Amifostine

Indications
 Intravenous
As a cytoprotective agent in chemotherapy
Adult: Initially, 910 mg/m2 BSA once daily, as an infusion given over 15 minutes, 30 minutes before start of chemotherapy. May reduce to 740 mg/m2 if patient is unable to tolerate the full dose. For patients receiving cisplatin doses <100 mg/m2, a dose of 740 mg/m2 may be given to reduce renal toxicity.
Intravenous
Prophylaxis of xerostomia in patients undergoing radiotherapy for head and neck cancer
Adult: 200 mg/m2 BSA once daily, as an infusion given over 3 minutes, beginning 15-30 minutes before radiotherapy.

Reconstitution: Each single-use vial contains 500 mg of anhydrous amifostine. Reconstitute with 9.7 mL of sterile 0.9% sodium chloride Inj and dilute with 0.9% sodium chloride to a final concentration of 5-40 mg/mL. Visual inspection for particulate matter and discoloration prior to admin is recommended. Do not use if cloudiness or precipitate is observed.
Incompatibility: Y-site incompatibility: Acyclovir, amphotericin B, chlorpromazine, cisplatin, ganciclovir, hydroxyzine HCl, prochlorperazine edisylate.
Contraindications
 Hypersensitivity, patients with low BP, dehydration, patients with renal or hepatic impairment, children and elderly >70 yr.
Warnings / Precautions
 Pregnancy and lactation. Patients should be well-hydrated and kept supine during infusion. Prolonged infusion causes greater side effects: Stop antihypertensive drugs 24 hr before infusion. Monitor BP regularly, at least before and immediately after infusion. Admin antiemetics before infusion especially when emetogenic drugs are used.
Adverse Reactions
 Hypotension during infusion. Systolic fall is greater. Transient and reversible loss of consciousness rarely. Nausea, vomiting, flushing, feeling of warmth, chills, dizziness, sneezing, cough and drowsiness, mild skin rashes.
Potentially Fatal: Severe skin reactions, including Stevens-Johnson syndrome.
Overdose Reactions
 May cause hypotension which can be managed by supportive care and normal saline infusion.
Drug Interactions
 Concurrent use with antihypertensives may cause severe hypotension.
See Below for More amifostine Drug Interactions
Mechanism of Actions
 Amifostine is a prodrug that is converted to a pharmacologically active metabolite (free thiol), which selectively protects non-cancer cells from the toxic effects of antineoplastics (eg, cisplatin) and radiation.
Distribution: Volume of distribution: 3.5L.
Metabolism: Dephosphorylated by alkaline phosphatase to an active metabolite, a free thiol compound.
Excretion: About 6% or less is excreted in the urine. Elimination half life after 15-minute IV infusion: <10 minutes.
Storage Conditions
 Intravenous: Vials containing lyophilized powder: Store at 20-25°C. Reconstituted solution (500 mg/10 mL): Chemically stable for up to 5 hr at room temperature (about 25°C) or up to 24 hr under refrigeration (2-8°C).
ATC Classification
 V03AF05 - amifostine ; Belongs to the class of detoxifying agents used in antineoplastic treatment.
Storage
 Intravenous: Vials containing lyophilized powder: Store at 20-25°C. Reconstituted solution (500 mg/10 mL): Chemically stable for up to 5 hr at room temperature (about 25°C) or up to 24 hr under refrigeration (2-8°C).
Available As
  • Amifostine 300 mg
  • Amifostine 500 mg

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