Comparative Pharmacology
Head-to-head clinical analysis: AMIFOSTINE versus ETHYOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: AMIFOSTINE versus ETHYOL.
AMIFOSTINE vs ETHYOL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Amifostine is a prodrug that is dephosphorylated by alkaline phosphatase to an active free thiol metabolite, which scavenges free radicals generated by chemotherapy and radiation therapy, thereby protecting normal tissues from cytotoxic damage.
Ethyl (amifostine) is a prodrug that is dephosphorylated by alkaline phosphatase to an active thiol metabolite, which scavenges free radicals and detoxifies reactive metabolites of cisplatin and radiation, thereby protecting normal tissues.
910 mg/m² IV over 15 minutes, once daily, 30 minutes prior to chemotherapy or radiotherapy.
For reduction of cisplatin-induced nephrotoxicity: 910 mg/m2 IV infused over 15 minutes, starting 30 minutes prior to cisplatin. For reduction of xerostomia from head and neck radiation: 200 mg/m2 IV bolus daily 15-30 minutes before radiation.
None Documented
None Documented
Clinical Note
moderateAmifostine + Etacrynic acid
"The risk or severity of adverse effects can be increased when Amifostine is combined with Etacrynic acid."
Clinical Note
moderateAmifostine + Furosemide
"The risk or severity of adverse effects can be increased when Amifostine is combined with Furosemide."
Clinical Note
moderateAmifostine + Bumetanide
"The risk or severity of adverse effects can be increased when Amifostine is combined with Bumetanide."
Clinical Note
moderateAmifostine + Methyclothiazide
Terminal elimination half-life approximately 8-9 minutes for the parent compound; active metabolite (WR-1065) has a half-life of about 1-2 hours. Clinical context: short half-life allows administration just before chemotherapy or radiation.
A single i.v. dose of amifostine (ETHYOL) exhibits a terminal elimination half-life of approximately 0.6-1.1 hours, representing rapid clearance of the free thiol form (WR-1065) from plasma. Clinical context: The active metabolite WR-1065 has a slightly longer half-life (about 1-2 hours). The short half-life suggests protective effects are limited to the time immediately after infusion.
Primarily renal; unchanged drug and metabolites (70-90% of administered dose recovered in urine within 24 hours). Biliary/fecal excretion negligible (<5%).
Renal: ~50-60% of the administered dose (including active metabolite WR-1065) excreted in urine within 24 hours, with minimal biliary/fecal elimination (<5%).
Category C
Category C
Cytoprotective Agent
Cytoprotective Agent
"The risk or severity of adverse effects can be increased when Amifostine is combined with Methyclothiazide."