Ferrum Lek solution for injection 100 mg ampoule 2 ml No. 5

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

Composition

active ingredient: iron (III) in the form of a complex of iron (III) hydroxide with dextran;

1 ampoule (2 ml of solution) contains 100 mg of iron (III) in the form of a complex of iron (III) hydroxide with dextran;

Excipients: sodium hydroxide, concentrated hydrochloric acid, water for injections.

Dosage form

Solution for injection.

Main physicochemical properties: opaque brown solution.

Pharmacotherapeutic group

Antianemic agents. Trivalent iron preparations for parenteral use. ATC code B0ZA C06.

Pharmacological properties

Pharmacodynamics.

Ferrum Lek injection solution contains iron in the form of a complex of iron (III) hydroxide with dextran, which is an analogue of the physiological form of iron in the body - ferritin (protein hydroxide-iron-phosphate complex). The concentration of ferritin in the blood serum reaches a maximum approximately 7-9 days after intravenous administration of a dose of Ferrum Lek and slowly returns to the initial level after approximately 3 weeks. Bone marrow studies of iron stores after long-term therapy with a complex of iron (III) hydroxide with dextran may be inaccurate, since residual iron complex with dextran may accumulate in reticuloendothelial cells.

Pharmacokinetics

After intramuscular injection, the complex of iron (III) hydroxide with dextran is absorbed mainly through the lymphatic system and diffuses into the blood after about 3 days. Data on bioavailability are not available, but it is known that a fairly large part of the complex is not absorbed from muscle tissue for a long period. The half-life of the complex of iron (III) hydroxide with dextran is 3–4 days.

The macromolecular dextran complex enters the reticuloendothelial system, where it is broken down into the iron-containing component and dextran. The iron then binds to ferritin or hemosiderin and, to a lesser extent, to transferrin and participates in hemoglobin synthesis. Dextran is metabolized or excreted. The amount of iron excreted is insignificant. Iron is not readily excreted from the body, and its accumulation can be toxic. Due to its size, the complex of iron (III) hydroxide with dextran is not excreted by the kidneys. A small amount of iron is excreted in the urine and feces.

Indication

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

Contraindication

Increased individual sensitivity to the active substance or to any other component of the medicinal product;

anemia not related to iron deficiency;

excess iron in the body (for example, hemochromatosis, hemosiderosis);

disorders of iron incorporation into hemoglobin (e.g., anemia caused by lead poisoning, sideroblastic anemia);

severe hemostasis disorders (hemophilia) due to possible hematomas;

known serious hypersensitivity to other parenteral forms of iron preparations;

I trimester of pregnancy (see section "Use during pregnancy or breastfeeding").

Interaction with other medicinal products and other types of interactions

As with other parenteral iron preparations, Ferrum Lek should not be used concomitantly with oral iron preparations, as this may lead to reduced absorption of orally administered iron. Therefore, treatment with oral iron preparations should be initiated no earlier than 5 days after the last injection of iron preparation.

The effectiveness of parenteral iron preparations is increased when they are used simultaneously with angiotensin-converting enzyme (ACE) inhibitors.

Application features

Ferrum Lek can only be used in patients with clearly established indications and after confirming the patient's condition with laboratory test results (for example, serum ferritin or hemoglobin (Hb) or hematocrit (Ht), transferrin iron saturation or red blood cell count, or determination of their parameters: mean erythrocyte volume, mean content or mean Hb concentration in the erythrocyte). In cases where there is suspicion of intestinal iron malabsorption, this should be additionally confirmed by an iron absorption test.

Hypersensitivity reactions have been reported, progressing to Kunis syndrome (acute allergic coronary arteriospasm, which can cause myocardial infarction - see section "Adverse reactions").

After administration of the drug, the patient should be under the supervision of a doctor for at least 30 minutes due to the risk of side effects.

Patients with asthma, eczema, other atopic allergies, or allergic reactions to other parenteral iron preparations are at particular risk of allergic or anaphylactic reactions.

The risk of hypersensitivity reactions when using parenteral forms of iron is increased in patients with immune or inflammatory conditions (e.g., systemic lupus erythematosus, rheumatoid arthritis), Crohn's disease, progressive chronic polyarthritis, and in patients with low serum iron binding capacity and/or folic acid deficiency.

It is necessary to be very careful when administering the drug to patients with hepatic and renal insufficiency. The use of iron preparations should be avoided in patients with impaired liver function caused by iron overload. It is recommended to carefully monitor iron levels to avoid overload.

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

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

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

Parenteral iron preparations should be used with caution in acute or chronic infections. In patients with chronic infections, a benefit/risk assessment should be performed. It is recommended to discontinue the use of Ferrum Lek in patients with bacteremia.

If anemia is caused by an infection or tumor, the iron introduced into the body accumulates in the reticuloendothelial system and begins to be used by the body only after the underlying disease is cured.

If patients are taking any dietary supplements or other products containing iron salts, special care should be taken when using Ferrum Lek to avoid possible risks associated with iron overdose.

If the ampoules are stored incorrectly, a precipitate may form, so they should be carefully inspected before use. Only ampoules containing a homogeneous solution without a precipitate should be used. The solution should be used immediately after opening the ampoule.

When using the drug, paravenous leaks should be avoided, since when administering the complex of iron (III) hydroxide with dextran, their presence at the injection site can cause pain, inflammation and brown discoloration of the skin.

Use during pregnancy or breastfeeding

Pregnancy.

Due to the lack of data from controlled clinical studies on the intramuscular administration of Ferrum Lek to pregnant women, its administration is possible only in case of extreme necessity after a careful assessment of the benefit/risk ratio. In most cases, iron preparations for oral administration are used to treat iron deficiency anemia in the first trimester of pregnancy. In the second and third trimesters of pregnancy, Ferrum Lek solution for injection can be used only when the expected benefit to the mother and fetus outweighs the potential risks.

When using parenteral forms of iron, fetal bradycardia may occur, which is usually reversible and is a consequence of maternal hypersensitivity. During intravenous administration of parenteral iron, a pregnant woman should carefully monitor the condition of the unborn child.

Breast-feeding.

It is not known whether iron (III) hydroxide dextran complex passes into breast milk. The drug is not recommended for use in women who are breastfeeding.

Ability to influence reaction speed when driving vehicles or other mechanisms

No data available. Impact on reaction speed when driving or using other mechanisms is unlikely.

Method of administration and doses

Ferrum Lek solution should only be administered intramuscularly! It cannot be administered by intravenous injection or infusion.

During and after administration of Ferrum Lek, patients should be observed for symptoms of hypersensitivity reactions. Intramuscular injections should only be performed by qualified personnel who can assess the patient's condition and immediately administer appropriate anaphylactic and resuscitation measures. After each administration, the patient should be observed for at least 30 minutes due to the risk of side effects.

The dose of the drug is determined individually depending on the overall iron deficiency; the calculation is carried out according to the formula:

target hemoglobin value = 130 g/l,

deposited iron = 15 mg/kg body weight;

Calculation example:

100 mg

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

If the total number of ampoules per course of treatment exceeds the maximum daily dose, it is necessary to divide the administration of the drug into several times. If after 1–2 weeks of therapy there is no normalization of hematological parameters, it is necessary to review the established diagnosis and treatment regimen.

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

1. If the amount of blood loss is known: when administering 200 mg of iron intramuscularly

(2 ampoules) there is an increase in hemoglobin level by 1 unit of blood (400 ml of blood with a hemoglobin content of 150 g/l).

Total iron (mg),

which the patient should receive = number of units of blood lost ´ 200

Total number of Ferrum Lek ampoules,

which the patient should receive = number of units of blood lost ´ 2.

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

Total iron (mg), = body weight (kg) ´ [target hemoglobin (g/L) –

which the patient should receive [actual hemoglobin level (g/l)] ´ 0.24.

A patient with a body weight of 60 kg and a hemoglobin deficiency of 10 g/l needs to be given 150 mg of iron

(1½ ampoules of Ferrum Lek).

Typically, Ferrum Lek solution is injected every other day deep into the upper outer quadrant of the gluteal muscle — alternately into the left and right.

To avoid pain and skin discoloration, it is important to perform the intramuscular injection properly, using a needle 50–60 mm long for adults (for obese patients, a needle 80–100 mm long should be used) and 32 mm for children. Before injection, the skin should be disinfected, the subcutaneous tissue should be pulled down by 2 cm to reduce the spread of the injected solution. After administration, the injection site should be pressed for 1 minute.

Children should be given 0.06 ml of the drug per 1 kg of body weight per day (3 mg of iron / kg per day).

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

Maximum daily doses:

for children - 0.14 ml of the drug per 1 kg of body weight (7 mg of iron / kg),

for adults - 4 ml (200 mg or 2 ampoules) of the drug.

Children

Due to lack of experience, the use of Ferrum Lek, solution for injection, in children under 4 months of age is not recommended (see section “Method of administration and dosage”).

Overdose

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

In case of overdose of the drug, no signs of poisoning and iron overload were observed, which is due to the absence of free iron in the digestive tract, as well as the fact that iron in the form of a complex with dextran is not transported in the body by passive diffusion.

Treatment. Symptomatic therapy. The specific antidote to iron is the chelating agent deferoxamine (an iron-binding agent) — 1 g intravenously (maximum 15 mg/kg/h).

Side effects

Acute severe anaphylactoid reactions are rare. They usually occur within the first few minutes after administration and are generally characterized by difficulty breathing and/or cardiovascular collapse, and fatalities have been reported.

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

Delayed drug reactions (from a few hours to 4 days after drug administration) are possible, which can be severe. Symptoms may last 2–4 days and resolve spontaneously or after the use of conventional analgesics.

With rheumatoid arthritis, there may be increased joint pain.

Local adverse reactions include pain and inflammation at the injection site.

With intramuscular administration of the drug, local reactions may occur at the injection site, such as skin spots, bleeding, inflammation of the subcutaneous tissue, tissue necrosis or atrophy, and pain.

Adverse reactions are classified by frequency of occurrence into the following categories: very common (≥ 1/10); common (≥ 1/100, < 1/10); uncommon (≥ 1/1000, < 1/100); rare (≥ 1/10,000, < 1/1000); rare (< 1/10,000), frequency unknown (cannot be estimated from the available data).

Adverse reactions associated with the use of the drug Ferrum Lek, solution for injection:

From the side of the cardiac system.

Rare: arrhythmia, tachycardia, chest pain and tightness.

Rare: fetal bradycardia, palpitations.

Frequency unknown: Kunis syndrome.

From the blood and lymphatic system.

Rare: hemolysis, lymphadenopathy.

Frequency unknown: leukocytosis.

From the nervous system.

Uncommon: blurred vision, loss of sensation;

Rare: convulsions, dizziness, anxiety, tremor.

Rare: headache, paresthesia.

Frequency unknown: short-term taste disturbance (especially metallic taste).

From the side of the organs of hearing and labyrinth.

Rare: short-term deafness.

On the part of the respiratory system, chest organs and mediastinum.

Uncommon: dyspnoea, bronchospasm.

Frequency unknown: respiratory arrest.

From the digestive tract.

Uncommon: nausea, vomiting, abdominal pain.

Uncommon: diarrhea.

On the part of the musculoskeletal system and connective tissue.

Uncommon: muscle spasms and cramps.

Uncommon: myalgia.

Frequency unknown: arthralgia, arthritis, back pain.

From the vascular system.

Uncommon: hot flushes.

Rare: hypotension, collapse.

Rare: hypertension.

General disorders and local reactions.

Uncommon: feeling hot.

Rare: anaphylactic reactions (in isolated cases including arthralgia), asthenia, general malaise.

Frequency unknown: fever, flu-like symptoms that may occur after a few hours or days, chills.

From the immune system.

Uncommon: anaphylactoid reactions, including dyspnea, urticaria, rash, pruritus, nausea, and tremor;

Rare: acute severe anaphylactoid reactions (sudden difficulty breathing and/or cardiovascular failure); fatal outcomes have been reported.

Mental disorders.

Isolated: change in mental status.

Frequency unknown: confusion.

On the skin and subcutaneous tissue.

Uncommon: pruritus, rash, urticaria, exanthema, erythema.

Rare: Quincke's edema, sweating, pain and brown discoloration at the injection site.

Frequency unknown: purpura.

Laboratory indicators.

Increased alanine aminotransferase, increased aspartate aminotransferase, increased gamma-glutamyltransferase, increased blood ferritin and lactate dehydrogenase, decreased blood phosphorus, increased alkaline phosphatase.

With intramuscular administration of the drug, local reactions may occur at the injection site, such as skin spots, bleeding, inflammation of the subcutaneous tissue, tissue necrosis or atrophy, and pain.

Adverse reactions reported with parenteral iron preparations during clinical trials and post-marketing studies*:

From the immune system.

Hypersensitivity, anaphylactoid reactions*, angioedema*.

From the nervous system.

Taste disturbance, headache, dizziness, paraesthesia, decreased sensitivity, fainting, drowsiness, distress*, confusion*, loss of consciousness*, anxiety, tremor.

From the side of the cardiac system.

Palpitations, bradycardia*, tachycardia*.

From the vascular system.

Arterial hypotension, arterial hypertension, hot flashes, phlebitis, circulatory collapse*, thrombophlebitis*.

On the part of the respiratory system, chest organs and mediastinum.

Dyspnea, bronchospasm*.

From the digestive tract.

Nausea, vomiting, abdominal pain, diarrhea, constipation.

On the skin and subcutaneous tissue.

Pruritus, rash, urticaria*, erythema*.

On the part of the musculoskeletal system and connective tissue.

Muscle spasms and cramps, myalgia, pain in extremities, back pain.

On the part of the kidneys and urinary system.

Chromaturia*.

General disorders and local reactions.

Injection site reactions**, chills, asthenia, weakness, peripheral edema, pain, chest pain, hyperhidrosis, fever, cold sweat*, fatigue*, pallor*.

The most common adverse reactions in clinical trials were taste changes, which occurred in 4.5 cases per 100 people. The most important serious adverse reactions were hypersensitivity reactions, which occurred in 0.25 cases per 100 people in clinical trials.

Reporting adverse reactions after registration of a medicinal product is important. This allows monitoring of the benefit/risk ratio of the medicinal product. Medical and pharmaceutical professionals, as well as patients or their legal representatives, should report all cases of suspected adverse reactions and lack of efficacy of the medicinal product via the Automated Pharmacovigilance System at the link: https://aisf.dec.gov.ua/.

Expiration date

5 years.

Storage conditions

Store at a temperature not exceeding 25 ° C. Do not freeze.

Keep out of reach of children.

Incompatibility

Ferrum Lek solution should not be mixed with other medicines.

Packaging

2 ml of solution in an ampoule; 5 or 10 ampoules in a blister, 1 (5 ´ 1) or 5 (10 ´ 5) blisters in a cardboard box.

Vacation category

According to the recipe.

Producer

Lek Pharmaceuticals dd, Slovenia.

Location of the manufacturer and address of its place of business

Verovskova 57, 1526 Ljubljana, Slovenia.