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PubChem
Name: Amifostine
PubChem Compound ID: 148139
Description: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
Molecular formula: C5H21N2O6PS
Molecular weight: 268.27 g/mol
Synonyms:
Ethanethiol, 2-((3-aminopropyl)amino)-, dihydrogen phosphate (ester), trihydrate; Amifostine (USP); NSC 296961; Amifostine [USAN:INN:BAN]; D00226; Ethyol (TN); Anifostine trihydrate; Amifostine; 112901-68-5; Ethyol
DrugBank
Identification
Name: Amifostine
Name (isomeric): DB01143
Drug Type: small molecule
Description: A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
Synonyms:
Aminopropylaminoethyl Thiophosphate; Amifostine Ethiofos; WR-1065; Gammaphos; Ethiofos; Apaetp; SAPEP
Brand: Ethyol
Category: Radiation-Protective Agents
CAS number: 20537-88-6
Pharmacology
Indication: For reduction in the cumulative renal toxicity in patients with ovarian cancer (using cisplatin) and moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer.
Pharmacology:
Amifostine is an organic thiophosphate cytoprotective agent indicated to reduce the cumulative renal toxicity associated with repeated administration of cisplatin in patients with advanced ovarian cancer or non-small cell lung cancer and also to reduce the incidence of moderate to severe xerostomia in patients undergoing post-operative radiation tr...
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Mechanism of Action:
The thiol metabolite is responsible for most of the cytoprotective and radioprotective properties of amifostine. It is readily taken up by cells where it binds to and detoxifies reactive metabolites of platinum and alkylating agents as well as scavenges free radicals. Other possible effects include inhibition of apoptosis, alteration of gene expres...
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Biotransformation: Amifostine is rapidly dephosphorylated by alkaline phosphatase in tissues primarily to the active free thiol metabolite and, subsequently, to a less active disulfide metabolite.
Route of elimination: After a 10-second bolus dose of 150 mg/m2 of ETHYOL, renal excretion of the parent drug and its two metabolites was low during the hour following drug administration, averaging 0.69%, 2.64% and 2.22% of the administered dose for the parent, thiol and disulfide, respectively.
Half Life: 8 minutes
Toxicity: Rat LD50: 826 mg/kg
Affected organisms: Humans and other mammals
Interactions
Drug interaction:
VerapamilVerapamil may enhance the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Verapamil should be withheld for 24 hours prior to Amifostine administration. Caution should be used at lower Amifostine doses used during radiotherapy, but routine interruption of Verapamil therapy is not recommended.
TrichlormethiazideTrichlormethiazide may increase the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Trichlomethiazide should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
TolazamideAdditive hypotensive effects may occur. At chemotherapeutic doses of Amifostine, Tolazamide should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
ValsartanAdditive hypotensive effects may occur. At chemotherapeutic doses of Amifostine, Valsartan should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
TelmisartanTelmisartan may increase the hypotensive effect of Amifostine. At chemotherapeutic doses of Amifostine, Telmisartan should be withheld for 24 hours prior to Amifostine administration. Use caution at lower doses of Amifostine.
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