Hypnotic, Nonbenzodiazepine

Short-term treatment of insomnia

C

Known hypersensitivity to zaleplon or any component

Symptomatic treatment of insomnia should be initiated only after careful evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric and/or medical illness.

use with caution in the elderly, those with compromised respiratory function, or renal and hepatic impairment. Because of the rapid onset of action, zaleplon should be administered immediately prior to bedtime or after the patient has gone to bed and is having difficulty falling asleep.

1% to 10%:

Cardiovascular: Peripheral edema

Dermatologic: Photosensitivity reaction, rash, pruritus

Gastrointestinal: Abdominal pain, anorexia, colitis, dyspepsia, nausea, constipation, xerostomia

Genitourinary: Dysmenorrhea

Neuromuscular & skeletal: Paresthesia, tremor, myalgia, weakness

Ocular: Abnormal vision, eye pain

Otic: Hyperacusis

Miscellaneous: Parosmia

Symptoms include CNS depression, ranging from drowsiness to coma. Mild overdose is associated with drowsiness, confusion, and lethargy. Serious case may result in ataxia, respiratory depression, hypotension, hypotonia, coma, and rarely death. Treatment is supportive.

CYP3A4 substrate (minor metabolic pathway)

CYP3A4 inducers (eg, phenytoin, carbamazepine, phenobarbital) could lead to ineffectiveness of zaleplon (rifampin decreased AUC 80%); consider an alternative hypnotic

Cimetidine inhibits both aldehyde oxidase and CYP3A4 leading to an 85% increase in C_max and AUC of zaleplon. Use 5 mg zaleplon as starting dose in patient receiving cimetidine.

Zaleplon is unrelated to benzodiazepines, barbiturates, or other hypnotics. However, it interacts with the benzodiazepine GABA receptor complex. Nonclinical studies have shown that it binds selectively to the brain omega-1 receptor situated on the alpha subunit of the GABA-A receptor complex.

Onset: Rapid

Peak effect: Within 1 hour

Duration: 6-8 hours

Absorption: Rapid and almost complete

Distribution: V_d: 1.4 L/kg

Protein binding: 60% ± 15%

Metabolism: Extensively metabolized with <1% of dose excreted unchanged in urine. Primarily metabolized by aldehyde oxidase to form 5-oxo-zaleplon and to a lesser extent by CYP3A4 to desethylzaleplon. All metabolites are pharmacologically inactive. Oral dose plasma clearance: 3 L/h/kg

Bioavailability: 30%

Half-life: 1 hour

Time to peak serum concentration: 1 hour

Elimination: In urine as metabolites

Adults: Oral: 10 mg at bedtime (range: 5-20 mg)

Elderly: 5 mg at bedtime

Dosage adjustment in renal impairment: No adjustment for mild to moderate renal impairment; use in severe renal impairment has not been adequately studied

Dosage adjustment in hepatic impairment: Mild to moderate impairment: 5 mg; not recommended for use in patients with severe hepatic impairment

High fat meal prolonged absorption; delayed t_max by 2 hours, and reduced C_max by 35%

Immediately before bedtime or when the patient is in bed and cannot fall asleep

No information available to require special precautions

No effects or complications reported

Use exactly as directed (do not increase dose or frequency or discontinue without consulting prescriber). Dose should be taken immediately before bedtime. May take with food to decrease GI upset (do not take with high fat foods). Avoid alcohol or other prescription or OTC medications (especially, pain medications, sedatives, antihistamines, or sleep medications) unless you consult prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, dizziness, lightheadedness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); or dry mouth or gastrointestinal discomfort (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, nightmares, persistent dizziness, memory impairment, impaired coordination); muscle pain or weakness or alterations in gait; swelling of extremities; skin rash; persistent GI distress (pain, nausea, constipation, sore mouth); vision changes; or ineffectiveness of medication. Pregnancy precautions: Inform prescriber if you are or intend to be pregnant.

Capsule: 5 mg, 10 mg

Prescription quantities should not exceed a 1-month supply