Zaleplone

Indications

Zaleplone is used for: Insomnia

Adult Dose

Oral Insomnia Adult: 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.

Child Dose

Not recommended

Renal Dose

Renal Impairment Mild to moderate impairmet: No dose adjustment necessary Severe impairment: Not studied

Administration

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

Contra Indications

Hypersensitivity. Severe hepatic impairment. Lactation.

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.

Pregnancy-Lactation

Pregnancy Category: C Lactation: small amount secreted in breast milk, not recommended

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.

Adverse Effects

Side effects of Zaleplone : >10% Headache (38%) 1-10% Dizziness (7-9%), Nausea (6-8%), Abdominal pain (6%), Weakness (5-7%), Dysmenorrhea (3-4%), Eye pain (3-4%), Amnesia (2-4%), Parasthesia (3%), Tremor (2%) <1% Fever, Photosensitivity, Anorexia, Colitis, Periphipheral edema, Amnesia, Anxiety, Depersonalization, Hallucination, Hypesthesia, Vertigo, Epistaxis, Abnl vision, Ear pain, Hyperacusis, Parosmia

Mechanism of Action

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.