Ashwin Lewis
Sleeping pills are prescription medications that contain tranquilizers to treat insomnia, restless sleep, or difficulty falling asleep. They are available over the counter (OTC) and by prescription. OTC sleep aids often contain antihistamines, which can cause drowsiness, while prescription sleeping pills are stronger and work in different ways. Benzodiazepines, for instance, stimulate the GABA neurotransmitter in the brain, causing sleepiness, muscle relaxation, and reduced anxiety. Z-drug sleeping pills, such as zolpidem (Ambien) and eszopiclone (Lunesta), slow down brain activity. While short-term use of sleeping pills is acceptable, they are not recommended for long-term use due to the risk of dependency and addiction, as well as potential side effects such as constipation, muscle weakness, and dizziness.
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What You'll Learn
Benzodiazepines
Some types of benzodiazepines include alprazolam (Xanax), clonazepam (Klonopin), diazepam (Diastat, Valium), estazolam (Prosom), orazepam (Ativan), and temazepam (Restoril). These drugs are widely used, with an estimated 30.5 million people in the US taking benzodiazepines in a 12-month period between 2014 and 2015.
While benzodiazepines can be effective in treating sleep disorders, they are typically prescribed for short-term use due to the risk of dependence and addiction. They can also cause various side effects, including amnesia, hostility, irritability, and vivid or disturbing dreams, as well as constipation, muscle weakness, and a hangover effect the next day, with feelings of drowsiness and muddled thinking.
It is important to note that lower doses of benzodiazepines may also be used during the day to help calm anxiety, while higher doses of long-acting benzodiazepines are typically used for treating anxiety disorders.
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Antidepressants
Trazodone is an example of an SSRI antidepressant. It was developed in Italy in the 1960s and was initially unpopular due to its negative side effects, such as dizziness, fainting, and irregular heartbeat. However, at lower doses, trazodone has sedative effects, inducing relaxation and sleepiness. It is now commonly prescribed as a sleep aid for patients with insomnia and is considered non-addictive.
Doxepin (Silenor) is a tricyclic antidepressant that is FDA-approved for treating insomnia characterized by difficulty staying asleep. Other tricyclic antidepressants, such as amitriptyline and nortriptyline, have also been prescribed off-label for insomnia but are less common due to their many potential side effects. Tetracyclic antidepressants, which are older drugs, are generally safe and not considered addictive, although they may cause unpleasant side effects like nausea, sweating, and flu-like symptoms.
It is important to note that while antidepressants can be effective in treating sleep disorders, they are intended for short-term use. Over-prescription can lead to unhealthy long-term habits, and patients may become dependent on these medications. Additionally, combining antidepressants with alcohol or illicit substances can be dangerous and, in some cases, fatal. Therefore, it is crucial to be open and honest with your doctor about your medical history and any substance use.
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Antihistamines
OTC sleep aids containing antihistamines are easily accessible without a prescription for anyone over the age of 18. However, it is recommended to check with a healthcare provider before taking them, as they can interfere with other medications or aggravate existing health conditions.
Prescription sleeping pills, on the other hand, are typically stronger than OTC options. They are usually recommended for short-term relief due to the risk of dependence and addiction. Examples of prescription sleeping pills include benzodiazepines, Z-drugs like zolpidem (Ambien) and eszopiclone (Lunesta), and barbiturates.
It is important to note that sleeping pills, whether OTC or prescription, can cause side effects such as constipation, diarrhoea, and muscle weakness. Approximately 8 out of 10 people experience a "hangover" effect the day after taking sleep medicine, feeling drowsy and having difficulties with thinking clearly, dizziness, and balance. Therefore, caution should be exercised when taking any sleep medication, and it is always best to consult a healthcare professional for personalized advice and recommendations.
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Orexin receptor antagonists
This class of drugs has several benefits over traditional sleep medications. For example, they do not modulate the activity of γ-aminobutyric acid receptors, which are the main inhibitory mechanism of the central nervous system. This means that orexin receptor antagonists may have fewer side effects and could be suitable for longer-term treatment. Additionally, they have been shown to improve various sleep parameters, including latency to persistent sleep, wake after sleep onset, sleep efficiency, total sleep time, and sleep quality.
Some examples of orexin receptor antagonists include suvorexant (Belsomra), daridorexant (nemorexant; Quviviq), and lemborexant (Dayvigo). These drugs have different elimination half-lives, ranging from 6 to 55 hours, and their pharmacokinetics may be influenced by factors such as age, sex, and obesity. While orexin receptor antagonists have been shown to be effective in treating insomnia, they may also cause side effects such as somnolence, daytime sleepiness, sedation, headache, abnormal dreams, fatigue, and dry mouth.
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Non-benzodiazepine (Non-BZD) or Z-drugs
Non-benzodiazepine or Z-drugs are commonly prescribed for insomnia and sleep initiation and maintenance. They are structurally different from benzodiazepines as they selectively bind to the alpha-1 subunit of the GABAA receptor, leading to sedation with a narrower side-effect profile. Z-drugs include zolpidem, zaleplon, zopiclone, and eszopiclone, which vary in efficacy and side effects due to differences in pharmacokinetic profiles.
Z-drugs have a faster onset and clearance than benzodiazepines, making them useful for treating insomnia without causing daytime sedation. Zolpidem, for example, is available in oral tablets, oral spray, and sublingual formulations for initial insomnia, while an extended-release version is approved for middle insomnia and a sublingual low-dose formulation. Zaleplon, the shortest-acting Z-drug, is also indicated for sleep initiation following middle-of-the-night awakenings. It has been found to have no association with increased motor vehicle accidents, even when taken for insomnia during the night.
Despite their benefits, Z-drugs are associated with adverse effects such as cognitive impairments, amnesia, hallucinations, and an increased risk of falls in older adults. Higher doses or concurrent use with other CNS depressants may lead to sleepwalking, sleep-driving, and other undesirable sleep-related behaviours. Z-drugs can accumulate in the body if the elimination half-life is long and with frequent use, resulting in increased side effects. They are not recommended for long-term use due to concerns about tolerance, dependence, and withdrawal symptoms upon abrupt discontinuation.
Z-drugs have been found to impair physical and cognitive performance, with detrimental effects on motor function, balance, attention, memory, and processing speed. While some research suggests that Z-drugs can enhance sleep architecture and positively impact memory performance, the majority of evidence highlights negative effects on cognitive performance.
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Frequently asked questions
There are various drugs used in sleeping pills, and they are typically prescribed by a doctor for short-term use. The main types of drugs in sleeping pills are:
- Benzodiazepines (benzos)
- Z-drugs
- Antidepressants
- Antihistamines
- Anticonvulsants
Benzodiazepines (BZD) are a powerful class of sleeping pills that help you fall asleep, relieve anxiety, and improve your learning and memory. Examples of benzodiazepines include alprazolam (Xanax), clonazepam (Klonopin), diazepam (Valium), and lorazepam.
Z-drugs, such as zolpidem (Ambien) and eszopiclone (Lunesta), are fast-acting sleeping pills that take effect within 30 minutes and can last up to 8 hours. They work by slowing down brain activity.
Yes, OTC sleeping pills are typically milder and contain antihistamines, which cause drowsiness by blocking histamines that induce alertness. Prescription sleeping pills, on the other hand, are stronger and may contain a variety of different drugs, including benzodiazepines and Z-drugs.
Yes, some people opt for natural remedies such as melatonin and valerian supplements. Melatonin is a hormone naturally produced by the body that promotes sleep, while valerian is an herb that is believed to aid relaxation and sleep.
