ethambutol dose. Ethambutol. Pharmacological action Ethambutol

Anti-tuberculosis drugs of different chemical groups.

Composition of Ethambutol

The active substance is Ethambutol.

Manufacturers

Akrikhin HFC (Russia), Makiz-Pharma (Russia), Pharmasyntez JSC (Russia), Shreya Life Sciences Pvt. Ltd (India)

pharmachologic effect

Anti-tuberculosis drug, acts bacteriostatically; penetrates into actively growing cells of mycobacteria, inhibiting RNA synthesis, disrupts cellular metabolism, causes cessation of reproduction and death of bacteria.

Active only against rapidly dividing cells.

Suppresses the growth and reproduction of mycobacterium tuberculosis resistant to streptomycin, isoniazid, PAS, ethionamide, kanamycin.

With monotherapy, resistance of mycobacteria develops quite quickly.

Ethambutol is well absorbed from the gastrointestinal tract, bioavailability - 75-80%.

Communication with plasma proteins - 20-30%.

The maximum concentration is reached 2-4 hours after ingestion.

It penetrates well into tissues and organs, as well as into biological fluids, with the exception of ascitic and pleural fluids (in the CSF only with meningitis).

The highest concentrations are in the kidneys, lungs, saliva, urine.

Penetrates into breast milk.

Does not penetrate through an undamaged BBB.

Partially metabolized in the liver (15%) with the formation of inactive metabolites.

The half-life is 3-4 hours, in case of impaired renal function - 8 hours.

Excreted by the kidneys - 80-90% (50% - unchanged, 15% - in the form of inactive metabolites) and with stool- 10-20% (unchanged).

side effects of ethambutol

From the nervous system and sensory organs:

• weakness,
• headache,
• dizziness,
• mental disorder,
• disorientation,
• hallucinations,
• depression,
• peripheral neuri,
• neuritis optic nerve.

From the digestive system:

• decreased appetite,
• nausea,
• vomiting,
• gastralgi,
• violation of liver function - increased activity of "liver" transaminases.

Allergic reactions:

• dermati,
• skin rash,
• arthralgia,
• fever,
• anaphylaxis.

Indications for use

Tuberculosis (all forms) - in the composition complex therapy.

Especially effective when combined with rifampicin in patients with chronic destructive pulmonary tuberculosis.

Contraindications Ethambutol

Hypersensitivity, optic neuritis, cataract, diabetic retinopathy, inflammatory diseases eye, gout, children's age (up to 13 years), chronic renal failure, pregnancy, lactation.

Method of application and dosage

When conducting primary treatment- 15 mg/kg once a day.

When conducting a second course of treatment - 25 mg / kg 1 time per day for 2 months, then go to 15 mg / kg 1 time per day.

Children - 20-25 mg / kg once, after breakfast.

Higher daily dose- 2y.

In renal failure, the dose is adjusted depending on the CC:

• with CC more than 100 ml / min, the daily dose is 20 mg / c,
• 70-100 ml / min - 15 mg / c,
• less than 70 ml / min - 10 mg / c,
• sick,
• on hemodialysis,
• - 5 mg/k,
• on the day of dialysis - 7 mg / kg.

Overdose

Symptoms:

• nausea,
• vomiting,
• hallucinations,
• polyneuritis.

Treatment:

• symptomatic.

Interaction

Enhances the effects of anti-tuberculosis drugs and neurotoxicity of aminoglycosides, asparaginase, carbamazepine, ciprofloxacin, imipenem, lithium salts, methotrexate, quinine.

special instructions

At the beginning of treatment, an increase in cough, an increase in the amount of sputum is possible.

During long-term therapy, it is necessary to regularly monitor the function of the organ of vision, the picture of peripheral blood, as well as the functional state of the liver and kidneys.

During the period of treatment, care must be taken when driving vehicles and engaging in other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Compound

Active ingredient: ethambutol;

1 tablet contains ethambutol hydrochloride 400 mg

Excipients: microcrystalline cellulose, methylcellulose, croscarmellose sodium, colloidal silicon dioxide, calcium stearate.

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Dosage form

Pills.

Main physicochemical characteristics: tablets of white or almost white color, flat-cylindrical shape, with a chamfer and risk. Marbling is allowed on the surface of the tablets.

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Pharmacological group

Antimicrobial agents for systemic use. Means acting on mycobacteria. Anti-tuberculosis drugs. Ethambutol.

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Pharmacological properties

Pharmacological.

Ethambutol is a second-line anti-tuberculosis drug. It has a bacteriostatic effect only on M. tuberculosis, including strains resistant to streptomycin, kanamycin, isoniazid, PAS and ethionamide. The mechanism of action is associated with rapid penetration into the cell, where lipid metabolism and RNA synthesis are disturbed; magnesium and copper ions bind, and the structure of ribosomes and protein synthesis are disturbed. With monotherapy, resistance to ethambutol develops rapidly. Active only against bacteria that divide intensively.

Pharmacokinetics.

After oral administration, about 80% of ethambutol is absorbed. Simultaneous food intake accelerates and enhances the absorption process. Serum concentration after administration is proportional to the applied dose. The maximum concentration of ethambutol in the blood is reached after 2:00. The concentration of the drug in the blood serum decreases within 8:00 to 50% and within 24 hours - up to 10%. Ethambutol accumulates in red blood cells; 2:00 after administration, the concentration of ethambutol in erythrocytes is approximately 2 times higher than its concentration in blood plasma. Plasma protein binding is highly concentration dependent and ranges from 10-40%. Ethambutol passes into the cerebrospinal fluid, breast milk and through the placenta. The half-life is 3.3-3.5 hours. Ethambutol is excreted mainly unchanged, mainly in the urine, completely excreted after a few days. During the first 24 hours, about 60% of the dose is excreted in the urine. Almost 10-20% is excreted in the feces as inactive metabolites (aldehyde, a dicarboxylic acid derivative). In violation of the excretory function of the kidneys, ethambutol can accumulate in the body.

Indications

Treatment various forms tuberculosis (only in combination with other anti-tuberculosis drugs).

Contraindications

Hypersensitivity to the components of the drug; optic neuritis cataract; diabetic retinopathy; inflammatory eye diseases gout; severe renal failure, a situation where it is impossible to check the state of vision (serious condition, mental disorders).

Interaction with other medicinal products and other forms of interaction

With the simultaneous use of the drug with other drugs, it is possible:

with anti-tuberculosis drugs - enhancing the effects of anti-tuberculosis drugs. For the treatment of tuberculosis in complex therapy with ethambutol, isoniazid, para-aminosalicylic acid (PAS), streptomycin, cycloserine, pyrazinamide can be used;

with ciprofloxacin, aminoglycosides, asparaginase, carbamazepine, lithium preparations, imipenem, methotrexate, quinine - enhancing the effects and increasing the neurotoxicity of the above drugs;

with digitoxin - a decrease in the effectiveness of the latter;

with disulfiram - an increase in the concentration of ethambutol and an increase in its toxicity;

with pyrazinamide - a synergistic effect on the excretion of uric acid

with isoniazid while the use of cyclosporine A - increased disintegration of cyclosporine A with the risk of transplant rejection;

with aluminum preparations and other antacids - the absorption of ethambutol from the digestive tract decreases.

Ethambutol does not affect the metabolism of certain trace elements, mainly zinc.

Application features

The drug is prescribed only in combination with other anti-TB drugs.

Before and during treatment with ethambutol, ophthalmological control should be carried out: examination of the fundus, intraocular pressure, refraction, visual fields, visual acuity and color perception (especially the differentiation of red and green, blue and green colors).

In patients with impaired renal function, ophthalmic monitoring should be carried out daily.

Ophthalmological control is carried out for each eye separately and for both together, since changes in visual acuity can be unilateral or bilateral.

It is necessary to inform the doctor about any changes in the function of the eye.

In the event of changes in the function of the organs of vision to prevent atrophy of the optic nerve, treatment with ethambutol should be discontinued. Visual changes are usually reversible after discontinuation of treatment disappear after a few weeks, in some cases - after a few months. In exceptional cases, changes in vision are irreversible due to atrophy of the optic nerve.

In case of visual impairment, hydroxycobalamin or cyanocobalamin is used.

Sick with kidney failure the dose of ethambutol should be reduced because medicine accumulates in the body.

Treatment with ethambutol can increase the concentration of urate in the blood, which is associated with a weakening of the excretion of uric acid by the kidneys.

Patients with hyperuricemia should be prescribed the drug with caution.

At the beginning of treatment, an increase in cough, an increase in the amount of sputum is possible. To reduce these symptoms, B vitamins, expectorants should be prescribed.

Bacterial resistance to ethambutol develops more frequently in patients previously treated with tuberculostatic drugs.

Prolonged or repeated use of ethambutol may lead to the development of secondary infections. If you suspect an infection, you should consult a doctor.

If the symptoms of tuberculosis do not disappear within 2-3 weeks, or if the condition worsens, it is recommended to consult a doctor.

It is necessary to complete the full course of drug treatment, regardless of whether there are symptoms of the disease or not, to prevent relapse or the development of resistance.

Ethyl alcohol enhances toxic effect ethambutol on the organ of vision, so alcohol should be avoided during treatment.

If side effects appear, a dose adjustment is necessary in the direction of its reduction, if such a step is impossible, a transition to an intermittent drug intake (every other day or 2 times a week).

This medicinal product contains 6.0 mg of croscarmellose sodium. Caution should be exercised when used in patients on a controlled sodium diet.

Use during pregnancy or lactation.

The drug is contraindicated during pregnancy or lactation.

The ability to influence the reaction rate when driving vehicles or operating other mechanisms.

During the period of treatment, it is not allowed to drive vehicles and engage in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Dosage and administration

Adults and children over 13 years old.

Primary treatment: the drug is prescribed at a dose of 15 mg / kg of body weight 1 time per day.

Repeated course of treatment: the drug is prescribed at a dose of 25 mg/kg 1 time per day, then they switch to taking the drug at a dose of 15 mg/kg 1 time per day.

During the period when the patient uses the drug at a dose of 25 mg / kg of body weight, a monthly examination by an ophthalmologist is recommended.

With functional kidney failure, the drug is prescribed depending on the creatinine clearance:

The maximum daily dose is 2 g.

The maximum daily dose for children is 1 g.

The duration of treatment depends on the form of tuberculosis and ranges from 6 to 12 months.

Taking ethambutol after meals improves tolerability.

The drug is contraindicated in children under 13 years of age.

Overdose

Symptoms: nausea, vomiting, anorexia, diarrhea, fever, headache, the development of neurological disorders, especially damage to the optic nerve, leading to blindness, deterioration of visual acuity or increased manifestations of other adverse reactions, dizziness, polyneuritis, confusion, headache, hallucinations, respiratory depression, asystole.

Treatment is symptomatic. Due to the rapid absorption of the drug, immediately after ingestion, vomiting or gastric lavage should be induced, and enterosorbents should be prescribed. Carry out supervision and measures to support vital important functions body, if necessary resuscitation. Shown: forced diuresis, peritoneal dialysis or hemodialysis. At allergic reactions shows the use of desensitizing agents. In threatening conditions, exchange transfusion is indicated, since this also removes erythrocytes, in which ethambutol accumulates in significant quantities. There is no specific antidote.

Adverse reactions

On the part of the organ of vision: retrobulbar inflammation of the optic nerve, optic neuropathy, unilateral or bilateral decrease in visual acuity, including irreversible blindness, impaired color perception (mainly green and red), development of central or peripheral scotoma, visual field limitations, retinal hemorrhage. The occurrence of visual impairment depends on the duration of treatment and previous or current eye diseases.

From the respiratory system, organs chest and mediastinum: lung infiltrates with or without eosinophilia, pneumonitis, bronchospasm.

From the side gastrointestinal tract: metallic taste in the mouth, nausea, vomiting, dyspepsia, heartburn, abdominal pain, diarrhea, anorexia, liver dysfunction - increased activity of hepatic transaminases, hepatitis, jaundice, pseudomembranous colitis (with joint application with rifampicin and isoniazid).

From the side of the kidneys and urinary system: increased creatinine levels, increased urea levels, interstitial nephritis.

From the nervous system: headache, dizziness, confusion, disorientation, hallucinations, convulsions, disorientation, depression, peripheral neuritis - paresthesia in the limbs, numbness, paresis.

From the side of cardio-vascular system: pericarditis, myocarditis, arterial hypotension, tachycardia, vasculitis.

From the blood and lymphatic system: leukopenia, neutropenia, thrombocytopenia, eosinophilia, lymphadenopathy, increased activity of hepatic transaminases.

From the side immune system: hypersensitivity reactions, including anaphylactic and anaphylactoid reactions, anaphylactic shock, Stevens-Johnson syndrome, Lyell's syndrome (toxic epidermal necrolysis), vasculitis.

Package

10 tablets in a blister pack, 5 blister packs in a pack; 1000 tablets in containers.

Ethambutol is a drug used to treat tuberculosis.

Release form and composition of Ethambutol

Ethambutol is available as white tablets. active substance which is Ethambutol hydrochloride, 200, 400, 600, 800 mg and 1 g each.

As excipients Ethambutol tablets used: starch, dibasic calcium phosphate, propylparaben, methylparaben, purified talc, gelatin, colloidal silicon dioxide, magnesium stearate, sodium starch glycolate, purified water.

pharmachologic effect

Ethambutol is a synthetic derivative of ethylenediamine. The drug has a specific antibacterial effect against Mycobacterium bovis and tuberculosis, certain atypical (nontuberculous, opportunistic) types of mycobacteria. Does not show activity against other bacteria, viruses, fungi. Has a bacteriostatic effect. It shows activity against mycobacteria resistant to other anti-tuberculosis drugs, and therefore, it is an anti-tuberculosis agent of the second line.

Primary resistance of M. tuberculosis and bovis to Ethambutol is quite rare, secondary resistance is developed slowly.

Ethambutol can be used in conjunction with other anti-TB drugs.

Indications for use of Ethambutol

According to the instructions, Ethambutol is prescribed for:

• pulmonary and extrapulmonary forms of tuberculosis (in combination with other anti-tuberculosis drugs);
• infections caused by susceptible atypical mycobacteria.

Contraindications to the use of ethambutol

According to the instructions, Ethambutol is not prescribed for:

• hypersensitivity to this medicinal product;
• severe renal failure;
• damage to the optic nerve, after optic neuritis;
• pregnancy and lactation.

The drug is used with caution:

• with diabetic retinopathy;
• with cataracts;
• under the age of 13;
• with disorders in the work of the kidneys.

Method of application and dosage of Ethambutol

The drug is intended for oral administration.

Ethambutol is prescribed for admission as part of complex therapy once a day at 15-25 mg per kg of body weight or 2 times a week at 50 mg per kg of body weight or 3 times a week at 25-30 mg per kg of body weight.

When the patient's condition stabilizes, Ethambutol is taken at 15 mg per kg of body weight per day.

how alternative method the drug is prescribed throughout the entire period of treatment at 15 mg per kg of body weight per day.

The tolerance of Ethambutol is increased if it is taken after meals.

The duration of drug therapy is determined by the form of the disease and the treatment regimen used. On average - 6-12 months.

Side effects

The drug may cause the following side effects:

• retinal hemorrhage, optic neuritis;
• headache, dizziness;
• disorientation;
• malaise;
• hallucinations;
• peripheral polyneuritis;
• confusion;
• paresthesia;
• hypersensitivity reactions in the form of rash, itching, fever, leukopenia, tachycardia, vasculitis, arthralgia, Lyell and Stevens-Johnson syndromes, anaphylactic shock;
• heartburn;
• anorexia;
• diarrhea
• vomiting;
• stomach ache;
• jaundice;
• metallic taste in the mouth;
• disorders in the liver;
• interstitial nephritis;
• thrombocytopenia;
• leukopenia;
• acute attack of gout;
• decreased clearance of uric acid.

Side effects of ethambutol most often occur in patients with diabetes, renal failure, chronic alcoholism, elderly patients.

Overdose

Symptoms of an overdose of Ethambutol are manifested in the form of neurological disorders (damage to the optic nerve), lack of appetite, diarrhea, vomiting, fever, dizziness, headache, hallucinations, confusion, respiratory depression, asystole.

Treatment of overdose is symptomatic. Gastric lavage, inducing vomiting, taking activated carbon it is advisable only immediately after taking the drug.

Forced diuresis, peritoneal dialysis or hemodialysis are also indicated. In threatening conditions, an exchange transfusion is done.

Use during pregnancy and lactation

Ethambutol is contraindicated during pregnancy.

In experimental studies, a teratogenic effect of the drug was found.

Since Ethambutol is excreted in breast milk, if it is necessary to use it during lactation, it is necessary to stop breastfeeding the baby.

Interaction with other drugs

When taking Ethambutol simultaneously with aluminum hydroxide, the absorption of Ethambutol from the digestive tract decreases.

Ethambutol may reduce the effectiveness of digitoxin.

When used concomitantly with isoniazid, optic neuropathy may increase,

Ethambutol may alter zinc metabolism.

Pyrazinamide and Ethambutol act synergistically to eliminate uric acid from the body.

When used simultaneously with disulfiram, the concentration of ethambutol in serum may increase and its toxicity may increase.

The toxic effect of ethambutol on vision is enhanced ethyl alcohol therefore, during therapy with the drug, it is necessary to abandon alcohol.

special instructions

Before starting therapy with Ethambutol, an ophthalmological examination of the patient should be performed to determine the ability to distinguish colors, visual acuity, visual fields, with an examination of the fundus, measurement of intraocular pressure.

During treatment with the drug every 2-4 weeks, it is necessary to undergo an examination by an ophthalmologist.

In persons with impaired renal function, an ophthalmological examination should be carried out every week.

Before starting therapy, the patient should be warned about possible visual impairment, side effects, in the event of which he should consult a doctor.

If visual disturbances occur, Ethambutol therapy is discontinued in order to prevent optic nerve atrophy.

Most often, visual impairments are reversible, especially if they are detected in the early stages of treatment.

For visual impairment caused by taking Ethambutol, cyanocobalamin or hydroxycobalamin is prescribed. Vision is restored within a few weeks (months). Sometimes vision changes are irreversible. The level of visual acuity reduction and optic neuritis depend on the duration of treatment with the drug and its dosage.

Ethambutol should be used very carefully in patients with hyperuricemia or gout.

Before starting therapy and during it, it is necessary to constantly monitor the functioning of the liver and kidneys.

Storage conditions

Ethambutol is stored at a temperature not exceeding 25ºC in a dark place out of the reach of children.

We have selected real reviews about the drug Ethambutol, which are published by our users. Most often, the review is written by mothers of small patients, but also describes a personal history of use. medicinal product on myself.

Indications for use

Tuberculosis (combined therapy of pulmonary and extrapulmonary forms).

Discussion of the drug Ethambutol in the records of mothers

I injection) Lomefloxacin (tablets) Pyrazinamide (tablets) Prothionamide (tablets) Rifabutin (capsules) Rifampicin (capsules, powder for injection) Streptomycin (powder for injection) Ethambutol (tablets, dragees) Ethionamide (drops) Antivirals Acyclovir (tablets, ointment) , cream, powder for injection) Ganciclovir (capsules, powder for injection) Didanosine (tablets, powder for oral solution) Zidovudine (capsules, syrup, injection) Indinavir (capsules) Ifavirenz (capsules) Lamivudine (tablets, oral solution ) Nevirapine (tablets, suspension) Stavudine (capsules, powder for oral solution) Antifungals...

Thromycin 3) tetracyclines 57 Doxycycline 4) fluoroquinolones 58 Norfloxacin 7. Antituberculosis drugs 59 Isoniazid 60 Metazide 61 Pyrazinamide 62 Rifampicin 63 Ethambutol 8. Antiprotozoal and antimalarial drugs 64 Chloroquine 9. Anticancer, immunosuppressive and concomitant drugs 1) cytostatic drugs and other herbal remedies 65 Vincristine b) alkylating agents 66 Melphalan 67 Chlorambucil 68 Cyclophosphamide c) antimetabolites 69 Hydroxyurea 70 Capecitabine 71 Methotrexate 72 Fluorouracil 2) antitumor antibiotics...

... ezny union). Group I (maximum activity) - isoniazid and rifampicin. Group II (drugs of average efficiency) - streptomycin, kanamycin, viomycin, cycloserine, as well as ethambutol, ethionamide, prothionamide, pyrazinamide. Group III (drugs of moderate effectiveness) - aminosalicylic acid, thioacetazone. Depending on preference. First-line drugs are the most effective and are considered essential components of any short-term course of chemotherapy. The drugs of choice are isoniazid and rifampicin. Additional drugs are pyrazinamide, ethambutol and streptomycin. Second-line drugs are clinically less effective and have more adverse reactions. Their n...

Awn to medicines: rpoB - to rifampicin, katG, inhA, oxyR, ahpC, kasA - to isoniazid, rpsL - to streptomycin, gyrA - to fluoroquinolones, pncA - to pyrazinamide, embCAB - to ethambutol. At the same time, in most cases, the studied clinical isolates resistant to rifampicin turned out to be resistant to other anti-TB drugs. Thus, rifampicin resistance is a marker of...

Her treatment was prescribed to us, because. many patients already have drug resistance (therefore, at least two types are prescribed). In our case, a consultation was held, pyrazinamide and ethambutol were prescribed, plus Revit, plus vitamin B6, while he is being treated for three months, this week the control should be diaskintest. I hope everything goes well. Why am I writing: when your child has a positive diaskintest, then this is NOT an allergy, go through prophylaxis, do not be afraid, you will protect your child from illness, or how we will suffer all our lives with treatment and be afraid of the return of the disease. It’s good if there is no stress and the child can cope on his own, but it can also turn into a serious form of the disease ...

Photo of the drug

Latin name: Ethambutol

ATX Code: J04AK02

Active substance:

Manufacturer: Pharmasyntez OJSC (Russia), Shreya Life Sciences (India), Makiz-Pharma (Russia), HFC Akrikhin (Russia), Darnitsa (Ukraine)

The description applies to: 21.12.17