Ashwin Lewis
The invention of sleeping pills can be traced back to the 19th century when scientists first began experimenting with evidence-based medical approaches to sleep. While early attempts included the use of alcohol, opium, and herbal remedies, it was the discovery of chloral hydrate, the first synthetic sedative-hypnotic drug, that marked a significant advancement. Introduced into medicine in 1869, chloral hydrate was widely used to treat insomnia, but its potential for addiction and overdose was soon recognised. This led to the development of barbiturates, which became the most popular sleeping pills in the early 20th century. However, barbiturates also carried serious side effects, including addiction and the risk of overdose. In the 1960s and 1970s, benzodiazepines emerged as a safer alternative, offering fewer side effects and a reduced risk of dependence. Despite these advancements, the search for safer and more effective sleeping aids continues, driven by the growing need for better sleep among people worldwide.
| Characteristics | Values |
|---|---|
| First synthetically produced sedative-hypnotic drug | Chloral hydrate |
| Year Chloral hydrate was first synthesized | 1832 |
| Person who discovered the effectiveness of Chloral hydrate in inducing sleep | Mathias E.O. Liebreich |
| Year Chloral hydrate was introduced into medicine | 1869 |
| Early 20th-century popular sleeping pills | Barbiturates |
| Number of Barbiturate compounds | 25,000 |
| Number of Barbiturate compounds marketed as prescription drugs | 50 |
| Examples of Barbiturates | Phenobarbital, Pentobarbital |
| Safer alternatives to Barbiturates | Benzodiazepines |
| Examples of Benzodiazepines | Valium |
| Early classes of drugs that have fallen out of use | Barbiturates |
| Percentage of individuals with sleep disorders taking or prescribed nonbenzodiazepines (Z-drugs) in the USA as of 2010 | 13.7% |
| Percentage of individuals with sleep disorders taking or prescribed benzodiazepines in the USA as of 2010 | 10.8% |
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What You'll Learn
Early sleep aids
Since ancient times, humans have used various substances to aid sleep. Alcohol, opium, cannabis, valerian, and other ancient herbal remedies were used regularly to induce sleep from antiquity until the 19th century. Early modern sleep recipes and household collections from England in the 16th and 17th centuries contain hints of a desire for safe and effective sleep aids. These recipes included dangerous and potentially lethal substances, such as laudanum, a narcotic drug, and tinctures of opium and alcohol.
In the 1890s, Hypnotica, a class of somniferous drugs, was tested in medicine. These included urethan, acetal, methylal, sulfonal, paraldehyde, amylenhydrate, hypnon, chloralurethan, ohloralamid, and chloralimid. In 1869, chloral hydrate was first used as a soporific, and it quickly gained popularity, along with various bromide salts. However, the risks associated with chloral hydrate, such as dependence, overdose toxicity, and organ damage, were not immediately recognized.
Barbiturates emerged as the first class of drugs for sleep in the early 1900s and were initially considered safer alternatives to bromides. Phenobarbital and other barbiturates were widely adopted, but they soon presented problems of addiction, withdrawal, and overdose toxicity. Barbiturates were popularised in Jacqueline Susanne's 1966 novel, 'The Valley of the Dolls', and in the Rolling Stones' song 'Mother's Little Helper'. Despite their effectiveness as sleep aids, barbiturates were eventually phased out due to their toxicity and serious withdrawal symptoms.
In the 1980s, a breakthrough in treating sleep apnea was achieved with the introduction of continuous positive airway pressure. The development of Dual Orexin Receptor Antagonists (DORAs) as a new class of sleep medication also offers a less habit-forming alternative to benzodiazepines and z-drugs, with sleep paralysis being a unique side effect.
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Scientific breakthroughs
The development of sleeping pills has a long history, with early attempts to create sleep aids dating back centuries. However, it was not until the 19th century that scientific breakthroughs in sleep medicine began to occur.
One of the earliest known sedative-hypnotic drugs was chloral hydrate, first synthesized in 1832 but introduced into medical practice in 1869 by Mathias E.O. Liebreich. It was used to treat insomnia and induce sleep before surgery. However, its addictive properties and overdose risks were soon recognised.
In the latter part of the 19th century, scientific experimentation on sleep began with Kohlschütter's study on the depth of sleep using acoustic stimuli. This was followed by investigations into physiological processes during sleep, such as blood volume distribution and muscular fatigue, made possible by advancements in natural sciences and instrumentation.
A significant breakthrough came in the second decade of the 20th century with the invention of the electroencephalogram (EEG) by Hans Berger. The EEG revealed that the human brain remains active during sleep and played a crucial role in understanding sleep brain activity.
In the early 20th century, barbiturates were the most popular sleeping pills available. While effective, they carried serious side effects, including high addiction potential and the risk of death from overdose. As a result, scientists sought safer alternatives, leading to the development of benzodiazepines in the 1960s and 1970s. Benzodiazepines, such as Valium, had fewer side effects and were considered safer. However, they did not eliminate issues of dependence and withdrawal.
In recent decades, the understanding of sleep medicine has advanced further with the recognition of circadian sleep-wake disorders as a distinct group of disturbances. Additionally, neurochemistry breakthroughs by French scientists Henri Pieron and Rene Legendre introduced the concept of chemically induced sleep using "hypnotoxin," derived from the blood of sleep-deprived dogs.
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Popular sleeping pills
The use of sleeping pills has evolved over the centuries, with alcohol, opium, cannabis, valerian, and other herbal remedies being historically used as sleep aids. Chloral hydrate and bromide salts gained popularity in the 19th century, but their risks, including overdose toxicity and organ damage, led to their decline. Barbiturates emerged as a "safer" alternative, but issues of addiction, withdrawal, and overdose soon became apparent.
Today, various prescription and over-the-counter (OTC) medications are available to treat insomnia and other sleep disorders. Here is a list of some popular sleeping pills:
Benzodiazepines
Benzodiazepines are commonly used to treat insomnia in the short term. They help people fall asleep faster, prolong sleep time, and reduce wakefulness. Examples include Lorazepam and Xanax. However, their use beyond 2 to 4 weeks is not recommended due to the risk of dependence.
Z-drugs
Z-drugs are nonbenzodiazepines that act on similar brain receptors. They are prescribed for insomnia and other sleep disorders. Examples include Ambien, Lunesta, and Dayvigo. Like benzodiazepines, Z-drugs can cause dependence and may have adverse effects, such as accidents and daytime fatigue.
Melatonin Antagonists
Melatonin is a naturally occurring substance in the body that regulates sleep. Ramelteon (Rozerem) is a melatonin antagonist that promotes sleep and improves circadian rhythms. It has a low risk of misuse or dependency and is prescribed for longer-term use.
Suvorexant (Belsomra)
Suvorexant is a prescription medication that helps people fall asleep and maintain sleep. It is a selective antagonist of the orexin receptor, which plays a role in regulating wakefulness.
Estazolam (Prosom)
Doctors prescribe estazolam for the short-term treatment of insomnia. It helps with falling and staying asleep but carries a risk of misuse and dependency.
Doxepin (Silenor)
Doxepin is a sleep aid with the brand name Silenor. Doctors may recommend it for people with insomnia for up to 3 months.
It is important to note that sleeping pills should be used with caution and under medical supervision due to potential side effects, interactions with other substances, and the risk of dependency.
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Side effects
While sleeping pills can be effective in treating insomnia and other sleep disorders, they can also have several side effects, and it is important to be aware of these before taking them. Sleeping pills should be used for short-term relief of sleeplessness only, as using them for too long can create dependence and other problems.
Some common side effects of sleeping pills include drowsiness, dizziness, and confusion, which can negatively impact your ability to drive, work, or complete daily tasks. This is especially true for older adults, who may experience falls, broken hips, and car accidents due to these side effects. Other potential side effects include digestive problems such as constipation or diarrhoea, muscle weakness, and worsened snoring or sleep apnea.
Sleeping pills can also cause parasomnias, which are complex sleep behaviours that occur when an individual is asleep and unaware of their actions. Parasomnias can include sleepwalking, sleep eating, making phone calls, or even sleep driving, which can be extremely dangerous.
Additionally, sleeping pills may cause a hangover effect the day after taking them, with some people experiencing muddled thinking and balance problems. They can also interfere with normal breathing and be dangerous for people with certain chronic lung problems such as asthma, emphysema, or chronic obstructive pulmonary disease (COPD).
Furthermore, sleeping pills have been associated with problems of addiction, withdrawal, and overdose toxicity, especially when used long-term. They may also cause rebound insomnia, where insomnia returns worse than before after stopping the medication. It is important to gradually reduce and stop taking sleeping pills under the guidance of a healthcare provider to minimise these risks.
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Safer alternatives
While sleeping pills can be effective in helping people get some sleep, they often come with side effects and safety concerns, especially when used long-term. Some common side effects include constipation or diarrhoea, muscle weakness, digestive problems, worsened snoring and sleep apnea, rebound insomnia, and dependence. There is also a risk of overdose, especially if mixed with other sedatives or alcohol.
Given these concerns, it is recommended that sleeping pills be used only for a short duration and that behavioural and environmental changes be considered first. Some safer alternatives to sleeping pills include:
- Cognitive Behavioural Therapy for Insomnia (CBT-i): This approach focuses on addressing the underlying thoughts and behaviours that may be contributing to sleep difficulties. It can help individuals improve their sleep hygiene, develop healthier sleep habits, and manage stress and anxiety that may interfere with sleep.
- Improving Sleep Hygiene: This involves making changes to one's sleep environment and habits to promote better sleep. This can include maintaining a consistent sleep schedule, creating a comfortable and technology-free bedroom environment, avoiding stimulating activities before bed, and establishing a relaxing bedtime routine.
- Avoiding Caffeine, Alcohol, and Stimulants: Caffeine and other stimulants can disrupt sleep by interfering with the natural sleep drive. Alcohol may help some people fall asleep initially but can disrupt sleep later in the night and worsen sleep quality. Avoiding these substances, especially close to bedtime, can improve sleep.
- Natural Sleep Aids: Certain natural substances and supplements have been found to promote sleep. These include lavender, magnesium, glycine, cannabidiol (CBD), melatonin, and valerian root. While these options may be safer than sleeping pills, it is still important to use them cautiously and consult a healthcare provider, especially when considering long-term use or when pregnant or breastfeeding.
- Non-drug Treatments for Older Adults: Older individuals are more susceptible to the side effects of sleeping pills, including daytime fatigue and cognitive impairment. Therefore, it is recommended that older adults explore non-drug treatments first, such as the aforementioned behavioural and environmental interventions.
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Frequently asked questions
The first sleeping pill was chloral hydrate, a synthetically produced sedative-hypnotic drug, which was first synthesized in 1832. However, it was not introduced into medicine until 1869, when Mathias E.O. Liebreich discovered its effectiveness in inducing sleep.
A therapeutic dose of chloral hydrate produces a deep sleep lasting four to eight hours with few after-effects. However, its risks of dependence, overdose toxicity, and kidney, heart, and liver damage were slow to be recognized.
Due to the dangers posed by chloral hydrate, scientists developed safer sleeping pills in the 1960s and 1970s, such as benzodiazepines, which have far fewer side effects and are less harmful.
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