Dolasetron

Brand name: Anzemet®

IUPAC: (3R)-10-oxo-8-azatricyclo[5.3.1.03,8]undec-5-yl 1H-indole-3-carboxylate

FDA approval: Yes

Usage:

Dolasetron mesylate (Anzemet®) is used to the prevent nausea and vomiting associated with cytotoxic effects of chemotherapy. Dolasetron is administered in pill form.1 In December 2010, the U.S. FDA blocked the use of the injected (intravenous) form of the drug for the prevention of nausea due to chemotherapy.2

1Anzemet.. Prescribing Information. Aventis Pharmaceuticals. September, 2016. [http://www.anzemet.com]
2Anzemet (dolasetron mesylate): Drug Safety Communication - Reports of Abnormal Heart Rhythms. Published 12-17-2010 by the U.S. Food and Drug Administration (FDA). [http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm237341.htm]

Mechanism:

Dolasteron works by blocking the reception of serotonin at 5-HT3 receptors. When these receptors are bound by serotonin, they induce nausea and the vomiting reflex.

The structure below shows the 3D conformer Dolasetron.

Side effects:

The most common side effects associated with the use of Anzemet® during chemotherapy regimens are headache, fatigue and diarrhea. The intravenous version of the drug was associated with abnormal heart rhythms.

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