INJECTAFER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for INJECTAFER (INJECTAFER).

How it works

Ferric carboxymaltose is a complex of ferric hydroxide with carboxymaltose, a carbohydrate polymer. It releases iron, which is transported by transferrin to erythroid precursor cells for incorporation into hemoglobin, replenishing iron stores.

What the body does with it

Metabolism	Ferric carboxymaltose is dissociated into iron and carboxymaltose. Iron is incorporated into hemoglobin or stored as ferritin. Carboxymaltose is either excreted renally or metabolized via endogenous pathways.
Excretion	Primarily reticuloendothelial system clearance of iron; negligible renal excretion (<1% unchanged). Biliary/fecal excretion accounts for <1% of administered dose.
Half-life	Terminal elimination half-life is approximately 12-20 hours for the ferric carboxymaltose complex; iron is redistributed and incorporated into hemoglobin with a functional half-life of 5-7 days.
Protein binding	Ferric carboxymaltose complex does not bind extensively to plasma proteins; iron is tightly bound within the carbohydrate shell, minimizing free iron (<1% free).
Volume of Distribution	Vd approximately 3 L (central compartment); distribution primarily into blood and bone marrow; limited extravascular distribution due to high molecular weight.
Bioavailability	100% bioavailability following intravenous administration; not administered via other routes.
Onset of Action	Intravenous administration: Increase in hemoglobin and reticulocyte count observed within 1-2 weeks; clinical improvement in iron deficiency symptoms may occur earlier.
Duration of Action	Single infusion provides iron supply for up to 2-3 months in iron deficiency anemia; duration depends on ongoing iron losses and erythropoiesis rate.

Classification & Brands

Dosing & administration

1000 mg intravenously (or 20 mg/kg IV) as a single dose, maximum 1000 mg per dose, administered at a rate of 100 mg/min.

Dosage form	SOLUTION
Renal impairment	For GFR < 30 mL/min/1.73 m²: dose as per usual but monitor iron levels closely. No specific dose reduction recommended, but total cumulative dose should not exceed iron deficiency replacement limits.
Liver impairment	No specific dose adjustment for Child-Pugh A or B. For Child-Pugh C: avoid use due to lack of studies.
Pediatric use	Weight-based dosing: 20 mg/kg IV as a single dose, maximum 1000 mg per dose. For children weighing < 50 kg, administer at 1 mL (50 mg) per second.
Geriatric use	No specific adjustment required; use same dosing as for younger adults but monitor for hypersensitivity reactions and fluid overload.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for INJECTAFER (INJECTAFER).

Breastfeeding	Minimal excretion into breast milk. M/P ratio unknown. Iron ferric carboxymaltose is a large complex and unlikely to transfer significantly. Caution: monitor infant for GI irritation. American Academy of Pediatrics considers compatible with breastfeeding.
Teratogenic Risk	Pregnancy Category C. Animal studies (rats, rabbits) at doses up to 13 mg/kg/day (IV) showed no teratogenicity but did show maternal toxicity and reduced fetal weight. No adequate human studies. Risk of fetal harm cannot be ruled out; use only if clearly needed.

Warnings & precautions

■ FDA Black Box Warning

Risk of serious hypersensitivity reactions, including anaphylactic-type reactions, some of which have been life-threatening or fatal. Resuscitation equipment and trained personnel must be available immediately. Observe patients for signs and symptoms of hypersensitivity for at least 30 minutes after each injection.

Side Effect Profile

Serious Effects

Absolute Contraindications

["Hypersensitivity to ferric carboxymaltose or any of its components","Evidence of iron overload (e.g., hemochromatosis, hemosiderosis)","Anemia not caused by iron deficiency (e.g., hemolytic anemia, myelodysplasia)","Patients with known hypersensitivity to any parenteral iron product"]

Clinical Precautions

Precautions

["Hypersensitivity reactions including anaphylaxis","Hypotension","Iron overload and toxicity","Risk of infection due to bacterial proliferation","Use in patients with hepatic impairment","Use in pregnancy (Category C)"]

Clinical Tips & Counseling

Drug interactions

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INJECTAFER

Clinical safety rating: caution

Comprehensive clinical and safety monograph for INJECTAFER (INJECTAFER).

How it works

What the body does with it

Metabolism	Ferric carboxymaltose is dissociated into iron and carboxymaltose. Iron is incorporated into hemoglobin or stored as ferritin. Carboxymaltose is either excreted renally or metabolized via endogenous pathways.
Excretion	Primarily reticuloendothelial system clearance of iron; negligible renal excretion (<1% unchanged). Biliary/fecal excretion accounts for <1% of administered dose.
Half-life	Terminal elimination half-life is approximately 12-20 hours for the ferric carboxymaltose complex; iron is redistributed and incorporated into hemoglobin with a functional half-life of 5-7 days.
Protein binding	Ferric carboxymaltose complex does not bind extensively to plasma proteins; iron is tightly bound within the carbohydrate shell, minimizing free iron (<1% free).
Volume of Distribution	Vd approximately 3 L (central compartment); distribution primarily into blood and bone marrow; limited extravascular distribution due to high molecular weight.
Bioavailability	100% bioavailability following intravenous administration; not administered via other routes.
Onset of Action	Intravenous administration: Increase in hemoglobin and reticulocyte count observed within 1-2 weeks; clinical improvement in iron deficiency symptoms may occur earlier.
Duration of Action	Single infusion provides iron supply for up to 2-3 months in iron deficiency anemia; duration depends on ongoing iron losses and erythropoiesis rate.

Classification & Brands

Dosing & administration

1000 mg intravenously (or 20 mg/kg IV) as a single dose, maximum 1000 mg per dose, administered at a rate of 100 mg/min.

Dosage form	SOLUTION
Renal impairment	For GFR < 30 mL/min/1.73 m²: dose as per usual but monitor iron levels closely. No specific dose reduction recommended, but total cumulative dose should not exceed iron deficiency replacement limits.
Liver impairment	No specific dose adjustment for Child-Pugh A or B. For Child-Pugh C: avoid use due to lack of studies.
Pediatric use	Weight-based dosing: 20 mg/kg IV as a single dose, maximum 1000 mg per dose. For children weighing < 50 kg, administer at 1 mL (50 mg) per second.
Geriatric use	No specific adjustment required; use same dosing as for younger adults but monitor for hypersensitivity reactions and fluid overload.

Use during pregnancy

1st trimester	Consult provider
2nd trimester	Consult provider
3rd trimester	Consult provider

Clinical note

Comprehensive clinical and safety monograph for INJECTAFER (INJECTAFER).

Breastfeeding	Minimal excretion into breast milk. M/P ratio unknown. Iron ferric carboxymaltose is a large complex and unlikely to transfer significantly. Caution: monitor infant for GI irritation. American Academy of Pediatrics considers compatible with breastfeeding.
Teratogenic Risk	Pregnancy Category C. Animal studies (rats, rabbits) at doses up to 13 mg/kg/day (IV) showed no teratogenicity but did show maternal toxicity and reduced fetal weight. No adequate human studies. Risk of fetal harm cannot be ruled out; use only if clearly needed.