Zolpidem chemical structure
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Zolpidem

Zolpidem is a prescription drug used for the short-term treatment of insomnia (sleeping pill). It works quickly (usually within 15 minutes) and has a short half-life (2-3 hours), but will last longer in patients with hepatic failure. Some trade names of zolpidem are Ambien®, Stilnox®, Stilnoct®, or Myslee®. Its sedative effects are similar to those of the benzodiazepines, but it is actually classified as an imidazopyridine, and the anticonvulsant and muscle relaxant effects only appear at 10 and 20 times the dose required for sedation, respectively. more...

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For that reason, it has never been approved for either muscle relaxation or seizure prevention. Such drastically increased doses are likely to induce one or more negative side effects, including hallucinations and/or amnesia.

The patent on zolpidem is held by the French pharmacutical corporation Sanofi-Aventis.

Uses

Zolpidem is approved for the short-term treatment of insomnia, but it has been studied for nightly use up to six months in a single-blind, open-label trial published in 1991, an open-label study lasting 180 days published in 1992 (with continued efficacy in patients who had kept taking it as of 180 days after the end of the trial), and in an open-label trial lasting 179 days published in 1993.

The United States Air Force uses zolpidem under trade name Ambien® as "no-go pills" to help the pilots sleep after the mission; another drug used for the same purpose is temazepam (Restoril®). (Cf. the "go-pills", amphetamine served under the name Dexedrine® as a stimulant for the pilots, or its recent modafinil (Provigil®) replacement).

It is also used off-label to treat restless leg syndrome.

As is the case with many prescription sedative/hypnotic drugs, zolpidem is sometimes used by stimulant users to "come down" after the use of stimulants such as methamphetamine, cocaine, methylenedioxymethamphetamine (MDMA), or pharmaceutical amphetamines.

Mechanism of action

In 1990, Pritchett and Seeburg noted that zolpidem binds with high affinity to the α1-, and with medium affinity to the α2- and α3-GABAA receptor subunits, and found that it had no affinity for the α5 subunit. Two years later, zolpidem was noted to have a high affinity for ω1-benzodiazepine receptors, a low affinity for ω2 and a very low affintity for ω3, respectively by Ruano et al in 1992. In other words, it has the highest affinity for ω1 binding sites on α-1GABAA receptor subunits, and it is this that mediates its sedative and weak anticonvulsant properties.

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Zolpidem
From Gale Encyclopedia of Cancer, by Bob Kirsch

Definition

Zolpidem is a medicine that helps a person get to sleep and stay asleep. The brand name of zolpidem in the U.S. is Ambien.

Purpose

Zolpidem is a sleep medication. It is intended for the short-term treatment of insomnia. Zolpidem may be particularly useful for people who have trouble falling asleep.

Description

Sleep medications are called sedatives or hypnotics. Zolpidem affects brain chemicals, resulting in sleep. It is somewhat similar in its actions on sleep to the group of drugs known as benzodiazepines. Zolpidem is only intended for short term use (seven-10 days). Although there is some information published about effectiveness with longer use, some side effects may increase with longer use.

Recommended dosage

The usual dose is 10 mg before bedtime in adults and 5 mg before bedtime in the elderly and in people with liver disease. The onset of effect occurs within about 30 minutes and the effects on sleep last for 6-8 hours.

Precautions

It is suggested that zolpidem not be discontinued abruptly after regular use (that is daily use for even as short a time as one week). Instead, the drug should be gradually tapered. The tapering is recommended to avoid the possibility of a withdrawal syndrome as well as to avoid the possibility of a rebound worsening of insomnia.

Side effects

The most common side effects of zolpidem include drowsiness, dizziness, and headache. Drowsiness, of course, is desirable when it occurs at bedtime. Daytime drowsiness that is left over from the night before would be considered a side effect. Other side effects include diarrhea, nausea and vomiting, and muscle aches. Rarely, amnesia, confusion, falls, and tremor are seen. Falls probably result from the drowsiness or dizziness.

Interactions

Increased effects of zolpidem (eg. more drowsiness, confusion) may be seen with alcohol consumption and with other drugs known to cause drowsiness.

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