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Pronunciation |
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(zole
PI
dem) |
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U.S. Brand
Names |
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Ambien™ |
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Generic
Available |
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No |
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Synonyms |
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Zolpidem Tartrate |
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Pharmacological Index |
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Hypnotic, Nonbenzodiazepine |
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Use |
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Short-term treatment of insomnia |
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Restrictions |
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C-IV |
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Pregnancy Risk
Factor |
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B |
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Contraindications |
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Known hypersensitivity to zolpidem |
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Warnings/Precautions |
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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. |
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Adverse
Reactions |
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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 |
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Overdosage/Toxicology |
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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. |
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Drug
Interactions |
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CYP3A3/4 enzyme substrate |
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Mechanism of
Action |
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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. |
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Pharmacodynamics/Kinetics |
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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
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Usual Dosage |
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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
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Dietary
Considerations |
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Alcohol: Additive CNS effect, avoid use |
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Administration |
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Ingest immediately before bedtime due to rapid onset of
action |
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Monitoring
Parameters |
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Respiratory, cardiac and mental status |
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Reference Range |
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80-150 ng/mL |
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Dental Health: Local
Anesthetic/Vasoconstrictor
Precautions |
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No information available to require special precautions |
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Dental Health:
Effects on Dental Treatment |
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No effects or complications reported |
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Patient
Information |
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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. |
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Nursing
Implications |
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Patients may require assistance with ambulation; lower doses in the elderly
are usually effective; institute safety measures |
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Dosage Forms |
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Tablet, as tartrate: 5 mg, 10 mg |
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References |
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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. |
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