Zaleplon

Pronunciation

(ZAL e plon)

U.S. Brand Names

Sonata®

Generic Available

Canadian Brand Names

Sonata®; Starnoc®

Use

Short-term (7-10 days) treatment of insomnia (has been demonstrated to be effective for up to 5 weeks in controlled trial)

Restrictions

C-IV

Pregnancy Risk Factor

Pregnancy Implications

Not recommended for use during pregnancy

Lactation

Enters breast milk/not recommended

Contraindications

Hypersensitivity to zaleplon or any component of the formulation

Warnings/Precautions

Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illness.

Use with caution in patients with depression, particularly if suicidal risk may be present. Use with caution in patients with a history of drug dependence. Abrupt discontinuance may lead to withdrawal symptoms. May impair physical and mental capabilities. Patients must be cautioned about performing tasks which require mental alertness (operating machinery or driving). Use with caution in patients receiving other CNS depressants or psychoactive medications. Effects with other sedative drugs or ethanol may be potentiated.

Use with caution in the elderly, those with compromised respiratory function, or renal and hepatic impairment. Because of the rapid onset of action, zaleplon should be administered immediately prior to bedtime or after the patient has gone to bed and is having difficulty falling asleep. Capsules contain tartrazine (FDC yellow #5); avoid in patients with sensitivity (caution in patients with asthma).

Adverse Reactions

1% to 10%:

Cardiovascular: Peripheral edema, chest pain

Central nervous system: Amnesia, anxiety, depersonalization, dizziness, hallucinations, hypesthesia, somnolence, vertigo, malaise, depression, lightheadedness, impaired coordination, fever, migraine

Dermatologic: Photosensitivity reaction, rash, pruritus

Gastrointestinal: Abdominal pain, anorexia, colitis, dyspepsia, nausea, constipation, xerostomia

Genitourinary: Dysmenorrhea

Neuromuscular & skeletal: Paresthesia, tremor, myalgia, weakness, back pain, arthralgia

Ocular: Abnormal vision, eye pain

Otic: Hyperacusis

Miscellaneous: Parosmia

<1% (Limited to important or life-threatening): Alopecia, angina, ataxia, bundle branch block, circumoral paresthesia, dysarthria, dystonia, eosinophilia, facial paralysis, glaucoma, intestinal obstruction, pericardial effusion, ptosis, pulmonary embolus, syncope, urinary retention, ventricular tachycardia

Overdosage/Toxicology

Symptoms include CNS depression, ranging from drowsiness to coma. Mild overdose is associated with drowsiness, confusion, and lethargy. Serious case may result in ataxia, respiratory depression, hypotension, hypotonia, coma, and rarely death. Treatment is supportive.

Drug Interactions

Substrate of CYP3A4 (minor)

Antipsychotics: Zaleplon potentiates the CNS effects of thioridazine (and potentially other antipsychotics)

Cimetidine: May increase zaleplon levels by decreasing its metabolism; cimetidine inhibits both aldehyde oxidase and CYP3A4 leading to an 85% increase in Cmax and AUC of zaleplon; use 5 mg zaleplon as starting dose in patients receiving cimetidine

CNS depressants: Sedative effects may be additive with psychotropics; monitor for increased effect; includes anticonvulsants, antipsychotics, barbiturates, benzodiazepines, narcotic analgesics, ethanol, and other sedative agents

Tricyclic antidepressants: Zaleplon potentiates the CNS effects of imipramine (and potentially other TCAs)

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase CNS depression).

Food: High fat meal prolonged absorption; delayed tmax by 2 hours, and reduced Cmax by 35%.

Herb/Nutraceutical: St John's wort may decrease zaleplon levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).

Stability

Store at controlled room temperature of 20°C to 25°C (68°F to 77°F); protect from light

Mechanism of Action

Zaleplon is unrelated to benzodiazepines, barbiturates, or other hypnotics. However, it interacts with the benzodiazepine GABA receptor complex. Nonclinical studies have shown that it binds selectively to the brain omega-1 receptor situated on the alpha subunit of the GABA-A receptor complex.

Pharmacodynamics/Kinetics

Onset of action: Rapid

Peak effect: ~1 hour

Duration: 6-8 hours

Absorption: Rapid and almost complete

Distribution: Vd: 1.4 L/kg

Protein binding: 60% ± 15%

Metabolism: Extensive, primarily via aldehyde oxidase to form 5-oxo-zaleplon and to a lesser extent by CYP3A4 to desethylzaleplon; all metabolites are pharmacologically inactive

Bioavailability: 30%

Half-life elimination: 1 hour

Time to peak, serum: 1 hour

Excretion: Urine (primarily metabolites, <1% as unchanged drug)

Clearance: Plasma: Oral: 3 L/hour/kg

Dosage

Oral:

Adults: 10 mg at bedtime (range: 5-20 mg); has been used for up to 5 weeks of treatment in controlled trial setting

Elderly: 5 mg at bedtime

Dosage adjustment in renal impairment: No adjustment for mild to moderate renal impairment; use in severe renal impairment has not been adequately studied

Dosage adjustment in hepatic impairment: Mild to moderate impairment: 5 mg; not recommended for use in patients with severe hepatic impairment

Administration

Immediately before bedtime or when the patient is in bed and cannot fall asleep

Patient Education

Take exactly as directed; immediately before bedtime, or when you cannot fall asleep. Do not alter dosage or frequency, may be habit forming. Avoid alcohol and other prescription or OTC medications (especially medications to relieve pain, induce sleep, reduce anxiety, treat or prevent cold, coughs, or allergies) unless approved by prescriber. You may experience drowsiness, dizziness, somnolence, vertigo, lightheadedness, blurred vision (avoid driving or engaging in activities that require alertness until response to drug is known); photosensitivity (avoid exposure to direct sunlight, wear protective clothing, and sunscreen); nausea or GI discomfort (small, frequent meals, good mouth care, chewing gum, or sucking hard candy may help); constipation (increase exercise, fluids, fruit, or fiber may help); or menstrual disturbances (reversible when drug is discontinued). Discontinue drug and report any severe CNS disturbances (hallucinations, acute nervousness or anxiety, persistent sleepiness or lethargy, impaired coordination, amnesia, or impaired thought processes); skin rash or irritation; eye pain or major vision changes; respiratory difficulty; chest pain; ear pain; or muscle weakness or pain. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Breast-feeding is not recommended.

Additional Information

Prescription quantities should not exceed a 1-month supply.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Dosage Forms

Capsule: 5 mg, 10 mg [contains tartrazine]

International Brand Names

Hegon® (AR); Sonata® (AT, BE, BR, CA, CH, CR, CZ, DE, DK, ES, FI, GB, GT, HN, HU, IE, IT, NL, PA, PL, SE, SV); Starnoc® (CA); Zalep® (HN, SV); Zaplon® (IN); Zelepion® (GB); Zerene® (IT)

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