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... Read more

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... Read more

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... Read more

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... Read more

Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Headache US
  • Kind: experimental
    • Percent: 14-19%
  • Clinical Trial
    Somnolence US
  • Kind: experimental
    • Percent: 6-15%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 8-12%
  • Clinical Trial
    Drowsiness US
  • Kind: experimental
    • Percent: 2-8%
  • Clinical Trial
    Headache US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 6%
  • Clinical Trial
    Nausea US
  • Kind: experimental
    • Percent: 7%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Nasopharyngitis US
  • Kind: experimental
    • Percent: 6%
  • Kind: placebo
    • Percent: 4%
  • Clinical Trial
    Dizziness US
  • Kind: experimental
    • Percent: 1-5%
  • Clinical Trial
    Allergy US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Sinusitis US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 3%
  • Clinical Trial
    Myalgia US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Hallucinations (hypnogogic, visual and NOS) US
  • Kind: experimental
    • Percent: 4%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Diarrhea US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Dry Mouth US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Back Pain US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Pharyngitis US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Drugged feeling US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Lethargy US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Anxiety US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Fatigue US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Visual Disturbance US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Paresthesia US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Memory Disorders US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Memory Impairment US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Anterograde amnesia US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Amnesia US
  • Kind: experimental
    • Percent: 1-3%
  • Clinical Trial
    Influenza US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Dysorientation US
  • Kind: experimental
    • Percent: 3%
  • Kind: placebo
    • Percent: 2%
  • Clinical Trial
    Abdominal Pain US
  • Kind: experimental
    • Percent: 2
  • Clinical Trial
    Influenza-like symptoms US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Rash US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Lightheadedness US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Blurred vision US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Hypoesthesia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Arthralgia US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Palpitations US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Psychomotor retardation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Constipation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Vertigo US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Muscle Cramp US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 1%
  • Clinical Trial
    Depression US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Psychomotor retardation US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Bing eating US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Depersonalization US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Disinhibition US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial
    Euphoric mood US
  • Kind: experimental
    • Percent: 2%
  • Kind: placebo
    • Percent: 0%
  • Clinical Trial

    Contraindications

    • Route:
      • Oral
    • Hypersensitivity:
      • true
    • Regions: US

    Food Interactions

    Avoid alcohol.

    Take separate from meals. This drug should not be administered with or immediately after a meal.