NK receptor antagonist that prevents vomiting ?
Correct Answer: Aprepitant
Description: Ans. is d i.e., Aprepitant Aprepitant Aprepitant is an antiemetic substance that belongs to a class of drugs called substance P antagonists. The compound mediates its effect by blocking the neurokinim 1 (NK1) receptor. Ceain regions of brain have high expression of NK1 receptors. Substance P acts on these receptors and is responsible for chemotheraphy induced nausea and vomiting. Aprepitant acts as a substance P antagonist on NK1 receptors. Aprepitant has little or no affinity for Serotonin 5-HT3, dopamine or coicosteroid receptors. Aprepitant crosses the blood brain barrier. Aprepitant is used for chemotherapy induced nausea & vomiting (CINV), and post- operative nausea & vomiting (PONY). After absorption aprepitant is bound extensively to plasma proteins (>95%); it is metabolized avidly, primarily by hepatic CYP 3A4 and is excreted in the stools. Aprepitant is contraindicated in patients on cisapride or pimozide, in which life threatening QT prolongation has been repoed. The recommended adult dose of a prepitant is 125 mg administered 1 hour before chemotherapy on day one, followed by 8 mg once daily in the morning on day 2 and 3 of the treatment regimen.
Category:
Pharmacology
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