Gina Johnson
Sleep is an essential part of a healthy life, and for those who struggle with sleep, there are a variety of sleeping pills available. Sleeping pills can be either prescription or over-the-counter, with prescription pills generally being stronger. Sleeping pills work by enhancing the effects of a neurotransmitter called gamma-aminobutyric acid (GABA) in the brain, which has a calming effect that can reduce anxiety and promote sleep. The strongest non-narcotic sleeping pills are typically considered to be benzodiazepine receptor agonists, also called Z drugs, and include eszopiclone (Lunesta), zolpidem (Ambien), and zaleplon (Sonata). These medications are prescription-only and are classified as Schedule IV controlled substances.
| Characteristics | Values |
|---|---|
| Drug Name | Doxepin (Silenor)Ramelteon (Rozerem)Eszopiclone (Lunesta)Zolpidem (Ambien)Zaleplon (Sonata)Lemborexant (Dayvigo)Dardorexant (Quviviq)Suvorexant (Belsomra)Estazolam (Prosom) |
| Availability | Prescription-only Prescription-only Prescription-only Prescription-only Prescription-only Prescription-only Prescription-only Prescription-only |
| Usage | Short-termLong-termShort-termShort-termShort-termN/AN/AN/A |
| Benefits | Helps with staying asleepLow risk of misuse and dependencyLong-term treatment for insomniaN/AN/AN/AN/AHelps with falling and staying asleep |
| Side Effects | CNS depressionAllergic reactionsSleepwalking, driving while asleep, impaired CNS, increased risk of suicideN/AN/AN/AN/AEdema, increased thoughts of suicide |
| Precautions | Avoid for pregnant/nursing women, children, glaucoma, urinary retention patientsAvoid for people with reduced liver function, older people, those with mental health issuesN/AN/AN/AN/ALimit alcohol consumption |
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What You'll Learn
Prescription vs. over-the-counter sleeping pills
Sleeping pills can be purchased over the counter or with a prescription, and they come in various strengths. The choice of a strong sleeping pill should always be tailored to individual circumstances, and it is recommended to consult a healthcare provider before starting any sleep aid.
Prescription sleeping pills are generally stronger than over-the-counter options. Providers may recommend prescription sleeping pills for short-term relief, but they are typically not recommended for long-term use due to the risk of dependence and addiction. Benzodiazepines, for example, are prescription sleeping pills that work by stimulating a chemical in the brain called GABA, which leads to sedation, muscle relaxation, and reduced anxiety. However, they are classified as Schedule IV controlled substances due to their potential for physical dependence, misuse, withdrawal, and addiction. Other prescription sleeping pills include non-benzodiazepine hypnotic sedatives like zolpidem (Ambien) and eszopiclone (Lunesta), which are also classified as Schedule IV controlled substances. Ramelteon (Rozerem) is another prescription option and is the only FDA-approved melatonin receptor agonist for treating insomnia. It is not a controlled substance as it has not been proven to have the potential for misuse and addiction.
Over-the-counter sleeping pills are available without a prescription and can be purchased at pharmacies or online. They are typically not as strong as prescription sleeping pills, but they can still be effective for some people. Melatonin supplements, for example, are widely available over the counter and can be helpful for regulating the sleep-wake cycle, especially in cases of jet lag. Other over-the-counter options include antihistamines such as diphenhydramine (Benadryl) and doxylamine (Unisom), which work by blocking histamines that cause alertness. While over-the-counter sleeping pills may be more convenient to access, it is still important to consult a healthcare provider before taking them, as they can also cause side effects similar to prescription sleeping pills, including constipation, diarrhoea, and muscle weakness.
In summary, prescription sleeping pills are generally stronger than over-the-counter options, but they also carry a higher risk of dependence and addiction. Over-the-counter sleeping pills can be effective for milder sleep issues or regulating the sleep-wake cycle, but they may not be sufficient for more severe or chronic insomnia. It is important to consult a healthcare provider to determine the most appropriate treatment based on individual needs and circumstances.
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Antidepressants as sleep aids
While antidepressants can improve mood, they can also worsen sleep, and poor sleep is both a symptom and a cause of depression. However, certain antidepressants can be used as sleep aids, particularly for patients with insomnia and depression. The right antidepressant can improve sleep architecture and sleep quality.
Doxepin (Silenor) is the only FDA-approved antidepressant for the treatment of insomnia. It produces sedating effects at low doses and helps people stay asleep. It is generally taken immediately before bedtime and has a quick onset of action. Doxepin is the only antidepressant that is not a controlled substance. Other tricyclic antidepressants such as amitriptyline, nortriptyline, and trimipramine have been prescribed off-label for treating insomnia but are rare due to their many potential side effects.
Mirtazapine and trazodone are two antidepressants that help patients fall asleep and improve their sleep architecture. Bupropion is also favourable for sleep, causing no more insomnia than SSRIs and having neutral or positive effects on sleep architecture. Quetiapine (Seroquel) has sedative effects and improves the deep, restorative phase of sleep. However, it carries too many risks to be recommended for primary insomnia.
While SSRIs can worsen insomnia and sleep quality, they may be beneficial for treating sleep apnea. They suppress REM sleep, which is when most apneas occur, and can also improve sleep apnea through direct effects on smooth muscle in the upper airway. However, they are not recommended for restless legs syndrome (RLS) as they can cause or worsen the condition. Instead, RLS can be treated with bupropion or pramipexole, an FDA-approved medication that can also treat depression.
It is important to note that antidepressants as sleep aids should generally be avoided in people without a diagnosis of depression. This is because the duration of sedative effects in these medications is shorter than other sleep aids, and the potential side effects may cause more risk than benefit.
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Benzodiazepine receptor agonists
Eszopiclone is a nonbenzodiazepine hypnotic pyrrolopyrazine derivative of the cyclopyrrolone class. Its precise mechanism of action is unknown, but it is believed to interact with GABA receptors close to or allosterically coupled to benzodiazepine receptors. It is indicated for insomnia to decrease sleep latency and improve sleep maintenance. It has a short half-life of 6 hours, with a starting dose of 1 mg taken immediately before bedtime, and at least 7-8 hours remaining before awakening. The dose may be increased to 2-3 mg for nonelderly adults, and 2 mg for elderly or debilitated patients.
Zaleplon is a nonbenzodiazepine receptor agonist with selectivity for GABAA receptors containing the α1 subunit, producing fewer adverse effects than non-selective BZRAs. It is approved for short-term use for the treatment of insomnia.
Ramelteon (Rozerem) is the only FDA-approved prescription melatonin receptor agonist for the treatment of insomnia. It is not a controlled substance as it has not been proven to have potential for misuse and addiction. It has high selectivity for human melatonin MT1 and MT2 receptors, which are thought to promote sleep and are involved in the maintenance of the circadian rhythm and normal sleep-wake cycle. It is indicated for insomnia characterised by difficulty with sleep onset.
While benzodiazepine receptor agonists are effective in treating insomnia, a study examining response and remission rates in patients with insomnia found that while many patients responded to chronic BzRA treatment, most did not remit. Remission rates were particularly low for comorbid insomnia, which is the most prevalent phenotype of the disorder.
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Orexin receptor antagonists
There are two types of orexins: orexin A and orexin B, which fit into two types of receptors: orexin receptor type 1 (Ox1R) and orexin receptor type 2 (Ox2R). Orexin receptor antagonists can block one or both orexin receptors. Dual orexin receptor antagonists (DORAs) are a subcategory that can block both Ox1R and Ox2R. DORAs tend to be well tolerated and work quickly to treat insomnia. They are considered safer than benzodiazepines and nonbenzodiazepines.
Three orexin receptor antagonists have been approved by the FDA for the treatment of insomnia: suvorexant (Belsomra), lemborexant (Dayvigo), and daridorexant (Quviviq). These medications have been classified as Schedule IV controlled substances and require a prescription. Suvorexant is available in 5-, 10-, 15-, and 20-mg tablets, with a starting dosage of 10 mg taken within 30 minutes before bedtime. If 10-mg dosing is ineffective, the dosage can be increased to a maximum of 20 mg once daily. Lemborexant has a half-life of 17 to 55 hours, while daridorexant has a half-life of 6 to 10 hours.
Side effects of orexin receptor antagonists include somnolence, daytime sleepiness and sedation, headache, abnormal dreams, fatigue, and dry mouth. Narcolepsy, a neurological disorder caused by orexin deficiency, is a contraindication for the use of orexin antagonists.
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Natural sleep aids
While there are prescription and over-the-counter sleeping pills available, natural sleep remedies can also help improve your sleep. Natural sleep aids are over-the-counter supplements that help you fall asleep faster or stay asleep throughout the night. They are usually plant-based, vitamins or minerals, or supplemental amounts of something produced by the body.
- Melatonin: This is a hormone that is naturally released in the brain four hours before we feel sleepy. It is triggered by the body's response to reduced light exposure, which should naturally happen at night. However, exposure to unnatural light from phones, laptops, or TVs can prevent its release, making it hard to fall asleep. Melatonin supplements are available over the counter and have become a popular sleep aid. They have been found to reduce the time it takes for people to fall asleep and improve overall sleep quality. However, melatonin can reduce the effectiveness of some medications and cause unwanted side effects when combined with others. It may not be recommended for people who have received organ transplants, experience depression, or have a bleeding or seizure disorder.
- Magnesium and Valerian Root: These supplements have also been found to promote better sleep.
- CBD and THC: Some studies suggest that THC and CBD, alone or in combination, help some people fall asleep, stay asleep, and enjoy higher-quality sleep. CBD has also been found to relieve anxiety, which can help improve sleep quality. However, marijuana and products containing THC can create dependence, and withdrawal from them can aggravate sleep problems. CBD is also not recommended for people who are pregnant or nursing and is classified as a controlled substance in some states.
- Lavender: This plant-based supplement can help promote sleep.
Other natural sleep aids include warm milk, chamomile tea, and tart cherry juice. While there isn't much scientific proof that these drinks improve sleep, they are still worth trying as they do not have side effects or drug interactions.
It is important to consult your doctor before starting any new supplement, as natural does not always mean safe for everyone. Many supplements should not be taken by people with certain allergies, conditions, or those taking other medications. Additionally, natural sleep aids are not strictly regulated, and the Food and Drug Administration does not verify their safety, efficacy, or labeling.
Apart from natural sleep aids, there are other ways to improve your sleep:
- Avoid working out within two hours of bedtime.
- Avoid the use of smartphones or other electronic devices before bed, as the light from the screen can interfere with sleep. If you need to get up at night, use a flashlight instead of turning on the lights.
- Sleep in layers so you can adjust your bedtime temperature as needed.
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Frequently asked questions
Sleeping pills are usually prescribed by doctors depending on the type of insomnia and the patient's circumstances. There is no one-size-fits-all solution. However, some common non-narcotic sleeping pills include:
- Ramelteon (Rozerem)
- Doxepin (Silenor)
- Eszopiclone (Lunesta)
- Zolpidem (Ambien)
- Zaleplon (Sonata)
Ramelteon is a melatonin receptor agonist that promotes sleep and positively affects circadian rhythms. It is the only FDA-approved prescription melatonin receptor agonist for treating insomnia. It is not a controlled substance and has a low risk of misuse and addiction.
Doxepin is a tricyclic antidepressant that is FDA-approved for treating insomnia characterised by difficulty staying asleep. It is available as an immediate-release tablet in 3 and 6 mg doses. It is not recommended for those taking monoamine oxidase inhibitors or people with glaucoma or urinary retention.
Eszopiclone is a nonbenzodiazepine prescription sleep aid. It is approved for the long-term treatment of insomnia. However, it may cause complex sleep behaviours such as sleepwalking or driving while asleep. It can also impair the central nervous system (CNS), making tasks like driving dangerous.
Zolpidem is a nonbenzodiazepine prescription sleep aid. It is available in sublingual form, which dissolves quickly under the tongue and is meant for those who wake up halfway through the night.
Zaleplon is a nonbenzodiazepine prescription sleep aid commonly used to help people fall asleep, especially if they do not have chronic insomnia.
