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Ambien

Zolpidem
Zolpidem.svg
Zolpidem ball-and-stick model.png
Clinical data
Trade names Ambien, others
AHFS/Drugs.com Monograph
MedlinePlus a693025
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Dependence
liability
High
Routes of
administration
Oral (tablet), sublingual, oromucosal (spray), rectal
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability 70% (oral)
Protein binding 92%
Metabolism Liver through CYP3A4
Biological half-life 2–3 hours
Duration of action 3 hours
Excretion Kidney (56%)
fecal (34%)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
ECHA InfoCard 100.115.604
Chemical and physical data
Formula C19H21N3O
Molar mass 307.395 g/mol
3D model (Jmol)
 NYesY (what is this?)  

Zolpidem, sold as the brand name Ambien among others, is a sedative primarily used for the treatment of trouble sleeping. It usually works usually within 15 minutes, and has a short half-life of two to three hours. Zolpidem has not adequately demonstrated effectiveness in maintaining sleep, unless delivered in a controlled-release (CR) form. However, it is effective in initiating sleep. Its hypnotic effects are similar to those of the benzodiazepine class of drugs.

In 2013, the Food and Drug Administration required manufacturers to decrease the recommended dose for women by half, after studies showed that the medicines can leave people drowsy in the morning and at risk for motor vehicle collisions. The FDA recommended that manufacturers extend the new dosage cuts to men as well, who process the drug at a faster rate; however, the reasons men and women metabolize the drugs at different rates are still unknown. In May 2013, the FDA approved label changes specifying new dosage recommendations for zolpidem products because of concerns regarding next-morning impairment. The underlying mechanism involves GABA.

It is a short-acting nonbenzodiazepine compound of the imidazopyridine class that increases the activity of GABA, an inhibitory neurotransmitter, by binding to GABAA receptors at the same location as benzodiazepines. It is molecularly distinct from the classical benzodiazepine molecule and is classified as an imidazopyridine. Flumazenil, a benzodiazepine receptor antagonist, which is used for benzodiazepine overdose, can also reverse zolpidem's sedative/hypnotic and memory-impairing effects.


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