Amifostine
- Atc Codes:V03AF05
- CAS Codes:112901-68-5#20537-88-6
- PHARMGKB ID:112901-68-5#20537-88-6
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Ethyol; Belgium: Ethyol; Cyprus: Ethyol; Czech Republic: Ethyol; Finland: Ethyol; France: Ethyol; Germany: Ethyol; Greece: Ethyol; Italy: Ethyol; Luxembourg: Ethyol; Netherlands: Ethyol; Poland: Ethyol; Portugal: Ethyol; Romania: Ethyol; Slovakia: Ethyol; Spain: Ethyol; Sweden: Ethyol.
North America
USA: Amifostine, Ethyol.
Latin America
Brazil: Ethyol; Mexico: Ethyol.
Drug combinations
Chemistry
Amifostine: C~5~H~15~N~2~O~3~PS 3H~2~O. Mw: 268.27. (1) Ethanethiol, 2-[(3-aminopropyl)amino]-, dihydrogen phosphate (ester), trihydrate; (2) S-[2-[(3-Aminopropyl)amino]ethyl] dihydrogen phosphorothioate, trihydrate. CAS-112901-68-5; CAS-20537-88-6 (anhydrous)(1991).
Pharmacologic Category
Protective Agents; Chemoprotective Agents (Cytoprotective). Antidote. (ATC-Code: V03AF05).
Mechanism of action
Prodrug dephosphorylated to a pharmacologically-active free thiol metabolite which binds to, and detoxifies, reactive metabolites of cisplatin. Scavenger of free radicals in tissues.
Therapeutic use
Reduction of xerostomia from head and neck cancer. Reduction of cisplatin-induced renal toxicity.
Pregnancy and lactiation implications
Animal studies have demonstrated embryotoxicity. There are no adequate and well-controlled studies in pregnant women. Use not recommended during lactation.
Unlabeled use
Contraindications
Hypersensitivity to amifostine, aminothiol compounds, or any component of the formulation.
Warnings and precautions
Hypersensitivity reactions (anaphylaxis and severe cutaneous reactions) reported. Hypocalcemia (rarely). Use with caution in cardiovascular disease or where the adverse effects of hypotension may have serious adverse events, cerebrovascular disease, or in patients where the adverse effects of nausea/vomiting may have serious adverse events. Administration of antiemetic medication is recommended prior to and in conjunction with amifostine. Antihypertensive therapy should be interrupted for 24 hours before amifostine. Adequate hydration prior to amifostine infusion and supine position during infusion.