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

Pharmacotherapeutic group:

Pharmacotherapy group:

ATC:

B.03.A.C.02 Iron oxide saccharate

Pharmacodynamics:

The multinuclear centers of iron (III) hydroxide are surrounded by many noncovalently bound sucrose molecules on the outside. This results in a complex with a molecular weight of approximately 43 kDa, making it impossible to excrete it unchanged through the kidneys.

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

After intravenous administration, iron from this complex is taken up primarily 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 administration of Iron [III] hydroxide sucrose complex containing 100 mg of iron, maximum iron concentration, averaging 538 μmol, is reached 10 minutes after injection. The distribution volume of the central chamber corresponds almost completely to the volume of serum (about 3 liters).

The elimination half-life is about 6 h. The volume of distribution in equilibrium is approximately 8 L, indicating low iron distribution in body fluids, due to the low stability of iron sugars compared to transferrin, there is a competitive exchange of iron in favor of transferrin and as a result, about 31 mg of iron is transported in 24 h.

The renal excretion of iron for the first 4 h after injection is less than 5% of total clearance. After 24 h, serum iron levels return to the original (pre-injection) value and approximately 75% of sucrose leaves the vascular stream.

Indications

Iron [III] hydroxide sucrose complex is used for the treatment of iron deficiency in the following cases:

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

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How to take, the dosage

Injection: Iron [III] hydroxide sucrose complex is administered only intravenously – slowly by trickle or drip and into the venous section of the dialysis system and is not intended for intramuscular administration. A full therapeutic dose of the drug should not be administered at one time.

Before administering the first therapeutic dose, a test dose should be administered. If intolerance occurs during the observation period, the drug administration should be stopped immediately. Before opening the ampoule should be inspected for possible precipitate and damage. Only the brown solution without residue may be used.

Drip administration: Iron [III] hydroxide sucrose complex is preferably administered by drip infusion in order to reduce the risk of marked decreases in arterial pressure (BP) and the risk of the solution entering the pericolumnar space. Immediately prior to infusion, the preparation Iron [III] hydroxide sucrose complex should be diluted with 0.9% sodium chloride solution at a ratio of 1:20 [e.g., I ml (20 mg of iron) in 20 ml of 0.9% sodium chloride solution]. The resulting solution is administered at the following rate: 100 mg of iron in at least 15 min; 200 mg of iron in 30 min; 300 mg of iron in 1.5 h; 400 mg of iron in 2.5 h; 500 mg of iron in 3.5 h. The maximum tolerated single dose of 7 mg of iron/kg body weight should be administered for at least 3.5 hours, regardless of the total dose of the drug.

Before the first drip administration of a therapeutic dose of Iron [III] hydroxide sucrose complex, a test dose: 20 mg of iron in adults and children with a body weight greater than 14 kg and half the daily dose (1.5 mg of iron/kg) in children with a body weight less than 14 kg should be given for 15 min. If there are no adverse events, the remainder of the solution should be administered at the recommended rate.

Stroke administration: Iron [III] hydroxide sucrose complex can also be administered as an undiluted solution intravenously slowly, at a rate of (normal) 1 ml of Iron [III] hydroxide sucrose complex (20 mg of iron) in one minute (5 ml of Iron [III] hydroxide sucrose complex (100 mg of iron) administered in at least 5 min). The maximum volume of the drug should not exceed 10 ml of the preparation of Iron [III] hydroxide sucrose complex (200 mg of iron) in one injection.

Before the first jet injection of the therapeutic dose of Iron [III] hydroxide sucrose complex, a test dose should be administered: 1 ml of Iron [III] hydroxide sucrose complex (20 mg of iron) to adults and children with a body weight greater than 14 kg, and half the daily dose (1.5 mg of iron/kg) to children with a body weight less than 14 kg for 1-2 min. If there are no adverse events during the next 15 min of observation, the remainder of the solution should be administered at the recommended rate. After injection, the patient is advised to fix the arm in an extended position for some time.

Injection into the dialysis system: Iron [III] hydroxide sucrose complex can be injected directly into the venous area 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 (patient’s normal Hb – Hb level) (g/l) x 0.24* + deposited iron (mg).

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

For patients with a body weight of more than 35 kg: normal Hb = 150 g/l, amount of iron deposited = 500 mg.

*Factor 0.24 = 0.0034 x 0.07 x 1000 (Hb iron content = 0.34%; blood volume = 7% of body weight; factor 1000 = conversion of “g” to “mg”).

The total volume of Iron [III] hydroxide sucrose complex to be administered (in ml) = Total iron deficiency (mg)/20 mg/mL.

1040

68

1500

63

97

1360

2120

<

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

If 1-2 weeks after initiation of treatment with Iron [III] hydroxide sucrose complex there is no improvement in hematologic parameters, the initial diagnosis should be reconsidered.

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

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

If the amount of blood lost is known: an intravenous injection of 200 mg of iron (= 10 ml of Iron [III] hydroxide sucrose complex preparation) results in the same increase in Hb concentration as a transfusion of I unit of blood (= 400 ml with an Hb concentration of 150 g/L).

The amount of iron to be replenished (mg) = number of units of blood lost x 200 OR

Amount of Iron [III] hydroxide sucrose complex required (ml) =

the number of units of blood lost x 10

If Hb: Use the previous formula, provided that the iron depot does not need to be replenished.

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

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

The 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 hemoglobin levels.

Children: There are only limited data on the use of the drug in children under 3 years of age. The recommended dose for children in other age groups is not more than 0.15 ml of the preparation Iron [III] hydroxide sucrose complex (3 mg of iron) per kg of body weight 1-3 times a week depending on hemoglobin level.

Maximum tolerated single dose:

Adults and elderly patients:

For jet injection: 10 ml of Iron [III] hydroxide sucrose complex (200 mg of iron), duration of administration at least 10 minutes.

For drip administration: depending on the indication, the single dose can be up to 500 mg of iron. The maximum permitted 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. See Methods of Administration and Dosages for administration times and dilution methods.

Interaction

Iron [III] hydroxide sucrose complex should not be administered simultaneously with oral iron dosage forms, because it reduces iron absorption from the gastrointestinal tract. Treatment with oral iron preparations can be started not earlier than 5 days after the last injection.

The preparation of Iron [III] hydroxide sucrose complex can be mixed in one syringe only with 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 polyvinylchloride), except glass, has not been studied.

Special Instructions

Iron [III] hydroxide sucrose complex should only be administered to patients in whom the diagnosis of anemia is confirmed by appropriate laboratory data (e.g. serum ferritin or hemoglobin and hematocrit levels, erythrocyte count and its parameters – mean erythrocyte volume, mean hemoglobin in the erythrocyte or mean: hemoglobin concentration in the erythrocyte).

Intravenous iron preparations can cause allergic or anaphylactoid reactions, which can be potentially life-threatening.

The speed of administration of Iron [III] hydroxide sucrose complex should be strictly observed (blood pressure may decrease if the drug is administered rapidly). A higher incidence of undesirable side effects (especially – decreased BP), which can also be severe, is associated with an increase in the dose. Therefore, the dosing times listed in the Methods of Use and Dosages section should be strictly adhered to, even if the patient is not receiving the drug in the maximum tolerated single dose.

Studies in patients with hypersensitivity reactions to iron dextran have shown no complications with treatment with preparations of iron [III] hydroxide sucrose complex.

Infiltration of the drug into the peroventricular space should be avoided, since ingress of iron [III] hydroxide sucrose complex beyond the vessel leads to tissue necrosis and brown staining of the skin. If this complication develops, 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 (the gel or ointment is applied with light movements, without rubbing).

The shelf life after the first opening of the container: Microbiologically, the drug should be used immediately.

Impact on ability to drive:

It is unlikely that Iron [III] hydroxide sucrose complex drug may have adverse effects on the ability to drive and operate machinery. However, if symptoms such as dizziness, confusion, or fainting state develop, patients should not drive vehicles or operate machinery until these symptoms disappear.

Contraindications

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

• anemia is not due to iron deficiency;
• there are signs of iron overload (hemosiderosis, hemochromatosis) or impaired iron utilization;
• there is hypersensitivity to the preparation 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 those with low serum iron-binding capacity and/or folic acid deficiency Iron [III] hydroxide sucrose complex should be prescribed with caution.

Particular caution is also required when administering iron preparations to patients with hepatic insufficiency, those with acute or chronic infectious disease, and those with elevated serum ferritin values due to the possibility that parenterally administered iron may have adverse effects in the presence of bacterial or viral infection.

Side effects

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

Very frequent (>1/10), frequent (>1/100 to < 1/10), infrequent (>1/1000-< 1/100), rare (>1/10000 to < 1/100), very rare (< 1/10000), frequency unknown (it is not possible to estimate their frequency from the available data).

Immune system disorders

Rare: anaphylactoid reactions.

Nervous system disorders

Frequent: taste disturbances. Infrequent: dizziness, headache. Rare: paresthesia, fainting, loss of consciousness, burning sensation. Frequent unknown: decreased levels of consciousness, confusion.

Cardiac disorders

Infrequent: tachycardia, palpitations. Unknown: bradycardia.

Vascular disorders

Infrequent: decreased BP. vascular collapse. Rare: increased BP.

Respiratory, thoracic cavity and mediastinum disorders

Infrequent: bronchospasm, dyspnea.

Gastrointestinal tract disorders

Infrequent: nausea, vomiting, abdominal pain, diarrhea.

Skin and subcutaneous tissue disorders

Infrequent: itching, urticaria, rash, erythema

Musculoskeletal and connective tissue disorders

Infrequent: muscle cramps, muscle pain.

Rare: joint swelling, pain in the joints.

General disorders and injection site reactions

Infrequent: pyrexia, chills, hot flashes, pain in the pelvis, injection site reactions (e.g., superficial phlebitis and edema). Rare: angioedema, peripheral edema, fatigue, asthenia, general malaise, fever, edema. Very rare: hyperhidrosis, back pain. Unknown: chromaturia.

Overdose

Overdose can cause acute iron overload, which manifests as symptoms of hemosiderosis.