Drug/Small Molecule:
zolpidem

2D structure

Overview

Generic Names: Zolpidem tartrate; Zolpidemum [Latin]
Trade Names: Ambien; Ivadal; Lorex; Niotal; Stilnoct; Stilnox
PharmGKB Accession Id: PA451976

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 (source: Drug Bank)

Indication

For the short-term treatment of insomnia. (source: Drug Bank)

ATC Therapeutic Category

  • N05CF:Benzodiazepine related drugs

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

Zolpidem modulates the alpha-subunit, known as the benzodiazepine receptor, within the GABA<sub>A</sub> receptor chloride channel macromolecular complex. Unlike the benzodiazepines, which non-selectively interact with all three alpha-receptor subtypes, Zolpidem preferentially binds to the alpha-1 receptor. (source: Drug Bank)

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. (source: Drug Bank)

Food Interactions

Avoid alcohol.
Take 30-60 minutes before breakfast. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Zolpidem is converted to inactive metabolites in the liver. (source: Drug Bank)

Protein Binding

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

Absorption

Zolpidem is rapidly absorbed from the GI tract. (source: Drug Bank)

Toxicity

Oral (male rat) LD<sub>50</sub> = 695 mg/kg. Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma. (source: Drug Bank)

Isomeric SMILES Code:

Cc1ccc(cc1)c2c(n3cc(ccc3n2)C)CC(=O)N(C)C (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
NR1I2
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  • FA
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
GABRA1 Uncurated Annotation (source: Drug Bank)
TSPO Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
caffeine
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  • PD
  • PK
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Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Sleep Initiation and Maintenance Disorders
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  • PK
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Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Physicochemical determinants of human renal clearance

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00425
KEGG Compound ID:
C07219
PubChem Compound ID:
5732
PubChem Substance ID:
199579

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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