In experimental studies found to cause arthropathy.

Application in childhood

Contraindicated in children and adolescents under 15 years of age.

For impaired renal function

Dosage adjustments are required in patients with impaired renal function.

Use in the elderly

Use with caution in elderly patients.

Description of the drug CIPROFLOXACIN is based on officially approved instructions for use and approved by the manufacturer.

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Ciprofloxacin is a broad-spectrum bactericidal antimicrobial drug from the group of fluoroquinolones.

Release form and composition

• coated/film-coated tablets ( appearance tablets and the form of packaging depend on the manufacturer and the dose of the active substance);
• solution for infusion: clear, colorless or slightly colored liquid (100 ml in vials; the number of vials in a package depends on the manufacturer);
• concentrate for solution for infusion: clear, colorless or slightly greenish-yellow liquid without mechanical impurities (10 ml in vials, 5 vials in a cardboard box);
• eye drops 0.3%: clear liquid, yellowish-greenish or slightly yellow (1 ml, 1.5 ml, 2 ml, 5 ml or 10 ml each in bottles or polyethylene dropper tubes with a valve / screw neck made of polyethylene, 1 bottle, 1 or 5 dropper tubes in a carton box);
• eye and ear drops 0.3%: clear, colorless or slightly yellowish liquid (5 ml each in polymer dropper bottles, 1 bottle in a cardboard pack).

Composition of 1 film-coated tablet:

• active ingredient: ciprofloxacin - 250, 500 or 750 mg;
• auxiliary components: starch 1500 or corn starch, lactose (milk sugar), magnesium stearate, crospovidone, MCC (microcrystalline cellulose), talc;
• shell: the content and quantity of components depend on the manufacturer.

Composition of 1 ml solution for infusion:

• active ingredient: ciprofloxacin (in the form of monohydrate hydrochloride) - 2 mg (2.33 mg);
• auxiliary components: lactic acid, sodium chloride, 1M sodium hydroxide solution, disodium salt of ethylenediaminetetraacetic acid, water for injection.

Composition of 1 ml concentrate for solution for infusion:

• active ingredient: ciprofloxacin (as hydrochloride) - 100 mg (111 mg);
• auxiliary components: disodium edetate dihydrate, lactic acid, hydrochloric acid, sodium hydroxide, water for injection.

Composition of 1 ml eye drops 0.3%:

• auxiliary components: mannitol, disodium edetate, sodium acetate, benzalkonium chloride, acetic acid, water for injection.

Composition of 1 ml eye and ear drops 0.3%:

• active ingredient: ciprofloxacin (in the form of monohydrate hydrochloride) - 3 mg;
• auxiliary components: mannitol, sodium acetate trihydrate, disodium edetate dihydrate, benzalkonium chloride, glacial acetic acid, purified water.

Pharmacological properties

Pharmacodynamics

Ciprofloxacin is a broad-spectrum antimicrobial agent. This quinolone derivative inhibits bacterial DNA gyrase (topoisomerases II and IV, which are responsible for the process of supercoiling of chromosomal DNA around RNA nuclei, which ensures the reading of the necessary genetic information), disrupts DNA production, inhibits the growth and reproduction of bacteria, and leads to pronounced changes in the morphological nature (in including cell membranes and walls) and immediate death of bacterial cells.

The substance has a bactericidal effect against gram-negative microorganisms during the period of division and rest (because it affects not only DNA gyrase, but also provokes lysis of cell walls). Ciprofloxacin affects gram-positive microorganisms only during the division period.

The low toxicity to macroorganism cells is due to the absence of DNA gyrase in them. Against the background of treatment with ciprofloxacin, parallel resistance to other antibiotics that are not included in the group of DNA gyrase inhibitors is not developed. This increases the effectiveness of the drug against bacteria resistant to tetracyclines, aminoglycosides, cephalosporins, penicillins.

Hypersensitivity to ciprofloxacin is characterized by:

• gram-negative aerobic bacteria: enterobacteria (Yersinia spp., Escherichia coli, Vibrio spp., Salmonella spp., Morganella morganii, Shigella spp., Providencia spp., Citrobacter spp., Edwardsiella tarda, Klebsiella spp., Hafnia alvei, Proteus vulgaris, Proteus mirabilis, Serratia marcescens), some intracellular pathogens (Mycobacterium kansasii, Mycobacterium tuberculosis, Legionella pneumophila, Listeria monocytogenes, Brucella spp.);
• Gram-positive aerobic bacteria: Streptococcus spp. (Streptococcus agalactiae, Streptococcus pyogenes), Staphylococcus spp. (Staphylococcus saprophyticus, Staphylococcus aureus, Staphylococcus hominis, Staphylococcus haemolyticus).

Ciprofloxacin is active against Bacillus anthracis. Most staphylococci that are resistant to methicillin show similar resistance to ciprofloxacin. The sensitivity of Mycobacterium avium, Enterococcus faecalis, Streptococcus pneumoniae (localized intracellularly) is moderate: high concentrations of the drug are required to suppress the vital activity of these microorganisms.

The drug has no effect on Nocardia asteroids, Bacteroides fragilis, Clostridium difficile, Ureaplasma urealyticum, Pseudomonas maltophilia, Pseudomonas cepacia. It is also not effective enough against Treponema pallidum.

Resistance develops quite slowly, since ciprofloxacin almost completely destroys persistent microorganisms, and bacterial cells do not have enzymes that inactivate it.

Pharmacokinetics

When taken orally, ciprofloxacin tablets are almost completely and rapidly absorbed from the gastrointestinal tract (mainly in the jejunum and duodenum). Eating inhibits absorption, but does not affect bioavailability and maximum concentration. Bioavailability is 50-85%, and the volume of distribution is 2-3.5 l / kg. Ciprofloxacin binds to plasma proteins by about 20-40%. The maximum level of the substance in the body when taken orally is reached after approximately 60-90 minutes. The maximum concentration is related to the magnitude of the dose taken in a linear relationship and is at doses of 1000, 750, 500 and 250 mg, respectively, 5.4, 4.3, 2.4 and 1.2 μg / ml. 12 hours after ingestion of 750, 500 and 250 mg of ciprofloxacin in plasma decreases to 0.4, 0.2 and 0.1 μg / ml, respectively.

The substance is well distributed in the tissues of the body (excluding tissues enriched with fats, for example, nervous tissue). Its content in tissues is 2-12 times higher than in blood plasma. Therapeutic concentrations are found in the skin, saliva, peritoneal fluid, tonsils, articular cartilage and synovial fluid, bone and muscle tissue, intestines, liver, bile, gallbladder, kidneys and urinary system, abdominal and pelvic organs (uterus, ovaries and fallopian tubes, endometrium), prostate tissues, seminal fluid, bronchial secretions, lung tissue.

Ciprofloxacin penetrates into the cerebrospinal fluid in small concentrations, where its content in the absence of an inflammatory process in the meninges is 6-10% of that in the blood serum, and with existing inflammatory foci - 14-37%.

Ciprofloxacin also penetrates well into the lymph, pleura, eye fluid, peritoneum and through the placenta. Its concentration in blood neutrophils is 2–7 times higher than in blood serum. The compound is metabolized in the liver by about 15-30%, forming inactive metabolites (formylciprofloxacin, diethylciprofloxacin, oxocyprofloxacin, sulfocyprofloxacin).

The half-life of ciprofloxacin is about 4 hours, with chronic renal failure increasing to 12 hours. It is excreted mainly through the kidneys through tubular secretion and tubular filtration in unchanged form (40-50%) and as metabolites (15%), the rest is excreted through the gastrointestinal tract. A small amount of ciprofloxacin is excreted in breast milk. Renal clearance is 3–5 ml/min/kg and total clearance is 8–10 ml/min/kg.

In chronic renal failure (CC more than 20 ml / min), the degree of excretion of ciprofloxacin through the kidneys decreases, but it does not accumulate in the body due to a compensatory increase in the metabolism of this substance and its excretion through the gastrointestinal tract.

When conducting an intravenous infusion of the drug at a dose of 200 mg, the maximum concentration of ciprofloxacin, which is 2.1 μg / ml, is reached after 60 minutes. After intravenous administration, the content of ciprofloxacin in the urine during the first 2 hours after infusion is almost 100 times higher than in blood plasma, which significantly exceeds the minimum inhibitory concentration for most pathogens of urinary tract infections.

When applied topically, ciprofloxacin penetrates well into the tissues of the eye: the anterior chamber and the cornea, especially when the corneal epithelial cover is damaged. When it is damaged, the substance accumulates in it in concentrations capable of destroying most pathogens of corneal infections.

After a single instillation, the content of ciprofloxacin in the moisture of the anterior chamber of the eye is determined after 10 minutes and is 100 μg / ml. The maximum concentration of the compound in the moisture of the anterior chamber is reached after 1 hour and is equal to 190 µg/ml. After 2 hours, the concentration of ciprofloxacin begins to decrease, however, its antibacterial effect in the tissues of the cornea is prolonged and lasts for 6 hours, in the moisture of the anterior chamber - up to 4 hours.

After instillation, systemic absorption of ciprofloxacin may occur. When it is used in the form of eye drops 4 times a day in both eyes for 7 days, the average concentration of the substance in the blood plasma does not exceed 2–2.5 ng / ml, and the maximum concentration is less than 5 ng / ml.

Indications for use

Systemic use (tablets, solution for infusion, concentrate for solution for infusion)

In adult patients, Ciprofloxacin is used for the treatment and prevention of infectious and inflammatory diseases caused by susceptible microorganisms:

• bronchitis (chronic in the acute stage and acute), bronchiectasis, pneumonia, cystic fibrosis and other respiratory tract infections;
• frontal sinusitis, sinusitis, pharyngitis, otitis media, sinusitis, tonsillitis, mastoiditis and other infections of the upper respiratory tract;
• pyelonephritis, cystitis and other infections of the kidneys and urinary tract;
• adnexitis, gonorrhea, prostatitis, chlamydia and other infections of the pelvic organs and genital organs;
• bacterial lesions of the gastrointestinal tract (gastrointestinal tract), bile ducts, intraperitoneal abscess and other infections of the abdominal organs;
• ulcerative infections, burns, abscesses, wounds, phlegmon and other infections of the skin and soft tissues;
• septic arthritis, osteomyelitis and other infections of bones and joints;
• surgical operations (to prevent infection);
• pulmonary form of anthrax (for prevention and therapy);
• infections against the background of immunodeficiency arising from therapy with immunosuppressive drugs or with neutropenia.

For children aged 5 to 17 years, systemically Ciprofloxacin is prescribed for cystic fibrosis of the lungs for the treatment of complications caused by Pseudomonas aeruginosa, as well as for the prevention and treatment of the pulmonary form of anthrax (Bacillus anthracis).

A solution for infusion and a concentrate for preparing a solution for infusion are also used for eye infections and severe general infection of the body - sepsis.

Tablets are prescribed for SDC (selective intestinal decontamination) for patients with reduced immunity.

Topical application (eye drops, eye and ear drops)

Ciprofloxacin drops are used to treat and prevent the following infectious inflammations caused by microorganisms sensitive to ciprofloxacin:

• ophthalmology (eye drops, eye and ear drops): blepharitis, subacute and acute conjunctivitis, blepharoconjunctivitis, keratitis, keratoconjunctivitis, meibomitis (barley), chronic dacryocystitis, bacterial corneal ulcer, bacterial eye damage due to trauma or foreign bodies, perioperative prevention of infection in ophthalmic surgery;
• otorhinolaryngology (eye and ear drops): otitis externa, treatment of infectious complications in the postoperative period.

Contraindications

Systemic application

Absolute:

• co-administration with tizanidine;
• pseudomembranous colitis;
• pregnancy and breastfeeding period;
• children and adolescents under 18 years of age, except for cases of treatment and prevention of the pulmonary form of anthrax (Bacillus anthracis), as well as the treatment of complications caused by Pseudomonas aeruginosa (Pseudomonas aeruginosa) in children with cystic fibrosis of the lungs aged 5 to 17 years;
• lactase deficiency, lactose intolerance, glucose-galactose malabsorption (for tablets);
• increased individual sensitivity to Ciprofloxacin, other fluoroquinolones and auxiliary ingredients of the drug.

Relative: systemically Ciprofloxacin is used with caution in severe cerebral atherosclerosis, cerebrovascular accident, mental illness, epilepsy, severe renal / hepatic insufficiency, in the elderly, with a history of tendon lesions during fluoroquinolone therapy. The solution for infusion (additionally) is used with caution at an increased risk of prolongation of the QT interval / development of arrhythmias such as torsade de pointes, including heart failure, bradycardia, myocardial infarction, congenital long QT interval syndrome and electrolyte imbalance (hypokalemia, hypomagnesemia).

Local application

Absolute contraindications to the local use of ciprofloxacin:

• ophthalmomycoses and viral eye lesions;
• pregnancy and breastfeeding period (for eye instillations);
• age up to 1 year (for eye instillations);
• increased individual sensitivity to the components.

The use of the drug in otorhinolaryngology (eye and ear drops) during pregnancy and during breastfeeding is permissible only if the possible benefit of therapy for the mother justifies the potential risk to the fetus or child.

Instructions for use Ciprofloxacin: method and dosage

After the disappearance clinical symptoms diseases and normalization of body temperature, Ciprofloxacin therapy is continued for at least 3 more days.

Film-coated/coated tablets

Ciprofloxacin tablets are taken orally after a meal, swallowed whole with a small amount of liquid. Taking tablets on an empty stomach accelerates the absorption of the active substance.

Dosage according to disease/condition:

• urinary tract infections: twice a day, 250-500 mg for a course of 7 to 10 days;
• chronic prostatitis: twice a day, 500 mg for 28 days;
• uncomplicated gonorrhea: 250–500 mg once;
• gonococcal infection in combination with chlamydia and mycoplasmosis: twice a day (1 time in 12 hours), 750 mg in a course of 7 to 10 days;
• chancroid: twice a day, 500 mg for several days;
• meningococcal carriage in the nasopharynx: 500-750 mg once;
• chronic carriage of salmonella: twice a day, 500 mg (if necessary, increase to 750 mg) for up to 28 days;
• severe infections (recurrent cystic fibrosis, infections of the abdominal cavity, bones, joints) caused by pseudomonads or staphylococci, acute pneumonia caused by streptococci, chlamydial infections of the urinary tract: twice a day (1 time in 12 hours) at a dose of 750 mg (a course of osteomyelitis therapy can last up to 60 days);
• infections of the gastrointestinal tract caused by Staphylococcus aureus: twice a day (1 time at 12 noon) at a dose of 750 mg for a course of 7 to 28 days;
• complications caused by Pseudomonas aeruginosa in children aged 5–17 years with cystic fibrosis of the lungs: twice a day, 20 mg / kg (maximum daily dose - 1500 mg) for a course of 10 to 14 days;
• pulmonary form of anthrax (treatment and prevention): twice a day for children, 15 mg / kg, adults - 500 mg ( maximum doses: single - 500 mg, daily - 1000 mg), course of treatment - up to 60 days, the drug should be started immediately after infection (suspected or confirmed).

The maximum daily dose of ciprofloxacin in renal failure:

• creatinine clearance (CC) 31-60 ml / min / 1.73 m2 or serum creatinine concentration 1.4-1.9 mg / 100 ml - 1000 mg;
• QC< 30 мл/мин/1,73 м2 или сывороточная концентрация креатинина >2 mg / 100 ml - 500 mg.

Patients on hemo- or peritoneal dialysis should take the tablets after the dialysis session.

Elderly patients require a dose reduction of 30%.

Solution for infusion, concentrate for solution for infusion

The drug is administered intravenously by drip, slowly, into a large vein, this reduces the risk of complications at the injection site. With the introduction of 200 mg of ciprofloxacin, the infusion lasts 30 minutes, 400 mg - 60 minutes.

The concentrate for solution for infusion must be diluted before use to a minimum volume of 50 ml in the following infusion solutions: 0.9% sodium chloride solution, Ringer's solution, 5% or 10% dextrose solution, 10% fructose solution, 5% dextrose solution with 0.225 -0.45% sodium chloride solution.

The solution for infusion is administered alone or together with compatible solutions for infusion: 0.9% sodium chloride solution, Ringer's solution and Ringer's Lactate, 5% or 10% dextrose solution, 10% fructose solution, 5% dextrose solution with 0.225–0.45 % sodium chloride solution. The solution obtained after mixing should be used as soon as possible in order to maintain its sterility.

In case of unconfirmed compatibility with another solution / drug substance, Ciprofloxacin infusion solution is administered separately. Visible signs of incompatibility are precipitation, turbidity or discoloration of the liquid. The pH of Ciprofloxacin infusion solution is 3.5-4.6, so it is incompatible with all solutions/drugs that are physically or chemically unstable at these pH values ​​(heparin solution, penicillins), especially with agents that change pH values to the alkaline side. Due to the storage of the solution at low temperatures, the formation of a precipitate soluble at room temperature is possible. It is not recommended to store the solution for infusion in the refrigerator and freeze it, since only a clean and clear solution is suitable for use.

• respiratory tract infections: depending on the patient's condition and the severity of the infection - 2 or 3 times a day, 400 mg;
• infections of the genitourinary system: acute, uncomplicated - 2 times a day from 200 to 400 mg, complicated - 2 or 3 times a day, 400 mg;
• adnexitis, chronic bacterial prostatitis, orchitis, epididymitis: 2 or 3 times a day, 400 mg;
• diarrhea: 2 times a day, 400 mg;
• other infections listed in the section "Indications for use": 2 times a day, 400 mg;
• severe life-threatening infections, especially those caused by Staphylococcus spp., Pseudomonas spp., Streptococcus spp., including pneumonia caused by Streptococcus spp., peritonitis, bone and joint infections, septicemia, recurrent infections in cystic fibrosis: 400 mg 3 times a day ;
• pulmonary (inhalation) form of anthrax: 2 times a day, 400 mg in a course of 60 days (for therapy and prevention).

Correction of the dose of ciprofloxacin in elderly patients is carried out downward, depending on the severity of the course of the disease and the CC index.

For the treatment of complications in cystic fibrosis of the lungs caused by Pseudomonas aeruginosa in children aged 5-17 years, a dose of 10 mg / kg (maximum daily - 1200 mg) is recommended 3 times a day for a course of 10-14 days. For the treatment and prevention of the pulmonary form of anthrax, 2 infusions per day of 10 mg / kg of ciprofloxacin are recommended (maximum single - 400 mg, daily - 800 mg), course - 60 days.

The maximum daily dose of ciprofloxacin in renal failure:

• creatinine clearance (CC) 31-60 ml / min / 1.73 m2 or serum creatinine concentration 1.4-1.9 mg / 100 ml - 800 mg;
• QC< 30 мл/мин/1,73 м2 или сывороточная концентрация креатинина >2 mg / 100 ml - 400 mg.

For patients on hemodialysis, ciprofloxacin is administered immediately after the session.

Average duration of therapy:

• acute uncomplicated gonorrhea - 1 day;
• infections of the kidneys, urinary tract and abdominal cavity - up to 7 days;
• osteomyelitis - no more than 60 days;
• streptococcal infections (due to the risk of late complications) - at least 10 days;
• infections against the background of immunodeficiency arising from therapy with immunosuppressive drugs - during the entire period of neutropenia;
• other infections - 7-14 days.

Eye drops, eye and ear drops

In ophthalmic practice, Ciprofloxacin drops (eye, eye and ear) are instilled into the conjunctival sac.

Instillation regimen depending on the type of infection and the severity of the inflammatory process:

• acute bacterial conjunctivitis, blepharitis (simple, scaly and ulcerative), meibomitis: 1-2 drops 4-8 times a day for 5-14 days;
• keratitis: 1 drop from 6 times a day for a course of 14–28 days;
• bacterial corneal ulcer: 1st day - 1 drop every 15 minutes for the first 6 hours of treatment, then during waking hours, 1 drop every 30 minutes; 2nd day - during waking hours, 1 drop every hour; 3-14th days - during waking hours, 1 drop every 4 hours. If epithelialization has not occurred after 14 days of therapy, treatment is allowed to continue for another 7 days;
• acute dacryocystitis: 1 drop 6-12 times a day for a course of no more than 14 days;
• eye injuries, including the ingress of foreign bodies (prevention of infectious complications): 1 drop 4–8 times a day for a course of 7–14 days;
• preoperative preparation: 1 drop 4 times a day for 2 days before surgery, 1 drop 5 times with an interval of 10 minutes immediately before surgery;
• postoperative period (prevention of infectious complications): 1 drop 4-6 times a day for the entire period, usually from 5 to 30 days.

In otorhinolaryngology, the drug (eye and ear drops) is instilled into the external ear canal after carefully cleaning it.

Recommended dosage regimen: 2-4 times a day (or more often, as needed) 3-4 drops. The duration of therapy should not exceed 5-10 days, except in cases where the local flora is sensitive, then an extension of the course is allowed.

For the procedure, it is recommended to bring the solution to room temperature or body temperature to avoid vestibular stimulation. The patient should lie on the side opposite the diseased ear and remain in this position for 5-10 minutes after instillation.

Sometimes, after local cleansing of the external auditory canal, it is allowed to put a cotton swab moistened with a solution of Ciprofloxacin into the ear and keep it there until the next instillation.

Side effects

Systemic application

• digestive system: nausea / vomiting, diarrhea, flatulence, abdominal pain, loss of appetite and reduced food intake, cholestatic jaundice (especially in patients with a history of liver disease), hepatitis, hepatonecrosis;
• nervous system: headache, dizziness, migraine, anxiety, fatigue, tremor, heavy dreams (nightmares), insomnia, peripheral paralgesia, hyperhidrosis, cerebral artery thrombosis, increased intracranial pressure, fainting, depression, confusion, hallucinations, other manifestations psychotic reactions, occasionally progressing to states in which the patient is able to harm himself;
• sensory organs: impaired sense of smell and taste, impaired vision (change in color perception, diplopia), noise and ringing in the ears, hearing impairment up to its loss;
• cardiovascular system: cardiac arrhythmias, tachycardia, decrease in blood pressure; for the solution additionally - vasodilation, benign intracranial hypertension, cardiovascular collapse;
• hematopoietic system: anemia, leukopenia, thrombocytopenia, granulocytopenia, leukocytosis, hemolytic anemia, thrombocytosis, depression of bone marrow hematopoiesis, pancytopenia;
• laboratory indicators: increased activity of liver enzymes, hyperglycemia, hypoglycemia, hypoprothrombinemia, hyperbilirubinemia, hypercreatininemia;
• urinary system: crystalluria, hematuria, glomerulonephritis, urinary retention, dysuria, polyuria, albuminuria, urethral bleeding, interstitial nephritis, decreased nitrogen excretion of the kidneys;
• musculoskeletal system: arthritis, arthralgia, tendovaginitis, myalgia, tendon ruptures;
• hypersensitivity reactions: shortness of breath, urticaria, pruritus, photosensitivity, angioedema, wheals (accompanied by bleeding), small nodules (forming scabs), petechiae (pinpoint hemorrhages on the skin), drug fever, swelling of the face/larynx, eosinophilia, vasculitis, nodular erythema, erythema multiforme exudative (including Stevens-Johnson syndrome), Lyell's syndrome (toxic epidermal necrolysis);
• other reactions: superinfections (including candidiasis), asthenia, flushing of the face;
• local reactions (for solution): swelling, soreness and phlebitis at the injection site.

In case of aggravation of the above or the manifestation of any other adverse reactions not indicated in the instructions, it is necessary to seek the advice of a doctor.

Local application

• hypersensitivity reactions: burning and itching, hyperemia and slight soreness of the conjunctiva (when instilled into the eyes) or in the area of ​​the outer ear and tympanic membrane (when instilled into the ear), the development of superinfection;
• other reactions (when instilled into the eyes): nausea, an unpleasant aftertaste in the mouth immediately after instillation, photophobia, swelling of the eyelids, lacrimation, sensation of a foreign body in the eye, decreased visual acuity, white crystalline precipitate (formed in patients with corneal ulcer), keratopathy , keratitis, corneal spotting/corneal infiltration.

Overdose

Symptoms of an overdose of ciprofloxacin when taken orally or intravenously are nausea, vomiting, mental agitation, clouded consciousness.

The specific antidote is unknown. When taking the drug inside, it is recommended to do a gastric lavage. It is also necessary to carefully monitor the patient's condition, if necessary, resort to measures emergency care and ensure that a large amount of fluid enters the body. Through hemo- or peritoneal dialysis, only a small (less than 10%) amount of ciprofloxacin is excreted.

Cases of overdose of Ciprofloxacin when applied topically have not been registered. When taken randomly medicinal product inside, the occurrence of overdose symptoms is unlikely, since the content of ciprofloxacin in 1 bottle of drops is negligible and amounts to only 15 mg at a maximum daily dose for adult patients of 1000 mg, for children - 500 mg. However, in case of inadvertent ingestion of the drug, you should consult your doctor.

special instructions

Systemic application

For the treatment of suspected / established pneumonia caused by Streptococcus pneumoniae pneumococcus, Ciprofloxacin is not the drug of choice.

In the event of prolonged severe diarrhea during or after therapy, the presence of pseudomembranous colitis should be ruled out, which requires immediate withdrawal of the drug and appropriate treatment.

Pain that appears in the tendons, or the first signs of tendovaginitis require immediate discontinuation of therapy, there are separate reports of inflammation and even rupture of the tendons during the use of fluoroquinolones.

During therapy with Ciprofloxacin, it is recommended to avoid intense artificial ultraviolet radiation and direct sunlight, and in case of a photosensitivity reaction (burn-like skin rashes), stop taking the drug.

With prolonged therapy, regular monitoring of the complete blood count and kidney / liver function is required.

Ciprofloxacin solution and concentrate contains sodium chloride, which should be taken into account in patients limiting sodium intake (with heart and kidney failure, nephrotic syndrome).

During treatment, due to the possibility of developing undesirable effects from the nervous system, such as dizziness, convulsions, drowsiness, caution is required when administering vehicles and complex machinery and engaging in other potentially hazardous activities.

Local application

Eye drops and ear drops (eye drops) are not intended for intraocular injection.

With the simultaneous use of Ciprofloxacin drops with other ophthalmic drugs, the interval between injections should be at least 5 minutes.

If any symptoms of hypersensitivity appear, the use of drops must be discontinued.

In the case of conjunctival hyperemia observed for a long time or increasing due to Ciprofloxacin therapy, stop using the drops and consult a doctor.

The use of soft contact lenses in conjunction with the use of ciprofloxacin drops is not recommended. When wearing hard contact lenses, they should be removed before instillation and reinserted 15–20 minutes after instillation.

Due to the possible blurring of visual perception as a result of instillation of the drug, it is recommended to start working with complex mechanisms and driving vehicles 15 minutes after the procedure.

Use during pregnancy and lactation

According to the instructions, Ciprofloxacin is contraindicated during pregnancy and lactation, as it penetrates the placental barrier and into breast milk. Studies have confirmed that the drug can provoke the development of arthropathy.

drug interaction

Due to the high pharmacological activity of Ciprofloxacin and the risk of adverse effects of drug interactions, the decision on the possible joint admission with other medicinal substances / preparations is taken by the attending physician.

Analogues of Ciprofloxacin in the form of tablets: Quintor, Procipro, Ceprova, Tsiprinol, Tsiprobay, Tsiprobid, Tsiprodox, Tsiprolet, Tsipropan, Tsifran, etc.

Analogues of solution for infusions and concentrate for solution for infusions Ciprofloxacin: Basigen, Ificipro, Quintor, Protsipro, Ceprova, Tsiprinol, Tsiprobid, etc.

Analogues of eye / eye and ear drops Ciprofloxacin: Betaciprol, Rocip, Tsiprolet, Ciprolon, Tsipromed, Ciprofloxacin-AKOS.

Terms and conditions of storage

Store in a dry, dark place at temperatures up to 25 ° C, infusion solution, concentrate and drops - do not freeze. Keep away from children.

Shelf life of tablets is from 2 to 5 years (depending on the manufacturer), solution and concentrate - 2 years, eye / eye and ear drops - 3 years.

After opening the bottle, eye and ear drops should be stored for no more than 28 days, eye drops - no more than 14 days.

Terms of dispensing from pharmacies

Ciprofloxacin in any form of release is dispensed by prescription.

Ciprofloxacin (ciprofloxacin)
- ciprofloxacin (as hydrochloride) (ciprofloxacin)

Composition and form of release of the drug

Film-coated tablets white or almost white, oval, notched, biconvex; in cross section, the nucleus is white to slightly yellowish.

Excipients: corn starch - 10.8 mg, pregelatinized corn starch - 90 mg, microcrystalline cellulose - 129.3 mg, crospovidone - 23.1 mg, magnesium stearate - 11.4 mg, lactose monohydrate - 39.9 mg, talc - 22.2 mg.

Auxiliary substances of the film shell: hypromellose - 17.34 mg, polyethylene glycol 6000 - 7.32 mg, titanium dioxide - 2.67 mg, polysorbate 80 - 2.67 mg.

5 pieces. - cellular contour packings (1) - packs of cardboard.
5 pieces. - cellular contour packings (2) - packs of cardboard.
5 pieces. - cellular contour packings (4) - packs of cardboard.
10 pieces. - cellular contour packings (1) - packs of cardboard.
10 pieces. - cellular contour packings (2) - packs of cardboard.
10 pieces. - cans (1) - packs of cardboard.
20 pcs. - cans (1) - packs of cardboard.

pharmachologic effect

A broad-spectrum agent of the fluoroquinolone group. It has a bactericidal effect. Suppresses DNA gyrase and inhibits the synthesis of bacterial DNA.

Highly active against most gram-negative bacteria: Pseudomonas aeruginosa, Haemophilus influenzae, Escherichia coli, Shigella spp., Salmonella spp., Neisseria meningitidis, Neisseria gonorrhoeae.

Active against Staphylococcus spp. (including strains producing and not producing penicillinase, methicillin-resistant strains), some strains of Enterococcus spp., Campylobacter spp., Legionella spp., Mycoplasma spp., Chlamydia spp., Mycobacterium spp.

Ciprofloxacin is active against bacteria producing β-lactamase.

Ureaplasma urealyticum, Clostridium difficile, Nocardia asteroides are resistant to ciprofloxacin. The action against Treponema pallidum has not been studied enough.

Pharmacokinetics

Rapidly absorbed from the gastrointestinal tract. Bioavailability after oral administration is 70%. Food intake has little effect on the absorption of ciprofloxacin. Protein binding is 20-40%. Distributed in tissues and body fluids. Penetrates into the cerebrospinal fluid: the concentration of ciprofloxacin in non-inflamed meninges reaches 10%, in inflamed - up to 37%. High concentrations are reached in bile. Excreted in urine and bile.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to ciprofloxacin, incl. diseases of the respiratory tract, abdominal cavity and pelvic organs, bones, joints, skin; septicemia; severe infections of the ENT organs. Treatment of postoperative infections. Prevention and treatment of infections in patients with reduced immunity.

For local use: acute and subacute conjunctivitis, blepharoconjunctivitis, blepharitis, bacterial corneal ulcers, keratitis, keratoconjunctivitis, chronic dacryocystitis, meibomitis. Infectious lesions of the eyes after injuries or foreign bodies. Preoperative prophylaxis in ophthalmic surgery.

Contraindications

Pregnancy, lactation (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to ciprofloxacin and other quinolone drugs.

Dosage

Individual. Inside - 250-750 mg 2 times / day. Duration of treatment - from 7-10 days to 4 weeks.

For intravenous administration, a single dose is 200-400 mg, the frequency of administration is 2 times / day; duration of treatment - 1-2 weeks, if necessary, and more. It can be given by intravenous bolus, but drip over 30 minutes is more preferred.

When applied topically, 1-2 drops are instilled into the lower conjunctival sac of the affected eye every 1-4 hours. After the condition improves, the intervals between instillations can be increased.

Maximum daily dose for adults when taken orally is 1.5 g.

Side effects

From the digestive system: nausea, vomiting, diarrhea, increased activity of hepatic transaminases, alkaline phosphatase, LDH, bilirubin, pseudomembranous colitis.

From the side of the central nervous system: headache, dizziness, fatigue, sleep disturbances, nightmares, hallucinations, fainting, visual disturbances.

From the urinary system: crystalluria, glomerulonephritis, dysuria, polyuria, albuminuria, hematuria, transient increase in serum creatinine.

From the hematopoietic system: eosinophilia, leukopenia, neutropenia, changes in platelet count.

From the side of the cardiovascular system: tachycardia, rhythm disturbances, arterial hypotension.

Allergic reactions: pruritus, urticaria, angioedema, Stevens-Johnson syndrome, arthralgia.

Adverse reactions associated with chemotherapeutic action: candidiasis.

Local reactions: soreness, phlebitis (with intravenous administration). When using eye drops, in some cases, mild soreness and hyperemia of the conjunctiva are possible.

Others: vasculitis.

drug interaction

With the simultaneous use of ciprofloxacin with didanosine, the absorption of ciprofloxacin is reduced due to the formation of ciprofloxacin chelators with the aluminum and magnesium buffers contained in didanosine.

With simultaneous use with increases the risk of bleeding.

With the simultaneous use of ciprofloxacin and theophylline, it is possible to increase the concentration of theophylline in the blood plasma, increase T 1/2, which leads to an increased risk of developing toxic effects associated with theophylline.

Simultaneous administration of antacids, as well as preparations containing aluminum, zinc, iron or magnesium ions, can cause a decrease in the absorption of ciprofloxacin, so the interval between the appointment of these drugs should be at least 4 hours.

special instructions

Dosage adjustments are required in patients with impaired renal function. Use with caution in elderly patients, with cerebral atherosclerosis, cerebrovascular accidents, epilepsy, convulsive syndrome of unclear etiology.

During treatment, patients should receive sufficient fluids.

In case of persistent diarrhea, ciprofloxacin should be discontinued.

With simultaneous intravenous administration of ciprofloxacin and barbiturates, monitoring of heart rate, blood pressure, ECG is necessary. In the process of treatment, it is necessary to control the concentration of urea, creatinine, and hepatic transaminases in the blood.

During the period of treatment, a decrease in reactivity is possible (especially when used simultaneously with alcohol).

Do not administer ciprofloxacin subconjunctivally or directly into the anterior chamber of the eye.

Use with caution in elderly patients.

Ciprofloxacin is able to effectively suppress the growth and reproduction of many pathogenic ( pathogenic) microorganisms. Some Gram-positive ( streptococci, staphylococci, enterococci) and Gram-negative bacteria ( Proteus, Shigella, Klebsiella, Enterobacter, Escherichia coli, Citrobacter, Serratia, etc.).

Release forms of ciprofloxacin

Also, ciprofloxacin has a huge number of analogues - Alcipro, Quintor, Tsifran, Tsiprolet, Tsipreks, Tsipraz, Tsiprinol, Tsiprobid, Tsipraded, Tsiprolon, Microflox, Tseprova, Tsiprosin, Tsiprobay, Betaciprol, Tsipronat, Ifitsipro, etc.

Manufacturers of ciprofloxacin

The mechanism of the therapeutic action of the drug

Ciprofloxacin inhibits a special bacterial enzyme DNA gyrase, which is responsible for the spiralization of genetic material ( DNA) microorganism. In the future, there is a violation of DNA synthesis, which leads to a cessation of growth and reproduction. Also, ciprofloxacin affects the cell wall of microbes, causing pronounced changes in it, which leads to rapid death ( lysis) microorganisms.

Ciprofloxacin has a fairly low toxicity to body tissues. Stability ( resistance) microorganisms to ciprofloxacin develops very slowly. This is due to the fact that after taking this antibiotic, almost all pathogens die, and also due to the fact that bacteria do not have enzymes that would be able to neutralize the effect of ciprofloxacin. This makes it highly effective against microorganisms that are resistant to antibiotics such as penicillins, cephalosporins, tetracyclines, etc.

Ciprofloxacin tablets are quickly and completely absorbed in the mucosa of the digestive tract ( especially in the duodenum and jejunum). To some extent slows down the absorption of the antibiotic food intake. Ciprofloxacin is able to penetrate into almost all tissues and body fluids. Ciprofloxacin is metabolized in the liver, and excreted through the kidneys and through the gastrointestinal tract. It should be noted that ciprofloxacin can, to a certain extent, cross the placenta and also pass into breast milk. Ciprofloxacin to some extent affects the central nervous system and therefore, during treatment with this antibiotic, it is worth refusing to drive a car or work with mechanisms due to a decrease in the reaction rate.

For what pathologies is it prescribed?

The use of ciprofloxacin

How to apply the medication?

Intravenous administration of ciprofloxacin is carried out at a dosage of 200 - 400 milligrams. The frequency of administration of the drug is twice a day. The duration of treatment is selected based on the pathology and, as a rule, is 7-15 days. If necessary, the course of treatment with ciprofloxacin can be extended. Ciprofloxacin can be administered both by bolus and drip for 30 minutes ( the last way is the most preferred).

Ciprofloxacin eye drops are instilled 1-2 drops under the lower eyelid every 2-4 hours. In the future, with the improvement of the condition, the intervals between instillation are gradually increased. The course of treatment depends on the type of eye disease.

If the patient has impaired liver function, the dosage does not change. In case of impaired renal function, the dosage of this antibiotic should be changed. The required dosage is selected taking into account creatinine clearance ( the rate at which creatinine is excreted from the body by the kidneys).

Dosage of ciprofloxacin depending on creatinine clearance

It should be noted that the elderly should reduce the single and daily dosage by 25-30%.

Possible side effects

While taking ciprofloxacin, the following side effects may be detected:

• disorders of the nervous system and sensory organs;
• disorders of the cardiovascular system;
• disorders of the gastrointestinal tract;
• violations of the hematopoietic system;
• disorders of the urinary system;
• allergic manifestations;
• other manifestations.

Disorders of the nervous system and sensory organs

There are the following side effects:

• taste disorders;
• smell disorders;
• visual impairment ( double vision);
• hearing loss;
• dizziness;
• anxiety;
• fatigue;
• impaired coordination of movements;
• fear;
• boost ;
• convulsions;
• tremor;
• thrombosis of cerebral arteries;
• peripheral paralgesia.

Thrombosis of the cerebral arteries It is characterized by blockage by a thrombus of the arteries that feed the brain. In the future, thrombosis leads to a partial or complete cessation of blood supply to brain tissues, which can cause a stroke. It should be noted that this violation is extremely rare.

Peripheral paralgesia is an abnormal perception of the feeling of pain. Pain may be overly pronounced or, conversely, there may be no pain at all when the nerve is irritated.

Cardiovascular disorders

Ciprofloxacin can lead to the following disorders from the cardiovascular system:

• heartbeat;
• heart rhythm disturbances;
• hypotension.

Heart rhythm disorders is a violation of the rhythm and frequency of contractions of the heart muscle. Most often, sinus tachycardia is observed, which is characterized by an increase in the number of heartbeats over 100 beats per minute.

liver necrosis characterized by complete destruction of a certain part of the liver cells. In the future, a scar is formed at the site of the dead liver cells ( connective tissue).

Hematopoietic system disorders

On the part of the hematopoietic system, the following side effects may be detected:

• leukopenia;
• leukocytosis.

Anemia(anemia) is a syndrome in which there is a decrease in the total number of red blood cells ( red blood cells) and hemoglobin ( special protein that carries oxygen and carbon dioxide). Anemia is characterized by symptoms such as weakness, pallor of the skin, changes in taste preferences ( addiction to salty, peppery and spicy foods), headache, dizziness, hair and nail damage. In rare cases, ciprofloxacin can lead to hemolytic anemia, in which there is an increased breakdown of red blood cells. With this anemia, a large amount of unbound bilirubin is released, which, being distributed throughout the body, stains the skin and mucous membranes in yellow (jaundice).

Thrombocytopenia- a decrease in the total number of platelets or platelets. These platelets play a critical role in the normal coagulation process ( coagulation) blood. With a lack of platelets in the blood, bleeding gums appear, as well as bleeding from the nasal passages. Quite often, with minor mechanical damage, large bruises appear on the skin. Thrombocytopenia subjectively does not affect the general condition in any way, but can cause massive internal bleeding.

Leukocytosis is an increase in the total number of white blood cells in the blood. In addition to reducing white blood cells, ciprofloxacin may also increase them. Leukocytosis during treatment with ciprofloxacin appears in isolated cases.

Urinary system disorders

In some cases, due to the use of ciprofloxacin, the following side effects may be detected:

• hematuria;
• crystalluria;
• dysuria;
• polyuria;
• albuminuria;

Hematuria characterized by the detection of red blood cells in the urine with the naked eye ( gross hematuria). With hematuria, the color of the urine changes to red or reddish. Hematuria occurs due to deformation of the renal glomeruli, through which erythrocytes are normally ( red blood cells) are unable to penetrate.

crystalluria is a pathology in which salt crystals form in the urine. Crystalluria occurs when the dissolved salts found in the urine precipitate ( form crystals) under the action of metabolites of ciprofloxacin.

Dysuria is a violation of the process of urination. Dysuria is characterized by frequent and painful urination.

Polyuria represents an increased production of urine ( over 1.7 - 2 liters). This pathological condition occurs due to damage to the renal tubules through which it is reabsorbed ( reabsorbed into the blood) less water.

Albuminuria or proteinuria - increased excretion of protein in the urine. Albuminuria occurs due to degenerative disorders in the renal glomeruli. It is worth noting that in some cases this condition can be caused by increased physical activity, and also appear with a protein diet.

Glomerulonephritis is an inflammation of the kidney tissue with damage to the nephrons ( renal glomeruli). This kidney disease is characterized by the appearance of protein and red blood cells in the urine. Glomerulonephritis is an autoimmune disease in which immune complexes attack one's own glomeruli, causing them to become inflamed. In rare cases, the cause of glomerulonephritis may be long-term use of high doses of ciprofloxacin.

Allergic manifestations

Ciprofloxacin can cause the following types drug allergy:

• Lyell's syndrome;
• Stevens-Johnson syndrome;
• eosinophilia;
• photosensitivity;

Stevens-Johnson syndrome is a very severe form of erythema ( pronounced redness of the skin due to the expansion of small vessels of the skin). Given pathological condition the skin, mucous membranes of the eyes, pharynx, mouth and genitals are affected. At the beginning of an allergic reaction, severe pain appears in large joints, then a fever appears, after which blisters appear on the body, which, when opened, leave behind bleeding areas.

Eosinophilia characterized by an increase in the total number of eosinophils ( type of white blood cells). Very often, eosinophilia appears against the background of various allergic processes. This is due to the fact that eosinophils are necessary to suppress allergies, since these cells are able to bind and suppress the action of histamine.

Hives is the most common type of allergy that occurs while taking medications. With this allergic reaction, flatly raised blisters appear on the skin, which are very itchy. Urticaria can affect both a small segment of the skin and be generalized ( skin rash spreads all over the skin). Often, urticaria is accompanied by symptoms such as abdominal pain, nausea, or even vomiting.

photosensitivity characterized by increased sensitivity human body to the sunlight ultraviolet rays). Ciprofloxacin, penetrating the skin, can lead to the occurrence of photoallergy, as well as a phototoxic reaction by the type of inflammation. Influencing the skin Sun rays react with this antibiotic and modify its configuration. In the future, the body, due to increased individual sensitivity, perceives the new substance as an allergen, which leads to photoallergy. It should be noted that this type of allergic reaction occurs only on those segments of the skin that have been exposed to ultraviolet radiation.

Anaphylactic shock- one of the most dangerous allergic reactions, which in more than 10% of all cases leads to death. Anaphylactic shock occurs due to a greatly increased sensitivity of the body to the drug. This reaction is manifested by the release of a very large amount of histamine ( immediate allergic reaction), which leads to instantaneous changes in blood circulation in organs and tissues. Anaphylactic shock is characterized by respiratory failure due to swelling of the pharynx, larynx and bronchi. There is also a state of collapse ( pronounced decrease in blood pressure). In anaphylactic shock, the provision of timely and adequate medical care is a top priority.

Other manifestations

While taking ciprofloxacin, the following side effects may also occur:

• muscle weakness;
• increased sweating;
• ligament breaks ( most often Achilles tendon);
• muscle pain;

Approximate cost of medication

Average cost of ciprofloxacin

Content

Ciprofloxacin occupies a special place among prescription bactericidal drugs - the instructions for use recommend it for anaerobic infections of soft tissues, joints, and upper respiratory tract. The main thing is that the sensitivity of bacteria to the drug is high. Ciprofloxacin has a detrimental effect on their cellular proteins. The antimicrobial drug even affects bacteria that are at rest. The medicine is produced in the most different forms, therefore, is used to treat organs from different body systems.

Antibiotic Ciprofloxacin

According to the instructions, the drug belongs to the category of fluoroquinolones and antibacterial drugs. Regarding pharmacology, it belongs to the group of fluoroquinolones. The function of the drug is to disrupt the structure of the DNA of aerobic and anaerobic microorganisms, to prevent the synthesis of the formation of protein structures. This effect is used for antibacterial therapy of infectious and inflammatory diseases caused by these pathogenic microorganisms.

Composition and form of release

The drug is available in several forms - eye and ear drops, tablets, injection solution, eye ointment. According to the instructions, the basis of each of them is ciprofloxacin hydrochloride. Only the dosage of this substance and auxiliary components differ. The composition of the drug is described in the table:

Pharmacological properties

According to the instructions, all forms of the drug have a wide antibacterial spectrum of action against gram-positive and gram-negative aerobic and anaerobic bacteria, such as:

• Mycobacterium tuberculosis;
• Brucella spp.;
• Listeria monocytogenes;
• Mycobacterium kansasii;
• Chlamydia trachomatis;
• Legionella pneumophila;
• Mycobacterium avium-intracellulare.

Staphylococci resistant to methicillin are also not sensitive to ciprofloxacin. Action on Treponema pallidum does not appear. The bacteria Streptococcus pneumoniae and Enterococcus faecalis are moderately sensitive to the drug. The drug acts on these microorganisms by inhibiting their DNA and suppressing DNA gyrase. The active substance penetrates well into the eye fluid, muscles, skin, bile, plasma, lymph. After internal use, bioavailability is 70%. The absorption of components is slightly affected by food intake.

Indications for use

Ciprofloxacin - instructions for use as common cause prescription indicates the treatment of bacterial infections of the skin, pelvic organs, joints, bones, respiratory tract, caused by drug-sensitive microorganisms. Among these pathologies, the instruction highlights the following:

• immunodeficiency states with neutropenia or after the use of immunosuppressants;
• bacterial prostatitis;
• hospital pneumonia associated with artificial ventilation of the lungs;
• infections of the hepatobiliary system;
• infectious diarrhea;
• prevention of infection in patients with pancreatic necrosis;
• acute and subacute conjunctivitis;
• chronic dacryocystitis;
• meibomite;
• bacterial ulcer of the cornea;
• keratitis;
• blepharitis;
• preoperative prevention of infections in ophthalmic surgery.

Method of application and dosage

The treatment regimen is determined by the type and severity of the infection. Ciprofloxacin - instructions for its use indicate 3 ways to use. The drug can be used externally, internally or by injection. The dosage is also affected by kidney function, and sometimes by age and body weight. For the elderly and children, it is much lower. Inside take pills, it is recommended to do it on an empty stomach. Injections are used in more severe cases so that the drug works faster. According to the instructions, before the appointment, a test for the sensitivity of the pathogen to the drug is performed.

Tablets Ciprofloxacin

For an adult, the daily dose ranges from 500 mg to 1.5 g. It is divided into 2 doses at intervals of 12 hours. To exclude the crystallization of salts, the antibiotic is washed down with a large amount of liquid (the main thing is not milk). Treatment lasts until the symptoms of an infectious disease are completely relieved and a couple of days after. The average duration of the course of treatment is 5-15 days. According to the instructions, therapy is extended up to 2 months for osteomyelitis, up to 4-6 weeks for lesions of bone tissue and joints.

Drops

An ophthalmic preparation is instilled 1-2 drops into the conjunctival sac of the affected eye every 4 hours. According to the instructions, for more severe infections, 2 drops are used. For the treatment of otolaryngology diseases, the ears are instilled with medicine, after having previously cleaned the external auditory canal. Use a dosage of 3-4 drops up to 4 times throughout the day. After the procedure, the patient needs to lie down for a couple of minutes on the opposite ear to the patient. The duration of therapy is from 7 to 10 days.

Ointment

Small amounts of eye ointment are applied over the lower eyelid of the affected eye several times throughout the day. This form of release is not so widespread, because there are drops. It is produced by only one plant - OAO Tatkhimfarmpreparaty. For this reason, and in view of the ease of use, it is more often used eye drops not ointment.

Ciprofloxacin intravenously

The solution is administered as an intravenous infusion. For an adult patient, ciprofloxacin in ampoules is prescribed by droppers with a daily dosage of 200-800 mg. With lesions of the joints and bones, 200-400 mg are administered twice a day. Treatment lasts approximately 7 to 10 days. Ampoules with a volume of 200 ml are prescribed intravenously for administration over half an hour, and 400 ml each - within an hour. They can be combined with a solution of sodium chloride. Ciprofloxacin injections for intramuscular injection patients are not prescribed.

special instructions

If the patient has a history of a pathology of the central nervous system, then Ciprofloxacin is not prescribed to him, because the drug has a number of side effects in relation to it. With caution, it is also used for epilepsy, severe cerebrosclerosis, brain damage and a reduced threshold for seizures. Elderly age, serious violations of kidney or liver function are also a reason for limiting Ciprofloxacin. Other features of the use of the drug:

• the appearance of signs of tendovaginitis and pain in the tendons is the reason for discontinuation of the drug, otherwise there is a risk of rupture or tendon disease;
• patients with alkaline urine reaction reduce the therapeutic dose to exclude the development of crystalluria;
• patients working with potentially dangerous devices should be aware that the drug can affect the speed of psychomotor reactions, especially when drinking alcohol;
• with prolonged diarrhea, it is necessary to exclude the diagnosis of pseudomembranous colitis;
• during treatment, you should avoid prolonged exposure to sunlight and increased physical activity, monitor the drinking regimen and the acidity of the urine.

Ciprofloxacin for children

Ciprofloxacin is allowed for children, but only from a certain age. The drug is used as a second or third line drug in the treatment of complicated infections in a child. urinary tract or pyelonephritis, which were provoked by Escherichia coli. Another indication for use is the risk of developing anthrax after contact with an infectious agent and pulmonary complications with cystic fibrosis. Studies concerned the appointment of Ciprofloxacin only in the treatment of these diseases. For other indications, experience with the drug is limited.

Interaction

The absorption of Ciprofloxacin is slowed down by antacids containing magnesium and aluminum. As a result, the concentration of active components in the blood and urine decreases. Probenecid leads to a delay in the excretion of the drug. Ciprofloxacin is able to enhance the effect of coumarin anticoagulants. When taking it, you need to reduce the dose of theophylline, since the drug reduces microsomal oxidation in hepatocytes, otherwise the concentration of theophylline in the blood will increase. Other interaction options:

• when used simultaneously with products containing cyclosporine, a short-term increase in creatinine concentration is observed;
• metoclopramide accelerates the absorption of ciprofloxacin;
• while taking oral anticoagulants, the bleeding time increases;
• against the background of taking Ciprofloxacin, resistance to other antibiotics that are not included in the group of inhibitors is not developed.

Side effects and drug overdose

The advantage of all forms of the drug is good tolerability, but some patients still experience adverse reactions, such as:

• headache;
• tremor;
• dizziness;
• fatigue;
• excitation.

These are common negative reactions to the use of ciprofloxacin. The instruction also indicates more rare side effects. In some cases, patients may experience:

• intracranial hypertension;
• hot flashes;
• sweating;
• abdominal pain;
• nausea or vomiting;
• hepatitis;
• tachycardia;
• depression;
• skin itching;
• flatulence.

Judging by the reviews, in exceptional cases, patients develop bronchospasm, anaphylactic shock, Lyell's syndrome, creatinine, vasculitis. when used in otology, the drug can cause tinnitus, dermatitis, headache. Using a medicine for the treatment of eyes, you can feel:

• sensation of the presence of a foreign body in the eye, discomfort and tingling;
• appearance white plaque on the eyeball;
• hyperemia of the conjunctiva;
• lacrimation;
• decreased visual acuity;
• photophobia;
• swelling of the eyelids;
• corneal staining.

Contraindications

According to the instructions, Ciprofloxacin is contraindicated in case of individual sensitivity or intolerance to the components of the drug. The drug in the form of a drop for the eyes and ears cannot be used for viral and fungal infections of these organs, as well as for the treatment of children under 15 years of age. Solution for intravenous administration is contraindicated up to 12 years. Other restrictions for use:

• breastfeeding and pregnancy (excreted in milk during lactation);
• alcohol intake;
• liver or kidney disease;
• a history of tendonitis caused by the use of quinolones that cause an increase in sensitivity to ciprofloxacin.

According to the instructions, with an overdose of the drug, no specific signs appear, side reactions can only increase. In this case, symptomatic treatment is indicated in the form of gastric lavage, creating an acid reaction of urine, taking emetics and drinking plenty of water. These activities are carried out against the backdrop of supporting vital organs and systems.

Terms of sale and storage

All forms of release of the drug are released only on prescription. The place for their storage should be hard to reach for children and poorly lit. According to the instructions, the recommended temperature is room temperature. The expiration date depends on the form of release and is:

• 3 years - for tablets;
• 2 years - for solution, ear and eye drops.

Analogues of Ciprofloxacin

Synonyms of Ciprofloxacin are Ciprodox, Basigen, Procipro, Promed, Ificipro, Ecoficol, Ceprova. The drugs that are similar to it according to the principle of action are the following:

• Nolicin;
• Gatispan;
• Zanocin;
• Abaktal;
• Levotek;
• Levofloxacin;
• Elefloks;
• Ivacin;
• Moximac;
• Oflocid.

Ciprofloxacin price

The cost of the drug varies depending on the place of purchase. The medicine can be bought at a pharmacy, but only if you have a prescription with you. The same applies to purchases in an online store - the courier also needs to present a doctor's prescription. Approximate prices for the drug are shown in the table: