Ferrofer

Iron sucrose.

Each mL contains 20 mg elemental iron (100 mg/5 mL) as iron sucrose in water or injection. It is available in 5 mL ampule. Iron sucrose injection is a dark brown colloidal solution for IV use. It has a molecular weight of approximately 34,000-60,000 Daltons and a proposed structural formula: Na₂Fe₅O₈·3(H₂O)n·m(C₁₂H₂₂O₁₁). Where: n is the degree of iron polymerization and m is the number of sucrose molecules associated with the iron (III)-hydroxide.

The polynuclear iron (III)-hydroxide cores are superficially surrounded by a large number of non-covalently bound sucrose molecules resulting in a complex whose molecular mass is approximately molecular weight 43 kD. This is sufficiently large to prohibit renal elimination. The resulting complex is stable and does not release ionic iron under physiological conditions. The iron in the polynuclear cores is bound in a similar structure as in the case of physiologically occurring ferritin.
Administration of iron sucrose causes physiological changes which involve the uptake of iron. Iron sucrose possesses a low toxicity with LD₅₀ of >200 mg Fe/kg body weight when administered to mice. It has a therapeutic index of about 30 (200/7).
Pharmacokinetics: The pharmacokinetics of iron (III)-hydroxide sucrose complex was investigated after IV injection of a single dose containing 100 mg Fe (III) in healthy volunteers. The maximum iron levels, averaging 538 micromol/L, are obtained 10 min after injection. The volume of distribution of the central compartment corresponds in good agreement to the volume of serum (approximately 3 L).
The iron injected is quickly cleared from the serum, the terminal t_½ is approximately 6 hrs. The volume of distribution at steady-state is about 8 L, which indicates a low iron distribution in the body water. Due to the lower stability of iron (III)-hydroxide sucrose complex in comparison to transferrin, a competitive exchange of iron to transferrin was observed. This results in an iron transport of approximately 31 mg Fe (III)/ 24 hrs.
Renal elimination of iron, occurring in the first 4 hrs after injection, corresponds to <5% of the total body clearance (approximately 20 mL/min). After 24 hrs, the serum levels of iron are reduced to the predose iron levels and about 75% of the dosage of sucrose is excreted.

Treatment of iron deficiency anemia in patients undergoing chronic hemodialysis who are receiving supplemental erythropoietin therapy.

Dosage: Calculation of Dosage: The dosage has to be individually adapted according to the total iron deficit calculated with the following formula:
Total iron deficit (mg) = body weight (kg) x target Hb - actual Hb (g/L) x 0.24* + depot iron (mg).
≤35 kg body weight target Hb = 130 g/L resp depot iron = 15 mg/kg body weight.
>35 kg body weight target Hb = 150 g/L resp depot iron = 500 mg.
* Factor 0.24 = 0.0034 x 0.07 x 1000.
Iron content of hemoglobin 0.34% blood volume = 7% of body weight/Factor 1000 = conversion from g to mg.
Total amount of iron sucrose injection to be administered (in mL) = Total iron deficit (mg) / 200 mg/mL. (See table.)

Click on icon to see table/diagram/image

If the total necessary dose exceeds the maximum allowed single dose, then the administration has to be split. If no response of the hematological parameters is observed after 1-2 weeks, the original diagnosis should be reconsidered.
Calculation of dosage for iron replacement secondary to blood loss and to support autologous blood donation: The required iron sucrose injection dose to compensate the iron deficit is calculated according to the following formulas:
If the quantity of blood lost is known: The administration of 200 mg IV iron (=10 mL iron sucrose injection) results in an increase in hemoglobin which is equivalent to 1 unit blood (=400 mL with 150 g/L Hb content). Iron to be replaced (mg) = number of blood units lost x 200 or amount of iron sucrose injection needed (mL) = number of blood units lost x 10.
If the Hb level is reduced: Use the previous formula considering that the depot iron does not need to be restored. Iron to be replaced (mg) = body weight x 0.24 x (target Hb - actual Hb) (g/L). Eg, body weight 60 kg, Hb deficit = 10 g/L = >Iron to be replaced 150 mg = >7.5 mL iron sucrose injection needed.
Adults and Elderly: 5-10 mL iron sucrose injection (100-200 mg iron) or 2-3 times a week depending on the hemoglobin level. Frequency of dosing should be no more than 3 times weekly.
Children: 0.15 mL iron sucrose injection/kg body weight (=3 mg iron/kg body weight) 2 or 3 times a week depending on the hemoglobin level.
Maximum Tolerated Single Dose: Adults and Elderly: As Injection: 10 mL iron sucrose injection (200 mg iron) injected in at least 10 min. As Infusion: If the clinical situation demands, the single dose may be increased to 0.35 mL iron sucrose injection/kg body weight (=7 mg iron/kg body weight) not exceeding 25 mL iron sucrose injection (500 mg iron), diluted in 500 mL 0.9% NaCl infused over at least 3.5 hrs once a week.
Administration: Iron sucrose is used as a source of iron for iron deficiency anemia. Iron sucrose is to be administered IV by slow injection or by infusion or when used in hemodialysis patients, into the venous limb of the dialyser.
Infusion: Iron sucrose injection may preferably be administered by infusion. Iron sucrose may be given undiluted at the rate of 20 mg/min, after a test dose of 20 mg of iron has been given over 1-2 min. Alternatively, 100 mg is diluted in a maximum of 100 mL of 0.9% NaCl and the first 25 mg given as a test dose over 15 min; the remaining portion is given at a rate not exceeding 50 mL/15 min.
Slow IV Injection: Iron sucrose injection may be administered by slow IV injection at a rate of 1 mL undiluted per min (ie, 5 min/5 mL amp) not exceeding 5 mL iron sucrose injection (100 mg iron) per injection. After an injection, extend the arm of the patient.
Injection into Dialyser: Iron sucrose injection may be administered directly into the venous limb of the dialyser under the same conditions as for IV injection.

Dosages of iron sucrose in excess of iron needs may lead to accumulation of iron in storage sites leading to hemosiderosis. Overdosage should be treated with efficient procedure. Iron-binding preparations should be used when necessary.

Anemia not caused by iron deficiency; iron overload or disturbances in utilization of iron; known hypersensitivity to iron mono- or disaccharide complexes.

Iron sucrose should be used with caution in patients with a history of asthma, eczema, anaphylaxis or other allergic disorder.
Use in pregnancy & lactation: Animal teratology studies have shown that iron sucrose has no teratogenic effect and does not cause abortion in non-anemic animals. But use of parenteral iron preparations during the first 3 months has to be discouraged. During the 2nd and 3rd term, the application has to be done with caution. None of its metabolites can be excreted into the breast milk.

Animal teratology studies have shown that iron sucrose has no teratogenic effect and does not cause abortion in non-anemic animals. But use of parenteral iron preparations during the first 3 months has to be discouraged. During the 2nd and 3rd term, the application has to be done with caution. None of its metabolites can be excreted into the breast milk.

Very rarely, allergic anaphylactic-like reactions may occur.
Occasionally, the following undesirable effects have been reported with a frequency of not less than 1%: Metallic taste, headache, nausea, vomiting, diarrhea, hypotension, elevated liver enzymes, cramps/leg cramps, chest pain, dizziness, dyspnea, pneumonia, cough, pruritus.
Less frequently, paresthesia, abdominal disorders, muscular pain, fever, urticaria, flushing, edema of the extremities, dyspnea and anaphylactoid (pseudoallergic) reactions have been reported. In the region of the punctured vein, phlebitis and venous spasm have been observed.

As with all parenteral administered iron preparations, iron sucrose should not be administered concomitantly with oral iron preparations since the absorption of oral iron can be reduced. Therefore, an oral therapy should at least be started 5 days after the last injection.

Store at temperatures not exceeding 30°C.
Shelf-Life: 36 months.

Vitamins & Minerals (Pre & Post Natal) / Antianemics

B03AC - Iron, parenteral preparations ; Used in the treatment of anemia

Non-Rx