Anzemet Generic Name & Formulations
Dolasetron mesylate 50mg, 100mg; tabs.
Selective 5-HT3 receptor antagonist.
Mechanism of Action
Dolasetron mesylate and its active metabolite, hydrodolasetron, are selective serotonin 5-HT3 receptor antagonists not shown to have activity at other known serotonin receptors and with low affinity for dopamine receptors. The serotonin 5-HT3 receptors are located on the nerve terminals of the vagus in the periphery and centrally in the chemoreceptor trigger zone of the area postrema.
Prevention of nausea & vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses.
Anzemet Dosage and Administration
≥16yrs: 100mg within 1hr before chemotherapy.
<2yrs: not established. 2–16yrs: Chemotherapy-induced: 1.8mg/kg (max 100mg) within 1hr before chemotherapy; or, may give IV soln and mix 1.8mg/kg (max 100mg) into apple or apple-grape juice and taken orally within 1hr before chemotherapy.
Inj soln administered by IV: Prevention of nausea & vomiting associated with emetogenic cancer chemotherapy, including initial and repeat courses in adults and children.
Anzemet Boxed Warnings
Increased risk of developing QTc, PR and QRS interval prolongation. Avoid in patients with congenital QT syndrome, hypokalemia, hypomagnesemia, complete heart block or risk of (unless paced). Correct electrolyte imbalances prior to therapy. Monitor ECG periodically. CHF. Bradycardia. Pre-existing conduction abnormalities and underlying structural heart disease. Sick sinus syndrome. Atrial fibrillation with slow ventricular response. Recent MI. Renal impairment. Elderly. Pregnancy (Cat.B). Nursing mothers.
Renal (61%). Half-life: 8.1 hours.
Caution with drugs which can prolong ECG intervals (eg, verapamil, flecainide, quinidine), diuretics, and with cumulative high-dose anthracycline therapy. Serotonin syndrome possible with concomitant serotonergic drugs (eg, SSRIs, SNRIs). Potentiated by cimetidine, atenolol (IV dolasetron). Antagonized by rifampin.
Anzemet Adverse Reactions
Headache, dizziness, pain, fatigue, diarrhea, bradycardia, tachycardia, dyspepsia, chills/shivers, ECG changes, 2nd- or 3rd-degree AV block; serotonin syndrome (discontinue if occurs).
Anzemet Clinical Trials
Anzemet Patient Counseling