Generic
Zaleplone
4 brands available in the market
At a glance
Zaleplone is a prescription medicine used to treat insomnia. It reduces sleep onset time and frequent awakening at night. This medicine improves sleep maintenance and therefore ensures sound sleep.
Description
Zaleplone is a nonbenzodiazepine hypnotic. Along with sedative, it may also have anxiolytic (panic-reducing or antianxiety), muscle relaxant properties. It works by binding GABA-A/chloride ion channel receptor complex.
Indications
- Insomnia
Therapeutic class
Benzodiazepine hypnotics
Pharmacological class
Non-benzodiazepine Hypnotic
Pharmacology
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.
Mechanism of action
Binds to the GABA-A/chloride ion channel receptor complex, relaxing the nerves and brain to help with sleep.
Dosage
Adult Dose (Oral):
- Insomnia: 5-10 mg before bedtime; max 20 mg daily
- Elderly (>65 yr): 5 mg before bedtime; max 10 mg daily
- Hepatic impairment: Mild to moderate: 5 mg at bedtime; Severe: Contra-indicated
Renal Impairment: Mild to moderate: no dose adjustment necessary; severe: not studied
Administration
- Take on an empty stomach
- Do not chew, crush or break
- Take 30 to 45 minutes before bedtime and only when you have time to sleep for at least 7 hours
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:
- Dizziness
- Lightheadedness
- Impaired coordination
- Paresthesia (tingling or pricking sensation)
Precautions & warnings
- May affect ability to drive
- Best taken without food as a high-fat meal can reduce its absorption and effect
- Makes you feel dizzy next morning; do not drive or do anything requiring concentration
- Inform your doctor if your sleep doesn't improve after 7 to 10 days of treatment
- Do not stop taking medication suddenly as it may lead to anxiety, mood changes, and restlessness
Contraindications
- Hypersensitivity
- Severe hepatic impairment
- Lactation
Drug interactions
- CNS depressants (TCA, alcohol, antihistamines, narcotic analgesics, thioridazine, diphenhydramine): additive CNS effects
- CYP3A4 inducers (rifampicin, phenytoin, carbamazepine, phenobarbital): decrease zaleplon concentrations
- Cimetidine and CYP3A4 inhibitors (erythromycin, ketoconazole): increased zaleplon concentration
Food interactions
It is unsafe to consume alcohol with Zaleplone.
Use in pregnancy
Use in Pregnancy: May be unsafe; animal studies show harmful effects; consult your doctor.
Pregnancy Category: C — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited human data suggests no significant risk; consult your doctor.
Pediatric use
Not recommended for use in children
Geriatric use
A dose of 5 mg is recommended for elderly patients; monitor closely
Renal / hepatic impairment
Renal Impairment: Caution in severe kidney disease; dose adjustment may be needed; mild to moderate: no dose adjustment recommended
Hepatic Impairment: Caution needed; dose adjustment may be needed; not recommended in severe liver disease
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.