Is your insomnia linked to stress? When you go to bed at night, are you suddenly aware of your heart beat, muscle tension, and bodily warmth?
A drug now in the pipeline may one day be available to treat stress-related insomnia—if it measures up to its developers’ expectations.
It’s Not a New Drug
New medications are expensive and time consuming to develop. So many drug companies are now bent on repurposing drugs whose side effects suggest other possible uses.
In the world of sleeping pills this is déjà vu. Over-the-counter sleep aids like ZzzQuil and Sominex, whose active ingredient is diphenhydramine, got their start with the first-generation antihistamines that came on the scene in the late 1940s and 1950s. These antihistamines were originally sold to combat allergies and relieve cold symptoms. But none were free of the side effect of drowsiness. So manufacturers like Rexall and J.B. Williams decided to cash in on that property and market them as sleeping pills instead.
Drowsiness is also a side effect of some antidepressant medications. Doxepin, an old tricylic antidepressant, is one such drug. It achieves its sedating effect by blocking transmission of histamine—even at very low doses. Somaxon Pharmaceuticals saw a money-making opportunity here. Silenor, a drug the company “developed” for treatment of sleep maintenance insomnia and which came to market in 2010, is the equivalent of low-dose doxepin.
A Beta Blocker for Insomnia
Now a company called Blake Insomnia Therapeutics is developing an insomnia drug whose main ingredient is the beta blocker nebivolol. As a class, beta blockers are used to treat hypertension and cardiovascular conditions. They block the effects of the stress hormone epinephrine (Adrenalin). This causes blood vessels to expand, lowering blood pressure and heart rate.
“But wait a minute,” you may be thinking. “Aren’t beta blockers known to cause insomnia in some users?”
Yes. First- and second-generation beta blockers have been found to cause insomnia and nightmares in some users, as well as reductions in REM sleep. Beta blockers also block secretion of melatonin, a sleep-friendly hormone released at night.
Nebivolol, a third-generation beta blocker, is different, the research shows. It does not inhibit melatonin secretion. Nor, taken in the evening, does it cause morning drowsiness—a common shortcoming of many sleeping pills on the market today.
How It Could Affect Sleep
Chronic stress-related insomnia is fueled by several factors that feed one another. Some are psychological, such as rumination and anxiety about sleep. Others are physiological, affecting heart rate and skeletal muscles, among other things. Awareness of the physiological symptoms of arousal—such as an increased or erratic heart beat and muscle tension—tends to escalate anxiety, which in turn exacerbates the physiological symptoms, and on and on. Pretty soon you’re caught up in a vicious circle and unable to calm down.
A nebivolol compound would be expected to dial down the physiological symptoms associated with stress-related insomnia. Without the troublesome physiological symptoms, insomniacs wouldn’t experience so much anxiety about sleep, company CEO Birger Jan Olsen maintains. He contends that by removing many of the physiological and psychological symptoms fueling stress-related insomnia, the drug will improve sleep. (It did so for Olsen’s mother. Her intractable insomnia responded to treatment with nebivolol.)
Will the Drug Ever Come to Market, and When?
The good news here is that the new compound, called Zleepax, is made from substances that are generally recognized as safe in the United States and Europe. So the company can skip phase I testing altogether. If the drug is eventually approved by the FDA, its main selling point will be that unlike many insomnia medications—scheduled drugs associated with the risk of developing tolerance when used long term—Zleepax does not cause morning drowsiness or carry the same long-term risks.
Phase II testing is set to begin this year. If all goes well, Phase III testing will follow. The company is projecting a product launch in 2022.
But the road to FDA approval is fraught with challenges. The company is still trying to raise money to fund the necessary trials. The drug’s performance could be lukewarm in large-scale tests. Undesirable side effects could be discovered along the way.
Even so, the drug sounds promising. Too bad the development process cannot be speeded up.
Does a drug like this sound like it might be helpful to you?