Dolasetron
ANZEMET
What it is5-HT3-antagonist prodrug converted to hydrodolasetron; prevention of postoperative nausea and vomiting.
Why this oneIts active metabolite prolongs cardiac conduction enough that the IV formulation lost its chemotherapy-nausea role.
What limits it⚑ IV use for chemotherapy nausea is contraindicated because of QT prolongation and torsades; assess rhythm risk even with oral use.
FDA label
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| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Prevention of chemotherapy-induced nausea/vomiting | Adults | 100 mg PO single dose within 1 h before chemotherapy | Same (single dose) | 100 mg/dose — do not exceed |
| Prevention of chemotherapy-induced nausea/vomiting | Peds 2-16 y | 1.8 mg/kg PO single dose within 1 h before chemotherapy | Same (single dose) | 100 mg/dose |
Renal No adjustment needed; ECG monitoring recommended in renal impairment
Hepatic No adjustment needed
Do not exceed recommended doses; ECG monitoring recommended for elderly and renally impaired
Instructions
- Give within 1 hour before chemotherapy
- Peds unable to take tablets: injection solution may be mixed in apple or apple-grape juice for oral dosing (stable 2 h at room temp)
Cautions
- Dose-dependent QT prolongation (IV dolasetron contraindicated for CINV prevention); ECG monitoring recommended in elderly and renal impairment
- Post-marketing: wide-complex/ventricular tachycardia and ventricular fibrillation cardiac arrest after IV administration
- Bradycardia, ECG interval changes observed in trials
Adverse reactions
- Headache (18-23%)
- Fatigue
- Diarrhea
- Bradycardia
- Dizziness
- Tachycardia
- Dyspepsia
- ECG changes
Pregnancy No fetal harm in rat/rabbit studies (8-16x human dose); no adequate human studies — use only if clearly needed
Lactation Undefined
NO BOXED WARNINGS
Principal riskQT prolongation; the IV form is contraindicated for chemotherapy nausea
Classes and tags
Clinical profile
Mechanism of action: Dolasetron ballicule
