Lerisetron

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

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

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

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

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.

See Also

• 5-HT3 antagonist
• Chemotherapy-induced nausea and vomiting
• Serotonin Syndrome