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Sleeping Pill Update: The Orexin Blockers

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Blog posts I’ve written about sleeping pills get a lot of traffic. Among people with sleep problems, interest in drugs to relieve insomnia is high.

Pharmaceutical companies don’t seem to share this interest, though. A quick survey suggests that few companies are actively working on new drugs for the treatment of insomnia. Those with sleeping pills in the pipeline are developing drugs similar to suvorexant (Belsomra). Here’s more about this relatively new class of insomnia drugs.

Calming the Orexin System

Suvorexant and other similar medications achieve their soporific effects by blocking the activity of neurons that produce two neuropeptides called orexin A and orexin B. These orexin-producing neurons, located in the hypothalamus and numbering about 70,000 in all, project to neurons that regulate wakefulness, arousal, attention, and motivation.

When the orexin neurons are firing in full force, we’re up and alert and doing things. But the orexin neurons are mostly quiet during sleep.

Studies have shown that an overabundance of orexin in mice and zebrafish results in insomnia-like states. The problem of insomnia might have to do with the overexpression of orexin, researchers reasoned, and drugs that could counteract the expression of orexin at night might help insomniacs sleep. In fact, studies subsequently showed that drugs that blocked orexin activity in mice, rats, dogs, and humans helped to promote sleep.

Development of Orexin Drugs

There are two types of orexin receptors in the human brain: OX1 and OX2. Early testing determined that arousal was mainly governed by OX2 receptor signaling, and that OX2 receptors had a more important role in maintaining a balance between sleep and waking than OX1 receptors. Blockade of OX2 receptors was also more effective at promoting sleep. Blockade of both receptors appeared to be even more effective.

So pharmaceutical companies starting formulating and testing drugs called “dual orexin receptor antagonists” (DORAs) that blocked both OX1 and OX2. Research on the first of these drugs, almorexant, was discontinued due to safety concerns. But the second DORA, suvorexant (Belsomra), made it through stage III testing and was approved for the treatment of insomnia by the FDA in 2014. Merck’s launch of Belsomra on the U.S. market occurred near the end of the year.

During the first half of 2015 (according to the most recent information I can find), sales of Belsomra were brisk. As the first insomnia drug in its class—and purportedly carrying fewer risks than other insomnia drugs—it was bound to have face appeal.

But people with sleep problems have offered different opinions on the drug’s effectiveness. Some reviewers have praised the drug on this website (see my blog post on Belsomra’s benefits and risks). More have complained about side effects and a lack of effectiveness. Among 170 reviewers weighing in on Drugs.com, Belsomra gets an average of 3.7 points out of 10.

Orexin Drugs in the Pipeline

Despite what looks like a rather lackluster start, as of the end of May 2016, two drug companies—Eisai Inc. and Minerva Neurosciences—were developing sleeping pills that would act on the orexin system. Eisai’s drug, a DORA, was to enter Phase III testing (the final round of testing a drug must go through before its maker can apply for approval from the FDA) near the end of 2015.

Minerva’s drug is a “selective orexin-2 receptor antagonist,” or SORA, that blocks only OX2 receptors. Results of lab experiments suggest it increases sleep time in rodents while preserving normal sleep staging. It was undergoing Phase II clinical trials as of December 2015.

Whether these insomnia drugs will ever come to market—and whether they’ll be better than Belsomra—is anybody’s guess. For now, insomniacs will have to look elsewhere in the quest for a better night’s rest. Check out CBT for insomnia if you haven’t tried it yet.

Coffee: The Sleepless, Too, Can Enjoy the Benefits

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I love coffee and I’m always glad to hear coffee is beneficial to my health. Two new studies—one of humans and the other of mice—add to this growing body of knowledge.

Yet coffee contains caffeine, and people with insomnia are often advised to cut down on caffeine because it interferes with sleep. Is there a middle course the sleepless can steer to avoid the harms and reap the benefits?

Decaf is always an option. Caffeinated coffee may be OK, too—if you’re willing to experiment. Here’s more on that following a brief look at the new findings:

Coffee Reduces Mortality

The latest study of coffee and mortality found that coffee drinkers live longer than non-coffee drinkers. In this large, multi-ethnic study, people who drank one cup a day were 12% less likely to die than non-coffee drinkers. The odds were even better for people who drank two or three cups a day: they were 18% less likely to die.

The particular chemical or compound in coffee that protects against heart disease, cancer, respiratory disease, stroke, diabetes, and kidney disease is still unknown. But it probably isn’t the caffeine. Coffee’s life-protecting benefits were significant for people who drank caffeinated coffee and for those who drank decaf. They were significant for smokers and non-smokers; African-Americans, Asians, Latinos, and whites; and people of all ages.

Caffeine Reduces Pain Sensitivity

Pain can interfere with sleep. But a growing body of literature suggests that lack of sleep or poor quality sleep increases our sensitivity to pain, and that insomnia exacerbates existing pain and predicts new-onset pain.

In a new study, Boston researchers found that sleep deprivation in healthy mice increased their pain sensitivity. The greater the sleep deprivation, the more exaggerated were their responses to pain. After a period of normal sleep, their reaction to pain was much less pronounced.

Then, while still in a state of sleep deprivation, the mice were given caffeine or modafinil (a drug that promotes alertness). Their pain tolerance increased, similar to what they experienced after a full period of normal sleep. So if you’re experiencing pain and trouble sleeping, a caffeinated beverage like coffee may reduce your pain more effectively than drugs prescribed for pain relief.

Reaping the Benefits, Avoiding the Harms

It looks like moderate coffee drinking is associated with better health and resilience to pain. But if you’re prone to insomnia, you’ll need to do a bit of experimenting to find out when and how much you can drink without harming your sleep.

Here are some facts to be aware of as you’re figuring it out:

  • The effects of caffeine vary greatly from one person to the next. This is largely attributable to genetic factors. Drinking coffee later in the day may keep you wakeful and degrade the quality of your sleep, or it may not affect your sleep at all.
  • Research has shown that early risers tend to be the most sensitive to caffeine. People who go to bed and wake up somewhat later have less caffeine sensitivity, and the sleep of night owls may not be affected by caffeine at all.
  • People metabolize caffeine at widely varying rates. The average half life of caffeine (the point at which the amount of caffeine in the blood has decreased by half) is 5 to 6 hours. But the half life of caffeine can vary from 2 to 12 hours. Smokers typically metabolize caffeine quickly; pregnant women, slowly. And we all metabolize caffeine more slowly as we age.

Timing Is Important, Too

When you can safely drink your last cup of coffee may depend in part on the insomnia symptoms you have. For example, I have sleep onset insomnia, or trouble falling asleep at the beginning of the night. I find that drinking coffee after 2 p.m. can keep me wakeful so I avoid coffee later in the day.

But Lesley, who comments on my posts from time to time, has trouble with sleep maintenance insomnia, falling asleep easily at the beginning of the night but waking up in the middle of the night. After successfully working to consolidate her sleep with sleep restriction, she worked out for herself a different coffee drinking routine:

I know I’m pretty caffeine sensitive and for a long time drank only decaffeinated drinks. . . . After reading recent research . . . on caffeine’s effects on sleep and the body clock, I’ve now added caffeine back into my daily routine. I have sleep maintenance insomnia plus an early to bed/early to rise body clock, and I commonly struggle to stay awake in the evenings, and even the late afternoon.

But with much experimentation I’ve found that one instant coffee in the late afternoon and another about 2.5 hours before bedtime helps massively, without affecting me getting to sleep. Of course we’re all different in our tolerance to caffeine, and it’s very much trial and error. But it’s an extremely useful tool to be aware of.

Lesley puts it well: with a bit of trial and error experimentation, we insomniacs may be able to have our coffee and drink it, too.

If you’re a coffee drinker, how does it affect your sleep?

Going Off Sleeping Pills

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Occasionally I hear from long-term users of sleeping pills who suspect the pills are doing more harm than good. Their sleep is not very satisfying and they don’t feel rested during the day. They’re toying with the idea of going off sleeping pills but afraid that if they do, their insomnia will return worse than ever.

If these are your concerns, discuss them with your doctor or a sleep specialist. Stopping sleeping pills is a medical issue requiring assistance from a medical professional.

That said, here’s why you might want to explore the idea of discontinuing sleeping pills and what to expect if you decide to do it.

Why Consider Going Off Hypnotics?

Sleeping pills have their place. They can be a godsend on long transmeridian flights, after traumatic events, and for occasional situational insomnia. But there are several reasons to consider discontinuing a hypnotic if you’ve used it nightly for months and years.

The first is the one I’ve mentioned: it doesn’t feel like the pill is doing your sleep—or your energy levels—much good. Used long-term, many hypnotics tend to degrade sleep quality. You may be sleeping an acceptable number of hours, but your sleep isn’t as deep and refreshing as you’d like it to be.

Sleeping pills come with a number of health risks, too. Every hypnotic is different, so it’s hard to make generalizations about the harm they may do. But long-term use of many sleeping pills is associated with increased vulnerability to infections, depression, some cancers, and cognitive impairment. Some studies (but not all) suggest long-term users may have an increased risk of mortality.

Older adults are the group most likely to be using sleeping pills on a nightly basis. Yet as we age, our bodies process drugs more slowly. Older adults taking sleeping pills are at increased risk for daytime grogginess, car crashes, and falls.

Finally, concerns about drug tolerance (the need to take more of a drug to get the same effect) and drug dependency may make you uncomfortable enough to want to explore the idea of discontinuing your sleeping pills.

How Not to Kick the Habit

Researchers and clinicians agree: if you’ve used sleeping pills for a long time, it’s not wise to go cold turkey. Rebound insomnia (a temporary worsening of sleep) will likely occur, tempting you to start taking the pills again. In addition to rebound insomnia, you may suffer withdrawal symptoms: anxiety, restlessness, tremor, sweating, agitation, and even seizures. Weaning off sleeping pills gradually is a better strategy.

A Drug Tapering Regimen

This is where the doctor comes in. Knowing your medical history and the particulars of the sleeping pill you’re taking, he or she can plan with you what the best tapering strategy will be.

It’s going to depend on a number of things:

  • How long you’ve been taking the drug.
  • The half-life of the drug and the likelihood of withdrawal symptoms. Some drugs take longer to pass through your system than others. Withdrawal symptoms can occur within 1 to 2 days for sleeping pills with short half-lives and within 3 to 7 days for sleeping pills with longer half-lives. The taper can be planned accordingly.
  • The nightly dose you’re taking. “Providers should consider moderate reductions at higher doses and smaller reductions at lower doses to prevent excessive withdrawal symptoms,” writes Sarah T. Melton, Doctor of Pharmacy, in a paper for Medscape.com.

The taper should occur slowly and gradually. Two commonly recommended dose reduction schedules are these:

  • A 25% reduction of the dose every 2 weeks
  • A 25% reduction the first week, a 25% reduction the second week, and a 10% weekly reduction thereafter

But in difficult situations, drug tapers may take as long as 6 months. The schedule the doctor proposes has to feel comfortable to you, too.

Tapering off sleeping pills while going through cognitive behavioral therapy for insomnia (CBT-I) can greatly improve your chances of success with the taper and improve your sleep at the same time. For details, check out this blog post on CBT and stopping sleep meds.

Q&A: Can’t Sleep Due to Temperature Sensitivity

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A reader named Gunjan recently asked a question about trouble sleeping due to temperature changes at night. Here it is, lightly edited:

“It seems my body is very sensitive to temperature while I am sleeping. Many times it has happened that I went to bed at an optimal temperature. But as soon as my body sleeps, I wake up feeling too cold. Then I go to bed after switching off the fan or covering myself with the bed sheet but then I can’t sleep because I’m too hot. This is quite frustrating. . . . Does anybody . . . have any help to offer?”

Insomnia and Thermosensitivity

Insomnia may have something to do with compromised thermoregulation, but the issue has not been fully investigated, say authors of a paper on sleep and thermosensitivity. Evidence shows that older adults may have an impaired ability to recognize the most comfortable temperature for sleep, and this may relate to abnormalities in the area of the brain that evaluates comfort. Not much else is known.

But I’m never surprised when people complain of trouble sleeping related to temperature sensitivity. I have the problem myself. I’ve gone to bed in very hot and very cold situations and lain awake for a good chunk of the night. Like Gunjan, I regularly have to make small temperature-related adjustments in the middle of the night. Now, with some nights warm and others cool, is the season when it’s trickiest to get it right.

Temperature Changes at Night

Core body temperature varies by about 1.5 degrees Fahrenheit over the course of the 24-hour day. From a temperature high in the evening, it descends and reaches its low point some 1 to 3 hours before normal wake-up time. If you keep the bedroom windows open at night (a cool bedroom is good for sleep), the room temperature will likely drop as well. The combination of internal and environmental temperatures falling could easily explain why you might wake up feeling cold at night.

Covering yourself with a blanket or a bed sheet is the obvious way to make yourself comfortable enough to get back to sleep. But what if, like Gunjan, you then feel too hot?

Covering up can create a closed system where, once the skin temperature has risen enough to dilate the blood vessels close to the skin, the body heat then released has no place to go. It’s similar to the situation created by an electric blanket. The blanket continues to add heat to the body, increasing skin and core body temperatures. The heat the body would normally throw off is then trapped underneath the blanket. You wake up feeling too hot to sleep.

Here are two ways to keep from overheating at night:

  • Use sheets and blankets made of a breathable fabric such as cotton. Fabrics like polyester are more likely to trap heat rather than allow for its release.
  • When you cover up, see if keeping your feet outside the covers helps. You lose lots of heat through your extremities, so keeping them uncovered, or partially covered, may make you comfortable enough to sleep through the night.

Help for Sleep Onset Insomnia

It’s easier to go to sleep when core body temperature is falling, and people who have problems falling asleep—sleep onset insomnia—may have trouble cooling down at night.

Ideally, the temperature in the bedroom should be a little lower than is comfortable during the day. But there are also ways to facilitate internal heat loss. Activities that increase skin temperature eventually help to cool you down. Warming the skin dilates blood vessels close to the skin. This enables the release of body heat and a lowering of core body temperature to occur for a few hours after the activity ends, in turn facilitating sleep.

Early in the evening these activities may trigger processes that help you fall asleep:

  • Take a hot shower or bath
  • Spend time in a sauna
  • Do a resistance workout or aerobic exercise

As you’re winding down on cooler nights, mild heating of the hands and feet may dilate the blood vessels enough to facilitate heat loss, lowering your core body temperature and inducing sleep. But this is a losing strategy on the warmer nights. Lightly clad and barefoot is the way you want to be.

If you’re sensitive to temperature changes at night, what have you found that helps?

Six Tips for Overcoming Sleep Onset Insomnia

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It’s been 10 years since I experienced persistent sleep onset insomnia, but I was reminded of what my nights used to feel like when recently I took a red-eye flight on Spirit Airlines.

Conditions on that plane were not conducive to sleep: seats locked in the upright position; flight attendants whose nattering could be heard over the noise of the engines; dim lighting rather than darkness; kicks to my seat as the 6-footer behind me shifted around in his coach class cubicle; turbulence. I didn’t sleep a wink.

Conditions like these can interfere with anyone’s sleep. But sleep onset insomniacs may find them particularly challenging, accustomed as we are to not falling asleep very quickly and being bothered by things that other sleepers readily tune out.

Why is it so hard for some insomniacs to fall asleep and what can help? Following are six ways to hold sleep onset insomnia at bay.

What Brain Waves Reveal About Insomnia

Research has shown that people with insomnia have a different pattern of cortical activity as we’re drifting off to sleep. Compared with good sleepers, insomniacs are more prone to high-frequency brain waves in the sleep onset period. Once sleep onset has occurred, delta, or slow, waves take longer to appear. This is often taken as evidence of hyperarousal. At night, and possibly during the daytime as well, people with insomnia have higher levels of cortical arousal.

Results of recent study argue otherwise. Here, in the sleep onset period, sleep onset insomniacs were found to experience less high-frequency brain activity than sleep maintenance insomniacs (those who tend to wake up in the middle of the night). But the high-frequency activity in the sleep onset insomniacs took longer to decline. Authors of this study suggest that sleep onset insomnia may be the result of “some form of fast wakefulness inhibition” rather than an expression of cortical hyperarousal.

Relief for Sleep Onset Insomnia

Whatever may be the case, habits I’ve developed over the past 10 years enable me to fall asleep quickly now (barring nights when I’m trying to sleep on a plane). They may help you, too:

  1. Adopt a regular sleep schedule. Be especially regular about getting up at the same time every day—even on weekends. This can be a challenge if you have an erratic daytime schedule or an active social life. If you find you’re really sleepy, catch up on sleep by allowing yourself to go to bed somewhat earlier than normal rather than sleeping in late. The problem with sleeping much later than usual to catch up on sleep is that it sets you up for trouble falling asleep the next night.
  2. Break the association between your bed and wakefulness by reserving your bed (and the bedroom) for sleep and sex. Reading, TV and movie watching, surfing the net, playing video games—all this should happen outside the bedroom. Only go to bed when you’re sleepy enough to fall asleep.
  3. Exercise late in the afternoon or early in the evening. Exercise warms your body up. This triggers an internal cooling mechanism, and when your body is cooling down it’s easier to fall asleep. Aerobic exercise is best but rigorous strength training may work as well.
  4. Observe a wind-down routine in the hour leading up to bedtime. Have the same routine—shower, put on pajamas, brush teeth, read or look at picture books—every night. Your brain will learn to expect that this sequence of activities ends in sleep.
  5. If clock watching at night makes you anxious, turn your clocks to the wall starting at about 9 or 10 p.m. Use a backlit alarm clock on your bedside table—the kind that stays dark at night except when you press the button on top.
  6. If you have to fly at night, arm yourself beforehand with all the accoutrements I forgot to pack in my carry-on: neck pillow, eye mask, earplugs. As for Spirit Airlines, they may say they’re the company with the newest fleet of planes, but seats that keep you locked in an upright position do not lend themselves to a good night’s sleep!

If you often fly at night, what measures do you take to get a decent night’s sleep?

An Insomnia Treatment in Brief

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Cognitive behavioral therapy for insomnia (CBT-I) has become the gold standard in drug-free treatments for insomnia. Between 70 and 80 percent of the people who try it see results: They fall asleep faster and have fewer awakenings. Their sleep quality improves and they feel more rested in the morning. The gains are often long lasting.

But CBT-I is not a quick fix for insomnia. Improvements in sleep occur gradually over 6 to 8 weeks of treatment, and not everyone can or wants to commit to attending weekly therapy sessions for 6 to 8 weeks. Treatment is costly, too.

Also, the number of therapists trained to provide CBT-I is relatively small. In some parts of the United States there are none at all. (Recently a woman from Billings, Montana, wrote to me asking if I could help her find a qualified therapist within driving distance of her home. Using an online locator, I could not find a single treatment provider in all of Montana or any of 4 nearby states!)

With these problems in mind, researchers have created and are now testing a briefer form of CBT-I called brief behavioral treatment for insomnia (BBTI). BBTI isn’t widely available yet. But with health insurance companies clamoring for providers to rein in costs, BBTI is the wave of the future.

How Is BBTI Different from CBT-I?

The therapies are more similar than different. The word cognitive might imply a psychological approach to treating insomnia, yet the key components of CBT-I are behavioral: sleep restriction (reducing time in bed) and stimulus control (keeping wakeful activities outside the bedroom). Sleep restriction and stimulus control form the backbone of both CBT-I and BBTI.

In CBT-I, the therapist also addresses psychological aspects of insomnia: negative beliefs about sleep, for example, or catastrophic thinking about insomnia. Clients are guided through a process designed to help them arrive at a more realistic mindset. (Read my blog on changing negative thoughts to get a sense of what the cognitive component of CBT-I involves.)

As described by researchers at the University of Pittsburgh, BBTI is an overtly behavioral approach to improving sleep. It holds that insomniacs can set our bodies’ sleep systems to right by simply changing habits.

A Shorter Course

BBTI is completed in 4 weeks. Therapist and patient meet twice during the course of treatment. There are also 2 phone conferences lasting 20 minutes or less.

While the treatment itself may be shorter than full-blown CBT-I, progress toward better sleep occurs gradually. But the results of the few studies conducted on brief behavioral treatments for insomnia show, at least in the short term, that the outcomes are similarly positive. University of Pittsburgh researchers also found that BBTI was equally efficacious in improving the sleep of people who were using sleeping pills as those who were not.

Patients also get a workbook. It contains supplementary information about the forces controlling sleep and waking and lays out rules for better sleep and adjustments to make as sleep improves.

BBTI May Have Broader Appeal

Pittsburgh investigators claim this strictly behavioral (as opposed to psychological and behavioral) approach to treating insomnia may be more acceptable in primary care settings–the first place many insomnia sufferers go for help. Healthcare professionals can be more quickly trained to administer BBTI. Treatments that are not “psychological” may be more attractive to people with insomnia, too.

Sleep specialists have been experimenting with briefer behavioral treatments for insomnia for several years. Now as before, the biggest problem seems to be the lack of professionals prepared to help those in need.

Q&A: Sleep Restriction: Tempted to Give Up

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Jessica recently wrote to Ask The Savvy Insomniac with concerns about sleep restriction.

I’m on Day 6 of sleep restriction and I don’t think it’s working. The first 3 nights were miserable. I kept looking at the clock and thinking, just 4 more hours to sleep, just 3 more, just 2 . . . I had so much anxiety I hardly slept at all!

But on the 4th night I passed out and overslept my alarm in the morning. I FELT GREAT. And I’m like, sleep restriction rocks! But . . . the next night was terrible. I barely got 2 hours, and the same thing happened again last night. Today I feel so bad I called in to work—something I never do unless I’m sick.

Now I’m wondering if it’s worth the punishment.  Am I just going to have to resign myself to insomnia for the rest of my life? Honestly I’m on the verge of giving up.

An Erratic Sleep Pattern

I can so relate to Jessica’s plight. The sleep pattern she describes was mine for several decades. Terrible sleep for 3 to 5 nights in a row, followed by a night where I conked out so completely I could sleep through ear-splitting thunder.

Mornings after super long nights felt great. But nothing is comforting about this kind of sleep pattern. Lurching from one bad night to the next, never knowing when I was finally going to pop off a good one, raised my anxiety sky high. I wanted good sleep to be regular. I wanted it to be dependable.

With Restriction, a Payoff

My first week of sleep restriction was pretty close to hell. Like Jessica, I had 3 really bad nights before I was sleepy enough to fall asleep at the bedtime I’d chosen. But sleep restriction also required getting up at a fixed time every morning. This rule contradicted one of the most ingrained notions I had about my sleep, namely, that on the rare nights when I could sleep, I’d better let myself sleep as long as possible—because I never knew when I’d get another chance.

So when the alarm rang at 5 a.m., the temptation was simply to roll over and go back to sleep. It felt like the middle of the night. It felt like I needed more sleep. Why deny myself something my body evidently needed?

By that time I was far enough along in my research to understand the theory behind sleep restriction; I understood the forces driving my insomnia well enough to know that letting myself sleep late was probably a road to nowhere. So I mustered up my willpower and hauled myself out of bed and into the day–and the next day, and the next.

Wasted is how I felt after those short nights, and definitely lame in the head. But I held fast to my sleep window, recalculating my time in bed at the end of each week. And in time my sleep became deeper, longer and more dependable. Amazing gifts for a guerrilla sleeper like me.

Rest for Success

Not every insomniac will benefit from sleep restriction. But research suggests many can. Set yourself up to be one of them by

  • choosing to go through treatment at a time when you’re not too busy with other things.
  • avoiding clocks after bedtime. Looking at the clock creates anxiety, and that’s something you want to avoid.
  • setting appropriate bed and wake times and observing them to the letter.

What problems have you encountered during sleep restriction?

Sleeping Pills: Too Risky, or a Red-State, Blue-State Affair?

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How do people with insomnia feel about sleeping pills?

Attitudes toward sleep medications differ from one American to the next, and between Americans and Australians, it turns out. Here’s a brief comparison that I hope will start a conversation.

How do people with insomnia feel about sleeping pills?

Among 51 insomnia sufferers interviewed by Australian researchers in Sydney, both users and non-users of sleeping pills (or sleeping tablets) held negative views of sleep medications.

When I asked this same question of the 90-odd American insomniacs I interviewed for my book, the response was more divided. Some people viewed prescription sleeping pills as harmful and said they’d never use them. Others felt their sleep medications were helpful and would not want to give them up. Here’s what I wrote:

Poll the sleepless about sleeping pills, and you come up with . . . a red-state, blue-state affair. In one camp are the pill abstainers . . . and in the other, insomniacs who’d sooner dump their iPhones than part with their pills.

Pro or con, attitudes about sleeping pills are often strongly held. Following is a brief comparison of Australian and American attitudes that I hope will start a conversation.

SAFETY VS. EFFECTIVENESS

Both the Australians and the Americans felt that pharmaceutical sleep aids were stronger and more effective at putting people to sleep than over-the-counter (OTC) sleep aids or “natural” sleep aids such as valerian or melatonin.

But most Australians said they didn’t like taking sleep medication. They expressed a definite preference for natural products based on the notion that natural products were gentler on the body and had fewer harmful effects. In the majority view, safety concerns outweighed concerns about sleeping tablets’ effectiveness.

“I’ll take something that isn’t as effective so it doesn’t have any negative consequences,” said a man quoted in the Australian study.

A woman, comparing how she felt about taking the sleeping pill temazepam (Restoril) with how she felt about about the prospect of taking melatonin, said this: “I felt it’s a more natural remedy than the temazepam. So I think I was less stressed about taking it.”

But the Australians were divided as to whether prescription or OTC medication was the safer option. Some thought OTC sleep aids (medications containing diphenhydramine, such as Benadryl and Tylenol PM in the United States) were safer because they were available without a prescription and therefore less potent and apt to have fewer side effects. Others felt the safer alternative was to go with a prescription medication recommended by a doctor who was familiar with one’s individual medical needs and could supervise the process.

AMONG AMERICANS, A SPLIT

About half of the insomniacs I interviewed felt they needed medication to get a good night’s sleep and were mainly concerned about medications’ effectiveness. Jane M. wrote the following comment on one of my earlier blogs. It epitomizes the feelings of insomniacs who were satisfied with the sleeping pills they were using, having decided the benefits outweighed concern about risks.

“I was first prescribed Ambien many years ago, and don’t think I could have continued my work life this long without it. I sleep soundly eight hours every night, wake up with lots of energy, and have always wanted to meet the discoverer of the formula to thank him or her.

“My gratitude is deeply felt. My mother, who died in 1983, sat up half the night for years. I think there are genetic issues, hormone issues, aging issues . . . I could walk 20 miles a day and I still wouldn’t be able to fall asleep. Some people have asked, ‘What if you become addicted?’ to which my answer has always been ‘So what?’ I am addicted to sleep, good health, and a strong work ethic. Ambien has made it all possible for me into my mid-70s.”

SOME AMERICANS CONCERNED ABOUT RISKS

The other half of my respondents voiced reservations about sleeping pills, similar to the Australians. Their reasons were mixed. Some did not think of insomnia as a medical problem, preferring to address it through changes in lifestyle or psychotherapy rather than with drugs.

Other insomniacs shied away from using sleeping pills because of negative feelings about medication overall and about prescription hypnotics in particular. Still others felt they simply couldn’t tolerate such potent medication.

“I can’t take any hardcore pharmaceuticals,” an insomniac told me. “A mild antidepressant, that’s something I’d consider. But I’m afraid of sleeping pills.”

Unlike the Australians, few of the American insomniacs I spoke with had anything good to say about so-called natural sleep aids—herbal teas, melatonin, lavender. Based on my interviews, I would venture to suggest that here in the United States, the concept of the natural sleep aid does not have the strongly positive connotation it has in Australia.

But some Americans said they got relief from insomnia using OTC sleep aids like Benadryl and Unisom, which they felt were likely to be gentler and less harmful than prescription pharmaceuticals.

ACCOUNTING FOR ATTITUDINAL DIFFERENCES

The differences (and similarities) spelled out here may not be representative of Australians and Americans overall. The sample sizes are small, and the years when the interviews were conducted were different (2013–2014 for the Australian study; 2004–2008 for my book). Physician prescribing patterns and the public health information patients receive about insomnia and sleeping pills may be different as well.

But my point is not to make an evidence-based claim about attitudes in Australia and the United States. Rather, I’m interested in knowing how readers of this blog feel about sleeping pills, OTC sleep medications, and “natural” complementary sleep aids, and why.

Please take a minute to comment below, and like and share on social media. Thank you!

Timed-Release Melatonin for Insomnia

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A friend recently called to talk about insomnia. Her problem, she said, was that she couldn’t sleep past 3 a.m. Her doctor recommended taking melatonin and she wanted to know what I thought of this advice. Coincidentally, last week ConsumerLab, a company that tests and reviews dietary supplements, published a review of melatonin supplements.

If you’ve got the type of insomnia where you wake up too early or too frequently (sleep maintenance insomnia), you may be interested in this update.

Hormone and Supplement

The melatonin found in supplements is chemically identical to the sleep-friendly hormone produced at night in the brain’s pineal gland. Secretion of melatonin begins about 2 hours before bedtime and continues through the night, falling off at wake-up time.

Melatonin supplements are thought to be quite safe. They can help night owls fall asleep at an earlier hour. Timed right, supplements can also ease jet lag. But as a treatment for people with sleep maintenance insomnia, melatonin supplements often come up short.

Melatonin and Aging

Melatonin production often falls off as people age. This may occur because of degeneration of neurons in the circadian system or partial calcification of the pineal gland. The resulting low levels of melatonin make it harder to get sound, restorative sleep.

In theory, supplementary melatonin should take care of the problem. The reality is that often it doesn’t. One reason is that the melatonin in most over-the-counter supplements is fast acting. It reaches its maximum strength and is metabolized by the body quickly. The half-life of most melatonin supplements is quite short: 20 to 45 minutes. (Half-life refers to the time it takes for a dose of a drug in the blood plasma to decrease by half.) Compare this to the 5-7-hour half-life of Lunesta, the top-selling prescription sleeping pill in 2013.

Taken before bedtime, most melatonin supplements lose potency too quickly to help users sleep through the night.

Timed-Release Melatonin Supplements

The answer to this problem may lie in some type of timed-release formulation of melatonin. Circadin is one such drug. It’s available by prescription for adults 55 and older in several countries outside the United States. The drug has a half-life of 3.5–4 hours, so it’s longer lasting than most melatonin supplements sold over-the-counter. Clinical trials suggest that compared with placebo, Circadin improves the sleep quality and morning alertness of older adults with insomnia. (Apparently, the trial results are not convincing enough for the drug to gain approval in the US.)

ConsumerLab’s review of melatonin supplements acquainted me with timed-release formulations now sold over-the-counter in the US. Here are some examples:

  • Natrol Melatonin Time Release (1, 3, 5, and 10 mg, advertised as released over 8 hours)
  • Source Naturals Timed-Release Melatonin (2 and 3 mg, advertised as released over 6 hours)
  • Life Extension 6 Hour Timed Release Melatonin (300 and 750 mcg and 3 mg, advertised as released over 6 hours)

No spokesperson I reached at these companies was able to explain exactly what sort of testing was done to establish the 6- and 8-hour release times. Unlike pharmaceutical companies, manufacturers of dietary supplements do not have to conduct clinical trials or obtain approval for their products from the US Food and Drug Administration. Supplement makers are essentially allowed to police themselves, required only to gather enough evidence to show that their products are safe and that claims they make about them are not untrue or misleading. (ConsumerLab did not test the timed-release feature of these drugs.) How long the melatonin in these products will remain active in your body, and how likely the supplements are to improve your sleep quality or reduce your nighttime wake-ups, is impossible to know.

Still, people with sleep maintenance insomnia who decide to try a melatonin supplement are probably better off with a timed-release product than the immediate-release type.

Dosing

Even low-dose melatonin supplements (0.1–0.5 mg) contain a lot more melatonin than humans produce naturally. So taking higher doses (2–10 mg) may leave you feeling groggy in the morning. This is especially true for older adults, who process drugs more slowly.

Starting with a low dose seems like a smart idea.

Have you tried a timed-release melatonin supplement? If so, did it help you sleep, and did you notice any negative effects?

Kava for Anxiety and Insomnia: Effective? Safe?

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Kava (Piper methysticum) holds promise as an alternative treatment for anxiety and insomnia. But I’ve refrained from blogging about kava and kava supplements due to concerns about liver toxicity.

Now a comprehensive review funded by the National Science Foundation and published in the journal Fitoterapia has eased those concerns. I can write about kava, native to Hawaii and other Pacific islands, as I would any other medicinal plant, summarizing benefits and risks.

Kava in Traditional Pacific Cultures

Traditional Pacific island cultures viewed the beverage they prepared from the kava root as sacred. Kava “was the food of the gods,” Hawaiian scholar Mary Kawena Pukui said. “No religious ritual was complete without it.”

Librarian-scholar Margaret Titcomb wrote that the custom of drinking kava “is of interest in Hawaii because it was a sacred drink of importance in many phases of Hawaiian life. . . . Its effect is to relax mind and body. . . . Medical kahunas (learned men) had many uses for it. . . . It was essential on occasions of hospitality and feasting, and as the drink of pleasure of the chiefs.”

Pacific islanders continue drinking kava today. Traditionally it’s mixed with water, strained by hand, and served on social occasions, often in coconut shells. Kava drinkers may consume several coconut shells of the beverage on one occasion.

Western Interest in Kava

Pacific islanders used different parts of the kava plant to treat various ailments, suggesting to Europeans who arrived in the 18th century that kava might have important medicinal uses. First the Europeans used it to treat venereal disease. By the 1880s, it was being used to relieve stress and anxiety. British herbalists have used it since the early 1900s to treat disorders of the urinary tract.

Kava in the 1990s became a popular herbal remedy for anxiety—an alternative treatment to benzodiazepine drugs such as Valium and Xanax. Consumed as a tablet or a tincture, kava supplements contain specific concentrations of kavalactones, which are extracted from the kava plant with alcohol, acetone, or water. Kavalactones are believed to be the main active ingredients in kava.

Anti-Anxiety and Sedative Effects

Studies of kava’s effects on animals show that it acts on many of the same neurotransmitter systems as anti-anxiety drugs. It results in GABA channel modulation and downregulates or inhibits systems that are active during arousal. In humans, quite a few studies have shown that kava is significantly more effective than placebo at lowering anxiety.

So far, though, only one randomized controlled trial has been conducted to investigate kava’s effects on sleep. In this 4-week study of people with sleep disturbances associated with anxiety, the authors compared 34 participants taking a kava extract with 27 participants taking placebo. By the end of the study, the kava group experienced a significant improvement in the quality of their sleep—but so did the group taking a placebo, although to a lesser extent.

So would taking a kava supplement improve the sleep of insomnia sufferers? No one knows, and no one will know unless more and better controlled studies are done. What the existing data do suggest is that kava might be helpful for people whose insomnia is closely associated with anxiety.

Why So Little Research?

Kava sales in the West fell off sharply at the turn of the 21st century. No Pacific islander was ever known to suffer liver failure related to kava, but between 1999 and 2002, 10 kava users in Europe and the United States had to undergo liver transplants. The need for the transplants was attributed to patients’ having consumed moderate doses of kava for anywhere from 2 to 12 months. Subsequently the CDC issued advisories in the United States. Germany banned kava in 2002.

On further examination, though, investigators found that kava could be implicated as a causal agent in only 3 liver failure cases. Germany overturned its ban on kava in 2014. Sales of kava products in the West are expected to rise again.

How Likely Is Liver Failure?

Why kava might trigger liver failure in a few of the millions of users is still an open question. It might have to do with

  • genetic factors;
  • the method of extraction. While the traditional drink is prepared by water extraction, extraction using acetone, ethanol, or methanol is used in the manufacture of supplements to achieve higher concentrations of kavalactones (which, most research suggests, are not themselves a source of toxicity);
  • interactions with drugs such as alcohol, barbiturates, and benzodiazepines;
  • the use of leaves, stems, and other plant parts in the manufacture of supplements rather than just the root; or
  • the use of inappropriate kava cultivars.

All these possibilities notwithstanding, instances of kava toxicity are relatively rare. Say authors of the review, “The incident rate of liver toxicity due to kava is one in 60 to 125 million patients.”

So the risk is pretty slim.

Have you tried kava for sleep or anxiety? How did you fare?