化合物信息

Drug Groups

approved

Description

Zolpidem is a prescription short-acting nonbenzodiazepine hypnotic that potentiates gamma-aminobutyric acid (GABA), an inhibitory neurotransmitter, by binding to benzodiazepine receptors which are located on the gamma-aminobutyric acid receptors. Zolpidem is used for the short-term treatment of insomnia. It works quickly (usually within 15 minutes) and has a short half-life (2-3 hours). It is classified as an imidazopyridine. As an anticonvulsant and muscle relaxant, the beneficial effects start to emerge at 10 and 20 times the dose required for sedation, respectively. For that reason, it has never been approved for either muscle relaxation or seizure prevention. Recently, zolpidem has been cited in various medical reports mainly in the United Kingdom as waking persistent vegetative state (PVS) patients, and dramatically improving the conditions of people with brain injuries. [Wikipedia]

Indication

For the short-term treatment of insomnia.

Pharmacology

Zolpidem is a sedative or hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties. It interacts with a GABA-BZ receptor complex and shares some of the pharmacological properties of the benzodiazepines. In contrast to the benzodiazepines, which non-selectively bind to and activate all three alpha receptor subtypes, zolpidem in vitro binds the (alpha1) receptor preferentially. The (alpha1) receptor is found primarily on the Lamina IV of the sensorimotor cortical regions, substantia nigra (pars reticulata), cerebellum molecular layer, olfactory bulb, ventral thalamic complex, pons, inferior colliculus, and globus pallidus.

Toxicity

Oral (male rat) LD₅₀ = 695 mg/kg. Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma.

Affected Organisms

Biotransformation

Zolpidem is converted to inactive metabolites in the liver.

Absorption

Zolpidem is rapidly absorbed from the GI tract.

Half Life

2.6 hours

Protein Binding

92.5 ± 0.1% (independent of concentration between 40 and 790 ng/mL)

Elimination

Zolpidem tartrate tablets are converted to inactive metabolites that are eliminated primarily by renal excretion.

References

External Links