Anzemet

— THERAPEUTIC CATEGORIES —
  • Nausea

Anzemet Generic Name & Formulations

General Description

Dolasetron mesylate 50mg, 100mg; tabs.

Pharmacological Class

Selective 5-HT3 receptor antagonist.

How Supplied

Tabs—5

Manufacturer

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.

Anzemet Indications

Indications

Prevention of nausea & vomiting associated with moderately emetogenic cancer chemotherapy, including initial and repeat courses.

Anzemet Dosage and Administration

Adult

≥16yrs: 100mg within 1hr before chemotherapy.

Children

<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.

Anzemet Contraindications

Contraindications

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

Not Applicable

Anzemet Warnings/Precautions

Warnings/Precautions

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.

Anzemet Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal (61%). Half-life: 8.1 hours.

Anzemet Interactions

Interactions

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

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

See Literature

Anzemet Note

Not Applicable

Anzemet Patient Counseling

See Literature