Actiferrin® [serine, iron sulfate]

Pharmacological properties

Iron is necessary for the life of the body: it is part of hemoglobin, myoglobin, various enzymes, reversibly binds oxygen and is involved in redox reactions, stimulates erythropoiesis. iron is also found in depot tissues (bone marrow, liver, spleen). the amino acid serine, which is part of actiferrin, promotes more efficient absorption of iron and its entry into the systemic circulation, which causes a rapid restoration of its content in the body to the required levels. this provides a better perception of the drug and allows you to reduce the required dose of iron.

Pharmacokinetics

Absorption. When ingested, about 10-15% of the iron in divalent form, as a rule, is absorbed in the duodenum and upper part of the small intestine. In addition, with increased intake of the body, passive transport of iron occurs.

Iron absorption increases significantly with iron deficiency in the body, as well as in the case of increased erythropoiesis. The highest level of absorption (50-60%) is observed at low levels of hemoglobin and iron content in the blood, and the intensity of absorption decreases again as these indicators normalize.

C_max serum iron is reached within 2-4 hours after taking the drug.

Distribution. In the blood, iron in trivalent form binds to transferrin and is transported to the site of hemostasis or deposition. When fully saturated, total serum transferrin can bind a maximum of 12 mg of iron. This value is relatively small, and in case of iron intoxication as a result of administration or parenteral administration, the iron-binding ability of transferrin may decrease, leading to the release of free unbound iron, which is toxic, into the plasma.

After binding to apoferritin, iron is deposited in the form of ferritin, in particular in the liver, spleen and bone marrow.

Iron crosses the placental barrier and in small amounts into breast milk.

Only about 1 mg of iron is excreted daily with dead skin cells and mucous membranes, with bile and urine. During menstruation, iron loss is about 1 mg / day.

Most of the iron formed as a result of the breakdown of hemoglobin (20-30 mg / day) is used by the body to re-synthesize hemoglobin.

Indications

Treatment of iron deficiency in the body.

Application

Actiferrin capsules should not be sucked, chewed or held in the mouth. capsules must be swallowed whole with water. the drug is taken 30 minutes before meals or during meals (depending on tolerance from the digestive tract), or with fruit juice containing ascorbic acid, which improves absorption in the small intestine. ingestion with food improves compatibility in the digestive tract. determination of the daily dose depends on the level of hemoglobin, body weight and age of the patient.

With oral administration of capsules, the daily dose is 1.3–4 mg of iron / kg body weight.

Children aged 6-12 years: 1 capsule 1 time per day.

Children aged 12 years: appoint 1 capsule 2 times a day.

Adults, depending on the severity of the patient’s condition, are prescribed 1 capsule 2-3 times a day at the beginning of therapy, then, if necessary, long-term treatment is necessary, the dose is gradually reduced to 1 capsule 1 time per day.

Drops of Actiferrin are prescribed primarily for children in their first year of life. Drops of Actiferrin are taken immediately before meals or during meals with a small amount of liquid (with water or fruit tea). The determination of the daily dose depends on the level of hemoglobin, body weight and age of the patient.

When administered orally in the form of oral drops, the daily dose is 1.3–4 mg of iron / kg body weight.

Estimated average dose for infants (children under the age of 1 year) - 10-15 drops 3 times a day.

The dose for children aged 1-2 years is 15-25 drops 3 times a day.

The dose for children aged 2–6 years is 25–35 drops 3 times a day.

For the treatment of children 6 years old and adults, it is advisable to take Actiferrin in the form of capsules.

To normalize the iron content in the body, the recommended course of treatment, both when taking capsules and drops, is 8 weeks. After reaching normal levels of iron concentration in blood serum, treatment should be continued for several more weeks to replenish iron stores in the body.

In case of impaired renal function and severe liver diseases, the drug should be taken only under the supervision of a doctor.

Contraindications

• Hypersensitivity to the active components or other components of the drug; hemosiderosis, hemochromatosis; anemia in violation of iron metabolism (iron deficiency anemia; siderochrestic anemia; anemia associated with chronic lead intoxication; thalassemia); other types of anemia not associated with iron deficiency (hemolytic anemia, megaloblastic anemia caused by vitamin B12 deficiency); simultaneous use of parenteral forms of iron; esophageal stenosis and / or other obstructive diseases of the digestive tract; intestinal diverticulosis, intestinal obstruction; regular blood transfusions.

Side effects

From the digestive tract: when using high doses, light gastrointestinal complications can occur, such as a feeling of heaviness in the stomach, flatulence, constipation or diarrhea, abdominal pain, nausea, epigastric pain, dyspepsia, vomiting. ingestion with food can reduce the frequency of these side effects (see section application). against the background of treatment, a dark color of the stool is possible, due to the release of iron, which was not absorbed in the digestive tract. this change has no clinical significance.

On the part of the immune system: allergic reactions, including anaphylactic reaction, skin rash, exanthema, urticaria, pruritus, cases of staining of tooth enamel in children.

special instructions

In order to avoid the risk of a possible overdose, special care must be taken when using food or other salt additives.

If there is a history of inflammation or ulceration of the gastrointestinal mucosa, the possible risk of an exacerbation of gastrointestinal diseases and the potential benefits of treatment should be carefully evaluated.

In the case of course administration of Actiferrin capsules, regular monitoring of serum iron and hemoglobin is necessary.

Monitoring during treatment: as necessary, approximately every 4 weeks, the following parameters are evaluated to determine the degree of iron deficiency, the response to treatment and the need to continue replenishing the body with iron: hemoglobin level, red blood cell count, average red blood cell volume (MCV), average value erythrocyte hemoglobin content (MCH), reticulocyte count, serum iron content, transferrin. Determination of ferritin in blood serum allows to assess the accumulation of iron; a serum ferritin of 15 mcg / l means no iron stores in the body.

Capsules Given the risk of ulcers of the oral mucosa and discolouration of tooth enamel, capsules should not be sucked, chewed or kept in the mouth. Capsules should be swallowed whole with water.

Actiferrin capsules contain sorbitol. Patients with rare hereditary fructose intolerance or with malabsorption of glucose galactose should not take this drug.

Drops. With the course of administration of drops of Actiferrin, a systematic monitoring of serum iron and hemoglobin is necessary.Patients with diabetes should take into account that the composition of the drug includes carbohydrates: 18 drops (1 ml) contain 64 mg of glucose, which is equivalent to 0.0053 XE.

To prevent the appearance of dark plaque on the teeth of patients, drops of Aktiferrin should not be taken undiluted; after taking the drug, it is recommended to brush your teeth thoroughly.

Against the background of treatment with Actiferrin, the stool may be black in color, due to the release of iron, which was not absorbed. It does not have clinical significance.

To prevent a decrease in iron absorption, it is not recommended to drink Aktiferrin with black tea, coffee and milk. Decreased absorption may also be due to bread, raw cereals, dairy products and eggs; components of vegetarian food (substances that form complex compounds of iron, such as phosphates, phytates and oxalates).

Iron preparations are used with caution in patients with the following diseases: leukemia, chronic liver and kidney diseases, inflammatory diseases of the gastrointestinal tract, gastric and duodenal ulcer, intestinal diseases (enteritis, ulcerative colitis, Crohns disease).

Use during pregnancy or lactation. There is evidence of impaired fetal development and spontaneous abortion due to iron intoxication. During pregnancy, Actiferrin should be taken only if the potential benefits prevail over the possible risk.

Iron-containing drugs in animal studies have not been adequately studied for embryotoxicity.

During breastfeeding, Actiferrin should be taken only if the potential benefit prevails over the possible risk.

Children

Capsules are used in children ≥6 years of age.

Drops can be used in pediatric practice (see APPLICATION).

The ability to influence the reaction rate when driving vehicles or working with other mechanisms. Not investigated.

Interactions

With the simultaneous use of iron salts, the absorption of the following drugs is reduced: tetracycline, dna gyrase inhibitors (e.g. ciprofloxacin, levofloxacin, norfloxacin, ofloxacin), bisphosphonates, penicillamine, levodopa, carbidopa and methyldopa.

Iron salts reduce the absorption of thyroxine, zinc.

Iron absorption decreases with the simultaneous use of colestyramine, antacids containing aluminum, magnesium, calcium, bismuth), as well as calcium and magnesium additives.

Iron absorption may be reduced when combined with chloramphenicol.

Actiferrin should not be taken within 2-3 hours after using one of the above drugs. Whenever possible, the effectiveness of the simultaneous use of drugs should be checked using clinical or laboratory diagnostic methods.

GCS can enhance the stimulation of erythropoiesis by Actiferrin.

Ascorbic / citric acid enhances iron absorption.

The simultaneous intake of vitamin E can reduce the pharmacological effect of iron in the body of the child.

The simultaneous use of iron salts and NSAIDs can enhance the irritating effect of iron on the gastrointestinal mucosa.

Overdose

Symptoms: abdominal pain, diarrhea, vomiting, cyanosis, confusion, symptoms of hyperventilation.

In young children, the risk of acute iron intoxication is particularly high; life-threatening intoxication is possible when taking 1 g of iron sulfate. After an unintentional intake of a large amount of Actiferrin, nausea, severe pain in the stomach, then diarrhea and vomiting with blood, due to the development of hemorrhagic gastroenteritis, first occur. In severe cases, cyanosis, impaired consciousness and hyperpnea may develop as a result of the development of acidosis and impaired peripheral circulation. After about 4–6 hours, remission usually occurs.In the future, after 12–48 hours, a severe shock may develop, accompanied by Cheyne – Stokes breathing, oliguria, toxic liver failure, and coagulopathy.

Treatment: before specific therapy, milk, raw eggs should be consumed.

Symptomatic therapy: flush the stomach with water or a solution of baking soda or phosphate-buffered solution. If necessary, treat shock and acidosis.

Special therapy: patients with symptoms of acute iron overdose with a serum iron level of ≥300–350 μg / dl should be given oral and parenteral deferoxamine. In acute poisoning, 5–10 g of the drug is prescribed inside to bind iron not yet absorbed in the gastrointestinal tract (the contents of 10–20 ampoules should be dissolved in water). To eliminate the absorbed iron, deferoxamine should be given i / m for 1–2 g every 3–12 hours. In severe cases accompanied by the development of shock, patients should be given iv infusion of 1 g of the drug and symptomatic treatment.

A prerequisite for effective treatment of an overdose is the constant release of iron complexes from the body, so patients with oliguria / anuria should be prescribed peritoneal dialysis or hemodialysis.

If necessary, mechanical ventilation is used during shock therapy, radiological monitoring of elimination of toxins from the body and repeated monitoring of the level of serum iron and other indicators of blood serum are carried out.

In case of severe intoxication, calcium diethylene triamine pentaacetate should be used parenterally.

Storage conditions

At a temperature not exceeding 25 ° c. the shelf life of vials with syrup and drops after opening is 1 year.