Trade Names:Ethyol- Injection, lyophilized powder for solution 500 mg
Amifostine is an organic thiophosphate cytoprotective agent that can reduce the toxicity of cisplatin or radiation. It binds to, and thereby detoxifies, reactive metabolites of cisplatin. It scavenges reactive oxygen species generated by exposure to cisplatin or radiation.
Distribution half-life is less than 1 min.
Amifostine is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to the active free thiol metabolite. A disulfide metabolite is then subsequently produced.
Rapidly cleared from plasma; elimination half-life is approximately 8 min. Renal excretion is 0.69% to 2.64% (parent compound and metabolites).
Prevent or reduce renal damage in patients receiving repeated cisplatin doses for advanced ovarian cancer; reduce incidence of moderate to severe xerostomia in patients undergoing radiation of the parotid gland for head and neck cancer.
Prevent or reduce cisplatin-induced neurotoxicity and cyclophosphamide-induced granulocytopenia; prevent or reduce toxicity of radiation therapy to other areas; reduce toxicity of paclitaxel.
Hypersensitivity to aminothiol compounds.
IV 910 mg/m 2 once daily as a 15-min IV infusion, 30 min before chemotherapy.Reduction of Moderate to Severe Xerostomia From Radiation of the Head and NeckAdults
IV 200 mg/m 2 once daily as a 3-min IV infusion, 15 to 30 min prior to standard fraction radiation therapy (1.8 to 2 Gy).
Store vials at 68° to 77°F. Reconstituted and diluted solutions are stable for up to 5 h at controlled room temperature or for up to 24 h if refrigerated (36° to 46°F).
Coadministration of drugs with similar pharmacologic effects may potentiate hypotension or cause additive side effects, including toxicity. Interrupt antihypertensive therapy 24 h preceding administration of amifostine.
None well documented.
Hypotension (all grades) (62%); arrhythmias (including atrial fibrillation/flutter and supraventricular tachycardia), cardiac arrest, chest pain, dyspnea, exacerbation of preexisting hypertension, extrasystoles, hypotension (associated with apnea, bradycardia, hypoxia, MI, respiratory and cardiac arrest, tachycardia), syncope, transient hypertension.
Dizziness, malaise, seizures, somnolence.
Erythema multiforme, exfoliative dermatitis, rash, Stevens-Johnson syndrome, TEN.
Nausea, vomiting (all grades) (96%).
Allergic reactions (including chest tightness, chills, cutaneous eruption, dyspnea, fever, hypotension, hypoxia, laryngeal edema, rigors, urticaria), anaphylactoid reactions.
Renal failure (rare).
Chills, feeling of coldness, feeling of warmth, fever, flushing.
Monitor BP every 5 min during the 15-min infusion and as clinically indicated thereafter. Monitor BP at least before and immediately after the 3-min infusion, and as clinically indicated thereafter. Monitor patient carefully prior to, during, and after amifostine administration for cutaneous reactions. Monitor the fluid balance of patients administered highly emetogenic chemotherapy. Monitor serum calcium levels in patients at risk of hypocalcemia.
Category C .
Safety and efficacy not established.
Use with caution.
Allergic manifestations, including anaphylaxis and severe cutaneous reactions, have occurred.
Use cautiously in patients with preexisting cardiovascular or cerebrovascular conditions, such as ischemic heart disease, arrhythmias, CHF, or history of stroke or TIA. Use with caution in patients in whom the common amifostine adverse effects of nausea/vomiting and hypotension may be more likely to have serious consequences.
Do not use in patients receiving chemotherapy for other malignancies in which chemotherapy can produce a significant survival benefit or cure.
Do not administer in patients receiving definitive radiotherapy.
Do not give to patients who are hypotensive or dehydrated. If symptomatic hypotension develops, discontinue the infusion, place the patient in the Trendelenburg position, and administer normal saline via a separate IV line.
Anxiety, hypotension, reversible urinary retention.
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