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