Lerisetron

Lerisetron is a pharmacological agent that is classified as a 5-HT3 antagonist. It is primarily used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV).

Pharmacology[edit | edit source]

Lerisetron works by blocking the action of serotonin, a natural substance that may cause nausea and vomiting. It is a potent and selective 5-HT3 receptor antagonist. The 5-HT3 receptors are located on the nerve terminals of the vagus nerve in the periphery, and centrally in the chemoreceptor trigger zone of the area postrema.

Clinical Use[edit | edit source]

Lerisetron is used to prevent nausea and vomiting caused by cancer chemotherapy. It is used in combination with other medications to prevent delayed nausea and vomiting that may occur a few days after receiving chemotherapy treatment.

Side Effects[edit | edit source]

Common side effects of Lerisetron include headache, constipation, and fatigue. Serious side effects may include Serotonin Syndrome, a potentially life-threatening condition that can occur with the use of 5-HT3 receptor antagonists.

History[edit | edit source]

Lerisetron was developed by Helsinn Healthcare, a Swiss pharmaceutical company, in the late 1990s. It was approved for medical use in Europe in 1997, but is not currently approved for use in the United States.

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