Names and pronunciation
(zal′eh-plon)
PDF page 1392
Loading InternPractice…
Drug reference
(zal′eh-plon)
PDF page 1392
Func. class.: Hypnotic, nonbarbiturate
PDF page 1392
Chem. class.: Pyrazolopyrimidine Controlled Substance Schedule IV
PDF page 1392
Do not confuse: Zaleplon/Zelapron/Zemplar/Zolpidem
PDF page 1392
ACTION: Binds selectively to omega-1 receptor of the GABAA receptor complex; results are sedation, hypnosis, skeletal muscle relaxation, anticonvulsant activity, anxiolytic action
PDF page 1392
USES: Insomnia (short-term treatment)
PDF page 1392
CONTRAINDICATIONS: Hyper sensitivity, severe hepatic disease
PDF page 1392
Black Box Warning: Complex sleep- related behaviors Precautions: Pregnancy, breastfeeding, children <15 yr, geriatric patients, respira tory/renal/hepatic disease, psychosis, angio edema, depression, sleep-related behaviors (sleep walking), Asian descent, CNS depression, suicidal ideation, sleep apnea; salicylate, tartrazine dye, hypersensitivity Black Box Warning: Complex sleep- related behaviors: Assess for previous complex sleep-related behaviors, and do not use with these patients, sleep eating, driving, walking, all while not fully awake • Beers: avoid in older adults with de lirium or at high risk for delirium; poten tial for worsening or inducing delirium Black Box Warning: That product may cause memory problems, dependence (if used for longer periods of time), changes in behavior/thinking, complex sleep- related behaviors (sleep eating/driving) • That product is for short-term use only and when patient can sleep ≥4 hr • To take immediately before going to bed • Not to ingest a high-fat/heavy meal be fore taking • To be aware that allergic reactions may occur • Pregnancy/breastfeeding: Identify if pregnancy is planned or suspected or if breastfeeding
PDF pages 1392, 1393
SIDE EFFECTS CNS: Lethargy, drowsiness, daytime sedation, dizziness, confusion, anxiety, amnesia, depersonalization, hallucinations, hyperesthesia, paresthesia, somnolence, tremors, vertigo, complex sleep-related reactions: sleep driving, sleep eating CV: Chest pain, peripheral edema EENT: Vision change, ear/eye pain, hyperacusis, parosmia GI: Nausea, abdominal pain, constipation, anorexia, colitis, dyspepsia, dry mouth MISC: Asthenia, fever, headache, myal gia, dysmenorrhea MS: Myalgia, back pain, arthritis RESP: Bronchitis SYST: Severe allergic reactions
PDF page 1392
INTERACTIONS Increase: effect of zaleplon—cimetidine Decrease: zaleplon bioavailability— CYP3A4 inducers Increase: CNS depression—CNS depressants Increase: respiratory depression, death— opioids Drug/Food • Prolonged absorption, sleep onset re duced: high-fat/heavy meal Drug/Lab Increase: lipids
PDF page 1392
DOSAGE AND ROUTES • Adult: PO 10 mg at bedtime; may in crease to 20 mg if needed; 5 mg may be used in low-weight persons, use for only 7-10 days • Geriatric/hepatic dose: PO 5 mg at bedtime; may increase if needed
PDF page 1392
Available forms: Caps 5, 10 mg
PDF page 1392
Administer: • Immediately before bedtime for sleep lessness • On empty stomach for fast onset • Store in tight container in cool envi ronment
PDF page 1392
Assess: • Mental status: mood, sensorium, af fect, memory (long, short term), exces sive sedation, impaired coordination • Sleep disorder: type of sleep problem: falling asleep, staying asleep
PDF page 1392
Evaluate: • Therapeutic response: ability to sleep at night, decreased amount of early morning awakening
PDF page 1393
CLINICAL CONSIDERATIONS
PDF page 1392
Patient and caregiver information: • To avoid driving or other activities re quiring alertness until product is stabilized • To avoid alcohol ingestion, advise pre scriber of all other OTC/Rx/herbals taken
PDF page 1393
PHARMACOKINETICS Rapid onset, metabolized by liver exten sively, excreted by kidneys (inactive metabolites), half-life 1 hr, onset, peak 1 hr, duration 3-4 hr
PDF page 1392
• Adult: PO 10 mg at bedtime; may in crease to 20 mg if needed; 5 mg may be used in low-weight persons, use for only 7-10 days
PDF page 1392
• Geriatric/hepatic dose: PO 5 mg at bedtime; may increase if needed
PDF page 1392