Zolpidem


Description

Zolpidem, also known as _Ambien_, is a hypnotic drug that was initially approved by the FDA in 1992 [FDA label]. Zolpidem improves sleep in patients with insomnia. It is aimed for use in patients with difficulties initiating sleep. This drug decreas...

Read more

Pharmacology

Indication

This drug is indicated for the short-term treatment of insomnia in adults characterized by difficult... Read more

Pharmacodynamic

**Effects on the central nervous system (CNS)**

This drug has CNS depressant effects, which may i...
Read more

Mechanism of action


Zolpidem, the active moiety of zolpidem tartrate, is a hypnotic substance with a chemical structur...
Read more

Absorption

Zolpidem is rapidly absorbed from the gastrointestinal tract. In a single-dose crossover study in 45... Read more

Protein binding

92.5 ± 0.1% [FDA label]

Volume of distribution

0.54 to 0.68 L/kg (in humans) [ Read more

Clearance

In a clinical trial, after a 20mg dose, total clearance of zolpidem 0.24 to 0.27 ml/min/kg [ Read more

Half life

The average zolpidem elimination half-life was 2.6 and 2.5 hours, for the 5 and 10 mg tablets, respe... Read more

Route of elimination

Zolpidem tartrate tablets are converted to inactive metabolites that are eliminated mainly by renal... Read more

Toxicity

Oral (male rat) LD50 = 695 mg/kg [MSDS].

**Overdose**

Symptoms of overdose include...
Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 14-19%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 6-15%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 8-12%
  • Clinical Trial
    Drowsiness US
  • Kind: experimental
    • Percent: 2-8%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Nasopharyngitis US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Allergy US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Hallucinations (hypnogogic, visual and NOS) US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Drugged feeling US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Lethargy US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Visual Disturbance US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Memory Disorders US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Memory Impairment US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Anterograde amnesia US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Influenza US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dysorientation US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2
  • Clinical Trial
    Influenza-like symptoms US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Lightheadedness US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hypoesthesia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Psychomotor retardation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Muscle Cramp US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Psychomotor retardation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Bing eating US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Depersonalization US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Disinhibition US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Euphoric mood US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Known hypersensitivity to zolpidem
        • Drugbank Id: DBCOND0117988

    Food Interactions

    • Avoid alcohol.
    • Should not be administered with or immediately after a meal.

    Interactions

    Type in a drug name to check for interaction with Zolpidem

    The metabolism of Zolpidem can be decreased when combined with (R)-warfarin.
    The metabolism of Zolpidem can be decreased when combined with (S)-Warfarin.
    The metabolism of Zolpidem can be decreased when combined with 1-(2-Phenylethyl)-4-phenyl-4-acetoxypiperidine.
    2,5-Dimethoxy-4-ethylthioamphetamine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    The metabolism of Zolpidem can be decreased when combined with 3,5-diiodothyropropionic acid.
    4-Bromo-2,5-dimethoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Zolpidem.
    4-Methoxyamphetamine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    The metabolism of Zolpidem can be decreased when combined with 5-androstenedione.
    5-methoxy-N,N-dimethyltryptamine may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    The metabolism of Zolpidem can be decreased when combined with 6-Deoxyerythronolide B.
    The metabolism of Zolpidem can be decreased when combined with 6-O-benzylguanine.
    The metabolism of Zolpidem can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    7-Nitroindazole may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
    The metabolism of 8-azaguanine can be decreased when combined with Zolpidem.
    The metabolism of 8-chlorotheophylline can be decreased when combined with Zolpidem.
    The metabolism of Zolpidem can be decreased when combined with 9-aminocamptothecin.
    The metabolism of 9-Deazaguanine can be decreased when combined with Zolpidem.
    The metabolism of 9-Methylguanine can be decreased when combined with Zolpidem.

    References

    • 1 . Lemmer B: The sleep-wake cycle and sleeping pills. Physiol Behav. 2007 Feb 28;90(2-3):285-93. Epub 2006 Oct 16. [PubMed: 17049955]
    • 2 . Depoortere H, Zivkovic B, Lloyd KG, Sanger DJ, Perrault G, Langer SZ, Bartholini G: Zolpidem, a novel nonbenzodiazepine hypnotic. I. Neuropharmacological and behavioral effects. J Pharmacol Exp Ther. 1986 May;237(2):649-58. [PubMed: 2871178]
    • 3 . Clauss RP, Guldenpfennig WM, Nel HW, Sathekge MM, Venkannagari RR: Extraordinary arousal from semi-comatose state on zolpidem. A case report. S Afr Med J. 2000 Jan;90(1):68-72. [PubMed: 10721397]
    • 4 . Schlich D, L'Heritier C, Coquelin JP, Attali P, Kryrein HJ: Long-term treatment of insomnia with zolpidem: a multicentre general practitioner study of 107 patients. J Int Med Res. 1991 May-Jun;19(3):271-9. [PubMed: 1670039]
    • 5 . Maarek L, Cramer P, Attali P, Coquelin JP, Morselli PL: The safety and efficacy of zolpidem in insomniac patients: a long-term open study in general practice. J Int Med Res. 1992 Apr;20(2):162-70. [PubMed: 1521672]
    • 6 . Swainston Harrison T, Keating GM: Zolpidem: a review of its use in the management of insomnia. CNS Drugs. 2005;19(1):65-89. doi: 10.2165/00023210-200519010-00008. [PubMed: 15651908]
    • 7 . Salva P, Costa J: Clinical pharmacokinetics and pharmacodynamics of zolpidem. Therapeutic implications. Clin Pharmacokinet. 1995 Sep;29(3):142-53. doi: 10.2165/00003088-199529030-00002. [PubMed: 8521677]
    • 8 . Fitzgerald AC, Wright BT, Heldt SA: The behavioral pharmacology of zolpidem: evidence for the functional significance of alpha1-containing GABA(A) receptors. Psychopharmacology (Berl). 2014 May;231(9):1865-96. doi: 10.1007/s00213-014-3457-x. Epub 2014 Feb 22. [PubMed: 24563183]
    • 9 . Du B, Shan A, Zhang Y, Zhong X, Chen D, Cai K: Zolpidem arouses patients in vegetative state after brain injury: quantitative evaluation and indications. Am J Med Sci. 2014 Mar;347(3):178-82. doi: 10.1097/MAJ.0b013e318287c79c. [PubMed: 23462249]
    • 10 . Guo T, Mao G, Zhao L, Xia D, Yang L: Comparative pharmacokinetics of zolpidem tartrate in five ethnic populations of China. Acta Pharm Sin B. 2014 Apr;4(2):146-50. doi: 10.1016/j.apsb.2014.02.001. Epub 2014 Mar 15. [PubMed: 26579377]
    • 11 . Tan KR, Rudolph U, Luscher C: Hooked on benzodiazepines: GABAA receptor subtypes and addiction. Trends Neurosci. 2011 Apr;34(4):188-97. doi: 10.1016/j.tins.2011.01.004. Epub 2011 Feb 25. [PubMed: 21353710]
    • 12 . Vlainic J, Pericic D: Effects of acute and repeated zolpidem treatment on pentylenetetrazole-induced seizure threshold and on locomotor activity: comparison with diazepam. Neuropharmacology. 2009 Jun;56(8):1124-30. doi: 10.1016/j.neuropharm.2009.03.010. Epub 2009 Apr 1. [PubMed: 19345234]
    • 13 . Crestani F, Martin JR, Mohler H, Rudolph U: Mechanism of action of the hypnotic zolpidem in vivo. Br J Pharmacol. 2000 Dec;131(7):1251-4. doi: 10.1038/sj.bjp.0703717. [PubMed: 11090095]
    • 14 . FDA Drug Safety Communication: FDA approves new label changes and dosing for zolpidem products and a recommendation to avoid driving the day after using Ambien CR [Link]
    • 15 . NIH Stat Pearls, Internet: Zolpidem [Link]
    • 16 . Questions and Answers: Risk of next-morning impairment after use of insomnia drugs; FDA requires lower recommended doses for certain drugs containing zolpidem (Ambien, Ambien CR, Edluar, and Zolpimist) [Link]
    • 17 . Ambien CR (extended release) label [File]

    Recent Questions