By S. Silva M.D.
Prescription sleep aides are among the most commonly administered of medications, and they can be a Godsend for many patients. Although once only approved by the FDA for brief trials, recently the FDA approved Ambien for long-term use. In actuality, any prescription sleeping pill can be used safely and reliably on a chronic (i.e., nightly) basis, with favorable results. The problem over time, however, is that a person develops tolerance to the sedative effect of these medications and requires ever-increasing dosages to reap the same benefit as when s/he first began taking them, which in many cases leads to drug dependence, withdrawal effects, and even in some cases addiction and/or overdose. This article addresses how to avoid the problem of escalating the dosage of a sleep aide, while maintaining considerable benefit from the prescribed medication.
When you have chronic insomnia that requires nightly dosing with a medication that cannot be increased indefinitely without risking serious side effects (to say nothing of the fact that, sooner rather than later, the higher dose itself will fail to work as expected), here's what you may be doing wrong, along with some secrets to preserving the efficacy of any sleeping preparation:
• Begin with the lowest effective dose of the medication and do not increase it unless or until absolutely necessary. This will conserve those higher doses for when you really need them. The sooner and faster you up the dosage, the more rapidly you will develop tolerance to the sedative effect of the drug, and the sooner you will become frustrated by the fact that the medication is apparently no longer working for you.
Once you have increased the dosage once or twice, feel free to back down on those subsequent nights when you already feel especially tired, or think that you might not have particular difficulty getting to sleep; better yet, skip the medication entirely whenever you can. This will preserve efficacy over time, because tolerance is always reversible.
• Take the full dose of the medication on an empty stomach, with plenty of water. This will speed the rate of absorption, which will maximize the medication's potency. With a sleeping pill, you want to absorb it rapidly and completely, so that you get to sleep in the same manner: quickly and fully. If you take the medication on a full stomach, this will result in its being absorbed more gradually over time, as it dissolves into the food present in your stomach; the food itself presents a physical barrier to absorption. This in turn results in a gradual relaxation that, if too gradual, may not tip you over into desired sleep. For example, 10mg of Ambien will have a much more impressive effect if you absorb it over a period of, say, 15-20 minutes than that same dosage will have if it takes an hour and a half to enter the bloodstream, and thus, reach the brain. This is true regardless of your body weight, liver function, or level of tolerance.
Along the same lines, take the full dose all at once. If you know you will need more than 5mg of Ambien to get to sleep, don't take 5mg an hour before bedtime and then wait to take another 5mg when you actually get in bed; you may find with this strategy that you are tempted to take yet another 5mg at 3 a.m., and still not get to sleep. This wastes the potency of the dosage you are needing. Take all 10mg or 15mg at once, preferably on an empty stomach, 10-20 minutes before lights out.
This is not to say that taking another 5 or 10mg later, if absolutely necessary (and okayed by your doctor), won't work: often extra doses do help, but it's a bad habit to get into, splitting the dosage of a sleeping pill. Take what you need when you need it and be done with it. Taking extra doses of a sleeping medication while under the influence of that medication is particularly unadvisable because this can lead to unintentionally taking more of the medication than is needed or safe, and exceeding your doctor's recommendation. This is because you will begin experiencing cognitive dysfunction after the first dose; even if you don't feel sleepy, you WILL be impaired, and that includes memory and judgment. You don’t want to be titrating your dose of sleeping medication once you become confused and forgetful. People have accidentally overdosed because they take extra doses of medication after they've taken doses they've forgotten they've taken!
• Take "drug holidays" when feasible. As previously stated, if you are already tired and feel like sleeping without it, or if it's the weekend and it's not absolutely necessary to be asleep before midnight, skip the medication entirely that night. This will delay and even reverse the tolerance you have built up for the drug up to that point, likewise preserving the efficacy of the medication over the long-term.
The more regularly you take a sleeping pill, the more surely you will develop some immunity to its sleep-inducing effect, but the more nights in a row that you go without the medication each time you take a "holiday" from the drug, the more you reverse any tolerance you have acquired up to that point. Frequent drug holidays can prevent the development of tolerance in the first place, which is ideal.
One way to take more drug holidays is to make sure you have good "sleep hygiene." Just follow the rules for maintaining good sleep that are well-known (see my article on How To Maintain Good Sleep Hygiene).
• Avoid consuming alcohol, because you will develop cross-tolerance to many prescription sleep aides if you regularly drink (especially the benzodiazepine class of medications, whose names end in "-pam," such as Valium, ****, Klonopin, Ativan and others, as well as Ambien, Sonata, Lunesta and most other, newer and commonly prescribed agents). While drinking alcohol and then taking sleeping pills can lead to a synergistic effect (which can actually be quite dangerous and is responsible for the majority of deaths due to accidental overdose), drinking alcohol in the early evening several hours before bedtime can lead to a direct state of rebound wakefulness as the effects of the alcohol diminish. This can lead to insomnia all on its own. In the context of treatment with a sleep aide, there is no longer an additive effect when a person takes the sleeping pill, but because of cross-tolerance due to alcohol consumption, the brain resists the sleepy effect of the medication. Cross-tolerance of sleeping pills with alcohol is more of a long-term effect, but drinking alcohol in the early evening can diminish the effects of a sleeping pill that night by this mechanism.
People who drink regularly and/or heavily often notice that they have a "built-in" resistance to sleeping medications from the start; that is, at the starting doses that are prescribed by doctors. This existing tolerance can be reversed, however, by laying off the alcohol in much the same way that any level of drug tolerance can be reversed by weaning off of the habit-forming substance and avoiding it as much as possible in the future.
People who take certain anti-anxiety medications during the day (for panic attacks, for example) will encounter the same phenomenon of not being as sensitive to the sedative effects of a given dosage of sleeping medication, if that medication is also a benzodiazepine or a medication like Ambien that is cross-tolerant with benzos.
• If you have chronic insomnia that requires nightly dosing with a medication that cannot be increased in dosage indefinitely (that would be all of them!), here's what you should realize:
When you first take a medication for sleep, the medication works powerfully to shut down your brain, assuming that your body hasn't already built up some immunity to it due to cross-tolerance with alcohol or other sedating substances. In that case, after you first take the medication and begin absorbing it, the drowsiness that comes upon you basically forces you to sleep. If you are already tucked in, that makes it easy to drift into unconsciousness. If you are still up and about, you will stop whatever it is you are doing and find your bed, because it's that, or fall on the floor.
However, once you have developed a tolerance to the medication, it will no longer "force" you unconscious; it will no longer compel you to find your bed whatever you may be doing. It will still help considerably in gently encouraging you--allowing you, as it were--to fall asleep…if you are comfortably in bed, in the right position, with the lights out, trying to relax and clear your mind. The medication that once put you to sleep now merely assists you in drifting off, and while this effect can also wane over time with tolerance, it rarely disappears completely. That is to say, you will definitely develop tolerance to being "knocked out" by a given dosage of a sleep medication, but that dosage or perhaps a slightly higher one will always significantly relax your mind and your muscles and it will always promote sleepiness to some degree. But in order to take advantage of that sleep assistance, you have to be sure that your mind and body are not working against you.
What happens is that, depending on how quickly and fully you absorb the medication, there will be a window of time during which your blood concentration of the medication will be peaking. It is during this window of opportunity that you should be in bed, ready to drift off. If you miss it--if you're emptying the trash or brushing your teeth or talking on the phone or yelling at the kids--when you do finally get in bed and turn the lights out, your blood levels may already be dropping and you may have missed your chance to take full advantage of the medication's soporific effect.
• This is a very common mistake people make: they take their pill before they are ready to commit to sleepytime, and while they are "waiting for it to kick in," they're paying bills, surfing the internet, reading, or seeing what's on TV.
This is a huge mistake. Take your medication and then GO TO BED. Don't take it and do other nighttime stuff, waiting to pass out. I once had a patient who admitted to me that she took her sleeping pill, then drove to the convenience store for a carton of milk! Besides being dangerous, she was obviously not ready for sleep. It's no wonder the medication didn't help her find sleep: she wasn't looking for it. And thank goodness she didn't find it on the way--or rather, that it didn't find her! (Even had she walked to the store it would not have been a good idea.)
• The thing to understand here is that, very soon after regularly taking a sleeping medication, it induces sleep more gently than it did the first few times, because your brain develops natural immunity to the sedative effect. The medication has to work harder to put your adapted brain to sleep, which means you either have to take more milligrams or you have to make it easier on your body to succumb to the medication's attenuated effect. Since it is neither feasible nor safe to continue escalating the dose of a sedating medication (or any medication, for that matter), if you want your sleeping pill to keep working you have to do everything you can to let it work, which means don't fight it with an alert mind and an active body. Take the medicine, lie down, close your eyes, clear your mind and relax into it.
• The other thing to remember is that, if you take a drug holiday, and you wait long enough, the medication will work like new the next time you take it. You should still follow the rules outlined in this article, but you will find that the medication works better--and at a significantly lower dosage--than it had been before you took the break.
