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Zaleplon information from DrugsUpdate  

See Available Brands of Zaleplon in India

P - Caution when used during pregnancy
L - Contraindicated in Lactation

Zaleplon (marketed under the brand names Sonata and Starnoc) is a sedative/hypnotic, mainly used for insomnia. It is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class. In terms of adverse effects zaleplon appears to offer little improvement compared to both benzodiazepines and other non-benzodiazepine Z-drugs.

Pharmacodynamics

Pharmacokinetics

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.

Zaleplon Indications / Zaleplon Uses

Information Not Available

Zaleplon Adverse Reactions / Zaleplon 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).

Precautions

General
Timing of Drug Administration
Zaleplon should be taken immediately before bedtime or after the patient has gone to bed and has experienced difficulty falling asleep. As with all sedative/hypnotics, taking Zaleplon while still up and about may result in short-term memory impairment, hallucinations, impaired coordination, dizziness, and lightheadedness.

Use in the Elderly and/or Debilitated Patients
Impaired motor and/or cognitive performance after repeated exposure or unusual sensitivity to sedative/hypnotic drugs is a concern in the treatment of elderly and/or debilitated patients. A dose of 5 mg is recommended for elderly patients to decrease the possibility of side effects Elderly and/or debilitated patients should be monitored closely.

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.

Other 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.

Other Interactions

Information Not Available

Dosage

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 on cimetidine should receive initial dose of 5 mg at bedtime.

Food(before/after)

May be taken with or without food. (Do not take w/ or immediately after a heavy or high fat meal.)

List of Contraindications

Zaleplon and Pregnancy

Caution when used during pregnancy.

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Zaleplon and Lactation

Contraindicated in lactation

Zaleplon and Children

Safety and efficacy not established

Zaleplon and Geriatic

Impaired motor or cognitive function with repeated exposure or unusual sensitivity is a concern.

Zaleplon and Other Contraindications

Hypersensitivity. Severe hepatic impairment. Lactation

Storage

Oral
Store at 20-25°C (68-77°F).

Lab interference

Oral
Store at 20-25°C (68-77°F).

Zaleplon brands in India:

Stilnite Zalep Zalpilo Zanlop Zaplon Zaso

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