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VARIOUS › ALL OTHER THERAPEUTIC PRODUCTS › ALL OTHER THERAPEUTIC PRODUCTS › Detoxifying agents for antineoplastic treatment
amifostine
V03AF05
Forms & Strengths
- Lyophilized powder for injection: 500 mg per vial
Adult Dosing
- Reduction of cumulative renal toxicity from cisplatin: 910 mg/m² administered as a 15-minute IV infusion starting 30 minutes prior to chemotherapy
- Reduction of moderate-to-severe xerostomia from postoperative radiation therapy for head and neck cancer: 200 mg/m² once daily as a 3-minute IV infusion, starting 15 to 30 minutes prior to standard fraction radiation therapy
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Reduction of cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer
- Reduction of moderate-to-severe xerostomia in patients undergoing postoperative radiation therapy for head and neck cancer
Mechanism of Action
- Prodrug that is dephosphorylated by alkaline phosphatase to an active free thiol metabolite (WR-1065)
- Scavenges reactive oxygen species generated by cytotoxic chemotherapy and radiation in normal tissues
- Selectively protects normal tissues over tumor tissues due to higher capillary alkaline phosphatase activity, higher pH, and better vascularity in normal cells
Contraindications
- Known hypersensitivity to aminothiol compounds or mannitol
- Hypotension or patients in a dehydrated state
- Acute or chronic conditions where hypotension can pose a severe health risk (e.g., ischemic heart disease, cerebrovascular disease)
Adverse Reactions
- Transient hypotension (frequent, requiring blood pressure monitoring)
- Nausea and vomiting (often severe, requiring antiemetic prophylaxis)
- Flushing and warm sensation
- Dizziness, somnolence, and hiccups
- Hypocalcemia (due to rapid decrease in serum calcium levels)
Drug Interactions
- Antihypertensive agents: Amifostine may potentiate hypotension; consider interrupting antihypertensive therapy 24 hours prior to amifostine administration
- Cisplatin: No pharmacokinetic interference observed when administered as indicated
- Cytotoxic agents: Careful timing required to ensure chemoprotection without compromising antitumor efficacy
Curated Content: Needs Vetting Before Put to Clinical Use