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QuickView for zolpidem (compound)


PubChem
Name: zolpidem
PubChem Compound ID: 441338
Molecular formula: C42H48N6O8
Molecular weight: 764.866 g/mol
Synonyms:
Ambien; 99294-93-6; Zolpidem tartrate; D00706; Ambien (TN); Zolpidem tartrate (JAN/USAN)
DrugBank
Identification
Name: zolpidem
Name (isomeric): DB00425
Drug Type: small molecule
Synonyms:
Zolpidem tartrate; Zolpidemum [Latin]
Brand: Ambien, Ivadal, Niotal, Stilnoct, Ambien CR, Stilnox, Lorex
Category: GABA Agonists, Hypnotics and Sedatives
CAS number: 82626-48-0
Pharmacology
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 act...
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Mechanism of Action: Zolpidem modulates the alpha-subunit, known as the benzodiazepine receptor, within the GABAA 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.
Absorption: Zolpidem is rapidly absorbed from the GI tract.
Protein binding: 92.5 ± 0.1% (independent of concentration between 40 and 790 ng/mL)
Biotransformation: Zolpidem is converted to inactive metabolites in the liver.
Route of elimination: Zolpidem tartrate tablets are converted to inactive metabolites that are eliminated primarily by renal excretion.
Half Life: 2.6 hours
Toxicity: Oral (male rat) LD50 = 695 mg/kg. Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma.
Affected organisms: Humans and other mammals
Interactions
Food interaction:
Avoid alcohol.
Should not be administered with or immediately after a meal.
Drug interaction:
ConivaptanConivaptan, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if conivaptan is initiated, discontinued or dose changed.
SaquinavirSaquinavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if saquinavir is initiated, discontinued or dose changed.
FluconazoleFluconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if fluconazole is initiated, discontinued or dose changed.
FosamprenavirFosamprenavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if fosamprenavir is initiated, discontinued or dose changed.
RitonavirRitonavir, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if ritonavir is initiated, discontinued or dose changed.
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