Zaleplon


Description

Zaleplon is a sedative/hypnotic, mainly used for insomnia. It is known as a nonbenzodiazepine hypnotic. Zaleplon interacts with the GABA receptor complex and shares some of the pharmacological properties of the benzodiazepines. Zaleplon is a schedule...

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Pharmacology

Indication

For the treatment of short-term treatment of insomnia in adults.

Pharmacodynamic

Zaleplon is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the... Read more

Mechanism of action

Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride cha... Read more

Absorption

Absorption Zaleplon is rapidly and almost completely absorbed following oral administration.

Protein binding

Approximately 60% (in vitro plasma protein binding).

Volume of distribution

1.4 L/kg

Clearance

1 L/h/kg

Half life

Approximately 1 hour

Route of elimination

Zaleplon is metabolized primarily by the liver and undergoes significant presystemic metabolism. Aft... Read more

Toxicity

Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 30-42%
  • Kind: placebo
    • Percent: 35%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 7-9%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 6-8%
  • Kind: placebo
    • Percent: 7%
  • Clinical Trial
    Asthenia US
  • Kind: experimental
    • Percent: 5-7%
  • Kind: placebo
    • Percent: 5%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 5-6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dysmenorrhea US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Eye Pain US
  • Kind: experimental
    • Percent: 3-4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: 2-4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Malaise US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Parosmia US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Hyperacusis US
  • Kind: experimental
    • Percent: 1-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Abnormal vision US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Tremor US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hyperthesia US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Despersonalization US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Anorexia US
  • Kind: experimental
    • Percent: 0-2%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Photosensitivity reaction US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Ear pain US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Epistaxis US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Hypertonia US
  • Kind: experimental
    • Percent: 1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Hallucinations US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Confusion US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Peripheral Edema US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: <1%
  • Clinical Trial
    Colitis US
  • Kind: experimental
    • Percent: 0-1%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vaginitis US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Urinary Incontinence US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Urinary Urgency US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Dysuria US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Hematuria US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Breast Pain US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Cystitis US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Decreased urine stream US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Menorrhagia US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Metrorrhagia US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Urinary Frequency US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Impotence US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Kidney calculus US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Kidney pain US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Dyspnea US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Asthma US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Nystagmus US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Neuralgia US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Libido decreased US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Insomnia US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Bladder pain US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Voice Alteration US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial
    Snoring US
  • Kind: experimental
    • Percent: <0.01%
  • Clinical Trial

    Contraindications

    Information currently not available.

    Food Interactions

      Information currently not available.

    Interactions

    Type in a drug name to check for interaction with Zaleplon

    The metabolism of (R)-warfarin can be decreased when combined with Zaleplon.
    The metabolism of (S)-Warfarin can be decreased when combined with Zaleplon.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
    Zaleplon may increase the excretion rate of 3-isobutyl-1-methyl-7H-xanthine which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Zaleplon.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 4-Bromo-2,5-dimethoxyamphetamine.
    The metabolism of 4-hydroxycoumarin can be decreased when combined with Zaleplon.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 4-Methoxyamphetamine.
    The metabolism of 5-androstenedione can be decreased when combined with Zaleplon.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 5-methoxy-N,N-dimethyltryptamine.
    The metabolism of Zaleplon can be decreased when combined with 6-Deoxyerythronolide B.
    Zaleplon may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Zaleplon may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of Zaleplon can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 7-Nitroindazole.
    The risk or severity of adverse effects can be increased when Zaleplon is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
    Zaleplon may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Zaleplon may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
    Zaleplon may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
    The metabolism of 9-aminocamptothecin can be decreased when combined with Zaleplon.

    References

    • 1 . Dundar Y, Dodd S, Strobl J, Boland A, Dickson R, Walley T: Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia: a systematic review and meta-analysis. Hum Psychopharmacol. 2004 Jul;19(5):305-22. [PubMed: 15252823]
    • 2 . Noguchi H, Kitazumi K, Mori M, Shiba T: Electroencephalographic properties of zaleplon, a non-benzodiazepine sedative/hypnotic, in rats. J Pharmacol Sci. 2004 Mar;94(3):246-51. [PubMed: 15037809]
    • 3 . Ramakrishnan K, Scheid DC: Treatment options for insomnia. Am Fam Physician. 2007 Aug 15;76(4):517-26. [PubMed: 17853625]
    • 4 . Barbera J, Shapiro C: Benefit-risk assessment of zaleplon in the treatment of insomnia. Drug Saf. 2005;28(4):301-18. [PubMed: 15783240]
    • 5 . Dooley M, Plosker GL: Zaleplon: a review of its use in the treatment of insomnia. Drugs. 2000 Aug;60(2):413-45. [PubMed: 10983740]
    • 6 . Holm KJ, Goa KL: Zolpidem: an update of its pharmacology, therapeutic efficacy and tolerability in the treatment of insomnia. Drugs. 2000 Apr;59(4):865-89. [PubMed: 10804040]
    • 7 . Patat A, Paty I, Hindmarch I: Pharmacodynamic profile of Zaleplon, a new non-benzodiazepine hypnotic agent. Hum Psychopharmacol. 2001 Jul;16(5):369-392. [PubMed: 12404558]

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