Amifostine
Pronunciation: (am-ih-FOSS-teen)Class: Cytoprotective agent
Trade Names:
Ethyol
- Powder for injection, lyophilized 500 mg (anhydrous basis)
Pharmacology
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Organic thiophosphate cytoprotective agent that can reduce the toxicity of cisplatin. It binds to and thereby detoxifies, reactive metabolites of cisplatin. It scavenges reactive oxygen species generated by exposure to cisplatin radiation.
Pharmacokinetics
Distribution
Distribution t ½ is less than 1 min.
Metabolism
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.
Elimination
Rapidly cleared from plasma; elimination t ½ is about 8 min. Renal excretion is 0.69% to 2.64% (parent compound and metabolites).
Indications and Usage
Prevent or reduce renal damage in patients receiving repeated cisplatin doses for advanced ovarian or non-small cell lung cancer; reduce incidence of moderate to severe xerostomia in patients undergoing radiation of the parotid gland for head and neck cancer.
Unlabeled Uses
Prevent or reduce cisplatin-induced neurotoxicity and cyclophosphamide-induced granulocytopenia; prevent or reduce toxicity of radiation therapy to other areas; reduce toxicity of paclitaxel.
Contraindications
Sensitivity to aminothiol compounds.
Dosage and Administration
Reduction of Cumulative Renal Toxicity with ChemotherapyAdults
IV Amifostine 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 Amifostine 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).
General Advice
- Reconstitute powder with 9.7 mL of 0.9% NaCl for a final amifostine concentration of 50 mg/mL.
- Prior to infusion further dilute amifostine in 0.9% NaCl to a final concentration of 5 to 40 mg/mL.
- Do not mix with other IV medications or IV fluids.
- Do not administer if cloudiness or particulate matter is noted.
Storage/Stability
Store vials at controlled room temperature (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).
Drug Interactions
AntihypertensivesCoadministration of drugs with similar pharmacologic effects may potentiate hypotension or cause additive side effects, including toxicity.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Hypotension (all grades 61%); hypotension (associated with apnea, dyspnea, hypoxia, tachycardia, bradycardia, extrasystoles, chest pain, MI, respiratory and cardiac arrest); arrhythmias (including atrial fibrillation/flutter and supraventricular tachycardia); cardiac arrest; transient hypertension; exacerbation of preexisting hypertension; syncope.
CNS
Dizziness; somnolence; seizures.
Dermatologic
Erythema multiforme; exfoliative dermatitis; Stevens-Johnson syndrome; toxic epidermal necrolysis.
GI
Nausea and vomiting (all grades 96%).
Metabolic
Hypocalcemia.
Renal
Renal failure.
Respiratory
Sneezing; hiccoughs.
Miscellaneous
Flushing; feeling of warmth; chills, feeling of coldness, fever; allergic reactions (including hypotension, fever, chills, rigors, dyspnea, hypoxia, chest tightness, cutaneous eruption, urticaria, laryngeal edema); anaphylactoid reactions.
Precautions
MonitorBPMonitor BP every 5 min during the 15 min infusion and thereafter as clinically indicated. Follow manufacturer's guidelines for interrupting and restarting amifostine if a decrease in systolic BP is noted. Stop the infusion for significant decreases in systolic BP. If systolic BP returns to normal and the patient is asymptomatic within 5 min, restart the infusion and continue to monitor BP. If systolic BP remains low, do not administer remainder of dose but administer reduced dose for subsequent cycles. |
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Safety and efficacy not established.
Hypersensitivity
Allergic manifestations including anaphylaxis and severe cutaneous reactions have occurred rarely.
Special Risk Patients
Avoid use in patients with hypersensitivity to amifostine and/or aminothiol compounds. Use cautiously in patients with cerebrovascular or CV disease or hypocalcemia.
Effectiveness of the cytotoxic regimen
Do not use in patients receiving chemotherapy for malignancies in which chemotherapy can produce a significant survival benefit or cure.
Effectiveness of radiotherapy
Do not administer in patients receiving definitive radiotherapy.
Hypotension
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.
Overdosage
Symptoms
Anxiety, reversible urinary retention, hypotension.
Patient Information
- Advise patient that medication will be prepared and administered by health care provider in a health care setting just before chemotherapy or radiation therapy.
- Advise patient to remain supine for 15 min after completion of infusion and to use caution when standing up.
- Instruct patient to inform health care provider if noting any of the following during the administration of drug: anxiety, sweating, rapid heart beat, shortness of breath or difficulty breathing, swelling of the throat, rash, itching.
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More Amifostine resources
amifostine Intravenous - Includes detailed dosage instructions.
Compare Amifostine with other medications for the treatment of:
Cancer, Ovarian Cancer, Non-Small Cell Lung Cancer
