Ethyol
Ethyol - General Information
A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia. [PubChem]
Pharmacology of Ethyol
Ethyol 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 treatment for head and neck cancer. Ethyol is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to a pharmacologically active free thiol metabolite, believed to be responsible for the reduction of the cumulative renal toxicity of cisplatin and for the reduction of the toxic effects of radiation on normal oral tissues. Healthy cells are preferentially protected because amifostine and metabolites are present in healthy cells at 100-fold greater concentrations than in tumour cells.
Ethyol for patients
Ethyol Interactions
Special consideration should be given to the administration of ETHYOL in patients receiving antihypertensive medications or other drugs that could cause or potentiate hypotension.
Ethyol Contraindications
ETHYOL is contraindicated in patients with known sensitivity to aminothiol compounds.
Additional information about Ethyol
Ethyol 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.
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 expression and modification of enzyme activity.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Amifostine
Synonyms: Aminopropylaminoethyl Thiophosphate; WR-1065; Apaetp; SAPEP; Amifostine Ethiofos; Ethiofos; Gammaphos
Drug Category: Radiation-Protective Agents
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Amifostine: Ethyol;
Absorption: Not Available
Toxicity (Overdose): Rat LD50: 826 mg/kg
Protein Binding: Not Available
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.
Half Life: 8 minutes
Dosage Forms of Ethyol: Powder, for solution Intravenous
Chemical IUPAC Name: 2-(3-aminopropylamino)ethylsulfanylphosphonic acid
Chemical Formula: C5H15N2O3PS
Amifostine on Wikipedia: https://en.wikipedia.org/wiki/Amifostine
Organisms Affected: Humans and other mammals
