Dolasetron

Dolasetron is a potent **5-HT3 receptor antagonist** utilized primarily as an antiemetic in veterinary medicine. It is particularly effective for managing severe nausea and vomiting associated with cancer chemotherapy in dogs and cats. * **Dosing Convenience**: Unlike ondansetron, which often requires multiple daily doses, dolasetron can typically be administered **once daily**. * **Formulation Challenges**: While the injectable form is highly practical for in-hospital use, the commercially available human oral tablets (50 mg and 100 mg) are too large for direct administration to most small animals. Consequently, oral use usually requires compounding. > **Clinical Pearl**: Due to cost and formulation constraints, other antiemetics like maropitant (Cerenia) or ondansetron are often preferred for routine outpatient use, reserving dolasetron for refractory cases or specific chemotherapy protocols.

Mecanismo: Dolasetron exerts its anti-nausea and antiemetic effects by selectively antagonizing **5-hydroxytryptamine 3 (5-HT3) receptors**. * **Peripheral Pathway**: Chemotherapy and severe GI insults cause the release of serotonin from mucosal enterochromaffin cells in the small intestine. Serotonin binds to 5-HT3 receptors on **vagal afferent nerve terminals**, sending emetogenic signals to the brain. Dolasetron blocks this interaction. * **Central Pathway**: Dolasetron also blocks 5-HT3 receptors located directly within the **Chemoreceptor Trigger Zone (CRTZ)** in the central nervous system. Once administered, dolasetron is rapidly converted by carbonyl reductase into its active metabolite, **hydrodolasetron**, which is primarily responsible for the pharmacological effects.

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