Zolpidem chemical structure
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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...

Zoledronic acid

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.


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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Get a good night's sleep: use our 10 simple and effective strategies for getting well rested and more revved
From Shape, 6/1/04 by Gwenda Blair

If you wake up every morning feeling refreshed and ready to roll, you can skip this article. But if you're like tens of millions of Americans, you're still exhausted when the alarm goes off. You know you're supposed to get about eight hours of sleep, but shaving that by at least an hour seems the only way to hold onto your job, fit in exercise and still have a life. By Friday night you're wiped out, yet trying to make up for lost sleep on weekends leaves you feeling groggy. The unhappy result: You've come to accept being tired as a given, which impedes your productivity and even puts you at risk for health problems, including high blood pressure, weight gain and the elevated glucose levels associated with diabetes.

The good news: "You can get the sleep you need," says Anne Remmes, M.D., co-director of the Columbia Headache Center and a neurologist at New York City's Columbia-Presbyterian Eastside who specializes in sleep disorders. "You just have to be willing to work at it." Here's how.

1. Meet your requirements. Count back eight hours from when you have to get up. "You need continuous sleep in long blocks," says James Maas, Ph.D., a professor of psychology at Cornell University in Ithaca, N.Y., and author of Power Sleep: The Revolutionary Program That Prepares Your Mind for Peak Performance (Quill, 1998). Note that individual sleep needs vary from seven hours a night to as many as 9 1/2. If you're still tired at the end of a week, Maas suggests moving your bedtime back by small increments--say, 15 minutes--until you wake up rested. You also should strive to log the same number of hours at the same bed and wake times.

2. Adjust the atmosphere. Because sleep requires a dip in core body temperature, you may nod off faster in a cool room--but don't make it too cool. For most people, 65-67[degrees] F is ideal, Maas says. To facilitate production of the sleep hormone melatonin, which requires darkness, you also should remove sources of light (including the TV and computer) and get blinds that completely black out your windows.

3. Steer clear of stimulants. Avoid caffeinated coffees and sodas, sugar-laden snacks and juices and nicotine--particularly later in the day. Regular exercise can help you fall asleep, but Remmes warns that a high-intensity evening workout could keep you up at night. "Figure out how long it takes you to quiet your body and your brain," she says. "Some people can keep going until they jump into bed, but others need several hours to shut everything down."

4. Don't multitask your mattress. "Condition yourself to associate your bed with the sleep phase in your body's biological rhythm," Maas says. That means reserving your bed for sleep (and sex) only and carrying out the rest of your life elsewhere. For instance, don't watch television, eat, read, talk on the phone or balance your checkbook while you're in bed, he says.

5. Shrink your siestas. Limit naps to a half-hour or less. According to Maas--who coined the term power nap--short naps will keep you from going into deep sleep and waking up disoriented and will also prevent difficulty falling asleep at your regular bedtime.

6. Nix the nightcaps and spicy snacks. Alcohol may help you fall asleep, but after four hours, as it's fully metabolized, you will either wake up or experience fragmented sleep. Don't go to bed hungry, either, since a rumbling stomach will likely wake you up in the middle of the night. But avoid foods that can cause sleep-impeding heartburn and gas, such as garlic and pizza, before going to bed.

7. Wind down wisely. A hot bath or shower and warm milk or herbal tea can be helpful sleep aids because they relax your muscles and raise your temperature slightly. When your body then cools off, the drop in temperature eases you into sleep. Also, try activities that allow you to unwind, such as meditation and yoga. Other sleep aids, Maas says, include sex, soothing music, slow breathing and visualization exercises.

8. Don't just lie there. If you haven't fallen asleep in 20 minutes or so, Remmes advises getting out of bed and sitting in a comfortable place with low lighting to read. "Don't look at the clock," she says. "Doing so will make you worried about how late it is, increasing adrenaline and agitation and making it even harder to get to sleep."

9. Rise and shine. Wake to a soothing alarm (check out Gaiam's Peaceful Awakenings Chime Clock, $98, at gaiam.com) rather than an ear-splitting buzzer. (But note that with enough sleep, you should be able to wake up without an alarm.) Get yourself moving with bright sunlight (or daylight-spectrum artificial light), coffee or tea and light exercise, such as a brisk 30- to 60-minute walk. Avoid intense workouts upon waking, Maas says, because your body temperature is still low, and you're not yet alert, making you vulnerable to injuries. As with any workout, make sure to warm up with at least five (preferably 10) minutes of light cardio.

10. Seek treatment. Insomnia is the most common sleep disorder, affecting approximately 30-40 percent of all American adults. Symptoms include difficulty falling asleep, waking up frequently during the night or not sleeping long enough (waking early). If you get a full night's sleep and still feel tired in the morning, you might have sleep apnea (a breathing disorder that causes sleep disruption) or restless legs syndrome (leg discomfort that leads to frequent movement while asleep). If these problems persist, you should consult a doctor.

Remember that getting enough sleep will make you more efficient at tasks that seem to take forever when you're tired and can translate into more energy and improved health. "If you add just one more hour of sleep [nightly] to what you get now," Maas says, "within 10 days you'll feel like a new person."

RELATED ARTICLE: Drug Facts for the Sleep-Deprived

What you need to know before you pop those pills

* A growing number of sleepyheads are seeking relief in pick-me-upper Provigil (modafinil), a prescription drug approved only for treating narcolepsy, but which can be prescribed to combat sleepiness, without causing the jitters. "It does make you feel alert even with minimal sleep," says James Maas, Ph.D., a professor of psychology at Cornell University. "But don't fool yourself--you're still vulnerable to all the health problems associated with inadequate sleep."

* Over-the-counter medications such as Unisom, Tylenol PM and Excedrin PM may knock you out if taken only occasionally, but sleep-disorder specialist Anne Remmes, M.D., says they lose their effectiveness if you take them night after night, and they may leave you with a "hangover" in the morning.

* Short-term use (seven to 10 days) of prescription sleeping pills such as Sonata CIV (zaleplon) or Ambien (zolpidem tartrate) can help you recover from bouts of insomnia, Maas says. Although these medications, as well as others expected on the market soon, are believed to be safer and more effective than their predecessors, Maas notes that "the only real solution is changing your lifestyle so you get adequate sleep on a regular basis."

Gwenda Blair is a freelance writer based in New York City.

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