Generic
Zaleplon
2 brands available in the market
At a glance
Zaleplon is indicated for the short-term treatment of insomnia. Zaleplon has been shown to decrease the time to sleep onset for up to 30 days in controlled clinical trials.
Description
Zaleplon is a newer non-benzodiazepine hypnotic from the pyrazolopyrimidine class. So, its chemical structure is unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties.
Indications
- Insomnia (short-term treatment)
Therapeutic class
Benzodiazepine hypnotics
Pharmacological class
Non-benzodiazepine Hypnotic
Pharmacology
Zaleplon is a newer non-benzodiazepine hypnotic from the pyrazolopyrimidine class. It interacts with the gamma aminobutyric acid-benzodiazepine (GABA-BZ) receptor complex.
Mechanism of action
Binds to the GABA-A receptor complex, relaxing the nerves and brain to help with sleep onset.
Dosage
Adult Dose (Oral):
- Most non-elderly adults: 10 mg immediately before bedtime
- For certain low weight individuals, 5 mg may be sufficient
- 20 mg dose has been shown to be adequately tolerated and may be considered
- Dosage above 20 mg has not been adequately evaluated and is not recommended
- Elderly: 5 mg; doses over 10 mg are not recommended
- Patients taking Cimetidine: initial dose of 5 mg
Renal Impairment: Mild to moderate: no dose adjustment necessary
Administration
- Take immediately before bedtime
- Taking with or immediately after a heavy, high-fat meal results in slower absorption
Missed dose
If you miss a dose, skip it and continue with your normal schedule; do not double the dose.
Side effects
Common Side Effects:
- Diarrhoea
- Nausea
- Vomiting
- Vertigo
- Headache
- Asthenia
- Nightmare
Precautions & warnings
- Use with caution in elderly and/or debilitated patients
- Caution in patients with compromised respiratory function
- Dose should be reduced to 5 mg in patients with mild to moderate hepatic impairment; not recommended in severe hepatic impairment
- Administer with caution to patients exhibiting signs or symptoms of depression
Contraindications
- Known hypersensitivity to any of its components
Drug interactions
- Minimal effects on the kinetics of Warfarin, Imipramine, Ethanol, Ibuprofen, Diphenhydramine, Thioridazine, and Digoxin
- CNS depressants: additive CNS effects may occur
- CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital): decrease zaleplon concentrations
- Cimetidine and CYP3A4 inhibitors (erythromycin, ketoconazole): increased zaleplon concentration
Food interactions
Food interactions are not significant.
Use in pregnancy
Use in Pregnancy: No studies in pregnant women; not recommended for use during pregnancy.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: A small amount is excreted in breast milk; not recommended in nursing mothers.
Pediatric use
Safety and effectiveness not established in pediatric patients
Geriatric use
A dose of 5 mg is recommended for elderly patients; monitor closely
Renal / hepatic impairment
Renal Impairment: Mild to moderate: no dose adjustment necessary; severe: not adequately studied
Hepatic Impairment: Mild to moderate: 5 mg; severe: not recommended
Overdose effects
Symptoms: Limited information.
Treatment: Supportive care.
Storage conditions
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.