Gina Johnson
Sleeping pills are used to treat insomnia, anxiety, and seizures, and are known by many names, including sedatives, sleep aids, hypnotics, and tranquilizers. They work by acting on the brain in some manner to help people fall asleep and stay asleep. While not all sleeping pills work in the same way, they all act on the brain's neurotransmitters, such as norepinephrine, dopamine, and serotonin, which are important in regulating sleep cycles. Some sleeping pills, like benzodiazepines, work by stimulating the neurotransmitter GABA, which has a sedative effect, leading to sedation, muscle relaxation, and reduced anxiety. Other sleeping pills, like Ramelteon, act directly on the body's sleep-wake cycle or circadian rhythm by binding to melatonin receptors in the brain. While sleeping pills can be effective in the short term, they should be used with caution as they can cause side effects and lead to dependency and drug tolerance over time.
| Characteristics | Values |
|---|---|
| Type of Neurotransmitters | Norepinephrine, dopamine, serotonin, and GABA |
| How they work | Sleeping pills act on the behaviour of the neurotransmitters. They enhance the signalling of the brain's major inhibitory neurotransmitter, γ-aminobutyric acid (GABA), via the type A receptor. |
| Examples | Benzodiazepines, Z-drugs (zolpidem, eszopiclone, and zaleplon), barbiturates, tricyclic antidepressants, and melatonin |
| Side effects | Memory issues, brain degeneration, Alzheimer's disease, depression, risk of accidental falls, respiratory depression, constipation, difficulty urinating, dry mouth or throat, decreased sex drive, weight gain, and withdrawal symptoms |
| Precautions | Not recommended for long-term use due to potential side effects and dependency. Should be used with caution and as prescribed. |
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What You'll Learn
Benzodiazepines and Z-drugs
Benzodiazepines are a group of medicines used to treat anxiety, sleeping problems, and other disorders. They work by affecting the way certain brain chemicals (neurotransmitters) transmit messages to brain cells. They decrease the excitability of many brain cells, which has a calming effect on various functions of the brain. Examples of Benzodiazepines include diazepam, lorazepam, chlordiazepoxide, oxazepam, temazepam, nitrazepam, loprazolam, lormetazepam, clobazam, and clonazepam.
Z-drugs, on the other hand, are nonbenzodiazepines, meaning they are structurally unrelated to benzodiazepines. However, they act in a similar way to benzodiazepines and are often used to treat insomnia and anxiety. Zolpidem, zopiclone, eszopiclone, and zaleplon are commonly prescribed Z-drugs.
Both Benzodiazepines and Z-drugs work best in situations where anxiety or sleeping difficulty is expected to last a short while. They are less effective for long-term anxiety or sleep issues and can even cause problems if taken for longer than 2-4 weeks.
Z-drugs have been associated with an increased risk of death, especially in older people, who are at a higher risk of fractures and falls. All three Z-drugs approved in the US (zolpidem, zaleplon, and eszopiclone) have been deemed unsuitable for older people by the 2023 Beers criteria. Z-drugs have also been linked to an increased incidence of dementia, with a 20% increase in risk overall, and a more profound effect in women.
While Z-drugs have been found to cause less residual effect on daytime wakefulness and driving than benzodiazepines, they are not without disadvantages. Side effects of Z-drugs include pronounced amnesia and, more rarely, hallucinations, especially when used in large doses. In rare cases, Z-drugs can also induce a fugue state, where patients may perform complex actions like cooking or driving while effectively unconscious and with no subsequent recollection.
Due to the risk of rebound withdrawal effects and acute withdrawal reactions, nonbenzodiazepines should not be discontinued abruptly if taken for more than a few weeks. Treatment usually involves gradually reducing the dosage over a period of weeks or months.
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Antidepressants
There are different types of antidepressants, but all types generally work as well as each other to treat symptoms of depression. SSRIs are usually the first type prescribed because the side effects are generally easier to manage, and they are less likely to cause serious problems if you take too much of the medicine. Some common side effects of antidepressants include mood changes, problems with sex, and sleepiness. It is important to continue treatment as it can take several weeks for symptoms to improve and up to 6 months after symptoms improve to continue taking the medication.
One specific antidepressant that can be used to treat insomnia is trazodone. Trazodone works by increasing levels of serotonin and noradrenaline. It can be taken as tablets, capsules, or liquid, and it is only available on prescription. Doctors usually prescribe trazodone when other antidepressants have not worked or have caused side effects. Similar to other antidepressants, trazodone can take 1 to 2 weeks to start working and up to 4 to 6 weeks to feel the full benefit. As it can make you feel sleepy, it is recommended to take trazodone in the evening or before bed.
Zopiclone is another medication that is specifically used as a short-term treatment for severe insomnia. It helps individuals fall asleep more quickly and prevents them from waking up during the night. Zopiclone is available as a tablet or liquid and is only available on prescription. It usually takes around 1 hour for zopiclone to work and is typically prescribed for 2 to 4 weeks due to the body quickly becoming accustomed to it. Common side effects include a metallic taste in the mouth, a dry mouth, and daytime sleepiness.
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Barbiturates
Historically, barbiturates were commonly used as anxiolytics, hypnotics, and anticonvulsants. However, due to the risks of misuse, side effects, and overdose, they have been largely replaced by benzodiazepines and nonbenzodiazepines ("Z-drugs") for the treatment of anxiety and insomnia. Barbiturates are still used in specific situations, such as general anesthesia, epilepsy treatment, and in veterinary medicine for euthanasia.
While barbiturates can be effective, they come with certain risks and side effects. They have a high risk of dependence and abuse, leading to their prescription primarily for short-term use. Additionally, they can cause tolerance, with individuals requiring higher doses over time. Abrupt discontinuation can result in severe withdrawal symptoms, and they have the potential for overdose, particularly when combined with other substances.
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Ramelteon
Sleeping pills are prescription medications that contain tranquilizers to treat insomnia, restless sleep, or difficulty falling asleep. They act on the brain to help a person fall asleep and stay asleep. While they can be effective in the short term, they can also be habit-forming and may have adverse effects on health in the long run.
Unlike traditional hypnotics, such as benzodiazepine receptor agonists (BZRAs), ramelteon does not act on the GABA receptor complex or other CNS receptors commonly associated with sedation, such as dopamine, opiate, or serotonin receptors. This unique mechanism of action gives ramelteon a low potential for abuse and dependence, as demonstrated in clinical trials involving insomnia patients and individuals with a history of substance abuse.
In summary, ramelteon is a novel hypnotic medication that acts on the MT1 and MT2 melatonin receptors to promote sleep and regulate circadian rhythms. It has a unique mechanism of action that differs from traditional hypnotics, resulting in a low potential for abuse and dependence. Clinical studies have demonstrated its effectiveness in reducing sleep onset latency and improving total sleep time, making it a promising therapeutic option for individuals struggling with insomnia.
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GABA
Gamma-Aminobutyric acid, or GABA, is a naturally occurring amino acid that acts as a neurotransmitter in the brain. It is the primary inhibitory neurotransmitter in the central nervous system, meaning it plays a crucial role in calming nervous activity. This makes it an important target for sleeping pills, which aim to induce relaxation and sleep.
Selective GABA medications target a specific type of GABA receptor believed to be dedicated to promoting sleep. These medicines are considered safer than benzodiazepines as they act on fewer GABA receptors throughout the brain, reducing the potential for side effects and addiction. However, selective GABA medicines are not without their risks, and mild side effects may still occur.
While benzodiazepines can be beneficial for some individuals in the short term, they should be used with caution. Regular use may lead to tolerance and physical dependence, and there is a risk of withdrawal symptoms upon discontinuation. Additionally, research into the long-term effects of benzodiazepines is still ongoing.
It is important to note that sleeping pills should generally not be used continuously over an extended period to avoid adverse side effects and health risks. They can be helpful as part of a comprehensive sleep improvement plan that includes behavioural changes and good sleep habits.
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Frequently asked questions
Sleeping pills that act on neurotransmitters include benzodiazepines, Z-drugs (zolpidem, eszopiclone, and zaleplon), and antidepressants. Benzodiazepines and Z-drugs enhance the signalling of the inhibitory neurotransmitter GABA, which slows down the activity of the central nervous system, leading to sedation, muscle relaxation, and reduced anxiety.
Side effects of benzodiazepines may include drug tolerance, dependency, and withdrawal symptoms such as rebound insomnia.
Ramelteon (Rozerem) is a newer prescription sleep medicine that acts on the body's sleep-wake cycle or circadian rhythm. It has fewer side effects than benzodiazepines and has essentially zero risk of physical dependence.
Melatonin and valerian are natural sleep aids that can help promote sleep. Melatonin influences when you fall asleep and wake up, while valerian has a calming effect on the nervous system.
Sleeping pills can cause side effects such as constipation, muscle weakness, and a hangover effect the following day. Long-term use of sleeping pills can lead to brain degeneration, Alzheimer's disease, and an increased risk of accidental falls. They should not be used continuously over an extended period to avoid adverse health effects.
