One pill makes you sleepy, one pill wakes you up

Do you have trouble falling asleep?

Do you have trouble waking up?

By one estimate, 75 percent of adults have some kind of sleep problem every week, so it’s not surprising some people use artificial means to both get to sleep and to wake up. According to a 1998 study from the Henry Ford Health Sciences Research Institute in Detroit, 13 percent of adult Americans had used alcohol to get to sleep in the previous year, and 18 percent had used sleeping pills.

On the flip side, plenty of people try to keep themselves awake after a sleepless night by the use of stimulants such as caffeine or nicotine. Sometimes they’re the same people, trapped in a “stimulant-sedative loop.”

It would be wonderful if we could do away with pharmaceutical sleep aids or stimulants altogether—but that it seems unlikely. Instead, as a recent article in New Scientist magazine (reprinted in Australia’s The Age) makes clear, scientists are working hard to come up with less damaging and more effective wake-you-up and put-you-to-sleep pills.

Most sleeping pills currently on the market work (as does alcohol) by making neurons in the brain more sensitive to a neurotransmitter called GABA, what New Scientist called “the brain’s all-purpose dimmer switch.”

However, the resulting sleep is short on the most restful “slow-wave” stage of sleep. A new drug called gaboxadol, on the other hand, which could be on the market next year, is a “slow-wave sleep promoter.” There’s at least one other in the works. The hope is these drugs can make a relatively short period of sleep more restful by filling it up with slow-wave sleep: they’re power-nap pills, as it were.

There are several other new approaches in the works for sleeping pills. One from Japan called Rozerem, which appeared last year, mimics the effect of the hormone melatonin, which promotes sleep.

Meanwhile, on the more stimulating side of the sleep-wake equation, there’s even more action, not least because the military has a strong interest in keeping personnel awake and alert.

One stimulant that’s been on the market for about seven years now is modafinil. It’s marketed for the treatment of sleep disorders such as narcolepsy, but it has also become popular as a “lifestyle” drug because it can keep you awake without apparent side effects. (It’s called a “eugeroic,” which means “good arousal” in Greek.)

Modafinil’s effects are so subtle most people aren’t even aware of them—they just don’t think about being tired. People taking it for medical reason just take enough to get through the day. The U.S. military has experimented with sequential doses, and found it works for about 48 hours. After that, sleep is required—but rather than needing 16 hours of sleep after staying awake for 48, modafinil users catch up just fine with about eight.

Another drug in development, currently called CX717, successfully kept 11 rhesus monkeys at Wake Forest University in Winstom-Salem, North Carolina, awake for 36 hours—after which they actually performed better on short-term memory and general alertness test than undrugged monkeys did after normal sleep! A test on humans showed that the drug could reverse the cognitive decline that you’d normally expect after 24 hours of sleep deprivation.

CX717 is an ampakine, a type of drug that increases brain activity by enhancing the action of glutamate, the brain’s main excitatory neurotransmitter.

There is even research being conducted into the possibility of using magnetic stimulation of specific areas of the brain to enhance wakefulness, raising the possibility that a pilot might be able to give him or herself a jolt of wakefulness just by flicking a switch on his or her helmet.

Within a decade or two, we may be able to structure our sleep/wake cycle to suit our lifestyles: staying awake when we need to, sleeping when it suits us. We might be able to greatly reduce the amount of time we sleep, too, staying awake for, say 22 hours and getting all the rest we need in just two hours.

There may be long-term effects to messing with the natural sleep-cycle, even with these new, safer drugs, that we don’t know about yet.

But in a world where people are already buying modafinil from online pharmacies just so they can party longer on weekends, it seems inevitable that the age-old cycle of 16 hours awake, eight hours asleep is about to become a dusty old relic, stored permanently beneath the bed of history.

Permanent link to this article: https://edwardwillett.com/2006/06/one-pill-makes-you-sleepy-one-pill-wakes-you-up/

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