Class: Sedative and hypnotic
- Capsules 5 mg
- Capsules 10 mg
Interacts with the gamma-aminobutyric acid receptor complex.
Rapid absorption. T max is about 1 h. Absolute bioavailability is about 30% because it undergoes significant presystemic metabolism. High fat meals prolonged the absorption, delaying T max about 2 h and reducing C max about 35%.
Vd is about 1.4 L/kg. Protein binding is about 60%.
Extensively metabolized with about 1% of dose excreted unchanged in the urine. Primarily metabolized by aldehyde oxidase to form 5-oxo-zaleplon. Metabolized to a lesser extent by CYP-450 3A4. Metabolites converted to glucoronides and eliminated in the urine.
T ½ is about 1 h. It is rapidly eliminated. Oral dose plasma Cl is about 3 L/h/kg. IV dose plasma Cl is about 1 L/h/kg. 70% of dose recovered in urine within 48 h.
Special PopulationsRenal Function Impairment
No dose adjustment in mild to moderate renal insufficiency. It has not been studied in severe renal insufficiency.Hepatic Function Impairment
Primarily metabolized by the liver and undergoes presystemic metabolism. Oral Cl was reduced 70% and 87% in compensated and decompensated patients, respectively. Reduce dose in mild to moderate hepatic function impairment. Do not use in severe hepatic insufficiency.Race
C max and AUC were increased 37% and 64%, respectively in Asian populations.
Indications and Usage
Short-term treatment of insomnia.
Dosage and AdministrationAdults
PO 5 to 20 mg at bedtime.Elderly/Debilitated Patients
PO 5 to 10 mg at bedtime.Hepatic Function Impairment (Mild to Moderate)
PO 5 mg at bedtime.
Store at room temperature in tightly closed, light-resistant container out of the reach of children.
Drug InteractionsAlcohol, other CNS depressants
Additive or potentiation of CNS depressant effects.Cimetidine
May elevate zaleplon plasma levels, increasing the therapeutic and adverse effects.Rifampin
May reduce zaleplon plasma levels, reducing the effectiveness.
Laboratory Test Interactions
None well documented.
Depression; hypertonia; nervousness; abnormal thinking; headache; anxiety; amnesia; dizziness; depersonalization; hallucinations; hypesthesia; paresthesia; somnolence; tremor; vertigo.
Pruritus; rash; photosensitivity.
Conjunctivitis; abnormal vision; ear pain; eye pain; hyperacusis; parosmia.
Constipation; dry mouth; anorexia; colitis; dyspepsia; nausea.
Back pain; chest pain; arthritis; abdominal pain; asthenia; fever; malaise; peripheral edema.
Category C .
Excreted in breast milk.
Safety and efficacy not established.
Impaired motor or cognitive function with repeated exposure or unusual sensitivity is a concern.
Use with caution and in reduced dosage.
Administer with caution to depressed patients or those with suicidal tendencies. Signs and symptoms of depression may be intensified.
Rebound insomnia on the first night following withdrawal occurs in some patients.
Drowsiness, mental confusion, lethargy, ataxia, hypotonia, hypotension, respiratory depression, coma, death.
- Instruct patient to take the medication exactly as directed. Do not increase or decrease the dose or use longer than as directed by health care provider.
- Instruct patient to take zaleplon immediately before going to bed or after going to bed if patient has difficulty falling asleep. Avoid taking medication after a high-fat or heavy meal.
- Instruct patient not to take zaleplon if able to get at least 4 h of sleep before active again and only for a short period of time (1 or 2 days and generally less than 1 or 2 wk) to avoid the problems of prolonged use.
- Discuss with primary caregiver and patient the benefits and risks of prolonged use including: memory problems, tolerance, dependence, changes in behavior and thinking, and withdrawal symptoms.
- Warn patient of the dangers of drinking alcohol and taking zaleplon or any other sleeping pill or CNS depressant.
- Caution patient that zaleplon may have some residual sedation at first and to not drive an automobile, operate dangerous machinery, or engage in activities that require mental alertness and coordination until knowing how the patient will react to this drug.
- Instruct patient to inform health care provider if experiencing any unusual or disturbing thoughts or if signs of depression occur.
- Inform patient of potential sleeping problems the first few nights after stopping the medication.
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