Zaleplon

Indications
 Oral
Insomnia
Adult: 10 mg before bedtime. Max: 20 mg daily.
Elderly: >65 yr: 5 mg before bedtime. Max: 10 mg daily.
Renal impairment: Severe: No studies done.
Hepatic impairment: Mild to moderate: 5 mg at bedtime. Severe: Contra-indicated.

Special Populations: Patients with mild to moderate hepatic impairment, or those receiving cimetidine concomitantly, should receive reduced dose of 5 mg.
Contraindications
 Hypersensitivity. Severe hepatic impairment. Lactation.
Warnings / Precautions
 May precipitate new psychiatric abnormalities. Depression; hepatic impairment. History of drug or alcohol dependence or abuse, elderly and debilitated patients. Childn <18 yr. Pregnancy. May impair ability to drive or operate machinery. Do not take zaleplon if there is <4 hr of sleep. Dose reduction or withdrawal of drug should be done gradually.
Adverse Reactions
 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).
Overdose Reactions
 Symptoms: Drowsiness, mental confusion, lethargy, ataxia, hypotonia, hypotension, respiratory depression, coma, and very rarely death. Management: Treatment is symptomatic and supportive. Gastric lavage may be performed to reduce absorption and IV fluids admin as needed.
Drug Interactions
 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.
See Below for More zaleplon Drug Interactions
Mechanism of Actions
 Zaleplon, a pyrazolopyrimidine, is a sedative and hypnotic agent structurally unrelated to the benzodiazepines and other sedative-hypnotic agents. It is shown to interact with GABA subtype A complex by binding selectively to benzodiazepine type 1 receptor. It reduces sleep latency without affecting sleep duration.
Absorption: Rapidly and completely absorbed. Peak plasma concentrations: 1 hr. Absorption reduced by heavy meal or high-fat diet. Bioavailability: 30%.
Distribution: Distributed into breast milk.
Metabolism: Undergo significant first-pass hepatic metabolism. Metabolised mainly by aldehyde oxidase and some by the cytochrome P450 isoenzyme CYP3A4. Plasma-elimination half-life: 1 hour.
Excretion: Excreted mainly in urine as inactive metabolites or their glucuronides (70%); <1% excreted unchanged. 17% of a dose excreted in the faeces, mainly as metabolites.
Administration
 May be taken with or without food. (Do not take w/ or immediately after a heavy or high fat meal.)
Storage Conditions
 Oral: Store at 20-25°C (68-77°F).
ATC Classification
 N05CF03 - zaleplon ; Belongs to the class of benzodiazepine related agents. Used as hypnotics and sedatives.
Storage
 Oral: Store at 20-25°C (68-77°F).
Available As
  • Zaleplon 10 mg
  • Zaleplon 5 mg

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