What is Zolpidem?

What is Zolpidem?

Zolpidem tartrate is the active ingredient of a type of sleeping pill, which was introduced to the European market around 1988. The pharmaceutical company, Synthelabo, was responsible for this introduction. Five years later a joint venture between this company and Searle saw the release of this therapeutic to the American and European markets under the trade name, Ambien.

As a non-benzodiazepine, this medicine was approved for use as a sedative and hypnotic in the United States (U.S) in 1992. With over a decade later, the popularity of this sedative medicine remained on the rise. Europeans and Americans have been prescribed this medication often for sleep-related problems, with millions of prescriptions filled each year. In 2017, this statistic topped the ranks making Ambien the 50th most frequently prescribed medication, from a large number of medications and categories.

Several global studies have revealed that the prevalence of insomnia constitutes 10-30% of the adult population. This can be as high as 50-60% in some instances. With this being one of the most frequent causes of poor sleep hygiene, it is no wonder a sleep medicine, such as zolpidem (generic name), is popular.

How Does Ambien Work?

The chemical structure of zolpidem sleeping pills falls into the group of imidazopyridines. This is nitrogen with a heterocycle (a class of organic compounds which have their atoms joined in a ring) and in general, the imidazopyridines are GABA antagonists.

GABA (gamma-amino butyric acid) is the chief neurotransmitter of the central nervous system (CNS). This therapeutic is known to work as a GABAA receptor chloride channel modulator, which potentiates the inhibitory function of GABA and thereby leads to sedating benefits. By decreasing brain activity, this will induce a calming effect and thereby allow the user to enter a state of relaxation and sleep.

The mode of action of this non-benzodiazepine is selective towards omega-1 receptors. These are GABAA receptor subtypes which contain alpha 1 subunit. The clinical profile, specifically the safety profile and efficacy, of this sedative may be owed to its high intrinsic activity and selectivity for omega-1 receptors.

Being a non-benzodizepine hypnotic agent, the sedative effects of this medication have been shown to be preferential over the anxiolytic, anticonvulsant and myorelaxant effects. Research shows that this medicine is able to decrease the number of nightly awakenings and improves both sleep latency and duration in patients with chronic insomnia, but is also efficient as a minor muscle relaxant (Bouchette et al., 2020).

What is Zolpidem Used to Treat?

The main therapeutic uses of zolpidem tartrate are:

  • To reduce the time taken to fall asleep
  • To increase the amount of total sleep time

Waking up early, having issues falling asleep, tiredness throughout the day and mental cognitive impairments are all characteristics of the most common sleep disorder, insomnia. Insomnia may be acute (short-term, lasting a few days to a few weeks) or it can be long-term and last for several months or years as seen in chronic patients.

Irrespective of the duration of this condition, the effects of insomnia can be detrimental physically, emotionally and mentally. Zolpidem tartrate is a proven, FDA approved sleeping tablet which can help you get a better night's sleep.

Other uses of this medication arise from the anti-anxiety, muscle relaxant and anti-convulsant properties. These effects are thought to be smaller or secondary to the sedative properties of zolpidem.

Take Zolpidem

How Do You Take Zolpidem?

The standard route of administration of sleep medicines are used for zolpidem as well.

  • Ingest the sedative tablets by mouth
  • Drink sufficient water when doing so the medication may pass from your mouth to the stomach and finally, the small intestines. This will allow for the active ingredients to be absorbed and bring about the desired effects. Swallowing the tablets without enough water may affect the functioning of the therapeutic.
  • The medication should be swallowed in whole form. Do not crush, chew or break up the tablet in any way as this may affect the therapeutic action.
  • You should ideally take the medication before you eat. Consuming with a meal or immediately after may decrease the onset of action.
  • Use this sleep aid an hour before bedtime and only when you have adequate time to dedicate to sleeping (a full night's sleep comprises of 7 to 8 hours)
  • The recommended dose for insomnia is 10 mg for the average adults. Seniors should halve this dosage.
  • Administration should be done in a single intake and not repeated within the same night of treatment
  • The typical treatment period from 2 days to 4 weeks
  • The sedative effects may last after the benefits have worn off. This can cause cognitive impairments and it is advised that the user does not engage in any activity which involved operating machinery or driving. These effects may also be heightened if used in conjunction with alcohol or medications of similar action.

Is Zolpidem a Benzodiazepine?

Benzodiazepines are a class of compounds designated with a chemical structure of a benzene ring fused with a diazepine ring. Benzodiazepines pharmacodynamics resemble those of non-benzodiazepines almost entirely and so the benefits and likelihood of harmful effects are similar. These classes are, however, different in chemical structure and are unrelated on a molecular level as such.

This treatment was one of the three first non-benzodiazepine medications to be marketed. These pharmaceuticals were found in the late 1980's and the early 1990's. They were developed with the intent of overcoming some of the disadvantages of benzodiazepines such as intense residual effects and slow onset of action.

Non-benzodiazepines are similar to benzodiazepines but present with better safety profiles. Since non-benzodiazepines may produce minimal depression of the respiratory system, they can be considered safer than benzodiazepines, for those known to have respiratory disorders.

Non-benzodiazepines are colloquially known as "Z-drugs" because many of the medication names begin with the letter "Z". In addition to producing less adverse events than benzodiazepines for sleep induction, this class of medication also does not disrupt the normal sleep architecture as much as the aforementioned class. This translates to treatments that offer long term benefits, even when used on a short term basis - a tremendous advantage to patients suffering from insomnia and related symptoms.

Updated: 14th January 2021
Review Due: January 2022

Steve

ABOUT STEVE

Fueled with a passion to try and help people less fortunate than himself Steve immersed himself in the medical industry. By researching new and innovative medical advancements and regularly sharing important information on social media Steve intends to make a difference where it matters most, people's health. His wealth of knowledge and keen eye for detail will help keep our readers informed and contribute towards improved health.

John Malcolm – Feb 25, 2021
Hi Steve, cracking article. Your knowledge of Zolpidem and other sleep aid medication has been incredibly helpful. As a sufferer of Insomnia I decided that I would try Zolpidem instead of the benzodiazepines I normally take. The change has been most agreeable and I am sleeping better than ever. Thanks again and keep up the good work. John Malcom

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