Fersinol solution for injection 100 mg ampoule 2 ml No. 5

Instructions Fersinol solution for injection 100 mg ampoule 2 ml No. 5

Composition

active ingredient: iron (III) hydroxide polymaltose complex;

1 ampoule (2 ml) contains iron (III) hydroxide polymaltose complex in terms of iron (III) 100 mg;

excipient: water for injections.

Dosage form

Solution for injection.

Main physicochemical properties: dark, reddish-brown homogeneous liquid without mechanical inclusions.

Pharmacotherapeutic group

Antianemic agents. Trivalent iron preparations for parenteral use. ATX code B03A C01.

Pharmacological properties

Pharmacodynamics.

After intramuscular administration, almost all of the iron from the polymaltose complex of iron (III) hydroxide as the active ingredient enters the reticuloendothelial system of the liver, and is also taken up by transferrin, apoferritin, spleen and bone marrow. There it combines with hemoglobin, myoglobin and iron-containing enzymes, and is also stored in the body in the form of ferritin. Changes in blood parameters with parenteral administration of iron do not occur faster than with oral administration of iron salts. Like other iron preparations, the drug does not affect erythropoiesis and is not effective in anemias not associated with iron deficiency.

Pharmacokinetics.

After intramuscular injection, the complex enters the bloodstream. The maximum iron concentration is reached approximately 24 hours after injection. In the blood, iron binds to transferrin. From the plasma, the macromolecular complex enters the reticuloendothelial system, where it is split into iron hydroxide and polymaltose. In the tissues, it is stored as part of ferritin, in the bone marrow it combines with hemoglobin and is used in the process of erythropoiesis.

Only small amounts of iron are excreted from the body. Polymaltose is metabolized by oxidation and excreted.

In small amounts, the unchanged complex can cross the placental barrier, and small amounts of it penetrate into breast milk. Iron bound to ferritin or transferrin can cross the placental barrier, and as part of lactoferrin is excreted into breast milk in small amounts.

The incorporation of iron into protoporphyrin depends on the degree of iron deficiency anemia. It is more intense in the case of low hemoglobin levels and decreases in accordance with the normalization of hemoglobin levels. The degree of iron utilization cannot be higher than the iron-binding capacity of transport proteins.

Indication

Treatment of iron deficiency anemia in the following cases:

in case of contraindications to oral therapy;

in case of impaired absorption of iron in the intestine;

in case of non-compliance by the patient with the treatment regimen with oral iron preparations or their persistent gastrointestinal intolerance.

Contraindication

Hypersensitivity to iron hydroxide polymaltose complex;

anemias not associated with iron deficiency (e.g., hemolytic anemia, megaloblastic anemia, impaired erythropoiesis, bone marrow hypoplasia);

excess iron in the body (hemosiderosis, hemochromatosis);

Osler–Randu–Weber syndrome;

chronic polyarthritis;

bronchial asthma;

infectious kidney diseases in the acute stage;

uncontrolled hyperparathyroidism;

uncompensated liver cirrhosis;

infectious hepatitis;

I trimester of pregnancy;

severe inflammation or infection of the kidneys or liver (due to the ability of elemental iron to accumulate in inflamed tissues).

Interaction with other medicinal products and other types of interactions

As with other parenteral iron preparations, the drug should not be used simultaneously with oral iron preparations, as this may lead to a decrease in the absorption of orally administered iron. Therefore, treatment with oral iron preparations should be started no earlier than 7 days after the last administration of parenteral iron preparations.

Concomitant use of ACE inhibitors (e.g. enalapril) may lead to increased systemic effects of parenteral iron preparations, such as erythema, abdominal cramps, nausea, vomiting and hypotension.

Interaction with laboratory test results.

High intravenous doses of iron preparations (250 mg of iron or more) may cause brown staining of plasma in blood samples taken 4 hours after their administration.

Iron supplements may cause falsely elevated plasma bilirubin levels and falsely low plasma calcium levels. Plasma iron measurements (especially colorimetric methods) may not be informative for up to 3 weeks after iron supplementation. Plasma iron measurements obtained 1–2 weeks after high-dose iron supplementation should be interpreted with caution.

Skeletal bone scans using Tc-99m diphosphonate, performed 1–6 days after intramuscular injection of iron, may show dense areas of activity in the femur that follow the contours of the iliac crest. Skeletal bone scans using Tc-99m-labeled imaging agents in the presence of high plasma ferritin concentrations or after intravenous iron infusions may demonstrate decreased bone resorption, marked renal activity, hyperperfusion, and soft tissue deposition.

Iron preparations may reduce the uptake of 67Ga-citrate during imaging of tumors and/or abscesses, which is a result of competition for the same binding sites.

The presence of iron may lead to false-positive results in the orthotoluidine test.

Application features

The drug should be used only in cases of iron deficiency confirmed by appropriate studies (for example, determination of plasma ferritin levels, hemoglobin, hematocrit, red blood cell count, as well as their parameters - mean erythrocyte volume, mean hemoglobin concentration in the red blood cell).

Unjustified use of parenteral iron preparations in patients whose anemia is not associated with iron deficiency (for example, patients with hemoglobinopathy) can lead to excessive iron accumulation and the development of a syndrome similar to hemosiderosis.

Since parenteral administration of iron preparations has resulted in the development of anaphylactoid reactions with fatal outcome, the drug should be used only in patients with a clearly established indication and after confirmation of the patient's condition by laboratory tests. In the event of a mild allergic reaction, antihistamines should be used.

With parenteral administration of iron preparations, there is a risk of hypersensitivity and anaphylactoid reactions with each dose. Anaphylactoid reactions most often occur within the first few minutes after administration and are usually characterized by sudden difficulty breathing, tachycardia, and hypotension. A test dose is not necessary, since the absence of such a reaction with a test dose does not mean that there will be no reaction with subsequent doses.

The product should only be administered when medical personnel trained in the assessment and treatment of anaphylactic reactions are available for immediate response and in a room equipped with adequate resuscitation facilities. Each patient should be observed for adverse reactions for at least 30 minutes after each intravenous administration of iron preparations. If any allergic reactions or signs of intolerance occur during administration of the product, treatment should be discontinued immediately.

Patients with bronchial asthma, low iron binding capacity and/or folic acid deficiency are at high risk of developing allergic or anaphylactic reactions.

The drug should be used with caution in patients with allergies, liver and kidney failure, or cardiovascular disease.

Patients with rheumatoid arthritis and possibly other inflammatory diseases (e.g. ankylosing spondylitis, systemic lupus erythematosus) may be at increased risk of developing delayed reactions, including fever and exacerbation or reactivation of joint pain.

In the post-marketing period, symptomatic hypophosphatemia, resulting in osteomalacia and fractures, requiring clinical intervention, including surgery, has been reported. Patients should be advised to seek medical advice if they experience increased fatigue with myalgia or bone pain. Plasma phosphate levels should be monitored during prolonged use or high doses, and in the presence of risk factors for hypophosphatemia. In the event of persistent hypophosphatemia, the use of the drug should be reconsidered.

Use during pregnancy or breastfeeding

Pregnancy.

The drug is contraindicated for use during the first trimester of pregnancy. There are no data from studies in animals or pregnant women. Embryofetal toxicity has been observed in animals receiving intravenous iron preparations.

During the II and III trimesters of pregnancy, the drug can be used only if the expected benefit to the mother outweighs the potential risk to the fetus.

Breastfeeding period.

There are no data from studies involving breastfeeding women. The possibility of iron passing into breast milk should be taken into account. In case of use of the drug during breastfeeding, the expected benefit to the mother and the potential risk to the child should be taken into account.

Ability to influence reaction speed when driving vehicles or other mechanisms

There are no relevant studies.

Method of administration and doses

The drug is intended for deep intramuscular injection. Intravenous administration is contraindicated.

Before injection, the ampoules and their contents should be carefully inspected. Only ampoules that are free of sediment and undamaged are acceptable for use. The drug should be administered immediately after opening the ampoule.

Injection technique is important. The solution should not be injected into the shoulder or damaged areas. Incorrect injection may cause pain and discoloration of the skin at the injection site.

It is recommended to inject the drug into the ventrogluteal area according to Hochstetter instead of the usual injection into the upper outer quadrant of the gluteal muscle.

The length of the needle should be at least 5–6 cm. The lumen of the needle should not be too wide.

Injection technique

1. Determine the injection site as follows: find point A, which corresponds to the anterior surface of the iliac crest. For example, if the patient is lying on his right side, the middle finger of the left hand should be placed at point A. The index finger should be moved away from the middle finger so that it is located under the line of the iliac crest at point B. The triangle located between the proximal phalanges of the middle and index fingers is the injection site. Disinfection is carried out by the usual method.

2. Before inserting the needle, pull the skin back about 2 cm from the injection site to create an S-shaped puncture channel. This prevents the injected solution from flowing back into the subcutaneous tissue and discoloring the skin.

3. Insert the needle almost vertically relative to the skin surface at an angle greater to the point of the iliac joint than to the point of the femoral joint.

4. After injection, slowly remove the needle and press the skin area adjacent to the injection site with your finger. Hold for approximately 1 minute.

5. After the injection, the patient should move.

Dosage

Dose calculation

The dose of the drug is calculated individually, according to the total iron deficiency according to the following formula:

* Factor 0.24 = 0.0034 × 0.07 × 1000 (iron content in hemoglobin - 0.34%/blood volume - 7% of body weight/factor 1000 - conversion from grams to milligrams).

The above formula can also be used to calculate total iron deficiency.

With a body weight of less than 35 kg: normal Hb level = 130 g/l, which corresponds to iron stores of 15 mg/kg of body weight.

With a body weight of more than 35 kg: normal Hb level = 150 g/l, which corresponds to iron stores of 500 mg.

Dosage table

Dosage table to determine the total amount of medicine required

The drug should be administered intramuscularly in a dose of 2 ml every other day until the total dose is obtained or 4 ml should be administered at longer intervals.

It is recommended to regularly measure Hb levels while using the drug.

Maximum dosage.

Children weighing up to 5 kg: 0.5 ml = 25 mg of iron (¼ ampoule).

Children weighing 5 to 10 kg: 1 ml = 50 mg of iron (½ ampoule).

Patients with a body weight of 10 to 45 kg: 2 ml = 100 mg of iron (1 ampoule) per day.

Adults with a body weight of 45 kg or more: 4 ml = 200 mg of iron (2 ampoules).

Children

The medicine can be used in children from 4 months of age.

Overdose

There are no reports of overdose.

Overdose may cause acute iron overload, manifested by symptoms of hemosiderosis. Treatment is symptomatic.

Periodic monitoring of plasma ferritin levels can aid in the early recognition of progressive iron overload.

If necessary, iron-binding agents (chelates), such as deferoxamine intravenously, are used.

When the drug is administered in very high doses, the complex cannot be removed from the body by hemodialysis due to the high molecular weight of the active substance.

Side effects

Adverse reactions occur infrequently. The following adverse reactions may occur after the use of parenteral iron preparations.

Blood and lymphatic system disorders:

generalized lymphadenopathy.

On the part of the immune system:

anaphylaxis.

From the digestive tract:

nausea, vomiting.

From the nervous system:

headache, dizziness.

From the respiratory system, chest organs and mediastinum:

bronchospasm with dyspnea.

From the cardiovascular system:

loss of consciousness, fainting, tachycardia, hypotension, circulatory collapse.

Skin and subcutaneous tissue disorders:

rash, urticaria, angioedema.

Musculoskeletal and connective tissue disorders:

joint and muscle pain, arthralgia, feeling of stiffness in the arms, legs or facial muscles, hypophosphatemic osteomalacia.

General disorders and administration site conditions:

flushing, pain behind the sternum and in the back, pain at the injection site, local inflammation with inguinal lymphadenopathy, pain in the lower quadrant of the abdomen.

Adverse reactions may occur with a delay of 1-2 days after treatment.

Reporting of suspected adverse reactions

Reporting suspected adverse reactions that occur after the registration of a medicinal product is very important. This allows for continuous monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals should report any suspected adverse reactions through the national pharmacovigilance system.

Expiration date

3 years.

Storage conditions

Store at a temperature not exceeding 25 °C out of the reach of children.

Incompatibility

The solution for injection should not be mixed with other drugs. The drug is compatible only with sterile 0.9% sodium chloride solution. Any other solutions should not be used.

Packaging

2 ml in an ampoule, 5 ampoules in a contour blister pack and a cardboard box.

Vacation category

According to the recipe.

Producer

PharmaVision San. in Tij. A.Sh. / PharmaVision San. ve Tic. AS

Location of the manufacturer and address of its place of business

Davutpasa Cad. No:145 Zeytinburnu Istanbul, Turkey.

Applicant

WORLD MEDICINE, LLC, Ukraine.