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Zaleplon

1. Medical Use and Effects: – Zaleplon treats insomnia by reducing time to fall asleep. – It may help with middle-of-the-night awakenings. – Zaleplon has […]

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1. Medical Use and Effects:
– Zaleplon treats insomnia by reducing time to fall asleep.
– It may help with middle-of-the-night awakenings.
– Zaleplon has minimal impact on driving performance.
– Zaleplon has fewer adverse effects compared to benzodiazepines.
– Zaleplon does not increase total sleep time.
– Elderly should avoid chronic use of zaleplon.
– Not recommended in pregnancy, lactation, or history of substance abuse.
– Efficacy and safety of long-term use need further study.
– Zaleplon has similar adverse effects to benzodiazepines but with less next-day sedation.
– Evidence suggests zaleplon is safe for use.

2. Pharmacology and Chemistry:
– Zaleplon enhances GABAergic inhibition in the CNS.
– Ultrashort half-life minimizes next-day effects.
– Zaleplon induces sleep without disrupting sleep architecture.
– Zaleplon is a pyrazolopyrimidine.
– Metabolized by aldehyde oxidase into inactive metabolites.
– Reaches peak concentration in about 45 minutes.
– EEG changes show zaleplon’s effect on brain activity.
– Few differences between zaleplon and benzodiazepines in clinical trials.

3. Interactions and Metabolism:
– CYP3A4 enzyme metabolizes 9% of zaleplon.
– CYP3A4 inducers can reduce zaleplon effectiveness.
– Additional sedation when combined with thioridazine.
– Diphenhydramine does not affect zaleplon pharmacokinetics.
– Consider other hypnotic drugs with CYP3A4 inducers.

4. Society, Culture, and Legal Aspects:
– Zaleplon has potential for recreational use.
– Can cause anterograde amnesia and addiction.
– FAA allows zaleplon with a 12-hour wait period for aviation use.
– US Air Force uses zaleplon as a no-go pill for aviators.
– Zaleplon has a short waiting period compared to other sleep medications.

5. Studies, Research, and Pharmacological Countermeasures:
– Clinical evaluation of zaleplon in the treatment of insomnia.
– Benefit-risk assessment of zaleplon in the treatment of insomnia.
– Mortality Risk of Hypnotics: Strengths and Limits of Evidence.
– Comparative efficacy of newer hypnotic drugs for the short-term management of insomnia.
– Fatigue in military aviation overview.
– US military-approved pharmacological countermeasures.

Zaleplon (Wikipedia)

Zaleplon, sold under the brand name Sonata among others, is a sedative and hypnotic which is used to treat insomnia. It is a nonbenzodiazepine or Z-drug of the pyrazolopyrimidine class. It was developed by King Pharmaceuticals and approved for medical use in the United States in 1999.

Zaleplon
Clinical data
Trade namesSonata, Starnoc, Andante, others
AHFS/Drugs.comMonograph
MedlinePlusa601251
Routes of
administration
By mouth
Drug classPyrazolopyrimidine
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability30% (oral)
MetabolismLiver aldehyde oxidase (91%), CYP3A4 (9%)
Elimination half-life1 hr
ExcretionKidney
Identifiers
  • N-(3-(3-cyanopyrazolo[1,5-a] pyrimidin-7-yl)phenyl)-N-ethylacetamide
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.126.674 Edit this at Wikidata
Chemical and physical data
FormulaC17H15N5O
Molar mass305.341 g·mol−1
3D model (JSmol)
  • CCN(C(C)=O)c1cccc(-c2ccnc3c(C#N)cnn23)c1
  • InChI=1S/C17H15N5O/c1-3-21(12(2)23)15-6-4-5-13(9-15)16-7-8-19-17-14(10-18)11-20-22(16)17/h4-9,11H,3H2,1-2H3 checkY
  • Key:HUNXMJYCHXQEGX-UHFFFAOYSA-N checkY
  (verify)
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