Sleep Medication and Its History – An Overview

Sleeping problems have haunted us for as long as we’ve been alive as a species. Luckily, over the years, sleep medication has developed.

Written by:

Tamara Smith

, Sleep Researcher
Last Updated: Sun, October 6, 2019
Fact checked by:

Marko Jevtic

, Sleep Specialist

Sleeping problems have haunted us for as long as we’ve been alive as a species. Of course, it was much harder to find proper solutions to any kind of illness back in the old days, so our ancestors would regularly perish from conditions we consider merely inconvenient today. The earliest records we’ve managed to find show that even ages ago, alcohol and various herbal mixtures (such as teas, soups or smoking mixtures) were used to alleviate the sleeping issues that people regularly ran into. It’s easy to take modern medicine for granted and rely on various prescription and over-the-counter drugs to combat insomnia and similar sleeping disorders.

Today, we will examine the history of how sleep medication has developed, as we feel it’s crucial to understanding how we developed our knowledge on sleep as a subject. Some methods we now recommend for those trying to maintain a healthy sleep schedule were unintentionally practiced many years ago by many people, simply as a part of daily life. The purpose of this article is to shed some light on how we’ve come to understand how sleep medicine “evolved” over the years, and help the people without a strong budget for direct medical therapy find some relief through the use of these tried-and-true, healthy habits. Let’s get into it:


The Earliest Records of Improvised Sleep Medicine

While modern sleep medicine can be traced to the mid-1800s, people have been experimenting with various substances for insomnia relief and general sleep enhancement for centuries prior. Try to remember advice from your grandparents you’d dismiss as superstition and dodgy ideas, and imagine the long line of other things people have attempted just to get some amount of healthy sleep. Remember that in those days, they didn’t have sleep-destroying factors such as blue light, but the lack of reliable modern medicine made it much harder to control a potential (and likely undiagnosed) sleep disorder.

Before we could develop even the most basic sedatives and decrease the time it takes a person to fall asleep, our ancestors regularly relied on alcohol as the main substance for relieving insomnia. While it may seem like alcohol was safer in the old days, before people had modern-day workplace safety concerns or traffic problems, alcohol remains, to this day, an incredibly risky short-term solution for sleeping problems. The initial buzz after a dose or two tends to decrease sleep onset latency (how long it takes you to fall asleep), but the consequences for our circadian rhythm and regular hormone production are only negative and serious enough to justify complete avoidance of alcohol. Drinking alcohol before bedtime almost always results in fragmented sleep, as melatonin production is crippled and body temperature fluctuates enough to wake the person up in the middle of the night.

Alcohol wasn’t the only option for people back then – many sought relief in various combinations of herbs that were considered sleep-friendly. These herbs would either be turned into teas and “sleeping potions,” or they would end up being eaten or smoked by the person trying to relax. To this day, various herbs are used in natural sleeping aids and tea mixtures under the (often justified and fulfilled) promises of easier relaxation and better sleep quality. While these sleep aids may not have the impact of prescription drugs, they’re far less risky for our body due to an absence of horrific side-effects. Herbs we use for sleep improvement these days include lavender, valerian (its root, to be specific), passion flower, etc. Opiates were a popular method of dealing with insomnia, and their use also extends to modern times, although their effectiveness is highly questionable.

It should be noted that our ancestors had much healthier daily habits than we do in modern times. If we look into isolated tribes still living without electricity or significant contact with any outside societies, it’s easy to make a connection between how they live and certain important pieces of advice we share with those trying to deal with insomnia (or any similar sleep disorder). Think about how often you’ve been told to exercise more in order to live healthier, or how healthy your diet could be if you discard sugar-heavy or greasy food. A lot of this lifestyle advice has been around for a very long time. Any current sleep medicine you run into works much better if you also reorganize your daily routine to include some of these healthy habits. Not only do they help you sleep easier, but you also gain other health benefits that improve your life, such as a stronger immune system and a higher daily energy level.


Formal Chemistry and Subsequent Breakthroughs

Around the mid-1800s, certain drugs were developed to serve a primarily anesthetic purpose. Diethyl ether (often referred to as just “ether”) was an anesthetic developed in the early nineteenth century, and it was often used (or more specifically, abused) to help someone fall asleep, despite how rare the actual prescriptions were. The first substance that was regularly prescribed for insomniacs is chloral hydrate, according to popular belief. While its sedative potency wasn’t all that impressive, it was a very frequent choice for decreasing sleep onset latency, and the first such drug that saw clinical use for treating sleep-disordered patients. There were other substances that saw use as improvised sleep aids during that period, particularly depressants like ammonium bromide, sodium bromide, and potassium bromide. Other options included morphine, an opium derivative that saw plenty of use in pain relief and sleep relaxation.

With the transition into the twentieth century, a new generation of drugs and substances entered the scene. As early as 1903, we saw the introduction of barbiturates (the salts derived from barbituric acid), the first of which was barbital. Barbiturates were prescribed very liberally by doctors, and not just for sleep disorders like insomnia. On top of sleep issues, they were used to treat anxiety and many other psychiatric conditions, as well as to sedate unruly or violent people. The main problem with barbiturates was that they were highly addictive, which led to many overdose cases – and subsequent deaths. The rich and famous often abused barbiturates without a proper prescription, which led to something resembling a “craze,” as the awareness of this drug was spread through pop culture thanks to film stars.

Around the 1960s, another heavy hitter appeared in the world of sleep medicine – benzodiazepine receptor agonists (often shortened to “benzodiazepines” for convenience). The most popular drug of this category was Diazepam, known more commonly under the name Valium. Valium’s popularity led it to become the single most prescribed drug between 1969 and 1982, in the United States. Benzodiazepines are considered one of the most effective categories of drugs for relieving anxiety or panic attacks and relaxing a patient’s muscles and still see use in epilepsy treatment, among other things. Their overdose risk is significantly less threatening than that of barbiturates, but their side-effects eventually saw them abandoned as a solution to insomnia in favor of drugs developed slightly later.

Over-the-counter sleeping aids were not represented at all until somewhere around 1980 when antihistamines received a stamp of approval from the FDA as a viable OTC sleep aid. Before that, they were used only through prescription, starting around the 1940s.

In the nineties, a category of drugs similar to benzodiazepines arrived onto the market, specifically targeting insomnia. They performed a similar job to benzodiazepines but had an improved chemical structure, which came with several important benefits. For one, these drugs were much safer to use, with fewer and less severe side-effects. They were named “non-benzodiazepines,” but a common name used for many of them is Z-drugs, as the names of drugs in this category often start with the letter Z. Commonly used examples include zaleplon (otherwise known as Sonata) and zolpidem (with its alternate name of Ambien). These drugs get prescribed to this day, as they’re very reliable.

More recently, we’ve seen a variety of drugs get introduced (and reintroduced). A derivative of zopiclone known as Lunesta (or eszopiclone) received FDA approval during the 2000s. The most promising, cutting edge sleep medication includes drugs such as ramelteon (a melatonin agonist) and suvorexant (an orexin agonist). Older drugs are being recreated and pushed onto the market in forms that make them less risky and more effective. Drugs like Circadin can potentially introduce melatonin into the body in a way that makes it much easier to metabolize. Overall, the state of sleep medicine keeps improving exponentially, following the pace of general technological advancement. With some luck, we might discover reliable cures to one or more sleep disorders that currently lack one.


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