ANZEMET
Clinical safety rating: caution
Comprehensive clinical and safety monograph for ANZEMET (ANZEMET).
Selective serotonin 5-HT3 receptor antagonist; blocks serotonin binding at 5-HT3 receptors in the chemoreceptor trigger zone and gastrointestinal tract, inhibiting emesis.
| Metabolism | Primarily metabolized by CYP1A1, CYP1A2, and CYP1B1; also undergoes reduction and conjugation. Active metabolite hydrodolasetron is formed via reduction. |
| Excretion | Approximately 70% of the dose is excreted in urine (mostly as metabolites, with less than 10% as unchanged drug) and about 20% in feces via biliary elimination. |
| Half-life | The terminal elimination half-life is approximately 5-7 hours in normal adults, but may be prolonged in patients with hepatic impairment (up to 11 hours) or severe renal impairment. |
| Protein binding | Approximately 69-77% bound to serum proteins, primarily to alpha1-acid glycoprotein. |
| Volume of Distribution | Volume of distribution is about 3.7 L/kg, indicating extensive extravascular distribution. |
| Bioavailability | Oral bioavailability is approximately 100% (due to minimal first-pass metabolism). |
| Onset of Action | Intravenous: onset of antiemetic effect within 1-3 minutes. Oral: onset within 1 hour. |
| Duration of Action | Duration of antiemetic effect is up to 24 hours. For prevention of nausea and vomiting, a single dose is typically sufficient for an entire day. |
100 mg orally once daily, or 1.8 mg/kg (maximum 100 mg) intravenously over 15 minutes once daily.
| Dosage form | TABLET |
| Renal impairment | No dosage adjustment required for mild to moderate renal impairment. For severe renal impairment (CrCl < 30 mL/min), reduce dose by 50%. |
| Liver impairment | No dosage adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). For severe hepatic impairment (Child-Pugh C), reduce dose by 50%. |
| Pediatric use | For chemotherapy-induced nausea and vomiting: 1.8 mg/kg (maximum 100 mg) intravenously over 15 minutes once daily. For postoperative nausea and vomiting: not recommended. |
| Geriatric use | No specific dose adjustments recommended; use with caution due to potential for increased sensitivity and renal impairment. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for ANZEMET (ANZEMET).
| Breastfeeding | It is not known whether dolasetron is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Anzemet is administered to a nursing woman. The M/P ratio is not available. The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Anzemet and any potential adverse effects on the breastfed child from the drug or underlying maternal condition. |
| Teratogenic Risk | Anzemet (dolasetron) is a 5-HT3 receptor antagonist. In animal studies, no teratogenic effects were observed at doses up to 60 mg/kg/day in rats and 120 mg/kg/day in rabbits, which are 19 and 78 times the recommended human dose, respectively. However, adequate and well-controlled studies in pregnant women are lacking. The drug should be used during pregnancy only if clearly needed. No specific trimester-specific risks have been identified in human data. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
["Hypersensitivity to dolasetron or any component of the formulation.","Patients with known QT interval prolongation, including congenital long QT syndrome."]
| Precautions | ["May cause QT interval prolongation; use caution in patients with pre-existing arrhythmias, electrolyte disturbances, or concomitant QT-prolonging drugs.","Serotonin syndrome risk when used with other serotonergic drugs (e.g., SSRIs, SNRIs, MAOIs).","Hypersensitivity reactions including anaphylaxis and bronchospasm reported.","Masking of progressive ileus or gastric distension after abdominal surgery or chemotherapy-induced emesis."] |
| Food/Dietary | No significant food interactions are reported. However, grapefruit may affect CYP3A4 metabolism; consider avoiding excessive grapefruit intake. |
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| Fetal Monitoring | No specific maternal or fetal monitoring is required beyond standard obstetric care. Observe for maternal adverse effects such as headache, dizziness, or cardiac arrhythmias (including QT prolongation). Fetal monitoring is not specifically indicated unless maternal condition warrants. |
| Fertility Effects | In animal studies, dolasetron did not impair fertility in male or female rats at oral doses up to 100 mg/kg/day (approximately 20 times the human dose). No human data are available on the effect of dolasetron on fertility. Based on available evidence, no significant impact on fertility is anticipated at therapeutic doses. |
| Clinical Pearls | ANZEMET (dolasetron) is a 5-HT3 receptor antagonist used for prevention of chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). Due to the risk of dose-dependent QTc interval prolongation, intravenous dolasetron is contraindicated for CINV but the oral form is still used. For PONV, the recommended IV dose is 12.5 mg. Monitor ECG in patients with electrolyte abnormalities, CHF, bradycardia, or those on other QT-prolonging drugs. Dolasetron is metabolized by CYP2D6 and CYP3A4; consider drug interactions. The active metabolite hydrodolasetron has a long half-life (6-8 hours). |
| Patient Advice | Take ANZEMET exactly as prescribed, usually 1 hour before chemotherapy or before surgery. · Side effects may include headache, dizziness, or constipation. Report any irregular heartbeat, fainting, or severe abdominal pain. · Avoid alcohol and other CNS depressants as they may worsen dizziness or drowsiness. · Inform your doctor if you have heart problems, electrolyte imbalance, or take other medications. |