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Pronunciation:

(zole PI dem)

U.S. Brand Names:

Ambien®

Synonyms:

Zolpidem Tartrate

Generic Available:

Canadian Brand Names:

Ambien®

Use:

Short-term treatment of insomnia

Restrictions:

C-IV

Pregnancy Risk Factor:

Lactation:

Enters breast milk/use caution (AAP rates "compatible")

Contraindications:

Hypersensitivity to zolpidem or any component of the formulation

Warnings/Precautions:

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.

Adverse Reactions:

1% to 10%:

Cardiovascular: Palpitations

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

Dermatologic: Rash

Gastrointestinal: Nausea, diarrhea, xerostomia, constipation

Respiratory: Sinusitis, pharyngitis

<1% (Limited to important or life-threatening): Confusion, depression, falls, impaired concentration, manic reaction, tremor, vomiting

Overdosage/Toxicology:

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.

Drug Interactions:

Substrate of CYP1A2 (minor), 2C8/9 (minor), 2C19 (minor), 2D6 (minor), 3A4 (major)

Antipsychotics: Sedative effects may be additive with antipsychotics, including phenothiazines; monitor for increased effect

CNS depressants: Sedative effects may be additive with other CNS depressants; monitor for increased effect; includes barbiturates, benzodiazepines, narcotic analgesics, ethanol, and other sedative agents

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of zolpidem. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of zolpidem. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

SSRIs: Sertraline and fluoxetine (to a lesser extent) have been demonstrated to increase zaleplon levels; pharmacodynamic effects were not significantly changed; monitor

Ethanol/Nutrition/Herb Interactions:

Ethanol: Avoid ethanol (may increase CNS depression).

Herb/Nutraceutical: St John's wort may decrease zolpidem levels. Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).

Mechanism of Action:

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 (with a high affinity ratio of the alpha 1/alpha 5 subunits); retains hypnotic and much of the anxiolytic properties of the BZD, but has reduced effects on skeletal muscle and seizure threshold.

Pharmacodynamics/Kinetics:

Onset of action: 30 minutes

Duration: 6-8 hours

Absorption: Rapid

Distribution: Very low amounts enter breast milk

Protein binding: 92%

Metabolism: Hepatic to inactive metabolites

Half-life elimination: 2-2.6 hours; Cirrhosis: Up to 9.9 hours

Dosage:

Duration of therapy should be limited to 7-10 days

Adults: Oral: 10 mg immediately before bedtime; maximum dose: 10 mg

Elderly: 5 mg immediately before bedtime

Hemodialysis: Not dialyzable

Dosing adjustment in hepatic impairment: Decrease dose to 5 mg

Administration:

Ingest immediately before bedtime due to rapid onset of action

Monitoring Parameters:

Daytime alertness; respiratory and cardiac status

Reference Range:

80-150 ng/mL

Patient Education:

Use exactly as directed; do not increase dose or frequency or discontinue without consulting prescriber. Drug 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; respiratory difficulty; chest pain or palpitations; or ineffectiveness of medication. Breast-feeding precaution: Consult prescriber if breast-feeding.

Nursing Implications:

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

Additional Information:

Causes less disturbances in sleep stages as compared to benzodiazepines. Time spent in sleep stages 3 and 4 are maintained; decreases sleep latency. Should not be prescribed in quantities exceeding a 1-month supply.

Anesthesia and Critical Care Concerns/Other Considerations:

Causes less disturbances in sleep stages as compared to benzodiazepines; time spent in sleep stages 3 and 4 are maintained. Zolpidem decreases sleep latency; should not be prescribed in quantities exceeding a 1-month supply.

Dental Health: Effects on Dental Treatment:

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

No information available to require special precautions

Dosage Forms:

Tablet, as tartrate: 5 mg, 10 mg

Ambien® PAK™ [dose pack]: 5 mg (30s), 10 mg (30s)

International Brand Names:

Adco-Zolpidem® (ZA); Adormix® (CL); Albapax® (EC); Ambien® (CA); Amsic® (DE); Bikalm® (DE); Cymerion® (PT); Dalparan® (ES); Dormilam® (CL); Eanox® (DK); Eudorm® (AR); Hipnoton® (CL); Hypnogen® (CZ); Ivadal® (AT, CH, RU); Lioram® (BR); Mondeal® (AT); Myslee® (JP); Nimadorm® (DK); Niotal® (IT); Nottem® (IT); Nytamel® (IE); Sanval® (HR, PL, RU, SI); Somit® (AR); Somnil® (CL, CO); Somnipron® (CL); Somno® (CL, EC); Stella® (FI); Stilnoct® (BE, DK, FI, GB, IE, LU, NL, NO, SE); Stilnox® (AU, BR, CH, CO, CR, CZ, DE, DK, DO, EC, ES, FR, GT, HN, HU, IL, IT, MT, PA, PL, PT, RO, SG, SV, TH, YU, ZA); Stilnox Europharma DK® (DK); Stilnox Paranova® (DK); Sucedal® (CL); Sumenan® (AR); Zimor® (CO); Zleep-5/10® (IN); zodormdura® (DE); Zodorm® (IL); Zoldem® (AT, DE, IE); Zoldorm® (CH); Zolirin® (DE); Zolnod® (IE); Zolpic® (PL); Zolpidem 1 A Pharma® (DE); Zolpidem AbZ® (DE); Zolpidem AL® (DE); Zolpidem "Alpharma"® (DK); Zolpidem Alpharma® (PT); Zolpidem AZU® (DE); Zolpidem Bayvit® (ES); Zolpidem Belmac® (ES); Zolpidem beta® (DE); Zolpidem Bexal® (ES); Zolpidem Biochemie® (FI); Zolpidem Chemo® (ES); Zolpidem Cuve® (ES); Zolpidem Davur® (ES); Zolpidem Edigen® (ES); Zolpidem® (GB, NO); Zolpidem GEA® (FI); Zolpidem Geminis® (ES); Zolpidem Heumann® (DE); Zolpidem Lasa® (ES); Zolpidem Merck® (ES); Zolpidem MK® (CO); Zolpidem Neuraxpharm® (DE); Zolpidem Normon® (ES); Zolpidem Puren® (DE); Zolpidem ratiopharm® (AT); Zolpidem-ratiopharm® (DE); Zolpidem ratiopharm® (DK, ES); Zolpidem-ratiopharm® (FI); Zolpidem real® (DE); Zolpidem Sandoz® (DE); Zolpidem Stada® (DE); Zolpidem TAD® (DE); Zolpidem TEVA® (DE); Zolpidem Ur® (ES); Zolpidem von ct® (DE); Zolpihexal® (ZA); Zolpi-Lich® (DE); Zolpinox® (DE); Zolpi Q® (DE); Zonoct® (DK)

References

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.

Mercurio M, De Roos F, and Hoffman RS, "Zolpidem (Ambien®): Exposure Assessment of a New Nonbenzodiazepine GABA Agonist,"Vet Hum Toxicol, 1994, 36:371.

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.

Queneau PE, Koch S, Hrusovsky S, et al, "Cytolytic Hepatitis Related to Zolpidem," 1st International Symposium on Hepatology and Clinical Pharmacology Liver and Drugs, Abstract, 1994, 39.

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.

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