ZALEPLON

ZALEPLON
(zal'ep-lon)
Sonata
Classifications: anxiolytic; sedative-hypnotic; nonbenzodiazepine;
Therapeutic: sedative-hypnotic
; antianxiety
Prototype: Zolpidem
Pregnancy Category: C
Controlled Substance: Schedule IV

Availability

5 mg, 10 mg capsules

Action

Short-acting nonbenzodiazepine with sedative-hypnotic, muscle relaxant, and anticonvulsant activity.

Therapeutic Effect

Reduces difficulty in initially falling asleep. Preserves deep sleep (stage 3 through stage 4) at hypnotic dose with minimal-to-absent rebound insomnia when discontinued.

Uses

Short-term treatment of insomnia.

Contraindications

Hypersensitivity to zaleplon, or tartrazine dye (Yellow 5); suicidal ideation; pregnancy (category C); lactation. Safe use in children not established.

Cautious Use

Hypersensitivity to salicylates; concurrent use of other CNS depressants (e.g., benzodiazepines, alcohol); chronic depression; history of drug abuse; COPD; respiratory insufficiency; hepatic or renal impairment; pulmonary disease.

Route & Dosage

Insomnia
Adult: PO 10 mg h.s. (max: 20 mg h.s.)
Geriatric: PO 5 mg h.s. (max: 10 mg h.s.)

Administration

Oral
  • Give immediately before bedtime; not while patient is still ambulating.
  • Give lower dose of 5 mg to older adult or debilitated patients.
  • Store at 20°–25° C (68°–77° F).

Adverse Effects (≥1%)

Body as a Whole: Asthenia, fever, headache, migraine, myalgia, back pain. CNS: Amnesia, dizziness, paresthesia, somnolence, tremor, vertigo, depression, hypertonia, nervousness, difficulty concentrating. GI: Abdominal pain, dyspepsia, nausea, constipation, dry mouth. Respiratory: Bronchitis. Skin: Pruritus, rash. Special Senses: Eye pain, hyperacusis, conjunctivitis. Urogenital: Dysmenorrhea.

Interactions

Drug: Alcohol, imipramine, thioridazine may cause additive CNS impairment; rifampin increases metabolism of zaleplon; cimetidine increases serum levels of zaleplon. Herbal: Valerian, melatonin may produce additive sedative effects. Food: High-fat meals may delay absorption.

Pharmacokinetics

Absorption: Rapidly and completely absorbed, 30% reaches systemic circulation. Onset: 15–20 min. Peak: 1 h. Duration: 3–4 h. Distribution: 60% protein bound. Metabolism: Extensively in liver (CYP3A4) to inactive metabolites. Elimination: 70% in urine, 17% in feces. Half-Life: 1 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor behavior and notify physician for significant changes. Use extra caution with preexisting clinical depression.
  • Provide safe environment and monitor ambulation after drug is ingested.
  • Monitor respiratory status with preexisting compromised pulmonary function.

Patient & Family Education

  • Exercise caution when walking; avoid all hazardous activities after taking zaleplon.
  • Do not take in combination with alcohol or any other sleep medication.
  • Note: Exhibits altered effectiveness if taken with/immediately after high-fat meal.
  • Do not use longer than 2–3 wk.
  • Expect possible mild/brief rebound insomnia after discontinuing regimen.
  • Report use of OTC medications to physician (e.g., cimetidine).
  • Report pregnancy to physician immediately.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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