Ferrolek-zdorovya

INSTRUCTIONS for medical use of the medicinal product FERROLEC-ZDOROVYE (FERROLEC-ZDOROVYE)

Composition:

Active substance: 1 ml of solution contains 50 mg of iron (III) as iron dextran;

Excipient: water for injections.

Pharmaceutical form. Solution for injection.

Main physicochemical characteristics: viscous red-brown liquid.

Pharmacotherapeutic group. Antianemic agents. Parenteral trivalent iron preparations. ATC code B03AC.

Pharmacological Properties.

Pharmacodynamics. Iron is an essential component of hemoglobin, myoglobin, and certain enzymes. Its primary role lies in electron and oxygen molecule transport, as well as in oxidative metabolism during tissue growth and proliferation. As a constituent of enzymes, iron acts as a catalyst in oxidation, hydroxylation, and other vital metabolic processes.

Iron deficiency develops due to inadequate dietary iron intake, impaired iron absorption in the gastrointestinal tract, increased iron requirements (e.g., during periods of rapid growth or pregnancy), and blood loss.

In blood plasma, iron is transported by the β-globulin transferrin, synthesized in the liver. Each transferrin molecule binds two iron atoms. In complex with transferrin, iron is delivered to body cells, where it reversibly binds to ferritin and is utilized for the synthesis of hemoglobin, myoglobin, and certain enzymes.

Following parenteral administration of iron dextran, hemoglobin levels rise more rapidly than after oral administration of iron salts, despite the fact that the kinetics of iron incorporation do not depend on the route of administration.

The iron dextran complex is sufficiently large in size, making its renal excretion impossible. This complex is stable under physiological conditions, and iron is not released in ionic form.

Pharmacokinetics. After intramuscular injection, iron dextran is primarily absorbed via the lymphatic system and diffuses into the bloodstream approximately within 3 days. Data on bioavailability are lacking, but it is known that a significant portion of the complex is not absorbed from muscle tissue over a prolonged period. The half-life (T½) of iron dextran is 3–4 days.

The macromolecular dextran complex enters the reticuloendothelial system, where it dissociates into an iron-containing component and dextran. Iron subsequently binds to ferritin or hemosiderin and, to a lesser extent, to transferrin, and is used for hemoglobin synthesis. Dextran is either metabolized or excreted. The amount of iron excreted is negligible.

Clinical characteristics.

Indications. Treatment of iron deficiency states when treatment with oral iron preparations is ineffective or impossible.

Contraindications. Hypersensitivity to the active substance or any of the excipients; iron overload (e.g., hemochromatosis, hemosiderosis); impaired iron incorporation into hemoglobin (e.g., anemia due to lead poisoning, sideroblastic anemia, thalassemia); anemia not caused by iron deficiency (e.g., hemolytic anemia, megaloblastic anemia); severe coagulation disorders (hemophilia) due to the risk of hematoma; disorders of erythropoiesis, bone marrow hypoplasia, cutaneous porphyria. History of serious hypersensitivity reactions to other parenteral iron preparations. I trimester of pregnancy.

Interaction with other medicinal products and other forms of interaction. The efficacy of parenteral iron preparations may be increased when used concomitantly with ACE inhibitors.

The product should not be administered simultaneously with oral iron preparations, as this may lead to reduced absorption of orally administered iron. Oral iron therapy should not be initiated earlier than 5 days after the last injection of the iron preparation.

Special precautions for use.

The drug should be administered only to patients with clearly established indications and after laboratory confirmation of the patient's condition (e.g., serum ferritin levels, hemoglobin (Hb), hematocrit (Ht), transferrin saturation with iron, red blood cell count, or determination of their parameters: mean corpuscular volume, mean corpuscular Hb content, or mean corpuscular Hb concentration). If intestinal iron malabsorption is suspected, this should be further confirmed by iron absorption testing.

Parenteral administration of iron-containing drugs may cause hypersensitivity reactions, including severe and potentially fatal anaphylactic/anaphylactoid reactions. Therefore, cardiopulmonary resuscitation equipment and anti-allergic therapy supplies must be readily available. In case of mild allergic reaction, antihistamines should be administered; in case of severe anaphylactic reaction, epinephrine should be administered and symptomatic therapy initiated. Hypersensitivity reactions have also occurred in patients who previously tolerated parenteral iron complexes. Hypersensitivity reactions progressing to Koellner's syndrome (acute allergic coronary artery spasm that may lead to myocardial infarction) have been reported (see section "Adverse reactions").

After administration, the patient must remain under medical supervision for at least 30 minutes due to the risk of adverse effects.

Patients with asthma, eczema, other atopic allergies, or allergic reactions to other parenteral iron preparations, Crohn's disease, progressive chronic polyarthritis, as well as patients with low serum iron-binding capacity and/or folic acid deficiency, are at increased risk of developing allergic or anaphylactic reactions.

Extreme caution is required when administering the drug to patients with hepatic or renal insufficiency. Iron preparations should be avoided in patients with liver dysfunction caused by iron overload. Careful monitoring of iron levels is recommended to prevent iron overload.

Cardiovascular complications may occur during iron therapy in patients with heart failure or circulatory disorders.

Adverse effects occurring in patients with cardiovascular diseases may worsen the course of the underlying disease.

In patients with elevated ferritin levels, parenteral iron preparations may negatively affect the course of bacterial or viral infections.

Parenteral iron preparations should be used with caution in cases of acute or chronic infection. In patients with chronic infection, benefit/risk ratio should be carefully evaluated. Discontinuation of the drug is recommended in patients with bacteremia.

If anemia is caused by infection or malignant neoplasm, administered iron accumulates in the reticuloendothelial system and is utilized by the body only after recovery from the underlying disease.

Special caution is required when administering the drug to patients taking any dietary supplements or other products containing iron salts, to avoid risks associated with iron overdose.

Sediment may form in ampoules if improperly stored; therefore, ampoules must be carefully inspected before use. Only ampoules containing a homogeneous solution without sediment should be used. The solution should be administered immediately after opening the ampoule.

Use during pregnancy or breastfeeding. Due to the lack of controlled clinical studies on intramuscular administration of the drug in pregnant women, its use is contraindicated during the first trimester of pregnancy. During the second and third trimesters of pregnancy, the drug may be used only when the expected benefit to the mother outweighs the potential risk to the fetus.

It is unknown whether iron(III) hydroxide-dextran complex is excreted in breast milk. The drug is not recommended for use in breastfeeding women.

Ability to affect reaction speed when driving or operating machinery. Data are lacking. The effect on reaction speed when driving or operating machinery is unlikely. However, if adverse reactions such as dizziness, confusion, or weakness occur after taking the drug, driving or operating machinery should be avoided until symptoms resolve.

Method of administration and dosage. The drug should be administered only intramuscularly. It must not be administered by intravenous injection or infusion.

Patients should be monitored during and after administration for signs of hypersensitivity reactions. Intramuscular injections should be administered only by qualified personnel capable of assessing the patient's condition and immediately providing appropriate treatment for anaphylactic reactions and resuscitation measures. After each administration, the patient must remain under medical supervision for at least 30 minutes due to the risk of adverse effects.

The dose is determined individually depending on the total iron deficit; calculation should be performed using the following formula:

Example calculation:

100 mg

Table for calculating the total number of vials of the drug required for one patient depending on body weight and hemoglobin level

If the total number of ampoules required for the treatment course exceeds the maximum daily dose, administration of the drug should be divided into several doses. If hematological parameters have not normalized after 1–2 weeks of therapy, the established diagnosis and treatment regimen must be reassessed.

Calculation of the total dose required to replenish iron losses due to blood loss.

1. If the volume of blood lost is known: administration of 200 mg of iron intramuscularly (2 ampoules) increases hemoglobin by one blood unit (400 mL of blood with a hemoglobin concentration of 150 g/L).

Total iron dose (mg)
the patient should receive = number of blood units lost × 200

Total number of ampoules of the drug
the patient should receive = number of blood units lost × 2

2. If the reduced hemoglobin level is known: the following formula should be used for calculation, assuming there is no need to replenish stored iron.

Total iron dose (mg) = body weight (kg) × [target hemoglobin level (g/L) –
the patient should receive actual hemoglobin level (g/L)] × 0.24

For a patient weighing 60 kg with a hemoglobin deficit of 10 g/L, 150 mg of iron should be administered (1.5 ampoules of the drug).

Typically, the drug solution is administered every other day, deeply into the upper outer quadrant of the gluteal muscle—alternating between left and right.

To avoid pain and skin discoloration, it is essential to perform the intramuscular injection correctly, using a 50–60 mm needle for adults (80–100 mm needle for obese patients) and a 32 mm needle for children. Prior to injection, the skin should be disinfected, and the subcutaneous tissue should be pulled downward by 2 cm to minimize dispersion of the injected solution.

After administration, pressure should be applied to the injection site for 1 minute.

Children: administer 0.06 mL of the drug per 1 kg of body weight per day (3 mg of iron/kg/day).

Adults and elderly patients: 1–2 ampoules of the drug (100–200 mg of iron) per day.

Maximum daily doses:

Children: 0.14 mL of the drug per 1 kg of body weight (7 mg of iron/kg),
Adults: 4 mL (200 mg or 2 ampoules) of the drug.

Children. Due to lack of experience, the use of the drug is not recommended in children under 4 months of age.

Overdose. Overdose may lead to acute iron overload, which may manifest as hemosiderosis.

No cases of poisoning or iron overload have been reported with overdose of the drug, due to the absence of free iron in the gastrointestinal tract and because iron in the form of a dextran complex is not transported in the body via passive diffusion.

Treatment. Symptomatic therapy. The specific antidote for iron is the chelating agent deferoxamine (an iron-chelating agent), 1 g intravenously (maximum 15 mg/kg/hour).

Adverse reactions.

Adverse reactions are mainly dose-dependent. Acute severe anaphylactoid reactions usually occur within the first few minutes after administration of the drug and are generally characterized by respiratory distress and/or cardiovascular collapse; fatal cases have been reported.

If signs of an anaphylactoid reaction occur, administration of the drug must be stopped immediately.

Delayed-type reactions to the drug have been described (occurring from several hours up to 4 days after administration), which may be severe. Symptoms may last 2–4 days and resolve spontaneously or after administration of conventional analgesics. Exacerbation of joint pain in rheumatoid arthritis may occur.

Cardiovascular system: arrhythmia, tachycardia, chest pain and sensation of tightness (discomfort) in the chest, embryonal bradycardia, palpitations, Kounis syndrome.

Blood and lymphatic system: hemolysis, lymphadenopathy, leukocytosis.

Nervous system: blurred vision, loss of sensation, decreased sensitivity, numbness, seizures, anxiety, dizziness, fainting, excitement, tremor, headache, paresthesia, transient taste disturbance (e.g., metallic taste), altered taste sensation, somnolence, distress.

Ear and labyrinth disorders: transient deafness.

Respiratory system: bronchospasm, dyspnea, respiratory arrest, shortness of breath.

Gastrointestinal system: nausea, vomiting, abdominal pain, diarrhea, constipation.

Skin and subcutaneous tissue: pruritus, urticaria, rash, exanthema, erythema, angioneurotic edema, increased sweating, purpura.

Musculoskeletal system: muscle spasms and cramps, myalgia, limb pain, arthralgia, arthritis, back pain.

Vascular system: sensation of flushing, arterial hypotension, circulatory collapse, arterial hypertension, phlebitis, thrombophlebitis.

General disorders and administration site reactions: feeling of warmth, increased fatigue, asthenia, malaise, fever, chills, peripheral edema, chromaturia, pallor, weakness, pain, chest pain, brownish skin discoloration at injection site, cold sweat. Local reactions reported include burning sensation, swelling, inflammation at or near the injection site, phlebitis, bleeding, abscess formation, tissue necrosis or atrophy, hematoma formation.

Immune system: anaphylactoid reactions, including dyspnea, urticaria, rash, pruritus, nausea, and tremor; acute severe anaphylactoid reactions (sudden respiratory distress and/or cardiovascular failure); hypersensitivity, angioedema; fatal outcomes have been reported. Delayed-type reactions are pronounced in nature and may be severe. They manifest as arthralgia, myalgia, and occasionally fever.

Psychiatric disorders: changes in mental status, impaired consciousness, confusion, loss of consciousness.

Shelf life. 5 years.

Storage conditions. Store in the original packaging at a temperature not exceeding 25 °C.

Do not freeze. Keep out of reach of children.

Incompatibility. The drug must not be mixed with other medicinal products in the same container.

Packaging. 2 ml in vials, 5 in a box; 5 in a blister pack in a box.

Prescription status. Prescription only.

Manufacturer. LIMITED LIABILITY COMPANY "CORPORATION "ZDOROVTYA".

Manufacturer's address and place of business. Ukraine, 61013, Kharkiv region, city of Kharkiv, Shevchenko Street, 22.