No

Hypnotic, Nonbenzodiazepine

Short-term treatment of insomnia

C-IV

B

Known hypersensitivity to zolpidem

Should be used only after evaluation of potential causes of sleep disturbance. Failure of sleep disturbance to resolve after 7-10 days may indicate psychiatric or medical illness. Use with caution in patients with depression. Behavioral changes have been associated with sedative-hypnotics. Causes CNS depression, which may impair physical and mental capabilities. Effects with other sedative drugs or ethanol may be potentiated. Closely monitor elderly or debilitated patients for impaired cognitive or motor performance; not recommended for use in children <18 years of age. Avoid use in patients with sleep apnea or a history of sedative-hypnotic abuse.

1% to 10%:

Central nervous system: Headache, drowsiness, dizziness, lethargy, lightheadedness, depression, abnormal dreams, amnesia

Dermatologic: Rash

Gastrointestinal: Nausea, diarrhea, xerostomia, constipation

Respiratory: Sinusitis, pharyngitis

Symptoms of overdose include coma and hypotension

Treatment for overdose is supportive. Rarely is mechanical ventilation required. Flumazenil has been shown to selectively block binding to CNS receptors, resulting in a reversal of CNS depression but not always respiratory depression.

CYP3A3/4 enzyme substrate

Structurally dissimilar to benzodiazepine, however, has much or all of its actions explained by its effects on benzodiazepine (BZD) receptors, especially the omega-1 receptor; retains hypnotic and much of the anxiolytic properties of the BZD, but has reduced effects on skeletal muscle and seizure threshold.

Onset of action: 30 minutes

Duration: 6-8 hours

Absorption: Rapid

Distribution: Very low amounts secreted into breast milk

Protein binding: 92%

Metabolism: Hepatic to inactive metabolites

Half-life: 2-2.6 hours, in cirrhosis increased to 9.9 hours

Duration of therapy should be limited to 7-10 days

Elderly: 5 mg immediately before bedtime

Hemodialysis: Not dialyzable

Dosing adjustment in hepatic impairment: Decrease dose to 5 mg

Alcohol: Additive CNS effect, avoid use

Ingest immediately before bedtime due to rapid onset of action

Respiratory, cardiac and mental status

80-150 ng/mL

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); may cause physical and/or psychological dependence. While using this medication, do not use alcohol or other prescription or OTC medications (especially, pain medications, sedatives, antihistamines, or hypnotics) without consulting prescriber. Maintain adequate hydration (2-3 L/day of fluids unless instructed to restrict fluid intake). You may experience drowsiness, dizziness, or blurred vision (use caution when driving or engaging in tasks requiring alertness until response to drug is known); nausea (small frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); or diarrhea (buttermilk, boiled milk, yogurt may help). Report CNS changes (confusion, depression, increased sedation, excitation, headache, abnormal thinking, insomnia, or nightmares); muscle pain or weakness; difficulty breathing; chest pain or palpitations; or ineffectiveness of medication. Breast-feeding precautions: Consult prescriber if breast-feeding.

Patients may require assistance with ambulation; lower doses in the elderly are usually effective; institute safety measures

Tablet, as tartrate: 5 mg, 10 mg

Garnier R, Guerault E, Muzard D, et al, "Acute Zolpidem Poisoning - Analysis of 344 Cases," J Toxicol Clin Toxicol, 1994, 32(4):391-404.

Langtry HD and Benfield P, "Zolpidem: A Review of Its Pharmacodynamic and Pharmacokinetic Properties and Therapeutic Potential," Drugs, 1990, 40(2):291-313.

Lheureux P, Debailleul G, De Witte O, et al, "Zolpidem Intoxication Mimicking Narcotic Overdose: Response to Flumazenil," Hum Exp Toxicol, 1990, 9(2):105-7.

Meram D and Descotes J, "Acute Poisoning By Zolpidem," Rev Med Interne, 1989, 10(5):466.

Pacifici GM, Viani A, Rizzo G, et al, "Plasma Protein Binding of Zolpidem in Liver and Renal Insufficiency," Int J Clin Pharmacol Ther Toxicol, 1988, 26(9):439-43.

Salva P and Costa J, "Clinical Pharmacokinetics and Pharmacodynamics of Zolpidem. Therapeutic Implications," Clin Pharmacokinet, 1995, 29(3):142-53.

Simcox DA, "Zolpidem-Associated Falls," Consult Pharm, 1995, 10:1378-80.