Sorbifer contraindications. "Sorbifer": side effects, purpose, release form, features of administration, dosage, composition, indications and contraindications. General information about the drug

Instructions for medical use

medicine

Sorbifer ® Durules ®

Tradename

Sorbifer ® Durules ®

International nonproprietary name

Dosage form

Film-coated tablets

Compound

One tablet contains

active substances: iron (II) sulfate dry 320 mg (equivalent to 100 mg iron (II)), ascorbic acid 60 mg,

Excipients: povidone (K-25), polyethene powder, carbomer 934 R, magnesium stearate,

shell composition: hypromellose, macrogol 6000, titanium dioxide E 171, iron (III) yellow oxide E 172, solid paraffin.

Description

Tablets are lenticular-shaped, slightly biconvex, ocher-coated - yellow color, with “Z” engraving on one side, with a characteristic smell.

Pharmacotherapeutic group

Hematopoiesis stimulants. Iron supplement. Fe++ preparations for oral administration.

ATX code B03A A

Pharmacological properties

Pharmacokinetics

"Durules" is a special production technology that ensures gradual release active substance(iron ions), uniform supply of the drug. Iron is absorbed primarily in duodenum and proximal jejunum. Taking 100 mg twice a day provides 30% greater absorption of iron from Sorbifer Durules compared to conventional iron supplements. Absorption and bioavailability of iron are high. Connection with plasma proteins - 90% or more. Deposited in the form of ferritin and hemosiderin in hepatocytes and cells of the phagocytic macrophage system, a small amount - in the form of myoglobin in muscles. The half-life is 6 hours.

Presence in the drug ascorbic acid creates more favorable conditions for the absorption of iron in the intestines. At the molecular level, ascorbic acid mobilizes iron from the crystalline core of ferritin in vitro, reducing Fe 3+ to Fe 2+ . At the intracellular level, ascorbic acid enhances iron-induced ferritin translation by promoting the conversion of iron regulatory protein (IRP) from its RNA-bound form to aconitase.

Pharmacodynamics

Iron is an essential component of the body, necessary for the formation of hemoglobin and the implementation of oxidative processes in living tissues. Active substance contained in a biologically indifferent plastic matrix with a spongy structure. When passing through the gastrointestinal tract from the porous matrix of the tablets (within 6 hours), a continuous release of ferrous ions occurs. The film coating of the tablet and the porous matrix provide long-term release of iron ions. The film coating of the tablet, which completely disintegrates under the action of intestinal peristalsis and releases the active ingredient, helps prevent the tablet from dissolving in the stomach. The slow release of iron ions does not create a high local concentration, which avoids irritation of the mucous membrane gastrointestinal tract.

Ascorbic acid slows down the breakdown of ferritin by blocking autophagy of ferritin by ferritin lysosomes and transformation into hemosiderin.

Ascorbic acid accelerates the absorption of iron in the gastrointestinal tract, reducing unbound heme iron (III) to iron (II) in the stomach.

Indications for use

Iron-deficiency anemia

Latent iron deficiency in the body (without anemia), associated with excessive iron losses (bleeding, including uterine bleeding, constant donation), poor nutrition

Conditions accompanied by an increased need for iron in the body (prevention during pregnancy, lactation and in blood donors)

Directions for use and doses

The tablet should be taken whole, without chewing, and at least half an hour before meals, with half a glass of water.

Adults and teenagers over 12 years old:

Patients with iron deficiency anemia II-III degrees, if necessary, on the recommendation of a doctor, the dose can be increased to 3-4 tablets 2 times a day (morning and evening) with a duration of use of 3-6 months.

During pregnancy:

The drug is used in cases of established iron deficiency (iron deficiency anemia and latent iron deficiency in the body)

Prophylactic dose: 1 tablet per day.

Therapeutic dose: 1 tablet 2 times a day (morning and evening).

Treatment should be carried out until hemoglobin levels normalize and continue until the iron depot is completely saturated for another 2 months. Individual long-term therapy (with or without interruptions) is indicated when significant iron loss occurs regularly (for example, with heavy menstruation).

Side effects

Frequency side effects from the outside digestive system increases with increasing dose from 100 to 400 mg per day.

Often (>1/100)

Nausea, abdominal pain, diarrhea, constipation

Rarely (<1/100)

- ulcerative lesions of the esophagus, stenosis of the esophagus

Allergic reactions (itching, rash, hyperemia)

Hyperthermia

Contraindications

Hypersensitivity to the active or any other inactive component of the drug

Esophageal stenosis and/or other obstructive changes in the digestive tract

Increased iron content in the body (hemosiderosis, hemochromatosis)

Repeated blood transfusions

Impaired iron utilization (lead anemia, sideroblastic anemia, hemolytic anemia)

Children under 12 years of age (due to lack of clinical data)

Drug interactions

- ciprofloxacin: Concomitant use reduces the absorption of ciprofloxacin by approximately 50%, so there is a risk that the content of ciprofloxacin in the blood plasma will be lower than necessary for a therapeutic effect.

- levofloxacin: simultaneous use reduces the absorption of levofloxacin.

-moxifloxacin: Concomitant use reduces the bioavailability of moxifloxacin by almost 40%, therefore, if simultaneous use is required, it is necessary to ensure the longest possible period between taking moxifloxacin and Sorbifer Durules.

- norfloxacin: Concomitant use reduces the absorption of norfloxacin by approximately 75%.

- ofloxacin: Concomitant use reduces the absorption of ofloxacin by approximately 30%.

When using Sorbifer Durules concomitantly with the following drugs, dosage adjustment of these drugs may be required. The recommended minimum time interval between taking Sorbifer Durules and these drugs should be at least 2 hours:

- calcium or dietary supplements containing magnesium carbonate, as well as aluminum or calcium hydroxide, antacids containing magnesium carbonate, together with iron salts they form a complex that reduces the absorption of each other.

- captopril: Concomitant use reduces the area under the plasma concentration-time curve for captopril by approximately 37%, presumably due to chemical reactions in the gastrointestinal tract.

- zinc: simultaneous use reduces the absorption of zinc salts.

- clodronate: Concomitant use may reduce the absorption of clodronate.

- deferoxamine: with simultaneous use, the absorption of deferoxamine and iron is reduced due to the formation of a compound.

- levodopa: When used concomitantly, ferrous sulfate reduces the bioavailability of single doses of levodopa by approximately 50% and of single doses of carbidopa by 75%, possibly due to the formation of a chelate.

- methyldopa: When used concomitantly, the bioavailability of methyldopa is reduced, possibly due to the formation of a chelate.

- penicillamine: Concomitant use of penicillamine and iron salts reduces their absorption, possibly due to the formation of a chelate.

- risedronate: carried out in vitro Studies have shown that preparations containing iron form compounds with risedronate. Although no drug interaction studies have been conducted in vivo, it can be assumed that the simultaneous use of these drugs reduces the absorption of risedronate.

- tetracyclines: with simultaneous use, the absorption of tetracyclines and iron is reduced. If simultaneous use is necessary, the recommended minimum time interval between taking Sorbifer Durules and these drugs should be at least 3 hours. When taken orally, iron inhibits the enterohepatic circulation of oxytetracyxine (doxycycline), as well as when administered intravenously.

- hormones thyroid gland : with the simultaneous use of iron and thyroxine preparations, a decrease in the absorption of thyroxine is possible, which reduces the effectiveness of replacement therapy.

-cimetidine: with simultaneous use, the decrease in gastric juice production caused by cimetidine reduces the absorption of iron. Therefore, the intervals between taking these drugs should be at least 2 hours.

-chloramphenicol: When taken simultaneously, the clinical effect of iron treatment may be delayed.

When taking the drug simultaneously with tea, coffee, eggs, dairy products, wheat bread, porridge or foods rich in plant fiber, iron absorption may be reduced.

special instructions

Iron supplements can cause poisoning in children. When using the drug, darkening of the stool appears, which has no clinical significance.

The drug is used with caution for gastric and duodenal ulcers, inflammatory bowel diseases (enteritis, diverticulitis, ulcerative colitis, Crohn's disease), chronic liver and kidney diseases.

Comprehensive laboratory and instrumental monitoring of the effectiveness of treatment is recommended to be carried out every 7-14 days, depending on the course of anemia.

Pregnancy and lactation

The drug can be used during pregnancy and lactation.

Features of the effect of the drug on the ability operate a vehicle or potentially dangerous machinery.

Does not affect.

Overdose

Symptoms: abdominal pain, vomiting and diarrhea (sometimes with blood), fatigue, weakness, pyrexia, paresthesia, pallor skin, cold clammy sweat, acidosis, weak pulse, decreased blood pressure, heartbeat. Signs of peripheral circulatory collapse, coagulopathy, hyperthermia, hypoglycemia, liver damage, renal failure, muscle cramps and coma may appear after 6-12 hours.

Treatment: gastric lavage, milk and a raw egg, drugs that provoke vomiting, symptomatic therapy.

If necessary, perform a gastric lavage with a solution of deferoxamine at a concentration of 2 g/l, then 5 g of deferoxamine is dissolved in 50-100 ml of water and this solution is left in the stomach.

In case of severe intoxication: in a state of shock and/or coma and in case of increased serum iron levels (> 90 mmol/l in children, > 142 mmol/l in adults), intensive care should be started immediately and deferoxamine should be administered (15 mg/l). kg/h intravenously slowly, maximum 80 mg/kg/24 hours). Too much high speed infusion may result in hypotension.

In less severe cases of intoxication, deferoxamine can be administered intramuscularly (50 mg/kg, total dose not more than 4 g).

Release form and packaging

30 and 50 tablets are placed in brown glass bottles, sealed with a polyethylene cap and equipped with an accordion shock absorber for glass bottles. The bottle, together with instructions for medical use in the state and Russian languages, is placed in a lithographed cardboard box.

Storage conditions

Store at a temperature not exceeding 25 °C.

Keep out of the reach of children!

Shelf life

Do not use after expiration date.

Conditions for dispensing from pharmacies

Over the counter

Manufacturer

JSC "EGIS PHARMACEUTICAL PLANT"

1106 BUDAPEST, st. Keresturi, 30-38 HUNGARY

Sorbifer ( international name– Ferrous sulfate + Ascorbic acid) belongs to the group of antianemic drugs that replenish iron deficiency. The drug is highly effective and safe, due to which it is prescribed during pregnancy and breastfeeding.

In this article we will look at why doctors prescribe Sorbifer Durules, including instructions for use, analogues and prices for this drug in pharmacies. Real REVIEWS of people who have already used Sorbifer Durules can be read in the comments.

Composition and release form

The drug Sorbifer Durules is available in dosage form tablets for oral administration. They have a round shape, a biconvex surface, and a yellow color. The drug contains several main active ingredients.

One tablet contains: 320 mg ferrous sulfate (including 100 mg iron) and 60 mg ascorbic acid.
Excipients: hypromellose, titanium dioxide, magnesium stearate, carbomer 934P, yellow iron oxide, paraffin, polyethylene powder, macrolog 6000 and povidone.

Clinical and pharmacological group: antianemic drug.

What is Sorbifer Durules used for?

Sorbifer Durules is used in the presence of iron deficiency anemia, when the amount of iron obtained from foods is too small, or there is a need to regularly replenish it during prolonged bleeding. And also as preventive measures during pregnancy and lactation, with heavy menstruation and blood donors. The drug is also prescribed if there is a need for increased amounts of iron - for children and the elderly.

Pharmacodynamics and pharmacokinetics

The medicinal properties of the drug are due to the presence of iron in its composition in combination with ascorbic acid. Iron, in itself, is an integral part of the human body, its important functional unit. It is part of hemoglobin and takes part in oxidative reactions in tissues. Ascorbic acid improves the quality and affects the rate of absorption of iron by the body.

Durules is a special technology for manufacturing the drug, which allows iron ions to be evenly and gradually released in the intestines not under the influence of digestive juices, but as a result of peristalsis (wave-like movements of the intestinal walls). This gradual (over 6 hours) release of iron ions prevents the creation increased amount them in the digestive organs and prevents the irritating effect of iron ions on the mucous membrane of the digestive tract.

Absorption of the drug in small intestine, thanks to this technology, is high, 30% higher than other iron preparations. It is Ascorbic acid that increases its absorption.

Instructions for use

According to the instructions for use, I take Sorbifer Durules orally. Film-coated tablets should not be split or chewed. The tablet should be swallowed whole and washed down with at least half a glass of liquid. The duration of therapy is determined individually depending on the concentration of iron in the blood plasma. The average duration of treatment is 3–6 months.

The standard dose is 1 tablet 2 times a day (morning/evening) 30 minutes before meals. The tablet should be swallowed whole with water (200 ml). During development adverse reactions the dose should be reduced by 50% (one tablet/day).
During the first 6 months of pregnancy, the recommended dose is 1 tablet/day, in the last trimester of pregnancy, during lactation—1 tablet 2 times/day.

After normalization of hemoglobin levels, administration of the drug Sorbifer Durules should be continued until iron reserves are completely restored (about 2 months).

Contraindications

The drug should not be used in the following cases:

Children under 12 years of age (due to lack of clinical data).
Impaired iron utilization (lead anemia, sideroblastic anemia, hemolytic anemia).
Hypersensitivity to the components of the drug.
Esophageal stenosis and/or obstructive changes in the digestive tract.
Increased iron content in the body (hemosiderosis, hemochromatosis).

Carefully: peptic ulcer stomach and duodenum, inflammatory diseases intestines (enteritis, diverticulitis, ulcerative colitis, Crohn's disease).

Side effects

While taking Sorbifer Durules tablets, it is possible to develop a number of pathological negative reactions from various organs and systems:

Allergic reactions - skin rash, itching, specific pathological changes in the form of swelling and rash, reminiscent of a nettle burn.
Nervous system – dizziness, periodic headache.
Digestive system – nausea, periodic vomiting, painful sensations in the abdominal area, bowel dysfunction (constipation or diarrhea).
Rarely, ulcerative lesions of the walls of the stomach, duodenum, as well as narrowing (stenosis) of the esophagus can develop.
Other: rarely – general weakness, skin hyperthermia.

When taking an excessive dose of the drug, the following are possible: vomiting, abdominal pain, diarrhea mixed with blood, pallor of the skin, weakness or fatigue, paresthesia, cold sticky sweat, hyperthermia, acidosis, decreased blood pressure, weak pulse, rapid heartbeat; in severe cases - hypoglycemia, coagulopathy, signs of peripheral circulatory collapse, hyperthermia, renal failure, liver damage, muscle cramps and coma may appear after 6-12 hours.

Film-coated tablets - 1 tablet. iron sulfate - 320 mg (which corresponds to 100 mg of iron II) ascorbic acid - 60 mg excipients: magnesium stearate; povidone K-25; polyethylene powder; carbomer 934P shell: hypromellose; macrogol 6000; titanium dioxide; iron oxide yellow; solid paraffin in dark glass bottles of 30 or 50 pcs.; 1 bottle in a cardboard pack.

Description of the dosage form

Round biconvex film-coated tablets light yellow color, with “Z” engraving on one side, core on the break gray, with a characteristic odor.

Pharmacokinetics

Durules® is a technology that ensures the gradual release of the active substance (ferrous ions) from tablets, uniform delivery of the drug into the blood. Taking 100 mg 2 times a day provides 30% greater absorption of iron from the drug Sorbifer® Durules® compared to conventional iron preparations. Absorption and bioavailability of iron are high. Iron is absorbed primarily in the duodenum and proximal jejunum. Plasma protein binding - 90% or more. Deposited in the form of ferritin or hemosiderin in hepatocytes and cells of the phagocytic macrophage system, a small amount - in the form of myoglobin in muscles. T1/2 is 6 hours.

Pharmacodynamics

Iron is an essential component of the body, necessary for the formation of hemoglobin and the occurrence of oxidative processes in tissues. Durules® technology provides a gradual release of the active ingredient (iron ions) over a long period of time. The plastic matrix of Sorbifer® Durules® tablets is inert in digestive juice, but completely disintegrates under the action of intestinal peristalsis, when the active ingredient is completely released.

Indications for use Sorbifer Durules

treatment and prevention of iron deficiency anemia.

Contraindications for use of Sorbifer Durules

Diseases accompanied by the accumulation of iron in the body: aplastic and hemolytic anemia, anemia, hemochromatosis.

Sorbifer Durules Use during pregnancy and children

There are no contraindications.

Sorbifer Durules Side effects

lack of appetite, nausea, vomiting, diarrhea;
skin rash, itching.

Drug interactions

May reduce the absorption of concomitantly used enoxacin, clodronate, grepafloxacin, levofloxacin, levodopa, methyldopa, penicillamine, tetracyclines and thyroid hormones. The simultaneous use of the drug Sorbifer® Durules® and antacids containing aluminum hydroxide and magnesium carbonate can reduce the absorption of iron (the interval between their administration should be at least 2 hours); in the case of taking tetracyclines, the minimum interval should be 3 hours. Sorbifer® Durules® does not should be combined with ciprofloxacin, doxycycline, norfloxacin and ofloxacin.

Dosage of Sorbifer Durules

Adults are prescribed 2 tablets 3 times a day; children - 1-2 tablets 3 times a day, newborns - 1 tablet 3 times a day.

Overdose

Symptoms: abdominal pain, vomiting, fatigue or weakness, hyperthermia, paresthesia, pale skin, palpitations. Treatment: gastric lavage, orally - raw egg, milk (to bind iron ions in the gastrointestinal tract), administration of deferoxamine, symptomatic therapy.

Iron is one of the constituent elements of human blood. It promotes the production of hemoglobin in the blood, which, in turn, saturates the tissues with oxygen. This element is also necessary for metabolic processes in the body, to maintain immune system. Pregnant women especially need it. Iron is necessary for normal fetal development. You can compensate for its deficiency with the help of products, but this does not always work out, so they prescribe medical supplies. One of these is Sorbifer. Side effects, indications, and features of administration will be discussed below.

Operating principle

Combination drug"Sorbifer" also contains ascorbic acid.

Iron plays a key role in binding and transporting oxygen and carbon dioxide. Absorbed in the duodenum and proximal jejunum.

Vitamin C increases the absorption of iron in the stomach and intestines, and is also involved in redox processes.

And vitamin C promotes iron absorption.

The manufacturing technology of the drug ensures the continuous release of iron ions. Over 6 hours, the slow release of the active substance prevents dangerously high concentrations of iron. This avoids irritation of the intestines and stomach.

Once in the intestines, iron binds to apopheritin. One part enters the bloodstream, and the other remains in the intestine in the form of feritin, which is excreted in the feces or enters the bloodstream after 1-2 days. In the blood, iron binds to apotransferin or turns into transferrin. In this form, it enters the organs and through endocytosis into the plasma.

What does the drug contain?

"Sorbifer" is produced in the form of biconvex round tablets. Covered with a shell, they have a light yellow color. Z engraving is on one side. They have a peculiar smell. Gray inside.

One tablet contains:

Auxiliary components of the drug:

magnesium stearate;
povidone K-25;
polyethene powder;
carbomer 934R.

Contains the shell:

hypromellose;
titanium dioxide;
macrogol 6000;
iron oxide yellow;
paraffin paraffin

The tablets are packaged in dark glass bottles of 30 or 50 pieces.

Who is prescribed

The following indications exist for taking a drug such as Sorbifer:

iron deficiency;
Iron-deficiency anemia.

Prescribed as a prophylactic agent:

Pregnant women, if indicated to use Sorbifer, side effects the drug should not be ignored. If any unusual symptoms When taking, you need to consult a doctor.

Contraindications

The instructions for the drug contain a list of diseases for which it should not be prescribed. Pregnant women and anyone who is prescribed this medicine should pay special attention to it in order to exclude these conditions. The list of contraindications includes:

It is important to follow the instructions for the drug “Sorbifer”; in this case, there will probably be a minimum of side effects.

How to take the drug

For preventive purposes, Sorbifer is prescribed:

Children over 12 years old: 1 tablet per day.
Adults - 1 tablet per day.

In case of treatment of iron deficiency anemia, the drug is taken:

Pregnant women should use Sorbifer as follows:

For the first 6 months, 1 tablet per day.
In the last trimester of pregnancy, 1 tablet 2 times a day.

During lactation the following is prescribed:

1 tablet 2 times a day.

During the treatment period, the iron content in the blood plasma is monitored. The duration of therapy depends on this.

After the level of hemoglobin in the blood is restored, it is recommended to take the drug for another 2 months.

When treating iron deficiency anemia, it is necessary to take the drug for 3 to 6 months.

Before taking Sorbifer, contraindications and side effects of the drug should be discussed with your doctor.

Features of application

When carrying a child, a woman should be especially careful when taking any medications. Therefore, it is necessary to familiarize yourself with the features of taking Sorbifer.

When taking Sorbifer, side effects in women are more likely to occur if they have the following diseases:

chronic liver and kidney diseases;
leukemia;
intestinal diseases;
inflammatory pathologies of the gastrointestinal tract;
ulcer of the stomach and duodenum.

Interaction with other drugs

The drug "Sorbifer" often exhibits side effects during pregnancy if the doctor prescribes several drugs.

Sorbifer should not be used together with the following medications:

"Moxifloxacin";
"Ciprofloxacin";
"Levofloxacin";
"Norfloxacin";
"Ofloxacin"

The absorption of these medications is significantly reduced.

It is necessary to maintain an interval of at least 2 hours between taking Sorbifer and the following drugs:

"Captopril";
medications containing zinc, calcium, magnesium;
"Clodronate";
"Methyldopa";
"Penicillinamine";
"Risedronate";
"Tocopherol";
thyroid hormones;
"Pancreatin";
"Tetracycline";
glucocorticosteroids;
"Cimetidine"

Simultaneous use with the drug "Sorbifer" reduces the effect of ascorbic acid:

oral contraceptives;
fruit and vegetable juices;
alkaline mineral water.

The drug Deferoxamine, together with ascorbic acid, increases iron toxicity, especially in the heart muscle.

Side effects

You should consider what side effects are possible when taking Sorbifer.

It is also possible that the metabolism of zinc and copper in the body is disrupted.

Sorbifer Durules is often prescribed during pregnancy. The doctor should warn the patient about the side effects of the drug.

Overdose

You need to know the symptoms of a drug overdose:

There is a risk of gastrointestinal perforation.

In severe cases, the health condition may improve for some period of time, but after 6-24 hours the situation worsens again. Convulsions, liver and kidney failure, heart failure, coma are possible.

It is also possible after a few weeks or months to develop cirrhosis of the liver and persistent narrowing of the pylorus of the stomach.

An overdose of vitamin C can lead to hemolytic anemia and severe acidosis.

It is very important to know the symptoms of overdose when taking Sorbifer Durules tablets. Side effects of the drug have similar symptoms, it is important to correctly assess the situation early stage. Timely provision of assistance is very important.

Providing assistance in case of overdose

In case of overdose, the following steps must be taken:

Drink enough liquid to induce vomiting. You can use milk.
Rinse the stomach with a solution of Desferoxamine 2 g/l.
"Desferoxamine" 5 g + 50-100 ml of water enter the stomach and leave.
An adult can take Sorbitol.
It is necessary to take an x-ray of the stomach after lavage to identify the remaining tablets.
In severe cases, maintenance therapy and intravenous Desferoxamine are prescribed.
For less severe intoxication, Desferoxamine is administered intramuscularly.

The patient must be under constant monitoring. It is necessary to monitor serum iron levels.

Side effects during pregnancy

It is worth paying attention to the fact that most often the drug is prescribed to pregnant women. Therefore, let us pay attention to the side effects that are recorded in pregnant women:

rash;
constipation;
diarrhea;
nausea;
heartburn;
headache;
sleep disturbance.

If women took Sorbifer, reviews of side effects during pregnancy included nausea and constipation.

As a rule, such deviations are very rarely noted. After consulting a doctor and adjusting the dose, the symptoms go away.

It is worth noting that many women appreciated the increase in hemoglobin in the blood in a short period of time when taking Sorbifer. Side effects, as noted in the reviews, did not appear in any way. The effectiveness of the drug is confirmed not only during pregnancy, but also during lactation.

INN: Ascorbic acid, Ferrous sulfate

Manufacturer: CJSC "EGIS Pharmaceutical Plant", licensed by Astra Zeneca, Sweden

Anatomical-therapeutic-chemical classification: Iron preparations (ferrous) for oral administration

Registration number in the Republic of Kazakhstan: No. RK-LS-5 No. 005192

Instructions

Tradename

Sorbifer® Durules®

International nonproprietary name

Dosage form

Film-coated tablets

Compound

One tablet contains

active substances: iron (II) sulfate dry 320 mg (equivalent to 100 mg iron (II)), ascorbic acid 60 mg,

Excipients: povidone (K-25), polyethene powder, carbomer 934 R, magnesium stearate,

shell composition: hypromellose, macrogol 6000, titanium dioxide E 171, iron (III) yellow oxide E 172, solid paraffin.

Description

Tablets are lenticular-shaped, slightly biconvex, ocher-coated, yellow in color, engraved “Z” on one side, with a characteristic odor.

Pharmacotherapeutic group

Hematopoiesis stimulants. Iron supplement. Fe++ preparations for oral administration.

ATX code B03AA

Pharmacological properties

Pharmacokinetics

“Durules” is a special production technology that ensures a gradual, long-term release of the active substance (iron ions) and a uniform supply of the drug.

Iron is absorbed primarily in the duodenum and proximal jejunum.

The absorption of heme-bound iron is about 20%, and that of non-heme-bound iron is about 10%. For effective absorption, iron must be in the form of Fe(II). After oral administration, ascorbic acid is completely absorbed from the gastrointestinal tract. Hydrochloric acid of the stomach and ascorbic acid stimulate the absorption of iron, reducing it from Fe 3+ to Fe 2+. The presence of ascorbic acid in the drug creates more favorable conditions for the absorption of iron in the intestines and improves the bioavailability of the drug. Iron Fe 2+ (ferro form) entering the intestinal epithelial cells undergoes intracellular oxidation to Fe 3+ (ferri form), which binds to apoferritin. Part of apoferritin enters the blood, the other part temporarily remains in the intestinal epithelial cells in the form of ferritin, which enters the blood after 1-2 days or is excreted from the body in feces during the desquamation of epithelial cells.

About 1/3 of the iron entering the blood binds to apotransferrin, the molecule of which is converted into transferrin. The iron-transferrin complex is transported to target organs and, after binding to receptors located on the surface of their cells, enters the cytoplasm via endocytosis. In the cytoplasm, iron dissociates from transferrin and recombines with apoferritin. Apoferritin oxidizes iron to Fe 3+, and flavoproteins participate in the reduction of iron.

There are no data on the pharmacokinetics of the drug in patients with impaired liver or kidney function.

Pharmacodynamics

Iron is an essential component of the body, necessary for the formation of hemoglobin and the implementation of oxidative processes in living tissues. The active substance is contained in a biologically indifferent plastic matrix with a spongy structure. When passing through the gastrointestinal tract from the porous matrix of the tablets (within 6 hours), a continuous release of ferrous ions occurs. The film coating of the tablet and the porous matrix provide long-term release of iron ions. The film coating of the tablet, which completely disintegrates under the action of intestinal peristalsis and releases the active ingredient, helps prevent the tablet from dissolving in the stomach. The slow release of iron ions does not lead to the creation of a high local concentration, which avoids irritation of the mucous membrane of the gastrointestinal tract.

Iron is deposited in significant amounts as myoglobin in muscles.

Ascorbic acid slows down the breakdown of ferritin by blocking autophagy of ferritin by ferritin lysosomes and transformation into hemosiderin.

Ascorbic acid accelerates the absorption of iron in the gastrointestinal tract, reducing unbound heme iron (III) to iron (II) in the stomach.

Indications for use

Prevention and treatment of iron deficiency anemia

Directions for use and doses

The tablet should be taken whole, without chewing, and at least half an hour before meals, with half a glass of water.

You should not take the tablets while lying down.

Adults and teenagers over 12 years old:

For patients with grade II-III iron deficiency anemia, if necessary, on the recommendation of a doctor, the dose can be increased to 3-4 tablets 2 times a day (morning and evening).

If side effects occur, the dose can be reduced by half (1 tablet per day).

Duration of treatment:

The duration of treatment is determined individually, based on the results of laboratory data on iron metabolism.

Treatment should be carried out until hemoglobin levels normalize, under the control of Fe levels in the blood, and continue until the iron depot is completely saturated for another 2 months. With severe iron deficiency average duration treatment is 3-6 months.

Side effects

Often (>1/100)

Nausea, abdominal pain, diarrhea, constipation

Rarely (<1/100)

- ulcerative lesions of the esophagus, stenosis of the esophagus

Frequency unknown (not determined from available data):

Hypersensitivity reactions (eg, rash, anaphylactic reaction, angioedema)

Reports of suspected adverse reactions

Providing data on suspected adverse drug reactions is very important to enable continuous monitoring of the risk/benefit ratio of the drug. Health care professionals should provide information about any suspected adverse reactions to the contacts listed at the end of the instructions, as well as through the national reporting system.

Contraindications

Hypersensitivity to the active or any other inactive component of the drug

Esophageal stenosis and/or other obstructive changes in the digestive tract

Increased iron content in the body (hemosiderosis, hemochromatosis)

Repeated blood transfusions

Other types of anemia not due to iron deficiency, unless another type of anemia also develops iron deficiency

Children under 12 years of age (due to lack of clinical data)

Drug interactions

- levofloxacin: simultaneous use reduces the absorption of levofloxacin.

- norfloxacin: Concomitant use reduces the absorption of norfloxacin by approximately 75%.

- ofloxacin: Concomitant use reduces the absorption of ofloxacin by approximately 30%.

- captopril: Concomitant use reduces the area under the plasma concentration-time curve for captopril by approximately 37%, presumably due to chemical reactions in the gastrointestinal tract.

- zinc: simultaneous use reduces the absorption of zinc salts.

- clodronate: research in vitro showed that preparations containing iron form a complex compound with clodronate; simultaneous use may reduce the absorption of clodronate.

- deferoxamine: with simultaneous use, the absorption of deferoxamine and iron is reduced due to the formation of a complex compound.

- methyldopa: When used concomitantly with iron salts (ferrous sulfate or gluconate), the bioavailability of methyldopa is reduced, possibly due to the formation of a chelate complex.

- penicillamine: Concomitant use of penicillamine and iron salts reduces their absorption, possibly due to the formation of a chelate complex.

- risedronate: carried out in vitro Studies have shown that preparations containing iron form complex compounds with risedronate. Although no drug interaction studies have been conducted in vivo, it can be assumed that the simultaneous use of these drugs reduces the absorption of risedronate.

- thyroid hormones: with the simultaneous use of iron and thyroxine preparations, a decrease in the absorption of thyroxine is possible, which reduces the effectiveness of replacement therapy.

- cimetidine: with simultaneous use, the decrease in gastric juice production caused by cimetidine reduces the absorption of iron. Therefore, the intervals between taking these drugs should be at least 2 hours.

- chloramphenicol: When taken simultaneously, the clinical effect of iron treatment may be delayed.

When taking the drug simultaneously with tea, coffee, eggs, dairy products, wheat bread, porridge or foods rich in plant fiber, iron absorption may be reduced.

Interactions associated with ascorbic acid:

Increases concentration salicylates in the blood (increases the risk of developing crystalluria), ethinyl estradiol, benzylpenicillin, And tetracyclines. - reduces concentration oral contraceptives.

Increases activity norepinephrine.

Reduces anticoagulant effect derivatives of coumarin, heparin.

Improves the absorption of iron preparations in the intestines, as well as iron from food (due to the conversion of Fe 3+ to Fe 2+).

Increases overall clearance ethyl alcohol.

May affect effectiveness disulfiram in the treatment of chronic alcoholism.

Simultaneous use of ascorbic acid and deferoxamine increases iron excretion.

Acetylsalicylic acid, oral contraceptives, fresh juices and alkaline drinks reduce the absorption and absorption of ascorbic acid.

special instructions

When using the drug, darkening of the stool appears, which has no clinical significance.

The drug is used with caution for gastric and duodenal ulcers, inflammatory bowel diseases (enteritis, diverticulitis, ulcerative colitis, Crohn's disease), chronic liver and kidney diseases.

Comprehensive laboratory and instrumental monitoring of the effectiveness of treatment is recommended to be carried out every 7-14 days, depending on the course of anemia.

The drug is effective only for iron deficiency. Before starting treatment, it is necessary to confirm the diagnosis of iron deficiency (low iron content in serum, high total iron-binding capacity of serum).

The drug is ineffective for other types of anemia not caused by iron deficiency (infectious anemia, anemia associated with chronic diseases, thalassemia).

Pregnancy and lactation

The drug can be used during pregnancy and lactation in therapeutic doses.

Features of the effect of the drug on the ability operate a vehicle or potentially dangerous machinery.

Does not affect.

Overdose

Relatively low amounts of iron can cause symptoms of intoxication. There is evidence that an iron content equivalent to 20 mg/kg can already cause some symptoms of intoxication, and with an iron content exceeding 60 mg/kg, the development of such symptoms is expected. Iron content equivalent to 200-250 mg/kg can be fatal.

Symptoms:

Less than 3 mcg/ml - mild poisoning

3-5 mcg/ml - moderate poisoning

> 5 mcg/ml - severe poisoning

The maximum concentration of iron is determined 4-6 hours after ingestion of iron.

Mild to moderate poisoning: Vomiting and diarrhea may occur within 6 hours of ingestion.

Severe poisoning: severe vomiting and diarrhea, lethargy, metabolic acidosis, shock, bleeding from the gastrointestinal tract, coma, convulsions, hepatotoxicity, later - stenosis of the gastrointestinal tract. Severe toxicity also causes liver necrosis and jaundice, hypoglycemia, bleeding disorders, oliguria, renal failure and pulmonary edema.

An overdose of iron salts is especially dangerous in children. early age.

An overdose of vitamin C can cause severe acidosis and hemolytic anemia in susceptible individuals (glucose-6-phosphate dehydrogenase deficiency).

Treatment:

Milk or vomiting inducers inside.

Gastric lavage with 5% sodium bicarbonate solution and saline laxatives (for example, sodium sulfate, at a dose of 30 g for adults); milk and eggs combined with 5 g of bismuth carbonate as emollients.

After gastric lavage, 5 g of deferoxamine dissolved in 50-100 ml of water is administered, and this solution is left in the stomach. To stimulate intestinal activity, adult patients can be given a solution of mannitol or sorbitol orally. Causing diarrhea in children, especially at a young age, can be dangerous and is not recommended. Patients should be carefully monitored to prevent aspiration.

On an x-ray, the tablets give a shadow, so using an x-ray of the abdomen, you can identify the tablets remaining after gastric lavage and induced vomiting. It is advisable to appoint intravenous infusion chelate compounds (sodium, calcium edetate, 500 mg/500 ml in the form of long-term infusion). Dimercaprol should not be used as it forms toxic complexes with iron. Desferoxamine is a specific drug that forms a chelate complex with iron. In case of acute, severe poisoning in children, desferoxamine should always be prescribed at a dose of 90 mg/kg intramuscularly, then 15 mg/kg intravenously, until the iron content in the blood serum corresponds to the iron-binding capacity of the serum. If the infusion rate is too high, hypotension may develop. In less severe cases of intoxication, desferoxamine is prescribed intramuscularly at a dose of 50 mg/kg, up to maximum dose in 4 g. In case of severe intoxication: in a state of shock and/or coma and in case of increased serum iron levels (> 90 mmol/l in children, > 142 mmol/l in adults), intensive supportive therapy should be started immediately. Blood or plasma transfusions are performed for shock, and oxygen therapy is prescribed for respiratory failure. After elimination of intoxication, it is recommended to monitor the level of iron in the blood serum throughout the course of treatment.

Release form and packaging

30 and 50 tablets are placed in brown glass bottles with an FG-7 polyethylene cap, tamper evident and equipped with an accordion shock absorber. The bottle, together with instructions for medical use in the state and Russian languages, is placed in a cardboard box.