zaleplon

zaleplon /zal·e·plon/ (zal´ĕ-plon) a nonbenzodiazepine sedative and hypnotic used in the short term treatment of insomnia.

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zaleplon,

a sedative/hypnotic.

indication This drug is used to treat insomnia.

contraindication Known hypersensitivity to this drug prohibits its use.

adverse effects Adverse effects of this drug include dizziness, confusion, anxiety, amnesia, depersonalization, hallucinations, hypesthesia, paresthesia, somnolence, tremor, vertigo, nausea, abdominal pain, constipation, anorexia, colitis, dyspepsia, dry mouth, vision changes, ear/eye pain, hyperacusis, parosmia, asthenia, fever, headache, myalgia, and dysmenorrhea. Common side effects include lethargy, drowsiness, and daytime sedation. It should not be used longer than 2 to 3 weeks or with alcohol. Its effectiveness is decreased when taken with a high-fat meal.

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zaleplon [zal´ĕ-plon]

a nonbenzodiazepine sedative and hypnotic used in the short term treatment of insomnia; administered orally.

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zaleplon

Sonata

Pharmacologic class: Pyrazolopyrimidine, nonbenzodiazepine hypnotic

Therapeutic class: Sedative-hypnotic

Controlled substance schedule IV

Pregnancy risk category C

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.

Route	Onset	Peak	Duration
P.O.	Rapid	1 hr	3-4 hr

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

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zaleplon

Sonata^®, see there