Trade Names:Anzemet- Injection 20 mg/mL- Tablets 50 mg- Tablets 100 mg
Selective serotonin (5-HT 3 ) receptor antagonist that inhibits serotonin receptors in the GI tract and chemoreceptor zone.
Parent drug rapidly eliminated and completely metabolized to hydrodolasetron (active). T max for hydrodolasetron is approximately 1 h (oral) and approximately 0.6 h (IV). Bioavailability is approximately 75% (determined by hydrodolasetron).
Vd approximately 5.8 L/kg (hydrodolasetron). Hydrodolasetron is 69% to 77% protein bound.
Reduced to hydrodolasetron by carbonyl reductase. Subsequent hydroxylation due to CYP2D6 and N-oxidation due to CYP3A and flavin monooxygenase.
Approximately 67% of dose recovered in the urine (61% as hydrodolasetron) and approximately 33% recovered in the feces.
t ½ less than 10 min for dolasetron (IV), approximately 7.3 h for hydrodolasetron (IV), and approximately 8.1 h (oral).
Cl approximately 9.4 mL/min/kg (IV) and approximately 13.4 mL/min/kg (oral) for hydrodolasetron.
Prevention of nausea and vomiting associated with initial and repeat courses of emetogenic chemotherapy; prevention of postoperative nausea and vomiting in patients at risk.Parenteral only
Treatment of postoperative nausea and vomiting.
Radiotherapy-induced nausea and vomiting.
PO 100 mg within 1 h before chemotherapy. IV 1.8 mg/kg (or 100 mg) infused rapidly over 30 sec or diluted and infused over 15 min, 30 min before chemotherapy.Children 2 to 16 yr of age
PO 1.8 mg/kg (max 100 mg) within 1 h before chemotherapy. IV 1.8 mg/kg (max 100 mg) infused rapidly over 30 sec or diluted and infused over 15 min, 30 min before chemotherapy.Prevention of Postoperative Nausea and Vomiting in Patients at RiskAdults and Children older than 16 yr of age
PO 100 mg within 2 h before surgery. IV 12.5 mg 15 min before cessation of anesthesia.Children 2 to 16 yr of age
PO 1.2 mg/kg (max of 100 mg) within 2 h before surgery. IV 0.35 mg/kg (max of 12.5 mg) 15 min before cessation of anesthesia.Treatment of Postoperative Nausea and VomitingAdults and Children older than 16 yr of age
IV 12.5 mg as a single dose as soon as nausea and vomiting presents.Children 2 to 16 yr of age
IV 0.35 mg/kg as a single dose as soon as nausea and vomiting present.
Diluted injection is stable for 24 h at room temperature or for 48 h if refrigerated. Store tablets and undiluted injection at room temperature protected from light.
Additive effects on conduction.Atenolol
Increased serum levels of active metabolite (IV only).Cimetidine
Increased serum levels of active metabolite.Rifampin
Decreased serum levels of active metabolite.
None well documented.
Tachycardia; bradycardia; flushing; hypertension; hypotension.
Headache; vertigo; dizziness agitation; drowsiness; sleep disorder; depersonalization.
Rash; itching; sweating.
Abdominal pain; constipation; diarrhea; dyspepsia; anorexia; taste perversion; abnormal liver function.
Oliguria; urinary retention.
Fever; fatigue; pain; chills; shivering.
Category B .
Safety and efficacy in children younger than 2 yr of age not established.Conditions predisposing to prolongation of cardiac conduction intervals (eg, electrolyte abnormalities, class 1A antiarrhythmias)
Use with caution.
Can cause ECG interval change (PR, QTc, JT) prolongation and QRS widening) which could cause CV consequences, including heart block and arrhythmias. These changes are related in magnitude and frequency to the active metabolite.
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