Amifostine
Amifostine Uses, Dosage, Side Effects, Food Interaction and all others data.
A phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.
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 treatment for head and neck cancer. Amifostine 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.
| Trade Name | Amifostine |
| Availability | Prescription only |
| Generic | Amifostine |
| Amifostine Other Names | Amifostina, Amifostine, Amifostinum, Aminopropylaminoethyl thiophosphate |
| Related Drugs | pilocarpine, glycerin topical, Salagen, trilaciclib, Biotene Mouthwash, XyliMelts, Cosela, Ethyol |
| Weight | 500mg, |
| Type | Intravenous Powder For Injection, Intravenous |
| Formula | C5H15N2O3PS |
| Weight | Average: 214.223 Monoisotopic: 214.054099558 |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Amifostine is a cytoprotective adjuvant used for reduction in the cumulative renal toxicity in patients with ovarian cancer and moderate to severe xerostomia in patients undergoing post-operative radiation treatment for head and neck cancer.
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.
Amifostine is also used to associated treatment for these conditions: Dry Mouth, Nephrotoxicity, Prophylaxis of Radiation proctitis
How Amifostine works
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.
Toxicity
Rat LD50: 826 mg/kg
Food Interaction
No interactions found.Amifostine Drug Interaction
Unknown: dexbrompheniramine / pseudoephedrine, dexbrompheniramine / pseudoephedrine, acetaminophen, acetaminophen, acetaminophen, acetaminophen, aspirin, aspirin, alprazolam, alprazolam, pseudoephedrine / triprolidine, pseudoephedrine / triprolidine, carboplatin, carboplatin, ciprofloxacin ophthalmic, ciprofloxacin ophthalmic, clotrimazole, clotrimazole, coal tar topical, coal tar topical
Amifostine Disease Interaction
Half Life
8 minutes
Elimination Route
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.
Innovators Monograph
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