Zolpidem tartrate
Zolpidem tartrate (Ambien)
Zolpidem tartrate
( ZOL-pih-dem)
Pregnancy Category: B Ambien (Rx) (C-IV)

Classification: Nonbarbiturate, nonbenzodiazepine sedative-hypnotic

Action/Kinetics: May act by subunit modulation of the GABA receptor chloride channel macromolecular complex resulting in sedative, anticonvulsant, anxiolytic, and myorelaxant properties. Although unrelated chemically to the benzodiazepines or barbiturates, it interacts with a GABA-benzodiazepine receptor complex and shares some of the pharmacologic effects of the benzodiazepines. Specifically, it binds the omega-1 receptor preferentially. No evidence of residual next-day effects or rebound insomnia at usual doses; little evidence for memory impairment. Sleep time spent in stage 3 to 4 (deep sleep) was comparable to placebo with only inconsistent, minor changes in REM sleep at recommended doses. Rapidly absorbed from the GI tract. t 1/2: About 2.5 hr (increased in geriatric clients and those with impaired hepatic function). Bound significantly (92.5%) to plasma proteins. Food decreases the bioavailability of zolpidem. Metabolized in the liver; inactive metabolites are excreted primarily through the urine.

Uses: Short-term treatment of insomnia.

Contraindications: Lactation.

Special Concerns: Use with caution and at reduced dosage in clients with impaired hepatic function, in compromised respiratory function, in those with impaired renal function, and in clients with S&S; of depression. Impaired motor or cognitive performance after repeated use or unusual sensitivity to hypnotic drugs may be noted in geriatric or debilitated clients. Closely observe individuals with a history of dependence on or abuse of drugs or alcohol. Safety and efficacy have not been determined in children less than 18 years of age.

Side Effects: Symptoms of withdrawal: Although there is no clear evidence of a withdrawal syndrome, the following symptoms were noted with zolpidem following placebo substitution: fatigue, nausea, flushing, lightheadedness, uncontrolled crying, emesis, stomach cramps, panic attack, nervousness, abdominal discomfort.
The most common side effects following use for up to 10 nights included drowsiness, dizziness, and diarrhea. The side effects listed in the following are for an incidence of 1% or greater. CNS: Headache, drowsiness, dizziness, lethargy, drugged feeling, lightheadedness, depression, abnormal dreams, amnesia, anxiety, nervousness, sleep disorder, ataxia, confusion, euphoria, insomnia, vertigo. GI: Nausea, diarrhea, dyspepsia, abdominal pain, constipation, anorexia, vomiting. Musculoskeletal: Myalgia, arthralgia. Respiratory: URI, sinusitis, pharyngitis, rhinitis. Body as a whole: Allergy, back pain, flu-like symptoms, chest pain, fatigue. Ophthalmologic: Diplopia, abnormal vision. Miscellaneous: Rash, UTI, palpitations, dry mouth, infection.

Laboratory Test Alterations: ALT, AST, BUN. Hyperglycemia, hypercholesterolemia, hyperlipidemia, abnormal hepatic function.

Overdose Management: Symptoms: Symptoms ranging from somnolence to light coma. Rarely, CV and respiratory compromise. Treatment: Gastric lavage if appropriate. General symptomatic and supportive measures. IV fluids as needed. Flumazenil may be effective in reversing CNS depression. Monitor hypotension and CNS depression and treat appropriately. Sedative drugs should not be used, even if excitation occurs. Zolpidem is not dialyzable.

Drug Interactions: CNS depressants/ Additive CNS depression Ketoconazole / Plasma ketoconazole levels

How Supplied: Tablet: 5 mg, 10 mg

Dosage
?Tablets Hypnotic.
Adults, individualized, usual: 10 mg just before bedtime. In hepatic insufficiency, use an initial dose of 5 mg.