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Zaleplon-sedative, also called a hypnotic.

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Zaleplon-sedative, also called a hypnotic.

Zaleplon is a sedative, also called a hypnotic. It affects chemicals in your brain that may become unbalanced and cause sleep problems (insomnia). Zaleplon is used to treat insomnia. This medication causes relaxation to help you fall asleep and stay asleep. More

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Description

Zaleplon is a sedative, also called a hypnotic. It affects chemicals in your brain that may become unbalanced and cause sleep problems (insomnia). Zaleplon is used to treat insomnia. This medication causes relaxation to help you fall asleep and stay asleep.

Generic Name

Zaleplon-sedative, also called a hypnotic.

Chemical names

Zaleplon; Sonata; Zerene; 151319-34-5; CL-284846

Brand names

Stilnite, Zalep, Zalpilo, Zanlop, Zaplon, Zaso

IUPAC name

N-(3-{3-cyanopyrazolo[1,5-a]pyrimidin-7-yl}phenyl)-N-ethylacetamide

Pharmacokinetics

30% bioavailability, distributed into breast milk.

Actions

Zaleplon exerts its action through subunit modulation of the GABABZ receptor chloride channel macromolecular complex. This drug also selectively binds to the brain omega-1 receptor located on the alpha subunit of the GABA-A/chloride ion channel receptor complex and potentiates t-butyl-bicyclophosphorothionate (TBPS) binding.

Dosage/Dosage form

10 mg before bedtime. Maximum dose is 20 mg daily.

Therapeutic uses

Treatment of insomnia

Adverse effects/Side effects

Headache, light headedness, asthenia, dizziness, nausea, somnolence, rash, myalgia, back pain, chest pain, taste perversion, fever, migraine, constipation, dry mouth, dyspepsia, arthralgia, anxiety, depression, difficulty concentrating, amnesia, confusion, hallucinations. Transient impairment of memory and psychomotor function. Decreased inhibition, behavioural changes (e.g. bizarre behaviour, depersonalisation), complex sleep related behaviour (e.g. sleep driving).

Interaction

  • Additive CNS effects may occur with CNS depressants e.g. TCA, alcohol, antihistamines, narcotic analgesics, thioridazine and diphenhydramine.
  • Cytochrome P450 CYP3A4 inducers e.g. rifampicin, phenytoin, carbamazepine and phenobarbital decrease zaleplon concentrations.
  • Increased zaleplon concentration with cimetidine and CYP 3A4 inhibitors e.g. erythromycin, ketoconazole.

Contraindications

  • Hypersensitivity.
  • Severe hepatic impairment.
  •  Lactation

Storage

Store at 20-25°C (68-77°F).

Information

Molecular weight

305.3339

Molecular formula

C17H15N5O

CAS number

151319-34-5

Precautions

  • May precipitate new psychiatric abnormalities. Depression; hepatic impairment.
  •  History of alcohol or drug dependence or abuse patients.
  • Children <18 yr.
  • Pregnancy.
  • May impair ability to drive or operate machinery.
  • Dose withdrawal or reduction of drug should be done gradually.
  • Do not take zaleplon if there is <4 hr of sleep. 

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