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|Amifostine |
Drugs search, click the first letter of a drug name: | A | B | C | D | E | F | G | H | I | J | K | L | M | N | O | P | Q | R | S | T | U | V | W | X | Y | Z | 1 | 2 | 3 | 4 | 5 | 6 | 8 | 9 Home AmifostinePronouncation: (am-ih-FOSS-teen)Class: Cytoprotective agent Trade Names: Mechanism of ActionPharmacologyOrganic 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. PharmacokineticsDistributionDistribution t ½ is less than 1 min. MetabolismAmifostine is a prodrug that is dephosphorylated by alkaline phosphatase in tissues to the active free thiol metabolite. A disulfide metabolite is then subsequently produced. EliminationRapidly cleared from plasma; elimination t ½ is about 8 min. Renal excretion is 0.69% to 2.64% (parent compound and metabolites). Indications and UsagePrevent 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 UsesPrevent or reduce cisplatin-induced neurotoxicity and cyclophosphamide-induced granulocytopenia; prevent or reduce toxicity of radiation therapy to other areas; reduce toxicity of paclitaxel. ContraindicationsSensitivity to aminothiol compounds. Dosage and AdministrationReduction 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
Storage/StabilityStore 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 InteractionsAntihypertensivesCoadministration of drugs with similar pharmacologic effects may potentiate hypotension or cause additive side effects, including toxicity. Laboratory Test InteractionsNone well documented. Adverse ReactionsCardiovascularHypotension (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. CNSDizziness; somnolence; seizures. DermatologicErythema multiforme; exfoliative dermatitis; Stevens-Johnson syndrome; toxic epidermal necrolysis. GINausea and vomiting (all grades 96%). MetabolicHypocalcemia. RenalRenal failure. RespiratorySneezing; hiccoughs. MiscellaneousFlushing; 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
PregnancyCategory C . LactationUndetermined. ChildrenSafety and efficacy not established. ElderlySafety and efficacy not established. HypersensitivityAllergic manifestations including anaphylaxis and severe cutaneous reactions have occurred rarely. Special Risk PatientsAvoid 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 regimenDo not use in patients receiving chemotherapy for malignancies in which chemotherapy can produce a significant survival benefit or cure. Effectiveness of radiotherapyDo not administer in patients receiving definitive radiotherapy. HypotensionDo 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. OverdosageSymptomsAnxiety, reversible urinary retention, hypotension. Patient Information
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