Description
Simple
A sleep medication used for short period of time to help with falling asleep.
Clinical
A sedative hypnotic used for the short-term treatment of insomnia to improve sleep latency.
Overview
Zolpidem, also known as _Ambien_, is a hypnotic drug that was initially approved by the FDA in 1992 [FDA label]. Zolpidem improves sleep in patients with insomnia. It is aimed for use in patients with difficulties initiating sleep. This drug decreases the time to fall asleep (sleep latency), increases the duration of sleep, and decreases the number of awakenings during sleep in patients with temporary (transient) insomnia. It is available in both immediate acting and extended release forms [FDA label], [17].
Its tolerability profile is favorable when administered according to the manufacturer’s instructions, with a low risk of drug withdrawal, drug dependence, and drug tolerance [6]. In addition, zolpidem improves sleep quality in patients suffering from chronic insomnia and can show mild muscle relaxant properties [15]. Research also shows that zolpidem is rapid and effective in restoring brain function for patients in a vegetative state following brain injury. This drug has the propensity to completely or partially reverse the abnormal metabolism of damaged...
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Pharmacology
Indication
This drug is indicated for the short-term treatment of insomnia in adults characterized by difficulties with sleep initiation [FDA label].
Pharmacodynamic
**Effects on the central nervous system (CNS)**
This drug has CNS depressant effects, which may include somnolence, decreased alertness, sedation, drowsiness, dizziness, and other changes in psychomotor function [FDA label]. Due to the above effects, the FDA has recommended an initial dose of z...
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Mechanism of action
Zolpidem, the active moiety of zolpidem tartrate, is a hypnotic substance with a chemical structure that is not related to the structure benzodiazepines, barbiturates, pyrrolopyrazines, pyrazolopyrimidines or other drugs exerting hypnotic effects. It interacts with a _GABA-BZ_ receptor complex and...
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Absorption
Zolpidem is rapidly absorbed from the gastrointestinal tract. In a single-dose crossover study in 45 healthy subjects given 5 and 10 mg zolpidem tartrate tablets, the average peak zolpidem concentrations (Cmax) were 59 and 121 ng/mL, respectively, occurring at a mean time (Tmax) of 1.6 hours for bot... Read more
Protein binding
92.5 ± 0.1% [FDA label]
Volume of distribution
0.54 to 0.68 L/kg (in humans) [7]. In patients with... Read more
Clearance
In a clinical trial, after a 20mg dose, total clearance of zolpidem 0.24 to 0.27 ml/min/kg [ Read more
Half life
The average zolpidem elimination half-life was 2.6 and 2.5 hours, for the 5 and 10 mg tablets, respectively [FDA label].
Route of elimination
Zolpidem tartrate tablets are converted to inactive metabolites that are eliminated mainly by renal excretion [FDA label].
Toxicity
Oral (male rat) LD50 = 695 mg/kg [MSDS].
**Overdose**
Symptoms of overdose include impairment of consciousness ranging from somnolence to light coma, in addition to cardiorespiratory collapse resulting in fatal outcomes have been reported [FDA label].
**Withdrawal effects**
F...
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Adverse Effects
Effect | Regions | Age Groups | Incidences | Evidence Type |
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Headache | US |
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Clinical Trial |
Somnolence | US |
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Clinical Trial |
Dizziness | US |
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Clinical Trial |
Drowsiness | US |
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Clinical Trial |
Headache | US |
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Clinical Trial |
Nausea | US |
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Clinical Trial |
Nasopharyngitis | US |
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Clinical Trial |
Dizziness | US |
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Clinical Trial |
Allergy | US |
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Clinical Trial |
Sinusitis | US |
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Clinical Trial |
Back Pain | US |
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Clinical Trial |
Myalgia | US |
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Clinical Trial |
Hallucinations (hypnogogic, visual and NOS) | US |
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Clinical Trial |
Diarrhea | US |
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Clinical Trial |
Dry Mouth | US |
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Clinical Trial |
Back Pain | US |
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Clinical Trial |
Pharyngitis | US |
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Drugged feeling | US |
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Lethargy | US |
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Anxiety | US |
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Fatigue | US |
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Visual Disturbance | US |
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Paresthesia | US |
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Clinical Trial |
Memory Disorders | US |
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Memory Impairment | US |
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Anterograde amnesia | US |
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Amnesia | US |
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Influenza | US |
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Dysorientation | US |
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Abdominal Pain | US |
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Influenza-like symptoms | US |
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Palpitation | US |
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Rash | US |
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Depression | US |
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Lightheadedness | US |
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Constipation | US |
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Blurred vision | US |
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Hypoesthesia | US |
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Arthralgia | US |
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Palpitations | US |
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Psychomotor retardation | US |
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Constipation | US |
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Clinical Trial |
Vertigo | US |
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Muscle Cramp | US |
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Depression | US |
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Psychomotor retardation | US |
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Bing eating | US |
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Depersonalization | US |
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Disinhibition | US |
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Euphoric mood | US |
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Contraindications
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Food Interactions
Avoid alcohol.
Take separate from meals. This drug should not be administered with or immediately after a meal.