Taking Sleep Medications

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Prescription medication should be taken only when authorized by a licensed physician and preferably when under his or her care. The authorities have designated these medicines as prescription-only because the can be dangerous, prone to abuse, or easy to make mistakes with. Over-the-counter medicines should be treated with respect, too. They are real drugs and can sometimes be powerful and cause unforeseen side effects. Pay close attention to your body when you use a drug, particularly when starting a new one.

Keep drugs in a specific area (that’s why they invented medicine cabinets) and away from pets, children, and mentally incompetent people who might be in the house. In the case of an overdose, call your local poison control center. In the US, you can call 1-800-222-1222.

Tips

Medicines are an aid. You still have to do your part by maintaining good sleep hygiene and habits. Use the medicine only while you need it (following any specific instructions given by your doctor, of course.) Medicines for insomnia, and other sleep disorders, generally treat the symptoms, not the underlying cause. They are not a cure.

You should also monitor your health and reaction to any medicines you take.

Many sleep drugs have a risk of becoming habit-forming. Your doctor and/or pharmacist can talk to you about this. Even with the risk of dependency, it is sometimes worth using a medicine if the potential benefits outweigh the risk. Also be aware that suddenly halting a medicine can result in uncomfortable withdrawal; you may wish to look into tapering off the medicine – this goes even for OTC medicines. General tips.

The common advice has been to take a sleeping pill 30 munutes before you go to bed. Research where patients experimented wuth differebt tumes suggests patient satisfaction is higher when the pills are taken later. The authors suggest targeting the desired wake-up time and taking the pill 7 hours before that time.

Interactions between medicines

Drugs can react with each other, and if you take more than one they can amplify or suppress each other or produce undesired or unforeseen consequences. The word “polypharmacy” was coined to refer to the issues and concerns involved when a person takes two or more drugs at the same time. An estimated 6 to 10 percent of Americans take hypnotics at some point during the year.

Discuss all medicines you take with your doctor, even over-the-counter ones. That means telling every doctor about prescriptions other doctors have you on. There should be no shame admitting you go to more than one doctor, if you do. Good doctors can Swallowing Sleeping Pillhandle that reality.

And good doctors are particularly cognizant of the dangers of drug interactions. All the guidance from the pharmaceutical companies, from the FDA, and from professional societies warns against interactions for certain drug combinations.

Pregnant or breast-feeding women should be particularly careful and reluctant to take medicine. Do so ONLY with the advice of your doctor. That includes over-the-counter pills.

Sleep medicine requires special care as much of it makes you sleepy (duh!) and that can be dangerous when “operating heavy machinery” as the chestnut goes. The most common heavy machinery most people operate is their cars, and drowsy driving (under the influence of drugs or not) is a major problem.

Caffeine and nicotine can contribute to insomnia beyond their stimulant properties. It worsens anxiety, manic thinking and behavior in people prone to that. When it wears off it can leave the person with lower energy and mood. Too much caffeine can result in insomnia, and so can reducing the consumption of caffeine! Many drugs have similar paradoxical properties.

Discontinuous Hypnotic Treatment

In a flexible dosing schedule, patients are instructed to take pills “as needed” They employ their judgement on any given night. Patients have medication, usually a benzodiazepine receptor agonist (a z-drug) or ramelteon, but they don’t take it every night. Some patients may be able to manage the regimen themselves and take medication only when really needed. Others may need a fixed dosing schedule which allows them to take medication only certain nights of the week. If patients use medication judiciously and do not take sedatives every night, they are more effective. In addition to medication, patients learn relaxation techniques and good sleep practices.

Stopping drugs

This is not always easy, especially if there are any addictive properties of the drug. Talk to your doctor about challenges and concerns when stopping a medicine. Tapering is often a good strategy for getting off a drug, especially one that can be habit-forming as some sleep aids are.

Definitions of Drug Actions

Agonists: drug compounds that bind to and cause a functional effect identical in quality and quantity to the endogenous ligand

Antagonist: drug compounds that bind but cause no functional effect;

Partial Agonist: causes functional effect that, at a maximum, is only a fraction of that of the endogenous ligand

  • Intrinsic activity – efficacy relative to endogenous ligand (% of activity in relation to 100% for endogenous ligand)
  • Intrinsic efficacy – is the intrinsic characteristic of the drug

Many medicines work because the body’s cells have receptors that interact with the drug molecules. An agonist is a drug that mimics the affect of a natural chemical in the body by binding to the receptor that the natural chemical occupies. An antagonist is a drug that blocks the natural chemical. You hear many drugs described as such-and-such agonists or antagonists. For instance, the headache medicine Imitrex is a serotonin agonist.

More on ADME of insomnia medicines.

Skepticism about cost-benefit of insomnia drugs

Prescription Drugs and Their Effect on Sleep

Medicines can profoundly affect sleep quality. Indeed, secondary insomnia is often caused by drugs.

Cardiovascular Drugs

Heart drugs can influence sleep architecture and may contribute to the prevalence of insomnia in older people. Beta blockers, prescribed for hypertension, seem to give people insomnia and even hallucinations. Whether the drugs directly cause these symptoms is of some question, but they are associated with them. Beta blockers do seem to reduce the amount of time spent in REM and increase nighttime awakenings. Medicinal chemists often classify substances as hydrophilic (liking water) or lipophilic (liking fat). It’s the lipophilic beta blockers such as propranolol that cause the problems rather than hydrophilic ones.

Alpha adrenergic agonists like clonidine increase sleep fragmentation and diminish REM sleep. They also increase sleepiness during daytime. Another heart drug, theophylline, has been shown to increase the amount of shallow stage 1 sleep and to increase sleep latency.

Stimulants and Sleep

Stimulants can make it difficult to sleep (duh). Ritalin and Adderall or other amphetamines make it harder to fall asleep, and shift the period during sleep away from deep stage 3 sleep to shallow stage 1 sleep. REM sleep also declines. Cold medicines often include ephedrine and/or pseudoephedrine, which are chemically related to amphetamine and have stimulant effects. Caffeine also impedes sleep, and is often used to stay awake. Some find stimulants help them to sleep. More find the same stimulant helps them sleep at times and stay awake at other times.

Pain Drugs and Sleep

Opioid drugs have a profound effect on sleep (morphine was named after Morpheus, god of sleep). Opioids are often given as analgesics to reduce severe pain. In healthy people they result in a lengthening of time spent in stage 2 and a reduction in stage 3 and REM sleep. Taking opioids can actually cause apnea as they can cause excessive relaxation of the throat muscles. Milder over-the-counter analgesics called NonSteroidalAntiInflammatory Drugs (e.g. aspirin, ibuprofen) might slightly reduce sleep efficiency, but the effect is minor. Pain drugs, although they may directly degrade sleep quality, can result in better sleep for the patient if they reduce discomfort that otherwise keeps the patient awake.

Antidepressant Medications and Sleep

Depression and sleep problems are intertwined. Both insomnia and hypersomnia are considered indicating symptoms of depression, and both depression and sleep disorders are common symptoms of other disorders. Antidepressant drugs – which encompass a large number of medicines – are prescribed widely today. Selective serotonin reuptake inhibitors (SSRIs) are the most well known and others include tricyclic drugs, monoamine oxidase inhibitors (MAOIs), and serotonin antagonist reuptake inhibitors (SARIs). Although SSRIs are technically stimulants, they facilitate sleep in many people. MAO inhibitors and tricyclic antidepressants are sedatives and patients tend to develop tolerance to the sedating effects within a couple weeks, so the FDA does not label these drugs for insomnia treatment unless the insomnia is a symptom of depression. Many doctors prescribe low doses of the tricyclic antidepressant doxepin (trade name Sinequan) off-label for insomnia.

With the exception of SARIs, antidepressant drugs suppress REM sleep. Patients spend less of their sleep time in REM than when they are not on the medication. Whether this is good or bad is not clear. Sleep restriction – stopping a person from sleeping as much as they want to – is an effective short-term treatment for depression in some cases. There could be a causal relationship between reducing REM sleep and increasing the patient’s mood.

Ritanserin, eplivanserin, and similar antidepressants are being investigated for their ability to enhance slow-wave sleep.

Epilepsy Drugs and Sleep

Older drugs used to treat epilepsy affect the central nervous system and extend slow-wave sleep in patients while decreasing REM sleep. Patients tend to develop tolerance to these effects in a few weeks. Newer epilepsy drugs work in the brain’s GABA (a neurotransmitter) system, enhancing activity there. They also extend slow-wave sleep and do not produce the tolerance that older drugs produce.

Others of Note

The gastroesophageal reflux disease medicine cimetidine, some steroids and laxatives, the anticonvulsant drug phenytoin, and the respiratory drug theophylline are all known to cause insomnia in some patients.

Drugs explicitly used to influence sleep

Benzodiazepines are used for anxiety disorders and other psychiatric indications. For years they were the go-to insomnia drug, and although less often prescribed just for sleep disorders today, they certainly affect patients’ sleep. Newer benzodiazepine receptor agonists (which have some similar biochemical actions) are the most common type of prescription insomnia medication used today. All of these drugs reduce sleep latency and the amount of time the patient spend waking during their time in bed. The true benzodiazepine derivatives reduce the amount of time spent in deep (stage 3) sleep. The newer benzodiazepine receptor agonists do not, which is partly why they are better as sleep aids. All of these drugs reduce the amount of time in stage 1 sleep, and none seem to have an effect on REM sleep time.

The melatonin agonist ramelteon was approved in 2005 and has proven effective in treatment of sleep onset insomnia. It binds to two of the three melatonin receptors in the body; this seems to limit the suprachiasmatic nucleus’ wake-promoting activity.

The benzodiazepine receptor agonists do not induce rapid tolerance, the way other sedative drugs do, which is why they are good for treating insomnia. There is rebound insomnia when the drug is discontinued, but that happens with most sleep aids.

Smoking, Caffeine, and Alcohol

Many pendants like to point out that the most widely used drugs are legal, non-prescription ones. People have been influencing/modifying their sleep and waking architecture with drugs forever.  Alcohol has been used to help people relax for millennia and caffeine use is widespread and deeply entrenched in human culture.  Anyone thinking about sleep aids has to consider their consumption of alcohol and caffeine as well.

Nicotine is a stimulant and smokers tend to have higher rates of insomnia.  Studies with polysomnography show that the smokers get less slow wave sleep (the most refreshing kind) than non-smokers.  Smokers also have longer sleep latency (time to fall asleep after getting into bed) and lower overall sleep time.

Caffeine is a stimulant that appears to work by slowing the action of the neurotransmitter adenosine. Individual reactions to caffeine vary considerably. Some people find it causes insomnia. Other seem to sleep better on caffeine. Indeed, the short-term caffeine nap involves intentional consumption of caffeine before sleep.

See our page on alcohol and sleep for information on that topic.

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