Iron [III] polimaltozat hydroxide - instructions for use, dosage, adverse effects, contraindications

The preparation of iron in the form of a polymaltose complex of hydroxide Fe³⁺ (is dextrin of iron, in contrast to Fe³⁺ hydroxide polyisomaltozate - iron dextran, does not contain dextrans, which cause a greater probability of anaphylactic reactions).

Outside the multinucleated centers of hydroxide Fe³⁺ are surrounded by many non-covalently bound polymaltose molecules, forming a complex with a total molecular mass of 50 kD, which is so large,that its diffusion through the membranes of the intestinal mucosa is approximately 40 times less than that of Fe hexahydrate²⁺.

This macromolecular complex is stable, does not release iron in the form of free ions, is similar in structure to the natural combination of iron and ferritin. Due to this similarity, Fe³⁺ from the intestine enters the blood only by active absorption, which explains the impossibility of an overdose (and intoxication) by the drug in contrast to simple iron salts, the absorption of which occurs along the concentration gradient. The absorbed iron is deposited in a ferritin-related form, mainly in the liver. Later, in the bone marrow it is included in the hemoglobin.

Iron, part of the composition of Fe³⁺-hydroxide polymaltose complex, does not have pro-oxidant properties (which are inherent in simple Fe salts²⁺), which leads to a decrease in the oxidation of LDL and VLDL. Rapidly replenishes iron deficiency in the body, stimulates erythropoiesis, restores hemoglobin.

Pharmacokinetics:

The degree of absorption after oral administration depends on the degree of iron deficiency (the greater the deficit, the higher the absorption) and the dose of the drug (the higher the dose, the worse the absorption).Absorbed mainly in the duodenum and small intestine. The non-sucked part of Fe³⁺ is excreted with caloric masses.

After intramuscular injection enters the bloodstream through the lymphatic system. The maximum concentration is observed through24 hours. In the reticuloendothelial system, the complex is split into hydroxide Fe³⁺ and polymaltose (metabolized by oxidation). In the bloodstream, iron binds to transferrin, is deposited in tissues in ferritin, in the bone marrow is included in hemoglobin and used in the process of erythropoiesis.

Physiological loss: the epidermis, hair, nails, faeces, sweat, breast milk, menstrual blood, urine - 1.1-1.4 mg per day (healthy men and postmenopausal women - 1 mg per day, healthy women of reproductive age - 1 , 5-2 mg per day).

Indications:

Oral forms: treatment of iron deficiency anemia of various genesis and latent iron deficiency in infants and young children; increased need for iron (pregnancy, lactation period, donation, period of intensive growth, vegetarianism, elderly age).

Solution for injection: treatment of iron deficiency anemia with inefficiency or impossibilityreception of oral iron-containing preparations (including in patients with gastrointestinal diseases and suffering from malabsorption syndrome).

ICD-10

III.D60-D64.D63.0 * Anemia in neoplasm (C00-D48 +)

III.D50-D53.D50 Iron-deficiency anemia

IV.E50-E64.E61.1 Insufficiency of iron

Contraindications:

Hypersensitivity.
Excess iron in the body (hemochromatosis, hemosiderosis).
Anemia not related to iron deficiency (hemolytic anemia or megaloblastic anemia, caused by a lack of cyanocobalamin, aplastic anemia).
Violation of the mechanisms of iron utilization (lead anemia, sideroblastic anemia, thalassemia, late porphyria of the skin).
Rundu-Weber-Osler disease, chronic polyarthritis, infectious kidney disease in acute stage, uncontrolled hyperparathyroidism, decompensated liver cirrhosis, infectious hepatitis.
Pregnancy (first trimester).
Introduction to children under 4 months of age is not recommended due to lack of experience. In children, parenteral iron preparations can adversely affect the course of the infectious process.

Carefully:

Care should be taken when using the drug in patients with allergies, as well as with hepatic and renal insufficiency.

Side effects that occur in patients with cardiovascular diseases may aggravate the course of the underlying disease.

Patients with bronchial asthma or having a low iron-binding capacity of blood serum and / or deficiency of folic acid belong to a group at high risk of developing allergic or anaphylactic reactions.

Pregnancy and lactation:

Category of recommendations FDA is not defined. Adequate and well-controlled studies on humans and animals have not been conducted. The use of the drug in pregnancy is possible only in cases where the intended benefit to the mother exceeds the potential risk to the fetus.

Information about penetration into breast milk is not present. If you need to use the drug during lactation, you should decide whether to stop breastfeeding (due to lack of experience).

Dosing and Administration:

Doses and timing of treatment depend on the degree of iron deficiency. The daily dose can be divided into several doses or taken once.

Inside.

Adults. Tablets should be chewed or swallowed whole during or after a meal. The daily dose can be taken in one step.Treatment of a clinically pronounced deficiency: 1 tablet 1-3 times a day for 3-5 months before the normalization of hemoglobin concentration. Reception continues for several months to restore iron stores in the body (per tablet per day). pregnant - 1 tablet 2-3 times a day (before normalization of hemoglobin) followed by administration of 1 tablet per day before delivery, for the treatment of latent iron deficiency and prevention of deficiency - 1 tablet per day.

Drops can be mixed with fruit and vegetable juices or artificial nutrient mixtures, without fear of a decrease in the activity of the drug. 1 ml (20 drops) contains 176.5 mg of iron hydroxide polymaltose complex (50 mg elemental iron) 1 drop - 2.5 mg of elemental iron. To treat clinically pronounced iron deficiency, adults are prescribed 40-120 drops per day, pregnant women - 80-120 drops per day. Duration of treatment - at least 2 months. With clinically pronounced iron deficiency, hemoglobin normalization is achieved only after 2-3 months after the start of treatment. To restore his internal reserves, taking in preventive doses continues for several months.To treat latent iron deficiency, adults are prescribed 20-40 drops per day, pregnant women - 40 drops per day. Prevention of iron deficiency: adults - 4-6 drops per day, pregnant - 6 drops per day.

1 ml of syrup contains 10 mg of iron. To treat a clinically pronounced deficiency, adults and lactating women are prescribed 10-30 ml per day, pregnant women - 20-30 ml per day; for the treatment of latent iron deficiency - 5-10 ml per day and 10 ml per day, respectively. To prevent iron deficiency in pregnant women, the drug is prescribed in a dose of 5-10 ml per day.

Children. Treatment of iron deficiency anemia of various genesis and latent iron deficiency in infants and young children: children of the first year of life - 6-10 drops per day; at the age of 1-12 years - 10-20 drops per day.

Treatment of clinically pronounced iron deficiency. Inside. Premature infants - 1-2 drops per 1 kg of body weight daily for 3-5 months, up to 1 year - 10-20 drops per day; 1-12 years - 20-40 drops per day. Duration of treatment - at least 2 months. Normalization of hemoglobin is achieved only after 2-3 months after the start of treatment. To restore the internal reserves of iron reception in preventive doses continue for several months.

Prevention of iron deficiency. Inside.Up to 1 year - 2-4 drops per day; 1-12 years - 4-6 drops per day.

Treatment of clinically pronounced iron deficiency. Up to 1 year - 2.5-5 ml per day (25-50 mg of iron); 1-12 years - 5-10 ml per day.

Treatment of latent iron deficiency. 1-12 years - 2.5-5 ml per day.

Intramuscularly.

Adults. Solution for injection is intended only for intramuscular injection. Of great importance is the technique of injection. Due to improper administration of the drug, soreness and staining of the skin at the injection site may occur. Instead of the generally accepted, a ventrocarriage injection (in the upper outer quadrant of the gluteus maximus muscle) is recommended. Only intact ampoules can be used. When a precipitate forms, the solution is not suitable for use. After opening the ampoule, it should be administered immediately.

The length of the needle should be at least 5-6 cm. The needle clearance should not be too wide. For children and adults with a small body weight, needles should be shorter and thinner.

In accordance with the recommendations Hochstetter the injection site is determined as follows: along the line of the spinal column at the level corresponding to the lumbosacral articulation, point A is fixed. If the patient lies on the right side, the middle finger of the left arm is located at point A.The index finger is removed from the middle so that it is under the iliac crest line at point B. The triangle, located between the proximal phalanges, the middle and index fingers, is the injection site.

Tools are disinfected in the usual way.

Before inserting the needle, shift the skin about 2 cm to close the puncture hole well after removing the needle. This prevents the penetration of the injected solution into the subcutaneous tissues and the dyeing of the skin. The needle is positioned vertically with respect to the skin surface, at a large angle to the point of the iliac articulation, than to the point of the femoral joint. After injection, the needle is slowly withdrawn and the skin area adjacent to the injection site is pressed against the finger for about 5 minutes. After the drug is administered, the patient needs to move.

Children. The efficacy and safety of intramuscular use have not been studied.

Side effects:

Ingestion: irritation, spasms and pain in the stomach (stomach). Contact irritation (pain in the throat, chest), especially when swallowing, irritation in the areas of ulcerative lesions (with prolonged passage of the drug through the gastrointestinal tract). Nausea, vomiting, diarrhea.

With prolonged admission: nausea, vomiting, constipation, diarrhea, darkening of the urine (dose-dependent effect), staining the enamel of the teeth (only when ingested liquid forms), heartburn.

Solution for intramuscular administration: arthralgia, lymphadenopathy, fever, headache, malaise, dyspepsia (nausea, vomiting), allergic reactions.

Local reactions (with the wrong technique of administration): dyeing of the skin, soreness, inflammation.

Overdose:

Early symptoms (only with ingestion): diarrhea (sometimes with blood), fever, acute pains and spasms in the stomach, severe nausea and vomiting (sometimes with blood). Perhaps the emergence of leukocytosis and hyperglycemia.

Late symptoms: cyanosis of the lips, palms and terminal phalanges of the hand, drowsiness, pale and clammy skin, increased respiration and palpitations, weakness, lethargy, convulsions, metabolic acidosis, hypotension, hypoglycemia, toxic hepatitis, hepatic insufficiency, collapse, GI disorder.

Treatment: induction of vomiting and gastric lavage (according to the state), correction of electrolyte disorders, blood transfusion, enema. Antidote - deferoxamine (contraindicated in renal failure!).With anuria and oliguria - removal of hemodialysis.

Interaction:

ACE Inhibitors - strengthening of systemic effects.

Antacids, pancreatin, preparations containing calcium, bicarbonates, carbonates, oxalates, phosphates - Reduction of iron absorption (iron is recommended 1 hour before or 2 hours later). Antacids Do not affect the absorption and effectiveness of iron in combination with ascorbic acid.

Ranitidine, famotidine, cimetidine - decrease in iron absorption (reception of the latter 2 hours before or after H₂-gistaminoblockers).

Zinc-containing preparations - Decreased absorption of zinc (intake 2 hours after the introduction of iron-containing drugs).

Food (coffee, tea, eggs, milk and dairy products containing carbonates, oxalates, phosphates, bread, cereals containing phytates, dietary fiber), when taken together - reduced iron absorption (taking the medications last 1 hour before or 2 hours after consumption food).

Acetohydroxamic acid (urease inhibitor) - decrease in absorption and effectiveness of both (if necessary, iron intake during treatment with acetohydroxamic acid, it is administered parenterally).

Vitamin E, chloramphenicol - Decreased hematologic response to iron therapy.

Sodium dimercaptopropanesulfonate - formation of a toxic complex. Do not use at the same time! When severe iron deficiency is recommended, blood transfusion is recommended.

Deferoxamine and other chelating compounds - decrease in iron absorption (taking the latter after 2 hours).

Doxycycline, tetracycline - decrease in absorption and effectiveness of both (iron intake 3 hours before or 2 hours later).

Levodopa - when combined, the bioavailability of levodopa decreases; it is recommended that the reception and control of the response to levodopa be disconnected.

Levothyroxine sodium, penicillamine, ethidronic acid - Decrease in their effectiveness (maximally dissociated intake of iron, at least after 2 hours).

Methyldopa - decrease in absorption; iron - an antagonist of the hypotensive effect of methyldopa (the most disconnected reception, with the impossibility of control - the choice of another antihypertensive drug).

Alcohol (a significant amount, a long reception) - increased absorption and deposition of iron, the risk of toxic effects of the latter.

Quinolones (hemifloxacin, mofoxacin, norfloxacin) - a decrease in the bioavailability of quinolones (simultaneously it is impossible to take, iron intake - 3 hours before receiving hemifloxacin or 2 hours after it)

Special instructions:

Before use, the ampoule should be inspected for sediment and damage. Use only ampoules without sediment and damage. After opening the ampoule, the drug should be administered immediately.

Do not mix with other medications.

Parenteral iron preparations can cause allergic and anaphylactic reactions. In the case of moderate allergic reactions should be prescribed antihistamines. With the development of severe anaphylactic reaction, immediate administration of epinephrine (adrenaline) is necessary. The means of cardiopulmonary resuscitation should be available.

Instructions

Iron [III] hydroxide polymaltosate (Ferri (III) hydroxydum polymaltosatum)