Likferr 100 solution 20mg/ml 5ml ampoules, 5pcs

Composition

Active ingredient:

iron (III) hydroxide sucrose complex (in terms of iron (III) 20 mg;

Auxiliary substances:

sodium hydroxide-up to pH 11;

water for injection – up to 1 ml

Pharmacological action

Likferr 100 – antianemic.

Pharmacodynamics

Iron preparation, regulates metabolic processes. It is a colloidal solution that consists of spheroidal iron-carbohydrate nanoparticles. In the core (center) of each particle is iron (III) hydroxide. The core is surrounded by a sucrose shell that stabilizes iron (III) hydroxide, slowly releases bioactive iron, and stores the resulting particles in a colloidal solution. As a result, a complex is formed with a molecular weight of approximately 43 kDa, so that its excretion through the kidneys in unchanged form is impossible. Iron (III) in this complex is bound to structures similar to natural ferritin.

The Active ingredient of the drug — iron (III) hydroxide sucrose complex-when ingested dissociates in the reticuloendothelial system into iron and sucrose. Due to the lower stability of iron saccharate compared to transferrin, there is a competitive exchange of iron in favor of transferrin. As a result, about 31 mg of iron is transferred in 24 hours. Polycyclic iron (III) hydroxide is partially preserved as ferritin after complexation with the protein ligand apoferritin of liver mitochondria. The hemoglobin index increases faster and with greater confidence than after therapy with drugs containing iron (II). The introduction of 100 mg of iron (III) leads to an increase in hemoglobin by 2-3%; during pregnancy-by 2%. The toxicity of the drug is very low. The therapeutic index is 30 (200/7).

Pharmacokinetics

After a single intravenous injection of Likferr 100® containing 100 mg of iron, _cmaxof iron (on average — 538 mmol) is reached 10 minutes after the injection. T_1/2-6 h. V_ssis approximately 8 l, which indicates a low distribution of iron in the body fluids.

Renal iron excretion in the first 4 hours after injection is less than 5% of the total clearance. After 24 hours, the serum iron content returns to its original (pre-use) value, and approximately 75% of sucrose leaves the vascular bed.

Indications

Iron deficiency conditions (including iron deficiency and acute post-hemorrhagic anemia) in patients with the following conditions:

• the need for rapid replenishment of iron;
• intolerance to oral iron preparations;
• the presence of gastrointestinal diseases that make it impossible to take oral iron preparations.

Use during pregnancy and lactation

The drug is contraindicated in the first trimester of pregnancy. In the second and third trimesters of pregnancy, it is used only if the intended benefit to the mother exceeds the potential risk to the fetus.

During lactation, the safety of using the drug has not been established. It is recommended to stop breastfeeding (if necessary, use the drug) or cancel the drug.

Contraindications

• hypersensitivity to the components of the drug Likferr 100®;
• anemia, not associated with iron deficiency;
• the presence of signs of iron overload (hemosiderosis, hemochromatosis) or a violation of the process of its utilization;
• I trimester of pregnancy (see “Use during pregnancy and lactation”).

With caution:  bronchial asthma; eczema; polyvalent allergy; allergic reactions to other parenteral iron preparations (due to a high risk of allergic reactions — see “Special Instructions”); liver failure; acute infectious diseases; low serum iron binding capacity and/or folic acid deficiency; diabetes mellitus (see “Special Instructions”); age up to 18 years (due to insufficient data on safety and efficacy).

Side effects

From the central nervous system:  dizziness, headache, loss of consciousness, paresthesia.

From the CCC side:  palpitations, tachycardia, decreased heart rate Blood pressure, collaptoid states, feeling hot, flushes of blood to the face, peripheral edema.

Respiratory system disorders:  bronchospasm, shortness of breath.

From the digestive system:  transient taste disturbances (especially metallic taste in the mouth), spilled abdominal pain, epigastric pain, diarrhea, taste distortion, nausea, vomiting.

From the side of the skin:  erythema, pruritus, rash, pigmentation disorder, increased sweating.

From the musculoskeletal system:  arthralgia, back pain, joint swelling, myalgia, pain in the extremities.

Allergic reactions:  anaphylactoid reactions, facial edema, laryngeal edema.

Other services:  asthenia, chest pain, back pain, feeling of heaviness in the chest, weakness, feeling unwell, pallor, fever, chills.

Local reactions:  pain and swelling at the injection site (especially with extravasal ingestion of the drug), phlebitis, burning sensation, hematoma.

Interaction

Concomitant use of Likferr 100® with medicinal forms of iron for oral use is unacceptable, since iron absorption from the gastrointestinal tract decreases. Treatment with oral iron supplements can be started no earlier than 5 days after the last injection.

Likferr 100® can only be mixed in a single syringe with 0.9% sodium chloride solution. No other intravenous solutions and therapeutic preparations are allowed to be added, as there is a risk of precipitation and / or other pharmaceutical interaction. Compatible with containers made of materials other than glass, PE and PVC, not studied.

If the patient is taking other medications, you should consult your doctor.

How to take, course of use and dosage

Intravenously (slowly by jet or drip), as well as in the venous section of the dialysis system. The drug is not intended for intravenous use. Simultaneous use of a full (cumulative) therapeutic dose of the drug is unacceptable.

Before the first therapeutic dose is administered, a test dose should be prescribed. If intolerance occurs during the follow-up period, the drug should be discontinued immediately. Before opening the ampoule, it is necessary to examine it for possible sediment and damage. You can only use a brown solution without sediment.

Drip introduction

Likferr 100® should preferably be administered as a drip infusion in order to reduce the risk of severe weight loss. Blood pressure and the risk of solution entering the parovenous space. Immediately before the infusion, Likferr 100® should be diluted with 0.9% sodium chloride solution in a ratio of 1: 20-for example,1 ml (20 mg of iron) in 20 ml of 0.9% sodium chloride solution. The resulting solution is introduced at the following rate: 100 mg of iron — for at least 15 minutes; 200 mg – for 30 minutes; 300 mg – for 1.5 hours; 400 mg – for 2.5 hours; 500 mg – for 3.5 hours. The maximum tolerated single dose of 7 mg of iron/kg should be administered for at least 3.5 hours, regardless of the total dose of the drug.

Before the first drop of the therapeutic dose of Likferr 100®, a test dose should be administered: 1 ml of Likferr 100® (20 mg of iron) for adults and children weighing more than 14 kg and half the daily dose (1.5 mg of iron/kg) for children weighing less than 14 kg for 15 minutes. In the absence of adverse events, the remaining part of the solution should be administered at the recommended rate.

Jet introduction

Likferr 100® can also be administered as an undiluted solution intravenously slowly, at a rate 1 ml of Likferr 100® (20 mg of iron) per minute — for example,5 ml of Likferr 100® (100 mg of iron) is administered within 5 minutes. The maximum volume of the drug should not exceed 10 ml of Likferr 100® (200 mg of iron) per injection.

After the injection, the patient is recommended to fix the arm in an extended position for some time.

Before the first jet dose of Likferr 100®, a test dose should be administered: 1 ml of Likferr 100® (20 mg of iron) for adults and children weighing more than 14 kg and half the daily dose (1.5 mg of iron/kg) for children weighing less than 14 kg for 1-2 minutes. If there are no adverse events during the next 15 minutes of observation, the remaining part of the solution should be administered at the recommended rate. After the injection, the patient is recommended to fix the arm in an extended position.

Introduction to the dialysis system

Likferr 100® can be administered directly into the venous section of the dialysis system, strictly following the rules described for intravenous injection.

Dose calculation

Before use, it is necessary to individually calculate the total iron deficiency in the body using the following formula: :

Total iron deficiency (mg) = body weight (kg) × (normal Hb-patient’s Hb (g / l) × 0.24 + deposited iron (mg).

For patients with a body weight of less than 35 kg:

• the amount of deposited iron = 15 mg / kg;
• normal Hb = 130 g/l.

For patients with a body weight of more than 35 kg:

• the amount of deposited iron = 500 mg;
• normal Hb = 150 g/l.

Coefficient 0.24 = 0.0034 × 0.07 × 1000 (iron content in hemoglobin = 0.34%; blood volume = 7% of body weight; coefficient 1000 = conversion from grams to milligrams).

Then you should calculate the cumulative (course) dose of Likferr 100®, which will need to be administered to compensate for iron deficiency in the body, using the following formula::

Total Drug Volume (ml) = Total iron deficiency (mg)/ 20 mg / ml.

Adults, including elderly (over 65 years of age) patients: 5-10 ml of Likferr 100® (100-200 mg of iron) 1-3 times a week.

Children: there are only limited data on the use of the drug in children. If necessary, it is recommended to administer no more than 0.15 ml of Likferr 100® (3 mg of iron) / kg 1-3 times a week, depending on the Hb indicator.

Maximum tolerated single dose for adults, including elderly (over 65 years of age) patients

For jet injection: 10 ml of Likferr 100® (200 mg of iron), the duration of use is at least 10 minutes.

For drip use: depending on the indications, a single dose can reach 500 mg of iron. The maximum allowable single dose is 7 mg of iron / kg and is administered once a week, but not more than 500 mg of iron.

Generally, higher doses are associated with a higher frequency of adverse events.

If the total therapeutic dose exceeds the maximum allowable single dose, fractional use of the drug is recommended.

If there is no improvement in hematological parameters 1-2 weeks after starting treatment with Likferr 100®, the initial diagnosis should be reviewed.

Calculation of the dose to replenish the iron content after blood loss or autologous blood donation

The dose of Likferr 100® required to compensate for iron deficiency is calculated using the formula below.

If the amount of blood lost is known: Intravenous use of 200 mg of iron (10 ml of Likferr 100®) leads to the same increase in Hb concentration as transfusion of 1 blood unit (400 ml with a Hb concentration of 150 g/l).

The amount of iron that needs to be replenished, mg = the number of units of blood lost × 200 or the required volume of Likferr 100®, ml = the number of units of blood lost × 10.

With a decrease in the Hb content: you should use the previous formula, provided that the iron depot does not need to be replenished.

The amount of iron that needs to be replenished, mg = body weight, kg × 0.24 × (normal indicator of Hb — Hb of the patient), g/l.

For example: body weight-60 kg, Hb deficiency = 10 g / l-the required amount of iron = 150 mg, the required volume of Likferr 100® = 7.5 ml.

Patients with chronic renal diseases undergoing hemodialysis and receiving additional treatment with erythropoietin

The drug is administered strictly intravenously. The injection itself should be carried out as slowly as possible, the duration of use increases as the dose increases. The procedure is not particularly difficult for hemodialysis patients, as they usually have a suitable IV access. The drug is administered in 0.9% sodium chloride solution for at least 15 minutes during the last 2 hours of the hemodialysis session.

Absolute iron deficiency (anemia correction phase)

• 30-50 mg of iron/dialysis session

or

• 1000 mg of iron for 6-10 weeks.

Maintenance therapy phase

Different doses are prescribed, in different modes:

• 10-25 mg of iron / dialysis session

or

• 100 mg of iron / 1 time per month (depending on the concentration of serum ferritin).

Hemoglobin correction phase

• 150 mg of iron to increase the concentration by 10 g/l.

Overdose

Symptoms: reduced blood pressure (signs of collapse appear within 30 minutes), symptoms of hemosiderosis.

Treatment: symptomatic, if necessary — drugs that bind iron (chelators), such as deferoxamine.

Special instructions

The rate of use of Likferr 100® should be strictly observed (with rapid use of the drug, blood pressure may decrease). A higher incidence of undesirable side effects (especially a decrease in blood pressure), including severe ones, is associated with an increase in the dose. Thus, the time of use of the drug, given in the section “Dosage and use”, should be strictly observed, even if the patient does not receive the drug in the maximum tolerated single dose.

During the use of Likferr 100®, hemodynamic parameters should be monitored.

Likferr 100® should be prescribed only to those patients whose diagnosis of anemia is confirmed by appropriate laboratory data (for example, the results of serum ferritin determination or indicators of hemoglobin and hematocrit, the number of red blood cells and their parameters — the average volume of red blood cells or the average hemoglobin content in red blood cells).

Intravenous iron supplements can cause allergic or anaphylactoid reactions that can be potentially life-threatening. Patients with bronchial asthma, eczema, atopic diseases, polyvalent allergies, allergic reactions to other iron preparations, as well as patients with low serum iron binding capacity and / or folic acid deficiency, have an increased risk of developing allergic or anaphylactoid reactions (see “Contraindications”)., With caution).

Studies conducted in patients with hypersensitivity reactions to iron dextran showed no complications during treatment with the drug.

Penetration of the drug into the parovenous space should be avoided, since ingestion of Likferr 100® outside the vessel leads to tissue necrosis and brown skin staining. If this complication develops, it is recommended (if the needle is still in the vessel) to introduce a small amount of 0.9% sodium chloride solution. To accelerate the removal of iron and prevent its further penetration into the surrounding tissues, it is recommended to apply heparin-containing preparations to the injection site (gel or ointment is applied with light movements, without rubbing).

It is unacceptable to introduce the drug in the presence of sediment.

1 ml of Likferr 100® contains 260 to 340 mg of sucrose. These data should be taken into account in patients with diabetes mellitus. With drip use of the drug, depending on the indications, the maximum tolerated single dose can reach 500 mg of iron, which corresponds to the introduction of 8.5 g of sucrose. When this amount of carbohydrates is converted to XE (1 XE = 12 g of carbohydrates), it corresponds to 0.7 XE.

During therapy with erythropoiesis stimulators, iron metabolism is monitored using indicators such as serum ferritin concentration and iron transferrin saturation (LVT). Determination of the number of hypochromic red blood cells and the concentration of hemoglobin in reticulocytes helps to decide whether to prescribe IV iron preparations when there is hyperferritinemia and low LV. The risk of iron overload is offset by blood loss during dialysis-related procedures (1-3 g of iron is lost per year). Serum ferritin concentrations should be monitored regularly. The concentration of serum ferritin above 500 mcg / l (with a normal C-reactive protein index), which persists for a long time, may indicate iatrogenic iron overload. In such cases, iron supplements should be discontinued (therapy with erythropoiesis stimulators should continue). Due to the fact that iron stimulates the growth of most microorganisms, iron supplements should be discontinued if acute bacterial infections develop. Intravenous iron therapy should also be used with caution in patients with permanent dialysis catheters.

Influence on the ability to drive vehicles or work with potentially dangerous mechanisms. It is recommended to use caution when driving a vehicle or working with potentially dangerous mechanisms.

Form of production

Solution for intravenous use

Storage conditions

At a temperature not exceeding 25 °C (do not freeze)

Shelf life

3 years

Active ingredient

Iron III hydroxide sucrose complex

Conditions of release from pharmacies

By prescription

Dosage form

solution for infusions

Purpose

Adults as prescribed by a doctor

Indications

From anemia