What You Should Know About Sleep Aids and Sleeping Pills
Whether you can’t fall asleep at night or you wake up after a few hours, you know how lousy you might feel the next day. Insomnia can leave you feeling fatigued, unmotivated and cranky. While an occasional poor night’s sleep should not have any lasting effects, if you’re chronically sleep deprived, that may be a different story.
To combat insomnia, some people turn to sleep aids. But are they effective, and how safe are they?
Learn about treating insomnia without sleeping pills using Cognitive Behavioral Therapy for Insomnia (CBT-I).
Sleep aids, also call hypnotics, can work in different ways. Some sleeping pills affect the areas of the brain that control alertness. Other sleep aids contain medication used to treat something other than insomnia but cause drowsiness as a side effect.
Over the counter sleep aids often contain diphenhydramine, which is used to treat allergy symptoms. One of the side effects of diphenhydramine is drowsiness, which is why it’s used in many popular sleep aids. Side effects of over the counter sleep aids containing diphenhydramine include dry mouth, constipation and nausea.
Prescription sleep aids may also be an option. There are different classifications of prescription sleep meds including benzodiazepines. Benzodiazepines are an older type of sleeping pill that targets various types of GABA receptors in the brain that promote sleep. But they should be used with caution since they can be addictive. Side effects including dizziness, muscle weakness and nausea are possible.
Selective gamma-aminobutyric acid medications are a newer classification of sleep aids. These drugs work by targeting specific GABA receptors in the brain that play a role in alertness or drowsiness. Since they only target specific receptors, they tend to result in fewer side effects than benzodiazepines and have a lower risk of becoming addictive. But mild side effects are still possible, such as memory problems and confusion. Some of these are the same as melatonin side effects.
If you decide to try sleep aids, it’s important to take certain precautions. Even over the counter sleep aids can lead to potential problems if not taken correctly. Consider the following:
|Sleep medication name||Helps to initiate sleep||Helps to maintain sleep|
Harvard Health Publications. Sleeping Pills and Natural Sleep Aids; What’s Best for You? http://www.helpguide.org/articles/sleep/sleeping-pills-and-natural-sleep-aids.htm
University of Maryland Medical Center. Sleeping Pills and Insomnia. http://ummidtown.org/programs/sleep/health/sleeping-pills-and-insomnia
The word ‘hypnotic’ can mean the following –
The word ‘hypnotic’ comes from the Greek word ‘Hypnos’, meaning sleep. ‘Hypnotic’ also refers to soporific drugs, otherwise known as sleeping pills: these come under the banner of psychoactive drugs. These drugs are used to induce sleep; they’re also used for surgical anesthesia and in the treatment of sleeplessness (insomnia).
This group of drugs are related to sedatives. The word ‘hypnotic’ typically describes drugs whose purpose is to sustain, lengthen, or even initiate sleep; whereas the word ‘sedative’ is used as a descriptive word for drugs used for relieving or calming anxiety.
Collectively, this group of drugs are typically referred to as sedative-hypnotic drugs, simply because the two functions described above often overlap; in addition to the fact that this group of drugs produce dose-dependent effects, which may range from anxiolysis right through to complete loss of consciousness.
It's very common for hypnotic drugs to be described for sleep disorders, including insomnia: in some countries, more than 95% of insomniacs are prescribed hypnotics. Because hypnotic drugs can be habit-forming, and because there are many factors that can disturb a person’s sleep pattern, before a physician prescribes medication to improve sleep it’s quite common for improved sleep hygiene, alterations to the environment both before and during sleep, and avoiding stimulating substances (such as caffeine) to be recommended. When hypnotic medication has been prescribed, it should be used for the shortest possible period of time.
Today, hypnotics prescribed are either Benzodiazepines or Non-Benzodiazepines. As at the year 2010, 10.8% of people with sleep disorders were prescribed or taking benzodiazepines, while 13.7% were taking non-benzodiazepines. Even though barbiturates are still prescribed in some instances, this class of drug is not commonly prescribed by most practices.
When it comes to children, unless the child experiences night terrors or sleepwalking (somnambulism), hypnotics are not usually prescribed. Older people are typically more sensitive to the side-effects of cognitive impairment and daytime fatigue, but it’s been determined that the risks of using hypnotics in the elderly generally outweigh the benefits.
When reviewing literature regarding Z Drugs and benzodiazepine hypnotics, it was concluded that there are adverse effects connected to these drugs, such as accidents and dependence. (Z Drugs are used in the treatment of insomnia). It was also determined that the ideal treatment is to use the lowest effective dose for the shortest possible therapeutic period of time; discontinuing gradually in an attempt to improve health, without affecting sleep.
The neuro-hormone, melatonin, has a hypnotic function and falls outside the above-mentioned categories.
The History of ‘Hypnotic’
Hypnotica was a class of sleep-inducing substances and drugs tested in the 1890s, which later included Acetal, Urethan, Paraldehyde, Sulfonal, Methylal, Chloralurethan, Hypnon, Amylenhydrate, and Ohloralamid or Chloralimid.
In the latter part of the 20th century more research was carried out using medications to treat insomnia. Back in 1869, psychiatric treatment for insomnia involved the use of chloral hydrate as a soporific. Then, in the early 1900s we had the emergence of barbiturates, with chemical substitutions allowing derivative compounds. And even though it was the most effective drug family at that time, meaning it had less side-effects and was less toxic, it was dangerous in overdose.
Benzodiazepines and Quinazolinones were introduced during the 1970s and were considered safer alternatives to barbiturates; with benzodiazepines emerging in the late 1970s as a safer drug. Of course, benzodiazepines have their own drawbacks, and these include the possibility of substance dependence, and the fact that death can occur from overdose – particularly when used in combination with other depressants and/or alcohol. In addition, questions have been raised as to whether benzodiazepines disturb sleep architecture.
The most recent development comes with non-benzodiazepines, and although it’s obvious that they’re less toxic than barbiturates, their efficiency over benzodiazepines hasn’t yet been established. It would be hard to determine this without longitudinal studies, but some psychiatrists are recommending these drugs because they believe they’re just as potent, but without the potential for abuse.
There are other sleep remedies that might be considered sedative-hypnotics, with psychiatrists often prescribing off-label medicines with sedating effects. Some examples of these include Quetiapine (an antipsychotic), Clonidine (often prescribed to regulate blood pressure), Mirtazapine (an antidepressant), and Diphenhydramine (an over-the-counter sleep aid known as Benadryl, which is an antihistamine). In certain instances, for example where patients have a history of substance abuse, off-label sleep remedies can be especially useful, particularly when first-line treatment is deemed unsafe or has proven unsuccessful.
Barbiturates are drugs: they act as a depressant of the central nervous system and, as such, can produce a wide range of effects, from relatively mild sedation through to complete anesthesia. They’re also effective as hypnotics, anxiolytics, and anti-convulsants. Barbiturates do have analgesic effects, but because the effects are quite weak it means that barbiturates can’t be used in surgery when other analgesics are unavailable. In addition, they have both physical and psychological dependence liability. In today’s routine medical practices, barbiturates have largely been replaced by benzodiazepines, in the treatment of insomnia and anxiety, for example, mostly because when it comes to overdose, benzodiazepines are much less dangerous. Barbiturates are derivatives of barbituric acid, and today, barbiturates are still used for epilepsy, general anesthesia, and assisted suicide.
The positive allosteric modulation of GABA receptors is believed to be barbiturates’ principal mechanism of action. Examples include Pentobarbital, Amobarbital, Phenobarbital, Sodium Thiopental, and Secobarbital.
Quinazolinones are another class of drugs containing a 4-quinazolinone core which function as hypnotic sedatives. Interestingly, it’s been proposed to use these drugs in the treatment of cancer.
Examples of quinazolinone drugs include Diproqualone, Cloroqualone, Mebroqualone, Etaqualone (Aolan, Athinazone, Ethinazone), Methaqualone (Quaalude), and Mecloqualone (Nubarene, Casfen).
Benzodiazepines can be very helpful for the short-term treatment of insomnia; however, due to the risk of dependence, it’s not recommended they be used beyond 2 to 4 weeks. In fact, Benzodiazepines should be used at the lowest effective dose and be taken intermittently. These drugs improve sleep-related problems by reducing wakefulness, shortening the length of time in bed prior to falling asleep, and prolonging sleep time. Very like alcohol, these drugs worsen sleep in the long term, so are typically used to treat short term insomnia: this includes both self-medicated and prescribed. Benzodiazepines can certainly put people to sleep by inhibiting NREM Stage I and 2 sleep; however, whilst the person is asleep the drugs disrupt sleep architecture, meaning they delay time to REM sleep, decrease sleep time, and decrease deep slow-wave sleep, which is the most important part of sleep when it comes to mood and energy. Other negatives of hypnotics, and this includes Benzodiazepines, include rebound insomnia, possible tolerance to their effect, reduced slow-wave sleep, and withdrawals, which may come in the form of insomnia, together with an extended period of agitation and anxiety.
In most countries, the list of Benzodiazepines approved for the treatment of insomnia is quite similar; however, the Benzodiazepines officially designated as first-line hypnotics when treating insomnia in different countries can vary a lot.
Some Benzodiazepines are typically not recommended, and these are the longer acting drugs like Diazepam and Nitrazepam, because their residual effects could well persist into the next day. It’s not known whether Z Drugs, the new non-benzodiazepine hypnotics, are more effective than the short-acting Benzodiazepines; however, the efficacy of these two medication groups is very similar.
The United States Agency for Healthcare Research and Quality stated that indirect comparisons suggest that benzodiazepine side-effects could be about twice as frequent as side-effects with non-benzodiazepines. It’s been suggested by some experts that non-benzodiazepines should be used as a first-line long-term treatment for insomnia. On the other hand, the NICE (United Kingdom National Institute for Health and Clinical Excellence) found no convincing evidence in favor of Z Drugs. Their review stated that, in clinical trials, short-acting Z Drugs were wrongly compared with Benzodiazepines (long-acting). In fact, no trials have been conducted which compared Z Drugs (short-acting) with relevant doses of Benzodiazepines (also short-acting); so, based on this fact, it was NICE’s recommendation that the hypnotic be chosen based on the patient’s preference, and cost.
Regarding older adults, unless other treatments have been ineffective, their insomnia should not be treated using Benzodiazepines; and if these drugs are used, then a discussion should occur between the physician, the patient themselves, and their caregiver, regarding the increased risk of harm. This increased risk includes evidence of falls and hip fracture among older patients, and twice the incidence of traffic accidents with patients who drive.
Non-benzodiazepines are a form of psychoactive drug; in nature, they’re very ‘benzodiazepine-like’. The pharmacodynamics of non-benzodiazepines are almost the same as benzodiazepines, and employ the same side-effects, benefits, and risks. However, non-benzodiazepines have very different chemical structures; which means that, on a molecular level, they’re unrelated to benzodiazepines. Examples include Eszopiclone (Lunesta), Zopiclone (Imovane, Zimovane), Zolpidem, (Stilnox, Ambien, Stilnoct), and Zaleplon (Sonata).
Even though research on non-benzodiazepines is new, it’s also conflicting. A team of researchers reviewing these drugs recommend their use by people who have trouble falling asleep, but not staying asleep. This is because there were minimal next-day impairments. They noted that these drugs were safe; however, more research was called for into long-term effectiveness when treating insomnia. Another team of researchers suggested that tolerance may be slower to develop with non-benzodiazepines than with benzodiazepines; and this team was quite skeptical, saying they found little benefit over benzodiazepines.
Among other functions, melatonin promotes sleep in diurnal mammals: melatonin is a hormone that’s produced in the brain, in the pineal gland. This hormone is secreted in darkness and in dim light. Because of its hypnotic properties, melatonin is available over-the-counter in many countries, and on prescription in others. A timed-release version of melatonin, Circadin®, was approved in Europe in the year 2007 for use as a primary insomnia treatment. Then, in the early 21st century, melatonin receptor agonists that bind to and activate melatonin receptors were developed. Ramelteon, TIK-301, Agomelatine, and Tasimelteon were prescribed for several sleep disorders. In the United States, Ramelteon (Rozerem®) was approved for the treatment of insomnia in the year 2005. In Europe, Agomelatine (Thymanax®, Melitor®, and Valdoxan®,) primarily used for depression, were approved in 2009. TIK-301 was approved in the United States in the year 2004, with Tasimelteon (Hetlioz®) being approved 10 years later for totally blind people suffering from the circadian rhythm sleep disorder, Non-24 Hour Sleep-Wake Disorder.
The term antihistamine commonly refers to compounds that only inhibit action at the H1 receptor, not H2, and so on. Clinically, certain allergies can be treated using H1 antagonists. A common side-effect of antihistamines is sedation, and some H1 antagonists, such as Doxylamine and Diphenhydramine (Benadryl) can also be used in the treatment of insomnia.
When compared to Benzodiazepines, which decrease the quality of sleep, some antidepressants have a sedating effect; while others may actually increase the quality of sleep.
Below are some examples of anti-psychotics which have sedation as a side effect:
© 2020 American Sleep Association.