Iron (III) hydroxide sucrose complex solution 20mg/ml 5ml ampoules, 5pcs

Composition

Each ampoule contains: Active ingredient: concentrate of iron [III] hydroxide sucrose complex in an amount equivalent to 100 mg of iron; excipients: sodium hydroxide-to regulate the pH value from 10.9 to 11.1, water for injection-up to 5 ml

Pharmacological action

Pharmacotherapeutic group:

Iron preparation

ATX:  

B. 03. A. C. 02 Iron Oxide Saccharate

Pharmacodynamics :

The multicore centers of iron (III) hydroxide are surrounded externally by many non-covalently bound sucrose molecules. 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.

This complex is stable and does not release iron ions under physiological conditions. The structure of the multicore iron-containing core is similar to that of the ferritin core, a physiological iron depot. This complex is designed to create a controlled source of recycled iron for transferrin and ferritin, which are responsible for the transport and deposition of iron in the body.

After intravenous use, iron from this complex is captured mainly by the liver, spleen and bone marrow, and then used for the synthesis of hemoglobin, myoglobin and other iron-containing enzymes, or stored in the liver in the form of ferritin.

Pharmacokinetics:

After a single intravenous use of Iron [III] hydroxide sucrose complex containing 100 mg of iron, the maximum iron concentration, on average 538 mmol, is reached 10 minutes after the injection. The volume of distribution of the central chamber almost completely corresponds to the volume of serum (about 3 liters).

The elimination half-life is about 6 h. The volume of distribution at steady state is approximately 8 L, which indicates a low distribution of iron in the body’s liquid media. Due to the low stability of iron saccharate in comparison with transferrin, there is a competitive exchange of iron in favor of transferrin and, as a result, about 31 mg of iron is transferred in 24 hours.

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

Indications

Iron [III] hydroxide sucrose complex is used to treat iron deficiency conditions in the following cases:

• if rapid iron supplementation is necessary;
• in patients who do not tolerate oral iron preparations or do not follow the treatment regimen;
• in the presence of active inflammatory bowel diseases, when oral iron preparations are ineffective.

Contraindications

The use of Iron [III] hydroxide sucrose complex is contraindicated if: :

• anemia is not associated with iron deficiency;
• there are signs of iron overload (hemosiderosis, hemochromatosis) or a violation of the process of its utilization;
• there is an increased sensitivity to the preparation of Iron [III] hydroxide sucrose complex or its components;
• I trimester of pregnancy.

With caution:

Patients with bronchial asthma, eczema, polyvalent allergies, allergic reactions to other parenteral iron preparations and persons with low serum iron-binding capacity and/or folic acid deficiency of Iron [III] sucrose hydroxide complex should be prescribed with caution.

Caution is also required when administering iron supplements to patients with hepatic insufficiency, acute or chronic infectious diseases, and individuals who have elevated serum ferritin levels due to the fact that parenterally administered iron may have an adverse effect in the presence of bacterial or viral infection.

Side effects

The most frequently reported adverse drug reactions when using Iron [III] hydroxide sucrose complex preparations were changes in taste sensations, decreased blood pressure, pyrexia and chills, injection site reactions, and nausea.

Very frequent (> 1/10), frequent (>>1/100 – >><1/10), infrequent (>1/1000-<1/10), infrequent (>< 1/100), rare (>1/10000 – < 1/100), rare (><1/100), very rare (

From the immune system

Rare: anaphylactoid reactions.

Nervous system

disorders Common: taste disorders. Infrequent: dizziness, headache. Rare: paresthesia, fainting, loss of consciousness, burning sensation. Frequency unknown: decreased levels of consciousness, confusion.

From the side of the heart

Infrequent: tachycardia, palpitations. Unknown: bradycardia.

From the side of blood vessels

Infrequent: decreased blood pressure. vascular collapse. Rare: increased blood pressure.

Respiratory, thoracic and mediastinal disorders

Infrequent: bronchospasm, shortness of breath.

From the gastrointestinal tract

Infrequent: nausea, vomiting, abdominal pain, diarrhea.

Skin and subcutaneous tissue disorders

Infrequent: pruritus, urticaria, rash, erythema

Musculoskeletal and connective tissue disorders

Infrequent: muscle spasms, muscle pain.

Rare: joint swelling, joint pain.

General disorders and reactions at the injection site

Infrequent: pyrexia, chills, hot flashes, abdominal pain, injection site reactions (for example, superficial phlebitis and edema). Rare: angioedema, peripheral edema, fatigue, asthenia, general malaise, feeling hot, edema. Very rare: hyperhidrosis, back pain. Unknown: chromaturia.

Interaction

of Iron [III] hydroxide sucrose complex should not be administered simultaneously with medicinal forms of iron for oral use, as it reduces the absorption of iron from the gastrointestinal tract. Treatment with oral iron supplements can be started no earlier than 5 days after the last injection. The preparation of Iron [III] hydroxide sucrose complex can be mixed in one syringe only with a sterile 0.9% sodium chloride solution. Incompatible with other intravenous solutions and therapeutic agents due to the risk of precipitation and / or other pharmaceutical interactions. Compatibility with containers made of other materials (polyethylene and polyvinyl chloride), with the exception of glass, has not been studied.

How to take, course of use and dosage

Introduction:  Iron [III] hydroxide sucrose complex is administered only intravenously-slowly by jet or drip, as well as in the venous section of the dialysis system and is not intended for intramuscular use. Simultaneous use of a full 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 should be examined for possible sediment and damage. You can only use a brown solution without sediment.

Drip introduction:  the preparation of Iron [III] hydroxide sucrose complex is preferable to be administered during a drip infusion in order to reduce the risk of a pronounced decrease in blood pressure (BP) and the risk of getting the solution into the parovenous space. Immediately before the infusion, the preparation of Iron [III] hydroxide sucrose complex should be diluted with 0.9% sodium chloride solution in a ratio of 1: 20 [for example, I 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 of iron – for 30 minutes; 300 mg of iron – for 1.5 hours; 400 mg of iron – for 2.5 hours; 500 mg of iron – for 3.5 hours. The maximum tolerated single dose of 7 mg of iron/kg of body weight 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 Iron [III] hydroxide sucrose complex, a test dose should be administered: 20 mg of iron for adults and children with a body weight of more than 14 kg and half the daily dose (1.5 mg of iron/kg) for children with a body weight of 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:  the preparation of Iron [III] hydroxide sucrose complex can also be administered as an undiluted solution intravenously slowly, at a rate (norm) 1 ml of Iron [III] hydroxide sucrose complex (20 mg of iron) per minute (5 ml of Iron [III] hydroxide sucrose complex (100 mg of iron) is administered at least 5 minutes). The maximum volume of the drug should not exceed 10 ml of Iron [III] hydroxide sucrose complex (200 mg of iron) per injection.

Before the first jet use of a therapeutic dose of Iron [III] hydroxide sucrose complex, a test dose should be prescribed: 1 ml of Iron [III] hydroxide sucrose complex (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 outstretched position for some time.

Introduction to the dialysis system:  Iron [III] hydroxide sucrose complex can be administered directly into the venous section of the dialysis system, strictly following the rules described for intravenous injection.

Dose calculation: The dose is calculated individually according to the total iron deficiency in the body using the formula:

Total iron deficiency (mg) = body weight (kg) x (normal patient Hb – Hb level) (g/l) x 0.24* + deposited iron (mg).

For patients with a body weight of less than 35 kg: normal Hb level= 130 g / l, the amount of deposited iron = 15 mg / kg of body weight.

For patients weighing more than 35 kg: normal level of Hb = 150 g/l, the amount of deposited iron = 500 mg.

*Factor 0.24 = 0,0034 x 0.07 x 1000 (the Content of iron in Hb = 0,34%; blood Volume = 7% of body weight; factor 1000 = the translation of the “g” in “mg”).

Total amount of Iron [III] hydroxide sucrose complex preparation to be administered (in ml) = Total iron deficiency (mg)/20 mg / ml.

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 Iron [III] hydroxide sucrose complex, the initial diagnosis should be reviewed.

Calculation of the dose to compensate for iron deficiency after blood loss or autologous blood donation:

The dose of the Iron [III] hydroxide sucrose complex preparation required to compensate for iron deficiency is calculated using the following formula:

If the amount of blood lost is known: intravenous use of 200 mg of iron (= 10 ml of Iron [III] hydroxide sucrose complex) leads to the same increase in Hb concentration as transfusion of I unit of blood (= 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 x 200 OR

Required volume of Iron [III] hydroxide sucrose complex preparation (ml) =

number of units of blood lost x 10

When Hb decreases: use the previous formula, provided that you don’t need to top up your iron depot.

The amount of iron to be replenished [mg] = body weight [kg] x 0.24 x (normal Hb level – patient’s Hb level) (g/L),

For example: body weight 60 kg, Hb deficiency = 10 g / l => required amount of iron in 150 mg = > > required volume of Iron [III] hydroxide sucrose complex preparation = 7.5 ml>>

Standard dosage:

Adults and elderly patients: 5-10 ml of Iron [III] hydroxide sucrose complex (100-200 mg of iron) 1-3 times a week, depending on the level of hemoglobin.

Children: There are only limited data on the use of the drug in children under 3 years of age. The recommended dose for children of other age groups is no more than 0.15 ml of Iron [III] hydroxide sucrose complex (3 mg of iron) per kg of body weight 1-3 times a week, depending on the level of hemoglobin.

Maximum tolerated single dose:

Adult and elderly patients:

For jet injection: 10 ml of the preparation Iron [III] hydroxide sucrose complex (200 mg of iron), the duration of use is not less than 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 per kg of body weight and is administered once a week, but it should not exceed 500 mg of iron. For the time of use of the drug and the method of dilution, see the section “Dosage and use methods”.

Overdose

Overdose can cause acute iron overload, which is manifested by symptoms of hemosiderosis. In case of overdose, it is recommended to use symptomatic agents and, if necessary, iron-binding substances (chelates), for example, intravenous deferoxamine.

Special instructions

Iron [III] hydroxide sucrose complex should be administered only to patients in whom the diagnosis of anemia is confirmed by appropriate laboratory data (e. g., results of the determination of serum ferritin or hemoglobin level and hematocrit, number of erythrocytes and their parameters – the average volume of the erythrocyte, the average content of hemoglobin in the erythrocyte or medium: the concentration of hemoglobin in the erythrocyte).

Intravenous iron supplements can cause allergic or anaphylactoid reactions that can be potentially life-threatening.

The rate of use of Iron [III] hydroxide sucrose complex 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), which can also be severe, is associated with an increase in the dose. Thus, the time of use of the drug, given in the section “Methods of use and doses”, should be strictly observed, even if the patient does not receive the drug in the maximum tolerated single dose.

Studies conducted in patients with hypersensitivity reactions to iron dextran showed no complications during treatment with iron [III] hydroxide sucrose complex preparations.

Penetration of the drug into the parovenous space should be avoided, since ingestion of the Iron [III] hydroxide sucrose complex preparation outside the vessel leads to tissue necrosis and brown skin staining. If this complication develops, it is recommended to apply heparin-containing preparations to the injection site (gel or ointment is applied with light movements, without rubbing) to accelerate the removal of iron and prevent its further penetration into the surrounding tissues.

Shelf life after the first opening of the container: From a microbiological point of view, the drug should be used immediately.

Influence on the ability to drive vehicles and mechanisms:

It is unlikely that the preparation of Iron [III] hydroxide sucrose complex can have an undesirable effect on the ability to drive a car and work with mechanisms. However, if symptoms such as dizziness, confusion, or semi-fainting develop, patients should not drive vehicles or mechanisms until these symptoms disappear.

Form of production

Solution for intravenous use of 20 mg / ml. 5 ml in ampoules of dark glass with a break ring or with a notch and a dot. 5 ampoules each in a plastic tray. 1 plastic pallet together with the instructions for use is placed in a pack of cardboard.

Storage conditions

In a protected place at a temperature not exceeding 25 °C. Keep out of reach of children.

Shelf

life is 3 years.

Active ingredient

Iron III hydroxide sucrose complex

Conditions of release from pharmacies

Prescription