Zaleplon


Concise Prescribing Info
Indications/Uses
Insomnia.
Dosage/Direction for Use
Adult : PO 10 mg/day at bedtime. Max: 20 mg/day.
Dosage Details
Oral
Insomnia
Adult: 10 mg before bedtime. Max: 20 mg daily.
Elderly: >65 yr: 5 mg before bedtime. Max: 10 mg daily.
Special Patient Group
Patients on cimetidine should receive initial dose of 5 mg at bedtime.
Renal Impairment
Severe: No studies done.
Hepatic Impairment
Mild to moderate: 5 mg at bedtime. Severe: Contra-indicated.
Administration
May be taken with or without food. Do not take w/ or immediately after a heavy or high fat meal.
Contraindications
Hypersensitivity. Severe hepatic impairment. Lactation.
Special 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).
Overdosage
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.
Action
Description: 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.
Pharmacokinetics:
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.
Storage
Store at 20-25°C (68-77°F).
Disclaimer: This information is independently developed by MIMS based on Zaleplon from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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