Description
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.
Description
Zolpidem (Item No. 15792) is an analytical reference material that is functionally categorized as a sedative. It is a non-benzodiazepine drug that is used in the treatment of insomnia, and it has been recreationally abused. This product is intended for research and forensic applications.
Description
Zolpidem (Item No. 20648) is a certified reference material that is functionally categorized as a sedative. It is a non-benzodiazepine drug that is used in the treatment of insomnia, and it has been recreationally abused. This product is intended for research and forensic applications.
Chemical Properties
Off-White Solid
Originator
Synthelabo (France)
Uses
A selective non-benzodiazepine GABAA receptor agonist. Sedative, hypnotic.
Controlled substance (depresssant).
Uses
A selective benzodiazepine receptor agonist not related chemically to benzodiazepines
Definition
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.
brand name
Ambien (Sanofi Aventis);Stilnox.
General Description
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.
