All are true about Remelteon except –
Correct Answer: It has a high addiction potential
Description: It has high addiction potential Ramelton is an orally acting hypnotic drug for the treatment of chronic and transient amnesia. - Unlike other hypnotics it has no GABA or opiate receptor affinity. - If has the first novel mechanism developed in last 35 years of sleep research. Ramelton is an analogue of melatonin. - It binds selectively to the melatonin receptors MT! and MT2. By bindind selectively to these receptors the drug mimics and enhances the action of endogenous melatonin which has been associated with maintenance of circadian rhythm)t through the inhibitory activity of MT) and MT2 receptors on excitatory wakefulness promoting circuits in the suprachiasmatic nucleus. - Melatonin has inhibitory effect on excitatory wakefulness promoting circuits of suprachiasmatic nucleus. - Suprachiasmatic nucleus is considered to be the masterclass regulating the 24 hour sleep wake cycle through the day and night phases. Suprachiasmatic nucleus is situated in the hypothalamus. It stimulates the pineal glands to produce melatonin. Melatonin acts on MT] and MT2 receptors located in the suprachiasmatic nucleus and induce sleep. - Ramelton is an analogue of melatonin that acts on MT] and MT2 receptors. It has even higher affinity .for these receptors than melatonin. The drug mimics and enhances the effect of endogenous melatonin. Pharmacokinetics Ramelton is characterized by undergoing extensive first pass metabolism along with having high oral bioavailability. Ramelton undergoes extensive metabolism in the liver. The major enzyme involved in the metabolism of Ramelton in the liver is CYPlA2 isoform of cytochrome P450. Ramelton is primarily oxidized to hydroxyl and carbonyl derivatives with secondary metabolism producing glucuronide conjugate. The major metabolite of Ramelton is M-II and has approximately I/10" and I/5th of the binding affinity of the parent molecule .for MTI and MT2 receptors and is 17-25 times less potent than Ramelton in vitro functional assays. Ramelton has no addiction potential Ramelton exes sleep promoting function without causing tearing and memory impairment, motor dysfunction and drug abuse liability.
Category:
Pharmacology
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