Description

Simple

A medication used to treat insomnia for the short term.

Clinical

A sedative used for short term treatment of insomnia in adults.

Overview

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 IV drug in the United States.

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 short-term treatment of insomnia. While Zaleplon is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts w... Read more

Mechanism of action

Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. Zaleplon also binds selectively to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicy... 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. After oral administration, zaleplon is extensively metabolized, with less than 1% of the dose excreted unchanged in urine. Renal excretion of unchanged zaleplon accounts for less than 1% of the administ... Read more

Toxicity

Side effects include abdominal pain, amnesia, dizziness, drowsiness, eye pain, headache, memory loss, menstrual pain, nausea, sleepiness, tingling, weakness

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of adverse effects can be increased when Zaleplon is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3-isobutyl-1-methyl-7H-xanthine
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.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of adverse effects can be increased when Zaleplon is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-Methoxyamphetamine
The risk or severity of adverse effects can be increased when Zaleplon is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of adverse effects can be increased when Zaleplon is combined with 5-methoxy-N,N-dimethyltryptamine.
6-O-benzylguanine
Zaleplon may increase the excretion rate of 6-O-benzylguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Deazaguanine
Zaleplon may increase the excretion rate of 7-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
7-Nitroindazole
The risk or severity of adverse effects can be increased when Zaleplon is combined with 7-Nitroindazole.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of adverse effects can be increased when Zaleplon is combined with 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline.
7,9-Dimethylguanine
Zaleplon may increase the excretion rate of 7,9-Dimethylguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-azaguanine
Zaleplon may increase the excretion rate of 8-azaguanine which could result in a lower serum level and potentially a reduction in efficacy.
8-chlorotheophylline
Zaleplon may increase the excretion rate of 8-chlorotheophylline which could result in a lower serum level and potentially a reduction in efficacy.
9-Deazaguanine
Zaleplon may increase the excretion rate of 9-Deazaguanine which could result in a lower serum level and potentially a reduction in efficacy.
9-Methylguanine
Zaleplon may increase the excretion rate of 9-Methylguanine which could result in a lower serum level and potentially a reduction in efficacy.
Abacavir
Zaleplon may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Zaleplon can be increased when combined with Abatacept.
Acalabrutinib
The metabolism of Zaleplon can be decreased when combined with Acalabrutinib.
Acarbose
Acarbose may decrease the excretion rate of Zaleplon which could result in a higher serum level.
Aceclofenac
Aceclofenac may decrease the excretion rate of Zaleplon which could result in a higher serum level.
Acefylline
Zaleplon may increase the excretion rate of Acefylline which could result in a lower serum level and potentially a reduction in efficacy.
7 References
  1. 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. 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. 3 . Ramakrishnan K, Scheid DC: Treatment options for insomnia. Am Fam Physician. 2007 Aug 15;76(4):517-26.PubMed: 17853625
  4. 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. 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. 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. 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