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UNDERSTANDING SLEEPING PILLS

Sleeping pills are medicines that are designed to help people fall asleep or stay asleep. Most sleeping pills are classified as sedative hypnotics and are prescription drugs (this may be regulated and handled differently depending on the country you are in). This specific class of drugs includes benzodiazepines, barbiturates, other hypnotics, and over-the-counter sleeping aids.

Benzodiazepines

Benzodiazepines (commonly called "benzos") are anti-anxiety drugs, which increase drowsiness and help people sleep. They are drugs that work on the central nervous system in the brain. Benzodiazepine agents attach to specific receptors in our brain to make the nerves in the brain less sensitive to stimulation, which has a calming effect on us. Note that all benzodiazepines are potentially addictive and can cause issues related to our memory and our attention. An addiction is characterized by the body building up its resistance level against the drug, which means the drug loses its impact. As a result of the higher resistance level, one would have to take higher dosages of the drug to maintain the same initial effect over time. Because of the danger of potential addiction, benzodiazepines are usually not recommended for long-term treatment of sleeping problems. Beside the short-term treatment of sleeping disorders, benzodiazepines are also used to treat other conditions, such as anxiety, panic disorders, seizures, alcohol withdrawal or as a muscle relaxant. Commonly used generic names (and brand names) of benzodiazepines are: alprazolam (Niravam, Xanax, Alprazolam Intenson), clonazepam (Klonopin), diazepam (Valium, Diazepam Intenson, Diastat), lorazepam (Ativan, Lorazepam Intensol), midazolam (Versed, Hypnovel, Dormonid, Dormicum), temazepam (Restoril), and triazolam (Halcion).

 

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Barbiturates

Barbiturates also belong to the sedative-hypnotic class of drugs. Barbiturates act as a depressant of the central nervous system and are prescribed as sedatives or sleeping pills. Depending on dosage, this drug can produce a wide range of effects, from mild sedation to complete anesthesia. Generally barbiturates are used as anesthesia and an overdose can be fatal. As with Benzodiazepines, with regular use of the drug the body builds a tolerance to the effects of barbiturates over time. Some common generic names (and brand names) of barbiturates are: secobarbital (Seconal, Seconal Sodium), mephobarbital (Mebaral), pentobarbital (Nembutal, Nembutal Sodium), butabarbital (Butisol Sodium), phenobarbital (Luminal), and amobarbital (Amytal Sodium).

Other Hypnotics

There are various other sedative or hypnotic drugs. Newer medications are designed to help reduce the time it takes to fall asleep and are somewhat less likely than benzodiazepines to be addictive or habit-forming. However, these drugs can over time still cause physical dependence, or in other words addiction. Some of these generic drugs, which work on the central nervous system by binding to the same receptors in the brain like benzodiazepines, include eszopiclone (Lunesta), zaleplon (Sonata) and zolpidem (Ambien, Edluar, Intermezzo, Stilnox). These drugs can work quickly to increase drowsiness and sleep.

 

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Another drug that is used to help falling asleep is ramelteon (Rozerem). Ramelteon works differently than the drugs covered earlier, as it’s stimulating receptors for melatonin in the brain. Melatonin and its receptors control the circadian rhythm of the body (see post "Our Body Clock), which controls the sleep/wake cycle. In other words, ramelteon doesn’t work on depressing the central nervous system, but acts by targeting the sleep/wake cycle. Ramelteon is not addictive or habit-forming. Another unique sleep aid is suvorexant (Belsomra). It affects a brain chemical called orexin, a hormone that promotes wakefulness and causes insomnia, and is also not addictive or habit-forming. Given that both drugs ramelteon and suvorexant are not addictive, they can be prescribed for long-term treatment of sleeping disorders. 

 

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Over-the-Counter Sleeping Aids

There are also sleeping aids that are seen safe enough to be sold over the counter, which means no prescription is necessary to buy them. Diphenhydramine (Brand names: Banophen, Siladryl, Benadryl, Robitussin, Sudafed) and doxylamine succinate (Brand names: Sleep Aid, Unisom SleepTabs, Equate Sleep Aid, Doxytex, Aleve PM) are both sedating antihistamines. While there is no specific proof that they work well against insomnia, they are also used as sleeping aids. Another over the counter perceived sleeping aid is melatonin supplements. There is some research suggesting that melatonin supplements might be helpful in treating jet lag or reducing the time to fall asleep. Typically, the effect of melatonin is mild. Valerian is another natural remedy used against insomnia. Supplements made from the plant valerian are sometimes taken as sleeping aides or to treat anxiety. While a few research studies indicate some therapeutic benefit of valerian, other studies haven’t found the same benefits.

Side Effects of Sleeping Pills

Like most other medications, sleeping pills do have side effects. Whether those side effects affected us though, we would only know after we took a pill. In any case, the use of sleeping pills should always be discussed with the doctor, who can alert us about possible side effects, especially for those with asthma or other health conditions. One potentially harmful side effect to be aware of is that sleeping pills can interfere with normal breathing, which means they can be a danger for people with certain chronic lung problems, such as asthma, emphysema (a condition where the air sacs of the lungs are damaged and enlarged, causing breathlessness), or chronic obstructive pulmonary disease (progressive lung diseases, like emphysema, chronic bronchitis, non-reversible asthma or bronchiectasis). Common side effects of sleeping pills are: burning or tingling in the hands, arms, feet or legs, changes in appetite, constipation, diarrhoea, difficulty keeping balance, dizziness, daytime drowsiness, dry mouth or throat, gas, headache, heartburn, impairment the next day, mental slowing, attention or memory problems, stomach pain or tenderness, uncontrollable shaking of body parts, unusual dreams, weakness. Any such side effect occurring should immediately be discussed with the doctor.

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Some sleeping pills have potentially harmful side effects, including Parasomnias. Parasomnias are actions, behaviours or movements over which we have no control (e.g. sleepwalking), as one is asleep and not aware of what’s happening. Parasomnias with sleeping pills may even include sleep eating, making phone calls, smoking, or having sex while in a state of sleep. Driving under the influence of a sleeping pill, while not being fully awake, is another serious side effect. In any case, it’s not recommended to either drive or operate heavy machinery after taking a sleeping pill. While parasomnias are relatively rare, they are quite difficult to detect once a sleeping pill takes effect. Complex sleep behaviours are more likely to occur if the dosage is increased, hence only take the dosage the doctor prescribes, and not more.


Lastly on side effects, some people could be allergic to the active ingredient of a drug or to any of its inactive ingredients (binders, coatings, dyes). The same possibility applies to sleeping pills. People who develop an allergic reaction to a sleeping pill should avoid taking the pill and immediately consult the doctor at the first sign of any of the following serious side effects: blurred vision or any eyesight problem, chest pain, breathing/swallowing difficulties. feeling of closing throat, hives, hoarseness, itching, nausea, pounding heartbeat, rash, shortness of breath, vomiting, swelling of eyes, face, lips, tongue or throat. Furthermore, a serious and potentially fatal side effect of any medicine someone is allergic to is anaphylaxis (an acute allergic reaction to an antigen to which the body has become hypersensitive). Another possible effect is angioedema, which is severe swelling, usually in the face near eyes and mouth. The swelling can also occur on the inside of the throat, which is a dangerous situation due to possible impairment of breathing. Those who are at risk of allergic reactions, should discuss these possibilities with the doctor. 


When to take Sleeping Pills?

The usual recommendation is to take a sleeping pill right before the desired bedtime. The doctor’s instructions on the pill prescription label apply and must be followed. It’s also strongly recommended to allow ample time to sleep before taking a sleeping pill.

 

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When NOT to take Sleeping Pills?

NEVER combine sleeping pills with the consumption of alcohol! Mixing the two can have additive sedating effects from both drugs, and the combination can cause someone to stop breathing , which can be fatal. Labels on sleeping pill packages warn against consuming alcohol while taking the drug. In addition, one should not eat grapefruit or drink grapefruit juice while taking sleeping pills. Grapefruit increases the amount of the drug absorbed into the bloodstream and how long it stays in the body, which can cause over-sedation. The Grapefruit phenomenon does not only apply to sleeping pills, but can interfere with other medications as well (e.g. immunosuppressant drugs).


Other Precautions

Diphenhydramine and doxylamine (usually non-prescription over-the-counter sleepigng aids) saren't recommended for people who have closed-angle glaucoma, asthma, chronic obstructive pulmonary disease, sleep apnea, severe liver disease, digestive system obstruction or urinary retention. Furthermore, sleeping aids pose risks for pregnant and/or breast-feeding women, and might pose risks to elderly people over the age of 75, such as an increased risk of strokes and dementia.


Sleeping Pill Dependency

Most sleeping pills are not suitable to treat insomnia long-term, as the effect may deteriorate after some time due to the body building up a tolerance to the drug. This is specially the case with benzodiazepines and barbiturates, but also with some other hypnotics and sedatives. One can also become psychologically dependent on sleeping pills, which is the case if going to bed without a sleeping pill causes anxiety. Finding it difficult to sleep without a sleeping pill could be a sign of a physical or emotional dependence (or both) on the drug. The best way to avoid such a condition is to always follow the doctor’s instructions and stop talking the drug when recommended.

A good night’s sleep is essential for our wellbeing, as discussed in more detail in the previous post “HOW LACK OF SLEEP IMPACTS OUR BRAIN AND BODY”. Continuous sleeping problems should be discussed with the doctor, who may recommend lifestyle changes or behavioural therapy to help learn new sleep habits and ways to make the sleeping environment more conducive to sleep. Depending on the case, short-term treatments with prescription drugs to help falling asleep or staying asleep might be recommended. In any case, it is highly recommended NOT to self-medicate with over-the-counter available non-prescription sleeping aids, but to consult a doctor.

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