Dolasetron — Drug Monograph

Brand names: Anzemet

Drug class: Supportive Care Agent

Mechanism of Action

Selective serotonin 5-HT3 receptor antagonist. Dolasetron is rapidly converted to its active metabolite, hydrodolasetron (MDL 74,156), which is the primary active compound mediating antiemetic activity by blocking 5-HT3 receptors peripherally and centrally.

FDA Indications

• Prevention of nausea and vomiting associated with moderately emetogenic chemotherapy (oral formulation only, as of 2010 FDA safety communication)
• Prevention of postoperative nausea and vomiting (PONV) — both oral and IV formulations

Common Side Effects

• Headache
• Diarrhea
• Dizziness
• Fatigue
• Bradycardia

Clinical Pearl

Dolasetron is the least preferred 5-HT3 antagonist in current oncology practice due to its higher cardiac risk profile, particularly QT prolongation and the historical withdrawal of IV CINV use. When choosing among 5-HT3 antagonists for HEC or MEC, palonosetron, ondansetron, or granisetron are preferred. Dolasetron oral remains an option for MEC but is rarely chosen in settings where alternatives are available.

Related Therapies & Mechanisms

• Aprepitant (Emend) — Supportive Care Agent
• Avatrombopag (Doptelet) — Supportive Care Agent
• Darbepoetin Alfa (Aranesp) — Supportive Care Agent
• Defibrotide (Defitelio) — Supportive Care Agent