Trade Names:Sonata- Capsules 5 mg- Capsules 10 mgSotacor (Canada)
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.
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.
Short-term treatment of insomnia.
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.
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.
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.
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