졸피뎀

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졸피뎀 C화학적 특성, 용도, 생산

개요

Zolpidem hemitamwe is a non-benzodiazepine hypnotic with specific agonist activity at type 1 benzodiazepine receptors, and is indicated for use in insomnia and other sleep disorders. Structurally zolpidem belongs to a chemically distinct class, thus lacking the side-effects and abuse potential of classical benzodiazepines. It is currently being studied as a pre-operative sedative.

화학적 성질

Off-White Solid

용도

A selective benzodiazepine receptor agonist not related chemically to benzodiazepines

정의

ChEBI: An imidazo[1,2-a]pyridine compound having a 4-tolyl group at the 2-position, an N,N-dimethylcarbamoylmethyl group at the 3-position and a methyl substituent at the 6-position.

일반 설명

Zolpidem (Ambien, an imidazopyridine) andeszopiclone (Lunesta, a cyclopyrrolone) are nonbenzodiazepinesand have been introduced as short- and moderate-acting hypnotics, respectively. Zolpidem exhibits ahigh selectivity for the α1 subunit of benzodiazepinebindingsite on GABAA receptor complex, whereas eszopicloneis a “superagonist” at BzRs with the subunitcomposition α1β2γ2 and α1β2γ3. Zolpidem has a rapidonset of action of 1.6 hours and good bioavailability(72%), mainly because it is lipophilic and has no ionizablegroups at physiological pH. Food can prolong the time topeak concentration without affecting the half-life probablyfor the same reason. It has short elimination half-life, becauseits aryl methyl groups is extensively α-hydroxylatedto inactive metabolites by CYP3A4 followed by furtheroxidation by aldehyde dehydrogenase to the ionic carboxylicacid. The metabolites are inactive, short-lived, andeliminated in the urine. Its half-life in the elderly or the patientswith liver disease is increased. Therefore, dosingshould be modified in patients with hepatic insufficiencyand the elderly. Because it has longer elimination half-lifethan zaleplon, it may be preferred for sleep maintenance.It was the most commonly prescribed drug for insomniain 2001.

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