FERIDEX I.V.

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FERIDEX I.V. (FERIDEX I.V.).

How it works

FERIDEX I.V. (ferumoxytol) is an iron oxide nanoparticle coated with a carbohydrate shell. After intravenous administration, ferumoxytol is taken up by macrophages of the reticuloendothelial system, releasing iron into the intracellular iron pool. Iron is transported by transferrin to erythroid precursor cells for hemoglobin synthesis, thereby replenishing iron stores.

What the body does with it

Metabolism	Ferumoxytol is taken up by macrophages and degraded in lysosomes; iron is incorporated into ferritin/hemosiderin. The carbohydrate shell is metabolized to glucose and other metabolites.
Excretion	Primarily eliminated via hepatobiliary and fecal routes as intact complex; renal excretion is minimal (<1%) for iron, but ferric carboxymaltose complex is not dialyzable. In patients with iron deficiency, ~50-60% of administered iron is incorporated into hemoglobin and red blood cells within 2-4 weeks; the remainder is stored as ferritin and hemosiderin. The carboxymaltose moiety is partially metabolized and excreted via urine and feces.
Half-life	Terminal elimination half-life (t½) of ferric carboxymaltose is approximately 7-12 hours (mean ~9 hours) in iron-deficient patients. Clinical context: The iron is rapidly delivered to the reticuloendothelial system for processing; reticulocyte response is seen within 1-2 weeks. The half-life reflects clearance of the complex from plasma, not iron turnover.
Protein binding	Highly bound to serum proteins, primarily transferrin (iron is transported as iron-transferrin complex). The ferric carboxymaltose complex itself binds to plasma proteins, with minimal free iron; less than 1% of total iron is free.
Volume of Distribution	Volume of distribution at steady state (Vdss) of ferric carboxymaltose is approximately 3-4 L in adults, which corresponds to ~0.05-0.06 L/kg. Clinical meaning: Confined largely to plasma volume, reflecting limited tissue distribution of the intact complex; iron is then distributed to bone marrow and storage sites after cellular uptake.
Bioavailability	100% via intravenous route; the drug is not intended for intramuscular or subcutaneous use. No oral formulation available. Bioavailability is not applicable for IV administration.
Onset of Action	Intravenous administration: Iron is immediately available for erythropoiesis; reticulocyte count increases within 1-2 weeks. Hemoglobin rise is measurable within 1-2 weeks, with peak effect at 2-4 weeks post-dose.
Duration of Action	Single IV dose provides sustained iron delivery for erythropoiesis over 2-4 weeks. Hemoglobin normalization may be maintained for weeks to months depending on ongoing iron loss or demand. Clinical note: Repeated dosing may be needed in chronic blood loss or continuous erythropoiesis stimulation.

Classification & Brands

Dosing & administration

15 mg/kg intravenous infusion over 4 hours, maximum single dose 1200 mg, repeat after 72 hours if ferritin <100 ng/mL and transferrin saturation <20%.

Dosage form	INJECTABLE
Renal impairment	No adjustment for mild to moderate impairment (GFR ≥30 mL/min). For GFR <30 mL/min: reduce dose to 10 mg/kg, maximum 800 mg per infusion.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 10 mg/kg, maximum 800 mg. Child-Pugh C: contraindicated.
Pediatric use	Children ≥2 years: 12 mg/kg intravenous infusion over 4 hours, maximum 600 mg; repeat after 72 hours if iron deficiency persists.
Geriatric use	Same as adult dosing; monitor for hypotension and infusion reactions due to increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for FERIDEX I.V. (FERIDEX I.V.).

Breastfeeding

Ferumoxytol is not expected to transfer into breast milk due to its large molecular weight (iron oxide core with carboxymethyldextran coating). M/P ratio not established. Iron from the drug, if any, would be negligible and non-bioavailable orally. Use is compatible with breastfeeding. Caution advised in infants with iron overload disorders.

Teratogenic Risk

Ferumoxytol (Feridex I.V.) is an iron oxide nanoparticle. Animal studies indicate no teratogenic effects at doses up to 25 times the human dose. In humans, data are limited; however, iron deficiency treatment is generally considered safe in pregnancy. There is no evidence of increased risk of major malformations. Risk in the first trimester is low. Second and third trimester use is common for maternal anemia. Theoretical risk of oxidative stress exists but not clinically significant at therapeutic doses.

Warnings & precautions

■ FDA Black Box Warning

WARNING: SERIOUS HYPERSENSITIVITY REACTIONS (including fatal anaphylactic reactions) have occurred. Administer only when personnel and therapies are immediately available for the treatment of anaphylaxis. Observe patients for at least 30 minutes after each injection.

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of anaphylaxis or severe hypersensitivity to ferumoxytol or any of its components","Evidence of iron overload (e.g., hemochromatosis, hemosiderosis)","Non-anemic patients"]

Clinical Precautions

Precautions

["Serious hypersensitivity reactions including anaphylaxis","Hypotension","Iron overload in patients with iron overload syndromes","Risk of extravasation with injection site reactions","May cause false low serum iron and false high transferrin levels","Do not use in patients with evidence of iron overload"]

Clinical Tips & Counseling

Drug interactions

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FERIDEX I.V.

Clinical safety rating: caution

Comprehensive clinical and safety monograph for FERIDEX I.V. (FERIDEX I.V.).

How it works

What the body does with it

Metabolism	Ferumoxytol is taken up by macrophages and degraded in lysosomes; iron is incorporated into ferritin/hemosiderin. The carbohydrate shell is metabolized to glucose and other metabolites.
Excretion	Primarily eliminated via hepatobiliary and fecal routes as intact complex; renal excretion is minimal (<1%) for iron, but ferric carboxymaltose complex is not dialyzable. In patients with iron deficiency, ~50-60% of administered iron is incorporated into hemoglobin and red blood cells within 2-4 weeks; the remainder is stored as ferritin and hemosiderin. The carboxymaltose moiety is partially metabolized and excreted via urine and feces.
Half-life	Terminal elimination half-life (t½) of ferric carboxymaltose is approximately 7-12 hours (mean ~9 hours) in iron-deficient patients. Clinical context: The iron is rapidly delivered to the reticuloendothelial system for processing; reticulocyte response is seen within 1-2 weeks. The half-life reflects clearance of the complex from plasma, not iron turnover.
Protein binding	Highly bound to serum proteins, primarily transferrin (iron is transported as iron-transferrin complex). The ferric carboxymaltose complex itself binds to plasma proteins, with minimal free iron; less than 1% of total iron is free.
Volume of Distribution	Volume of distribution at steady state (Vdss) of ferric carboxymaltose is approximately 3-4 L in adults, which corresponds to ~0.05-0.06 L/kg. Clinical meaning: Confined largely to plasma volume, reflecting limited tissue distribution of the intact complex; iron is then distributed to bone marrow and storage sites after cellular uptake.
Bioavailability	100% via intravenous route; the drug is not intended for intramuscular or subcutaneous use. No oral formulation available. Bioavailability is not applicable for IV administration.
Onset of Action	Intravenous administration: Iron is immediately available for erythropoiesis; reticulocyte count increases within 1-2 weeks. Hemoglobin rise is measurable within 1-2 weeks, with peak effect at 2-4 weeks post-dose.
Duration of Action	Single IV dose provides sustained iron delivery for erythropoiesis over 2-4 weeks. Hemoglobin normalization may be maintained for weeks to months depending on ongoing iron loss or demand. Clinical note: Repeated dosing may be needed in chronic blood loss or continuous erythropoiesis stimulation.

Classification & Brands

Dosing & administration

15 mg/kg intravenous infusion over 4 hours, maximum single dose 1200 mg, repeat after 72 hours if ferritin <100 ng/mL and transferrin saturation <20%.

Dosage form	INJECTABLE
Renal impairment	No adjustment for mild to moderate impairment (GFR ≥30 mL/min). For GFR <30 mL/min: reduce dose to 10 mg/kg, maximum 800 mg per infusion.
Liver impairment	Child-Pugh A: no adjustment. Child-Pugh B: reduce dose to 10 mg/kg, maximum 800 mg. Child-Pugh C: contraindicated.
Pediatric use	Children ≥2 years: 12 mg/kg intravenous infusion over 4 hours, maximum 600 mg; repeat after 72 hours if iron deficiency persists.
Geriatric use	Same as adult dosing; monitor for hypotension and infusion reactions due to increased sensitivity.

Use during pregnancy

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

Clinical note

Comprehensive clinical and safety monograph for FERIDEX I.V. (FERIDEX I.V.).

Breastfeeding

Teratogenic Risk

Warnings & precautions

■ FDA Black Box Warning

Side Effect Profile

Serious Effects

Absolute Contraindications

["History of anaphylaxis or severe hypersensitivity to ferumoxytol or any of its components","Evidence of iron overload (e.g., hemochromatosis, hemosiderosis)","Non-anemic patients"]