Ashwin Lewis
Sleep is regulated by chemicals that are naturally produced by the human body. As one gets ready for sleep, histamine levels in the brain decrease, inducing non-rapid eye movement sleep (NREM). Antihistamines, such as diphenhydramine and doxylamine succinate, block histamine release and cross the blood-brain barrier, mimicking this natural function. This is why antihistamines can make people feel sleepy, and some over-the-counter sleeping pills contain them. However, antihistamines are not recommended as a long-term solution for insomnia due to their side effects and potential risks, including an increased risk for dementia and Alzheimer's disease. Instead, experts recommend cognitive behavioral therapy (CBT), good sleep hygiene, and natural sleep aids like melatonin.
| Characteristics | Values |
|---|---|
| Are sleeping pills antihistamines? | Most over-the-counter sleeping pills contain antihistamines. |
| How do antihistamines work? | Antihistamines block histamines, which are substances in your body that cause alertness. |
| What are common antihistamines? | Diphenhydramine, doxylamine succinate, and Benadryl. |
| Are antihistamines safe for sleep? | No, antihistamines are not recommended for long-term use as they can have side effects such as dizziness, altered mental state, urinary retention, and dry mouth. They can also increase the risk of dementia and Alzheimer's disease. |
| What are some alternatives to antihistamines for sleep? | Cognitive behavioral therapy (CBT), melatonin, good sleep hygiene, and prescription sleep medications. |
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What You'll Learn
Antihistamines and sleep aids
Antihistamines are drugs that block histamines, which are substances in your body that cause alertness. As you get ready for sleep, histamine levels in the brain decrease, inducing non-rapid eye movement sleep (NREM). Antihistamines, such as diphenhydramine and doxylamine succinate, cross the blood-brain barrier, mimicking this natural function. This is why you may feel sleepy when you take medications containing them.
Many over-the-counter sleep aids are simply antihistaminic drugs repackaged and labelled as something to help you achieve sleep. However, while they may help you fall asleep, they do not improve overall sleep quality. Furthermore, they have no long-term benefits, and most people develop a tolerance to them very quickly. They also carry the risk of side effects such as an altered mental state, urinary retention, and dry mouth, and can lead to sleepwalking and other parasomnias. Due to these risks, the American Academy of Sleep Medicine (AASM) has officially recommended against treating chronic insomnia with common over-the-counter antihistamine sleep aids.
Instead, experts recommend cognitive behavioural therapy (CBT) as a first-line treatment for insomnia. CBT focuses on sleep hygiene and strengthening the bed-sleep connection. It helps adjust circadian rhythm and reduces anxiety about insomnia. Other natural sleep aids that may be considered include melatonin and L-theanine (γ-glutamylethylamide). Melatonin is a hormone that is produced naturally by the body to help it get ready for sleep, while L-theanine is an amino acid found in tea leaves.
If you are experiencing chronic insomnia, it is important to talk to a healthcare professional. They may be able to prescribe medications that can help, such as benzodiazepines, which stimulate a chemical in the brain called GABA, leading to sedation, muscle relaxation, and reduced anxiety. However, prescription sleep aids are typically recommended only for short-term use and may not be appropriate for everyone due to potential risks.
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Side effects of antihistamines
Antihistamines are medicines that treat allergy symptoms by blocking the effects of histamine. Histamine is a chemical that causes the body to develop allergic symptoms such as sneezing, itching, a runny nose, and hives. Antihistamines are available over the counter and via prescription. They come in the form of pills, chewable tablets, capsules, liquids, nasal sprays, eye drops, and skin creams.
While antihistamines are generally considered safe, they can have side effects. The most common side effect is drowsiness, which is why some people use antihistamines as sleep aids. However, using antihistamines as sleep aids is not recommended because they do not improve overall sleep quality and can lead to dependence. Other side effects of antihistamines include altered mental state, urinary retention, and dry mouth. Antihistamines can also cause dizziness and impaired coordination, movement, and concentration. Antihistamines can also increase the risk for dementia and Alzheimer's disease if taken long-term. Additionally, antihistamines may interact with other medications and increase the sedative effects of alcohol. Children and older people may be more likely to experience side effects from antihistamines.
Instead of taking antihistamines as sleep aids, experts recommend cognitive behavioral therapy (CBT) as a first-line treatment for insomnia. CBT focuses on sleep hygiene and strengthening the bed-sleep connection. It helps adjust circadian rhythm and reduces anxiety about insomnia. Natural sleep aids such as melatonin and L-theanine are also recommended.
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Safety of antihistamines for pregnant/nursing people
The use of antihistamines during pregnancy and nursing is a controversial topic due to the possible teratogenic effects of these drugs. Antihistamines are commonly used to treat allergic rhinitis, insomnia, nausea, and other ailments. While they can help with sleep, they are not recommended as a long-term solution due to the risk of developing a tolerance and potential side effects such as altered mental state, urinary retention, and dry mouth.
First-generation antihistamines, such as chlorpheniramine and tripelennamine, are generally considered safe to use during pregnancy by organizations like the American College of Obstetricians and Gynecologists (ACOG) and the American College of Allergy, Asthma, and Immunology (ACAAI). These drugs have not been found to increase fetal risk when used at any time during pregnancy, according to epidemiologic data and large-scale studies. However, there are conflicting opinions on the safety of first-generation antihistamines like Benadryl and Unisom during pregnancy, with some studies suggesting they should be avoided.
Second-generation antihistamines, including loratadine, fexofenadine, cetirizine, and azelastine, have fewer associated data during pregnancy, but published studies are reassuring and suggest that they are also safe. Non-sedating antihistamines such as Zyrtec (cetirizine) and Claritin (loratadine) may be suitable options for pregnant people.
When it comes to nursing, antihistamines are generally considered safe as minimal amounts are excreted in breast milk, and they are not expected to cause adverse effects in breastfeeding infants. However, it is important to note that the sedative effects of some antihistamines can be passed through breast milk, so they should be used sparingly or avoided while nursing.
It is always recommended to consult with a healthcare provider before taking any medication during pregnancy or nursing, as they can advise on the benefits and risks of different treatment options. Alternative treatments for insomnia, such as cognitive behavioral therapy (CBT), good sleep hygiene, and natural sleep aids like melatonin, may also be considered.
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Natural sleep aids
While antihistamines can be used as sleep aids, they are associated with certain side effects and health risks. Natural sleep aids are a great alternative for those who want to avoid the adverse effects of antihistamines and prescription sleep medications. These natural remedies can help you fall asleep faster and improve your overall sleep quality. Here are some natural sleep aids you can consider:
Melatonin
Melatonin is a hormone naturally produced by the body. It is influenced by the time of day, with levels rising in the evening to signal sleepiness and falling in the morning. Melatonin supplements have become a popular natural sleep aid, helping individuals fall asleep faster and improve sleep quality. They are easily accessible over the counter. However, it is important to note that melatonin may reduce the effectiveness of certain medications and cause unwanted side effects in individuals with specific medical conditions.
Magnesium
Magnesium is a natural mineral that can help promote sleep. It is often included in natural sleep supplements or taken as a standalone supplement.
Valerian Root
Valerian root is a natural remedy that has been used for centuries to promote sleep and relaxation. It is available in supplement form or as a tea.
CBD and THC
CBD (cannabidiol) and THC (delta-tetrahydrocannabinol) are cannabinoids derived from the cannabis plant. Studies suggest that these compounds can help individuals fall asleep, stay asleep, and improve overall sleep quality. However, it is important to note that marijuana and THC products can be habit-forming, and withdrawal can aggravate sleep problems. Additionally, CBD is not recommended for pregnant or nursing individuals, and its legality varies depending on location.
L-theanine
L-theanine is an amino acid found in tea leaves. It is a natural compound that can help promote relaxation and improve sleep.
Lifestyle and Environmental Adjustments
In addition to supplements, making certain lifestyle and environmental adjustments can improve sleep:
- Avoid electronic devices at least 30 minutes before bed, as the light from smartphones and laptops can interfere with sleep.
- Maintain a consistent sleep schedule, even on weekends.
- Avoid alcohol, caffeine, and large meals close to bedtime.
- Avoid working out within two hours of bedtime, as it can raise your core body temperature and make it harder to fall asleep.
- Drink warm milk, chamomile tea, or tart cherry juice before bed. These drinks are believed to have sleep-promoting properties without causing side effects or drug interactions.
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Alternatives to antihistamines for sleep
Antihistamines are not recommended for long-term use as sleep aids because they can have side effects and health risks. These include an altered mental state, urinary retention, dry mouth, and sleepwalking. Additionally, people can develop a tolerance to antihistamines, and they may not be effective in improving sleep quality.
- Cognitive-Behavioural Therapy (CBT): CBT is recommended by the American Academy of Sleep Medicine as a first-line treatment for insomnia. It focuses on sleep hygiene, strengthening the connection between bed and sleep, adjusting the circadian rhythm, and reducing anxiety about insomnia. CBT can help improve sleep habits and behaviours without the need for medication.
- Melatonin: Melatonin is a hormone naturally produced by the body to regulate the sleep-wake cycle. Taking melatonin supplements can help promote sleep without directly causing drowsiness. It is available in short-acting and long-acting forms and is useful for occasional insomnia and jet lag.
- L-theanine: L-theanine is an amino acid found in tea leaves. It is a natural sleep aid that can help promote relaxation and improve sleep quality.
- Good Sleep Hygiene: Maintaining good sleep habits is crucial for improving sleep. This includes practising a consistent sleep schedule, avoiding alcohol, caffeine, and large meals in the evening, and refraining from using electronic devices at least 30 minutes before bedtime.
- Prescription Sleep Aids: If you suffer from chronic insomnia or long-term sleep problems, it is advisable to consult a physician or a sleep specialist. They can recommend or prescribe appropriate medications or treatments, such as antidepressants with sedating effects, to address the underlying causes of your sleep issues.
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Frequently asked questions
Yes, most over-the-counter sleeping pills contain antihistamines. Antihistamines work by blocking histamines, which are substances in your body that cause alertness.
Side effects of using antihistamines as sleeping pills include altered mental state, urinary retention, dry mouth, sleepwalking, and other parasomnias. They may also increase the risk of dementia and Alzheimer's disease if taken long term.
Yes, there are several alternatives to antihistamines as sleeping pills, including natural sleep aids such as melatonin, good sleep hygiene, cognitive behavioral therapy (CBT), and prescription sleep medications like benzodiazepines.
