History of Sleep Medication

Last updated: March 26, 2019

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People have been searching for a way to solve sleep disorders for a long time now. The medications that allow us to sleep properly were not developed yesterday. These incredibly useful products are the result of research that started centuries ago. As civilization progresses, so does our knowledge of science and health-related technologies. In this article, we will explore the roots of modern-day sleeping pills.

Ancient Sleep Medications

The quest for a good night’s sleep is not a modern endeavor. Even our ancestors have grappled with the problems brought by sleep disorders. Needless to say, they had neither the technology nor the knowledge that we have today.

In ancient times, they used alcohol and opiates as sleep medication. Alcohol did help them go to sleep. However, as we know now, it gets broken down by the body quickly. This means that people under the influence of alcohol often wake up in the middle of the night when the effects of the alcohol have worn off. They often wake up feeling disoriented and unrefreshed.

The other approach that they used in the past is herbal. Most of the medicines that people used during those times were plant-based so it is not surprising that they will turn to herbs for their sleep problems. The most commonly used sleep aids were those that came from poppy. They used morphine and heroin.

Morphine and heroin are painkillers. And just like modern-day painkillers, they are also sedatives that can put a person in a drowsy euphoric state. It is interesting to note that morphine is named after the Greek god of dreams, Morpheus. Hypnotics, on the other hand, is named after Hypnos, the god of sleep. There is a downside to using these sedatives though, especially for those who have never taken them before. If a person has never tried using morphine or heroin before, the result is a reduction of slow-wave-sleep or deep sleep. On the other hand, for those who are dependent on opiates, the effects are short-term and they have shorter REM sleep.

The early sleeping pills

The modern sleeping pills that we use now started in the mid-nineteenth century. This was when they discovered chloral hydrate. The use of barbiturates as sedatives started at the beginning of the twentieth century. The most popular sleeping pills during that time were methaqualone and glutethimide. These two were the first potent sleeping pills.

Unfortunately, their popularity dwindled when health experts discovered drawbacks to their use. They found that the effects of these sleeping pills reduced over time. This is what we call tolerance nowadays. Most users also became dependent on these pills. To top it off, there were severe withdrawal syndromes associated with them. These pills are also highly toxic in overdose. Even as little as ten doses can be fatal.

Benzodiazepines

Leo Sternbach discovered the sleep drugs that we know as benzodiazepines or benzos in the 1950s. He discovered a crystalline compound with sedative, anticonvulsant, and muscle relaxant properties. It was in 1960 when it came out in the market as the benzodiazepine tranquilizer Librium. Ten years later, in the 1970s, benzodiazepines were the most popular and most prescribed drugs in the world.

The first benzodiazepine specifically made as a sleep aid was Flurazepam. It came out in 1970 and was the most prescribed sleeping pill at that time. The appeal of benzodiazepine stemmed from the fact that it is not as toxic as glutethimide and methaqualone. Benzos are also more appealing compared to barbiturates because it doesn’t cause any reduction in REM sleep. As the years go by, the use of benzos has declined because of the realization that they can also cause dependence. The development of the Z-drugs also contributed to this decline although benzos are still used widely.

Z-drugs

Zolpidem is the first among the Z-drugs. This hypnotic was introduced in Europe in 1988. However, it only became available in the US in 1993. Z-drugs are better than benzos because they don’t have the effects on memory, muscle relaxation and coordination that benzos have. Z-drugs are also less prone to abuse, unlike benzos. These drugs also produce less daytime sedation.

Newer sleep medication

All of the sleep medications work by facilitating the action of the inhibitory neurotransmitter called GABA. After the Z-drugs, scientist developed new sleep medications that function differently. Suvorexant, for instance, works by blocking the arousal neurotransmitter called orexins. And then you have Ramelteon, which works by binding to receptors for the hormone melatonin.

Sleep medication has come a long way from the herbs that our ancestors used. We now have medications that are more effective than those used 40 years ago. Modern sleep medication also doesn’t have the severe, and sometimes deadly, side effects of older sleeping pills.

The quick-acting sleeping pills that we use now are by no means perfect. They still have side effects and they are still prone to misuse and abuse. Newer and better sleep medications are being developed each year. With the advancements in technology and research that we have, don’t be surprised if a sleeping pill without any side effects or drawbacks come out in the market tomorrow.

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