
Sleeping pills are medications that can help with sleep difficulties and insomnia. They are available over the counter (OTC), as natural supplements, or by prescription. OTC sleep aids often contain antihistamines, which block histamines in the body that cause alertness. Common antihistamines include diphenhydramine and doxylamine succinate, which is found in Unisom SleepTabs. Natural sleep aids may contain melatonin, a hormone that promotes sleep, or valerian, an herb that aids relaxation. Prescription sleeping pills include benzodiazepines, which stimulate the GABA chemical in the brain, leading to sedation and reduced anxiety, and Z-drugs, which are used to treat severe insomnia and have generic names beginning with the letter 'Z', such as zolpidem and zopiclone.
| Characteristics | Values |
|---|---|
| OTC sleeping pills | antihistamines (e.g. diphenhydramine, doxylamine succinate) |
| Natural sleep aids | melatonin, valerian |
| Prescription sleep medications | Benzodiazepines, Z-drugs (zolpidem, zopiclone) |
| Side effects | constipation, muscle weakness, hangover effect, drowsiness, dry mouth, dizziness, memory problems |
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What You'll Learn
- Antihistamines, like diphenhydramine and doxylamine succinate, block histamines to induce drowsiness
- Melatonin is a hormone that promotes sleep
- Valerian is an herb that aids relaxation
- Benzodiazepines stimulate GABA, causing sedation and muscle relaxation
- Z-drugs, like Zolpidem, are short-acting and less likely to cause a hangover effect

Antihistamines, like diphenhydramine and doxylamine succinate, block histamines to induce drowsiness
Antihistamines, such as diphenhydramine and doxylamine succinate, are a common ingredient in over-the-counter (OTC) sleeping pills. They work by blocking histamines, which are substances in the body that cause alertness. As bedtime approaches, histamine levels in the brain decrease, facilitating non-rapid eye movement sleep (NREM). Antihistamines mimic this natural process by crossing the blood-brain barrier and blocking histamines, thereby inducing drowsiness.
Diphenhydramine is a versatile medication used to treat allergies, insomnia, and cold symptoms. It is widely available over the counter under various brand names, as well as lower-cost generics. While diphenhydramine can effectively induce drowsiness, it may also cause next-day drowsiness as a side effect. It is important to carefully follow the package instructions and avoid long-term use without consulting a healthcare provider.
Doxylamine succinate, another type of antihistamine, is also used to aid sleep. It is commonly found in nighttime cold medications. Doxylamine has a longer half-life than diphenhydramine, remaining in the body for a more extended period. Consequently, doxylamine may be more likely to cause next-day drowsiness. Similar to diphenhydramine, doxylamine is intended for short-term use and should not be taken continuously without medical advice.
Both diphenhydramine and doxylamine are first-generation antihistamines, which tend to cause significant drowsiness. While these antihistamines can be helpful for short-term sleep difficulties, they may not be recommended for chronic insomnia. Additionally, long-term use of these medications may increase the risk for dementia and Alzheimer's disease. It is advisable to consult a healthcare professional for guidance on safe and effective sleep aids, including alternatives such as melatonin, good sleep hygiene, and cognitive behavioral therapy.
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Melatonin is a hormone that promotes sleep
Sleeping pills are medications that can help with sleep difficulties, which become more common as people age. They are available over the counter (OTC), as natural supplements, or by prescription. Over-the-counter sleep aids often contain antihistamines, which block histamines in the body that cause alertness. Common antihistamines include diphenhydramine and doxylamine succinate, which is the active ingredient in Unisom SleepTabs. However, antihistamines can have side effects like daytime drowsiness, dry mouth, dizziness, and memory problems.
The production of melatonin in the body is influenced by exposure to light and darkness. Typically, melatonin levels begin to rise in the evening when it gets dark, signalling to the body that it's time to prepare for sleep. During the night, while we sleep, melatonin production remains high. As the sun rises and daylight increases, melatonin levels gradually decrease, helping the body prepare for waking up and becoming alert.
Supplemental melatonin is often recommended for individuals with sleep issues due to their body's irregular production of melatonin. For example, those with insomnia may not produce enough melatonin or may produce it at irregular times, disrupting their sleep-wake cycles. By taking melatonin supplements, individuals can help regulate their sleep patterns and improve their overall sleep quality.
It is important to note that while melatonin is a natural hormone, taking melatonin supplements may still have side effects. It is always advisable to consult a healthcare professional before taking any sleep aids or supplements, even if they are available over the counter. Additionally, it is generally recommended to use sleeping pills or sleep aids for a short period, typically not exceeding three weeks, to avoid potential long-term side effects.
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Valerian is an herb that aids relaxation
Valerian (Valeriana officinalis) is an herb native to Europe and parts of Asia. It is commonly used to promote relaxation and sleep. Valerian has a long history as a sedative, dating back to ancient Greek and Roman times. The herb has a strong odour and can grow to just over six feet tall.
Valerian root is renowned as a natural sleep aid, and it has been shown to improve sleep quality. It is often used to treat insomnia and is thought to have a calming effect on the nervous system. In one study, participants who took 530mg of valerian root one hour before bedtime for one month reported higher-quality sleep than those who took a placebo. Continuous use for up to four weeks may be needed before the effects are noticeable. It is typically taken in doses of 300-600mg by mouth daily for up to six weeks.
Valerian is also used to treat anxiety and stress, although there is limited scientific evidence to support these uses. It is often used in combination with other sedative herbs, such as hops, passion flower, and lemon balm. However, long-term use of valerian may lead to dependence, and withdrawal symptoms may occur upon cessation.
Although valerian is generally considered safe, rare cases of liver injury have been associated with its use, especially when combined with other herbs. It should not be taken during pregnancy or breastfeeding and should not be given to children or teenagers without medical supervision. As with any herbal supplement, it is important to consult a healthcare professional before taking valerian to ensure it is safe and appropriate for your individual needs.
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Benzodiazepines stimulate GABA, causing sedation and muscle relaxation
Sleeping pills are medications that can help with sleep. They are available over the counter (OTC), as natural supplements, or by prescription. Prescription sleep medications work differently from OTC medications. Benzodiazepines, a class of drugs, are one such prescription medication. They work by stimulating a neurotransmitter called GABA (gamma-aminobutyric acid) at the GABAA receptor. This stimulation enhances GABA's inhibitory activity, reducing the output of excitatory neurons in the brain.
GABA is the chief inhibitory neurotransmitter in the mammalian central nervous system. It plays a crucial role in reducing neuronal excitability. When the nervous system is overly active, GABA acts as a "brake" to calm and slow it down. By binding to specific sites called GABA-A receptors on the receiving neuron, GABA sends inhibitory signals that lead to sedation and muscle relaxation.
Benzodiazepines interact with these GABA-A receptors, acting as a booster to enhance GABA's function. This interaction allows more negative chloride ions to enter the neuron, making it less responsive to excitatory neurotransmitters such as norepinephrine, serotonin, acetylcholine, and dopamine. As a result, benzodiazepines produce sedative, hypnotic (sleep-inducing), anxiolytic (anti-anxiety), anticonvulsant, and muscle relaxant effects. These properties make them useful in treating various conditions, including anxiety, panic disorders, insomnia, seizures, and muscle spasms.
While benzodiazepines can be effective in the short term, they may cause tolerance, dependence, and withdrawal symptoms with prolonged use. They can also lead to cognitive impairments, memory issues, and adverse effects on mood and behaviour. Additionally, benzodiazepines have binding sites in the periphery, such as in immune cells and the gastrointestinal tract, but their muscle relaxation effects are not mediated through these peripheral receptors.
In summary, benzodiazepines stimulate GABA, causing sedation and muscle relaxation by enhancing GABA's inhibitory activity in the brain and allowing the nervous system to calm down. This stimulation results in a range of effects, including sedation, anxiety reduction, and muscle relaxation, making benzodiazepines a clinically useful medication for various disorders. However, their long-term use should be approached with caution due to potential side effects and the risk of dependence and withdrawal.
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Z-drugs, like Zolpidem, are short-acting and less likely to cause a hangover effect
Sleeping pills are medications that can help with sleep. They are available over the counter (OTC), as natural supplements, or by prescription. OTC sleeping pills often contain antihistamines, which work by blocking histamines—the substances that cause alertness in the body. Common antihistamine ingredients include diphenhydramine and doxylamine. Natural sleep aids may contain melatonin, a hormone that promotes sleep, or valerian, an herb that has a calming effect on the nervous system.
Prescription sleep medications work differently. For example, Benzodiazepines stimulate GABA, a chemical in the brain that leads to sedation, muscle relaxation, and reduced anxiety.
Z-drugs, like Zolpidem, are short-acting prescription medications used to treat insomnia. They work by slowing down the activity in the brain and increasing the activity of GABA, a natural chemical that helps the body relax. Zolpidem is available as Ambien, Ambien CR, Edluar, and generic zolpidem. It is meant to be taken orally and should be stored at room temperature. Zolpidem is fast-acting and should only be used for short periods, such as one or two days, and for no longer than one or two weeks. It is also available as a sublingual tablet, which should be placed under the tongue to dissolve.
Zolpidem may cause side effects such as dizziness, drowsiness, and memory loss. It may also worsen depression and cause suicidal thoughts or actions in rare cases. It is important to note that Zolpidem may cause a hangover effect the next day, especially if taken with less than a full night's sleep or with alcohol. However, compared to Benzodiazepines, Z-drugs like Zolpidem are less likely to cause a hangover effect due to their shorter half-life.
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Frequently asked questions
OTC sleeping pills often contain antihistamines, which block histamines in the body that cause alertness. Common antihistamines found in sleeping pills include diphenhydramine and doxylamine succinate.
Prescription sleeping pills include benzodiazepines and non-benzodiazepines, also known as Z-drugs. Zolpidem and zopiclone are examples of Z-drugs currently licensed for prescription in the UK.
Natural sleep aids often contain melatonin, a hormone that promotes sleep, or valerian, an herb that aids relaxation and sleep.
Sleeping pills may contain inactive ingredients such as anhydrous dibasic calcium phosphate, magnesium stearate, and microcrystalline cellulose. These inactive ingredients vary depending on the specific product and brand.























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