Zolpidem (Oromucosal, Sublingual)

Zolpidem is a sleeping aid prescribed to treat insomnia, anxiety, and seizure disorders.

Overview

Zolpidem is used primarily as an alternative to more commonly prescribed sleeping aids, due to the less severe side effects and shorter duration of zolpidem. Normally, sleeping aids have a tendency to last for prolonged periods of time, but zolpidem has a duration period of roughly three hours. It helps patients with sleep initiation problems but its effectiveness in maintaining sleep is limited. Patients will need to find a way to maintain the sleep once it has begun through other means.

Additionally, zolpidem is used frequently as a muscle relaxant and anticonvulsant. It appears to be effective when used to relieve seizures, due to its ability to reduce the tension believed to cause seizures. Other disorders characterized by tightening of the muscles can be relieved by zolpidem as well.

Zolpidem achieves most of its effects through positive modulation of the GABA receptors. These receptors in the brain allow us to inhibit behaviors and brain activity when we need to rest, but some people possess dysfunctional GABA receptors. Zolpidem helps the body stimulate them to increase the concentration of neurotransmitters needed for sleep. This makes it ideal for a large variety of conditions beyond insomnia, such as anxiety disorders.

Zolpidem is a potent drug usually prescribed for short periods of time, although doctors may prescribe it in bursts as needed by patients. This limited use of zolpidem is caused by concerns over the myriad side effects often observed. Patients experience everything from mild discomfort to sleepwalking as a result of use. Sometimes, these symptoms result in displays of bizarre behavior, such as preparing entire meals or driving vehicles while asleep. Despite these potential side effects, patients can benefit from the use of zolpidem.

Zolpidem was developed as an alternative to benzodiazepines and barbiturates. These drugs have a much higher abuse potential and produce very severe side effects. Additionally, there are many patients that simply won't respond to the effects of these drugs and need something that will alleviate their insomnia quickly. This is exactly what they receive when they use zolpidem. The effects are quickly felt and patients are able to finally rest after dealing with the frustrating symptoms of sleeping disorders.

Condition(s) treated

  • Insomnia

Type of medicine

  • Sleep aid

Side effects

While zolpidem is a short-lasting drug, it carries a wide array of side effects. Nausea, headaches and lethargy are often reported. These symptoms are often reported with initial use, but tend to decline as patients become adjusted to the treatment. These side effects are generally of no serious concern, but some more severe issues can arise. Memory loss is a great example of one of the most serious issues that may develop. Some zolpidem users report loss of short-term memory and difficulty recalling details they have tried to remember. Patients who use zolpidem for prolonged periods are more likely to see these side effects remain.

Patients with acid reflux disease tend to experience longer periods of reflux when they use this medication. Although the exact mechanism behind this hasn't been fully studied, it is generally believed that GABA agonism suppresses muscles in the esophagus. The suppressed muscles are less able to stop the reflux, leading to longer episodes. Although patients with acid reflux disease suffer from these issues, this is not considered serious enough to warrant avoiding prescriptions.

Sleepwalking is one of the most serious side effects zolpidem can produce. About 5% of all patients will experience sleepwalking to some extent. This sleepwalking can simply involve walking around a room, or it can include very complex behaviors such as preparing food. Patients will often have no memory of what they've done after the episode of sleepwalking is over, despite experiencing great distress over the occurrence.

Emotional disturbances are commonly seen in those who take zolpidem. These disturbances are usually episodic and occur over the course of treatment. Many patients will experience sudden moments of agitation or depressed mood, but they usually don't last very long because zolpidem is a fast-acting drug. In rare cases, these emotional disturbances take on a more severe and complex form, involving changes to the patient's personality. In such cases, the doctor may prescribe something to alleviate the emotional imbalance. The interaction between zolpidem and antidepressants can reduce many of the negative symptoms associated with insomnia.

Zolpidem has the potential to lead to dependency in some individuals. As tolerance to the effects builds up and the body adjusts to the dosage, withdrawals and other symptoms of dependency occur. Most doctors will take precautions to make sure this doesn't happen to their patients by paying close attention to dosages and by ending the prescription before the patient develops a persistent need to use zolpidem. The symptoms of dependency strongly resemble those seen with alcohol and other GABA receptor agonists. The patient will often complain about delirium, a state of confusion and disturbance, and experience physical symptoms, such as trembling. Usually, these symptoms are treated by giving the patient another drug. Dependency on zolpidem is generally treated by giving the patient another sleeping aid, such as benzodiazepines.

Dosage

Zolpidem is taken as a nasal spray or as a sublingual tablet under the names Intermezzo and Edluar. In both forms, it is a potent drug, to be taken with precaution. Zolpidem should be taken before going to sleep, as it works quickly. It works faster if taken on an empty stomach, so, in most cases, it shouldn't be taken with food, but if your doctor advises you take it a particular way, follow their instructions.

Prior to using zolpidem as a spray, you must prime it by spraying it five times in a safe direction away from anyone else. After you have primed it, take one spray for a 5mg dose. If you need a higher dose, spray twice for a 10mg dose. As a sublingual tablet, zolpidem must be placed under the tongue. It will quickly dissolve and release the medicine into your system.

The dosage of zolpidem needed for sleep initiation is relatively low. A 5mg dose is usually enough for most patients, but a 10mg dose may also be used if that proves to be insufficient. The dosage will be given to the patient daily over the course of 1 to 2 weeks. Doctors will rarely give patients zolpidem for more than a brief period of time, but some patients may receive prescriptions for a more prolonged period. Elderly patients should take precaution when using Intermezzo, a sublingual tablet form of zolpidem. Only take 1.75mg doses shortly before going to sleep, as the drug's effects are more potent when used by elderly patients.

Doctors advise against taking double doses of zolpidem. The combined effects of two doses can be enough to trigger unwanted side effects. Trying to make up for missed doses is not advised either. Zolpidem is generally considered far too risky to give to children, but doctors who decide to will often make very specific recommendations. The effects of the drug are strong enough to cause long-lasting effects on children even after the drug is no longer in use. Research has already shown pregnant women who take zolpidem tend to have children with more behavioral issues and heart defects. It is likely that such issues will occur in children exposed, though limited research is available.

Interactions

Zolpidem is a sleeping aid and it will naturally interact in a synergistic way whenever you use it without sleeping aids. Benzodiazepines are enhanced when used with zolpidem, as are barbiturates. These drugs target GABA receptors, which means that patients will experience an extreme inhibition of essential functions. The side effects of benzodiazepines are often enhanced, and memory loss and poor muscle control also often display themselves. Benzodiazepines are often used as a replacement for zolpidem when dependency develops, but the initial switch can lead to dangerous overlap. Outside of benzodiazepines, zolpidem can produce a strange effect when combined with stimulants. Stimulants are often delayed or weakened by zolpidem. In some cases, the effects are completely canceled out.

Zolpidem's ability to relax muscles means other drugs known to affect the muscles of the body are going to alter results, too. Gabapentin can be taken with zolpidem to increase muscle relaxation and further the intended muscle relaxant effect. This effect is sometimes desirable, but it can cause issues if patients do not take precautions. Opioid painkillers and zolpidem can cause fatal reactions when ingested together. Both drugs are known to cause respiratory failure and both have the potential to lead to death. The lethargy caused by zolpidem can make the situation even worse by preventing patients from seeking medical attention.

These drug interactions aren't the only ones that can occur with zolpidem. Other drugs have the potential to bring out issues as well, when patients take them without caution. Over the counter drugs, antibiotics, and heart medications can potentially lead to serious side effects, due to drug interactions. To better under drug interactions, you should keep your doctor fully informed on everything that has happened. Using the advice of a doctor can help you make better decisions.

Warnings

The most serious issue most patients will need to worry about is prolonged use. Zolpidem can easily produce dependency in those who are susceptible when taken for more than a few weeks. When taken for prolonged periods of time, many people using zolpidem will begin to experience issues with cognitive functions. Short term memory is often the first faculty to experience decline, but it isn't uncommon to see emotional disturbances and other issues spring up instead. The risk of permanent damage increases with each treatment period and is compounded with dosages exceeding 10mg.

Of all the dangers of zolpidem, nothing is more dangerous than sleepwalking. Sleepwalkers have been known to endanger themselves by walking into traffic, misusing sharp objects and consuming toxic substances while in a dreaming state. This danger can only be handled by someone other than the patient. Usually, a loved one will notice the sleepwalking and inform the doctor of what's going on before the sleepwalking can further endanger anyone. As soon as sleepwalking is noticed, any zolpidem prescription must be discontinued and no further prescriptions can be allowed.

As a GABA receptor agonist, zolpidem has cross tolerance with a number of drugs. Alcohol can produce tolerance to zolpidem and prevent patients from fully benefiting from treatment. For this reason, it is generally advised that patients avoid using alcohol while on zolpidem and that alcoholics seek other treatment options instead. While taking zolpidem, alcohol consumption can make physical side effects much worse. Diarrhea, vomiting, and muscle pain are often intensified from alcohol abuse.

Pregnant women are advised against using zolpidem. The effects on fully developed adults tend to be devastating, but the effects on fetuses haven't been fully studied. What has been studied suggests that zolpidem can cause permanent and severe harm to the developing fetus. The GABA receptors inhibit many bodily functions including growth and development. Pregnant women who use zolpidem are far more likely to give birth to babies with learning difficulties and behavioral problems than the general population. Physical abnormalities may also develop as well. The GABA receptors can inhibit many receptors considered vital to proper limb development, as well as many associated with hormone secretion. Boys are often born with deficient levels of testosterone and may have issues with puberty and fertility later in life. All genders may experience kidney and heart disease problems.

Elderly patients face special risks when they are treated with zolpidem. The aging process already damages their brain and reduces cognitive function, but zolpidem has the potential to inflict devastating damage to the brain. Zolpidem dependency is known to cause delirium and dementia; patients will generally see their condition worsen during treatment. Older people, particularly those who are over the age of 65, are prone to pneumonia and other illnesses worsened by respiratory failure. The consensus in the medical community is against the use of zolpidem for elderly patients. It doesn't appear to be more effective for treating them and it seems to carry more consequences in the end. Zolpidem is rarely prescribed to elderly patients and most doctors will only prescribe treatments for very short periods of time.

The effects of long term use of zolpidem are not well understood. Most research does not indicate any significant benefits for patients who continue to use zolpidem for than a few weeks. After three weeks, patients develop a tolerance and the effectiveness declines. However, the damage caused by zolpidem begins to increase exponentially at this point. By the end of one month's use, most patients will experience difficulties with keeping track of time and detailed information. Over the course of a year, patients often lose the ability to perform complex tasks, due to losses in spatial and verbal reasoning.

Zolpidem greatly impairs the ability to drive and operate heavy machinery. The typical blood levels of zolpidem in intoxicated drivers is at least 1000mg/liter. Most patients are simply unable to drive themselves around their own. Overdosing generally occurs when a patient has at least 7000mg/liter of bodily fluid in their system. At this level, patients will exhibit dilated pupils, complete lack of energy, and possibly respiratory failure. Respiratory failure can reach a point that a patient enters a coma or even dies.

Allergic reactions to zolpidem sometimes occur in sensitive patients. Normally, the symptoms of zolpidem allergies are easily observed. Patients may display swelling in the tongue, fever, and nausea after consuming the drug. Often, these symptoms can be treated by making sure patients reach a doctor before the symptoms worsen, but fatalities are known to occur. If an allergic reaction occurs after using the medication, discontinue all use until advised otherwise by a doctor.

Beyond the mentioned dangers there are others that may arise. Contact your doctor and keep them fully aware of anything that has occurred. Some symptoms of zolpidem can only be properly assessed with extensive knowledge of the human body and testing. Intuition and guesses simply are not enough to give you a fair way of understanding everything that might go wrong. Patients are often not even aware of what might be going wrong before their condition worsens.

Storage

Always store zolpidem in a dry, cool place. Zolpidem should never be exposed to extremely low temperatures or extremely high temperatures. Under both circumstances, the drug may degrade in quality until the patient will not be able to use it. Make sure to close the pill bottle after use, with the bottles or sprays being located on a high shelf. Children and animals may find a way to access zolpidem them if you do not keep it and away from them.

Do not store zolpidem in anything but the bottle that you received them in. Particularly with pills, you may lose track of them or end up losing count of how many you have already taken. If you decide to travel anywhere, you must keep any paperwork you received from your pharmacist with you. This will help you remember any important information and keep a reminder of how you need to be taking your medication. Without it, you may fall into bad habits or forget important notes from medical professionals.

When your doctor has decided they no longer want to prescribe zolpidem, it is important to figure how you will dispose of them. Do not attempt to dispose of them in your trash can or by flushing them down a toilet. This may expose others to the medications or provide a means for those who should not have the drugs to acquire them. Keep all unused medicine and bottles in a container until you decide what you are going to do with them.

Summary

Zolpidem is a fast acting drug used to help patients initiate sleep. As a spray and sublingual tablet, it provides an easy way for patients to get the full night's rest they desire. Prior to the development of zolpidem, the primary choices for sleeping aids were benzodiazepines or barbiturates. There were no options on the market that would give people the same hypnotic effects without all of the baggage. Unlike its alternatives, zolpidem works over the course of a couple of hours rather than as a prolonged drug. This prevents many of the issues commonly seen in prescription sleeping aids, although side effects are seen in many patients.

Zolpidem has gained an undeserved reputation as the 'sleep walking' drug, due to stories describing patients who have experienced sleepwalking as a symptom. Sleep walking has even evolved into eating and driving while asleep. While these stories do happen, they do not represent what most people experience during zolpidem use. The majority of symptoms are mild and often fleeting, although there are times when the drug can be fatal. Physical side effects are often seen as well, because zolpidem reduces a number of key biological activities. For example, patients with acid reflux disease often experience exaggerated reflux periods due to the patients inability to fight the acid's impact on the esophagus.

Alcohol use is associated with negative interactions with zolpidem due to shared similarities in terms of targeted receptors. Other interactions have also been observed for opioids and other drugs that act upon the respiratory system. These drugs are known to stimulate GABA receptors and inhibit respiratory function. Patients who ingest alcohol or other sedatives can easily cause their respiratory system to fail altogether. Cross tolerance is known to develop when people who use one drug, alcohol for example, and later find zolpidem isn't able to provide them with much relief.

While zolpidem is not a drug intended for prolonged use, it is absolutely vital for helping insomniacs steer themselves in the right direction. They can begin developing a solution to their ailment, but zolpidem alone is rarely the answer. It can only be prescribed for a set amount of time, two weeks at most, before serious issues begin to materialize. For this reason patients must think of zolpidem as a step towards either life without any medication or towards the use of more reliable prescription medication. With the advice and guidance of a doctor, patients will understand whether or not zolpidem is right for them.

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Last Reviewed:
December 23, 2017
Last Updated:
April 12, 2018
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