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Searching for the ideal sleeping pill

, September 1, 2013, 0 Comments

Sleeping pills have a bad reputation. They’re said to be dangerous, addictive, and to be avoided at all costs. But for people with chronic insomnia, chemical assistance is often their only hope.

It started nineteen years ago: Anne-Marie simply couldn’t get to sleep anymore. “Nineteen miserable years,” she tells DW. “Insomnia is a pain in the butt. Anyone who doesn’t have it cannot imagine how terrible it is.”

Her insomnia started after her mother died. She still remembers touching her mother’s dead body. “I hadn’t known that a human body could be that cold. I was shocked.” She began to lay awake at night, unable to sleep at all.

After a few days, she went to see a doctor. “I started to cry because I was completely exhausted.”

Anne-Marie, now 68 years old, lives in Lohmar near Bonn. It takes her half an hour to tell the tale of all the doctors she has seen in the last 19 years. There were so many: “But nobody could help me.”

After several years, Anne-Marie finally found a way to cope with her illness. Almost every night she takes a quarter of a sleeping pill.

“There’s no other way for me,” she says. “Ten years ago I thought: Either I take these, or I will die. Sleep is as important as eating and drinking.”

Tension: the enemy of sleep

According to the Robert Koch Institute, part of Germany’s Federal Ministry of Health, 25 percent of all Germans suffer some symptoms of insomnia. In the US, 10 to15 percent of all adults say they have chronic insomnia, according to the US National Center for Sleep Disorders Research at the National Institute of Health.

The causes are often psychological, says Hans-Günter Weeß, director of the sleeping center in the Pfalzklinikum in Klingenmünster, a hospital for psychiatry and neurology. “The patients have forgotten how to relax. They brood over the tasks in their everyday lives.”

Other illnesses, like malfunction of the thyroid, can also result in insomnia.

Forcing the brain to go to sleep

Falling asleep naturally is always the preferred option, but some people, like Anne-Marie, just can’t manage without help. Researchers have therefore been trying to find the ideal sleeping pill – one that has no side effects.

In previous years, barbiturates were touted as the solution. But in the 1950s, doctors realized that they had the potential to become severely addictive.

Then benzodiazepines conquered the market. Valium was one brand that became particularly well-known. Like barbiturates, they bind to GABA receptors and enhance their effect, thus promoting sleep.

“These GABA receptors act throughout the brain, including the regions important for cognition, motor coordination and mood,” says Jason Uslaner, who works for the chemical and pharmaceutical company Merck in West Point, Pennsylvania. Up to 20 percent of all brain neurons produce the GABA neurotransmitter.

Although benzodiazepines are still on the market, there is now a new alternative: the so-called “Z-drugs”, such as Zolpidem and Zopiclone, called cyclopyrrolones. They also bind to the GABA receptor, but to a specific subunit, and have fewer side effects than benzodiazepines. These are now the gold standard in the treatment of insomnia.

There are of course also natural substances like valerian that help people relax and go to sleep. But they often don’t work on people with severe insomnia. Anne-Marie says that, while valerian sometimes helps her in high doses, often it doesn’t.

No natural sleep

All sleeping pills – or hypnotics, as the experts call them – have one thing in common: They change the patient’s sleep profile.

“They suppress the deep-sleep and the REM-sleep phases,” Weeß explains. REM is short for rapid eye movement, and is the sleep stage in which people dream.

The modern sleeping pills may have fewer side effects, but that doesn’t mean there are none. People can feel tired and groggy the next day, and might not be able to drive. The substances can sometimes lead to dependence and tolerance when taken for more than two weeks, meaning that people either can’t go to sleep without them anymore, or else the pills stop working.

“Hypnotics are only suitable for short-term use,” Weeß says.

There simply hasn’t been a perfect hypnotic up to now.

Hope for a new hypnotic

However, there might be some other substances that will help insomnia patients in the future: so-called dual orexin receptor antagonists, or DORAs.

Researchers recently discovered that the neurotransmitter orexin played a central role in controlling the body’s circadian rhythm. “During the day, orexin levels are high, to keep you awake,” Uslaner explains. “At night they fall to lower levels to allow you to go asleep.”

DORAs block these receptors so that the neurotransmitter cannot have an effect – and people go to sleep. Uslaner and his team at Merck are working on this new class of hypnotics.

“As opposed to GABA, orexin is found in very discrete brain regions,” he says. Researchers therefore expect that DORAs will not have the side effects of other sleeping pills.

“These substances are promising,” Weeß says. “It seems that they affect the natural sleep very little.”

So far, though, the substances have only passed preclinical tests in rodents and non-human primates. It will be some time before researchers know whether they are suitable for humans.

Only an emergency solution

Anne-Marie says she tried almost everything to go to sleep. She even founded a support group for insomnia patients, but it doesn’t exist any more. “People were too tired in the evenings to attend the meetings,” she says.

In the end, only her quarter of a sleeping pill can give her what she needs. Her doctor prescribes the medications without problems, she says, “because he knows I don’t take much.”

But Weeß warns that sleeping pills are only an emergency solution: “They don’t heal insomnia, they don’t remove the cause of it – they only relieve the symptoms.” For Anne-Marie, though, that’s more than enough.

Source: Deutsche Welle |