Action

Binds to omega-1 receptor of gamma-aminobutyric acid receptor complex, relaxing smooth muscles, reducing anxiety, and producing sedation. Also has anticonvulsant effect.

Availability

Capsules: 5 mg, 10 mg

Indications and dosages

➣ Insomnia

Adults younger than age 65: 10 mg P.O. at bedtime. Dosage above 20 mg is not recommended.

Dosage adjustment

• Mild to moderate hepatic impairment

• Elderly or debilitated patients

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:

• tartrazine sensitivity

• severe renal impairment (use not recommended), mild to moderate hepatic impairment, respiratory impairment, depression

• history of suicide attempt

• patients weighing less than 50 kg (110 lb)

• patients older than age 65

• pregnant or breastfeeding patients (use not recommended)

• children younger than age 18 (safety not established).

Administration

• Give at bedtime.

• Don't administer with high-fat meal.

Adverse reactions

CNS: headache, amnesia, anxiety, hallucinations, light-headedness, dizziness, drowsiness, depersonalization, transient memory or psychomotor impairment, incoordination, malaise, vertigo, asthenia, hyperesthesia, paresthesia, tremor

CV: peripheral edema

EENT: abnormal vision, eye pain, ear pain, hearing sensitivity, epistaxis

GI: nausea, abdominal pain, colitis, dyspepsia, anorexia

GU: dysmenorrhea

Musculoskeletal: myalgia

Skin: photosensitivity

Other: altered sense of smell, fever

Interactions

Drug-drug. Cimetidine: decreased metabolism and increased effects of zaleplon

CNS depressants (including antihistamines, opioids, other sedative-hypnotics, phenothiazines, tricyclic antidepressants): additive CNS depression

CYP450-3A4 inducers (such as carbamazepine, phenobarbital, phenytoin, rifampin): decreased blood level and reduced efficacy of zaleplon

CYP450-3A4 inhibitors (such as erythromycin, ketoconazole): increased zaleplon blood level

Drug-food. High-fat meal: delayed drug absorption

Drug-herbs. Chamomile, hops, kava, skullcap, valerian: increased CNS depression

Drug-behaviors. Alcohol use: increased CNS depression

Patient monitoring

• Monitor drug efficacy. Insomnia persisting after 7 to 10 days warrants reevaluation for underlying psychological or physical illness.

• Stay alert for adverse drug reactions.

Patient teaching

• Explain therapy to patient. Emphasize importance of taking drug just before bedtime or after trying to sleep-but only if he will be able to get at least 4 hours of sleep.

• Inform patient that high-fat meal slows drug absorption and delays drug effects.

• Caution patient to avoid driving and other hazardous activities while under drug's influence.

• Instruct patient to avoid alcohol during therapy.

• Tell patient rebound insomnia may occur for 1 or 2 nights after he stops taking drug.

• Advise female of childbearing age to notify prescriber if she is or plans to become pregnant or if she is breastfeeding.

• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, herbs, and behaviors mentioned above.