Sleep Medications: What is So Bad about Drugs for Insomnia?

Sleep medications are widely used and one of the most popular types of medications. In my opinion, over-the-counter and prescription sleep drugs should be a last resort. There are so many dietary and lifestyle changes that can improve sleep instead. Those changes can address the root causes of your insomnia instead of just treating the symptoms.

To read more about insomnia and why you need to sleep, see this page.

All of the sleep medications can cause dependence, at least a psychological dependence. Some of them also cause a physical dependence. “Tolerance” means that the medication loses its effectiveness at the same dose so you need a higher dosage to get effects. “Dependence” is addiction with withdrawal symptoms if the dose is missed.

Also, persistent sleeplessness can be a symptom of a more serious health problem and using sleep medications can mask the underlying problem.

Therefore, sleep medications are not a long-term solution for sleep problems, especially when you understand how they work to deal with the symptoms, but not the causes, of sleep problems and what their bad effects may be.

What are the Side Effects of Insomnia Drugs?

As you might imagine, the greater the number of possible body parts affected by a substance, the more likely that side effects can occur. Unfortunately, many sleep medications (and other drugs) do not have specific, targeted actions because the body is a complicated, interconnected thing and what affects one part most likely affects other parts as well. This results in multiple side effects.

People may also not realize that other medications or alcohol can affect how sleep medications work in their bodies. Never mix alcohol and sleep meds!

Note that many of these drugs can affect your GI tract. While most of them have not been investigated for their specific actions on the gut microbiota, some are known as non-antibiotic antimicrobials that can negatively affect Gram-positive and/or Gram-negative bacteria, which includes probiotic ones. While specific actions against the microbiota have not been investigated in most cases, it is not hard to imagine that if the GI tract is affected by nausea, vomiting, constipation or diarrhea, then there is the possibility that the microbiota is altered due to that effect.

OTC Sleep Medications

Most OTC (over-the-counter) insomnia drugs are only supposed to be used for up to 2 weeks in the younger population and not at all in people over 65. In general, OTC sleep medications do not work precisely, meaning that it can take you longer to fall asleep and longer to feel fully awake the next day. Many of them use an antihistamine as the active ingredient and you can actually develop a tolerance to one of the antihistamines, diphenhydramine (the main ingredient in Benadryl, Unisom SleepGels, Nytol, many generic or store-brand sleep aids and many of the pain-relievers with “PM” added to the name).

Antihistamines work by stopping the action of histamine in the body in one of several ways. Histamine is a neurotransmitter as well as a signaling molecule and is produced in all tissues, but is especially abundant in the skin, lung and GI tract. The sites of histamine action are called histamine receptors. The histamine-1 (H1) receptor is found in the smooth muscles (such as intestines, bronchial tubes, blood vessels, gallbladder, uterus, urinary bladder and iris of the eye.)

Diphenhydramine is an H1 receptor antagonist, which means that it binds to the H1 receptor so that histamine in the body cannot activate those receptors in the smooth muscle. Thus, diphenhydramine can affect any of those smooth muscle listed above. Additionally, diphenhydramine has a chemical structure which enables it to cross the blood-brain barrier and exert anticholinergic (anti-acetylcholine) side effects. These actions in the brain account for the non-smooth muscle side effects of the drug. 

A few of the side effects of these sleep medications are what you would expect from these antihistamines such as: sleepiness; dizziness; disturbed coordination; drying and thickening of oral, nasal and bronchial secretions; dry mouth, nose and throat; nausea, vomiting, loss of appetite, constipation; increased chest congestion; headache; muscle weakness; nervousness; vision problems; and urinary retention. There are many other possible side effects.

Some OTC sleep drugs use doxylamine succinate (Unisom SleepTabs) which blocks histamine like other H1 antihistamines. It, too, blocks acetylcholine, the body’s main neurotransmitter in the brain, in the inner adrenal glands, in smooth muscle such as those mentioned above, in the heart, in sweat glands, in salivary glands and in skeletal muscles. As you might expect, the side effects of doxylamine succinate are similar to those for diphenhydramine.

These OTC sleeping pills typically affect a person for 4-6 hours but sleepiness may last longer.

Prescription Insomnia Drugs

Many of the prescription insomnia medications are not supposed to be used for more than 2 weeks.

Central nervous system depressants are barbiturates that either cause mild sedation or sleep, depending on the dose. Higher dosages can be used in anesthesia. They act by inhibiting the actions of neurons in the brain with an exaggerated GABA response. They can be addictive. Examples are:

  • Butisol sodium
  • Carbrital (pentobarbital and carbromal)
  • Seconal (secobarbital sodium)

Selective GABA medications work on the GABA receptors in the brain to enhance relaxation. Effects are usually felt within 30 minutes. GABA is one of the neurotransmitters that is calming. Those actions sound harmless and desirable. However, the keep reading because these and many other sleep medications required stronger warnings on the products’ labels because of the risk of “complex behaviors”, described later in this article.

Some selective GABA medications are:

  • Ambien (zolpidem tartrate)
  • Ambien CR (zolpidem tartrate extended release)
  • Stilnox (zolpidem tartrate)
  • Lunesta (eszopiclone)
  • Sonata (zaleplon)

These drugs share some of the pharmacological properties of the benzodiazepines, including temporary amnesia during the effect of the drugs.

In addition to complex behaviors caused by temporary amnesia described below, potential side effects of selective GABA medicines may include memory disturbances, clumsiness, confusion, depression, behavior changes prior to sleep and hallucinations as well as abdominal or stomach pain, abnormal or decreased touch sensation, appetite disorder, bladder pain, bloody or cloudy urine, blurred vision and many others. These sleep medications can also be habit-forming.

If they are selective-GABA medications, why are there so many side effects? Numerous side effects exist because the drugs do not bind to GABA receptors like your endogenous (produced within the body) GABA does. Therefore they do not have the same actions as your endogenous GABA and can affect other things.

Selective GABA medicines typically affect a person for 6-8 hours.

Benzodiazepines have been around for a long time. Benzodiazepines activate GABA receptors in the brain; however, they are not specific to only sleep issues. Like the selective-GABA medications, they do not exactly affect GABA receptors like endogenous GABA does. They are also used an anti-anxiety medications and muscle relaxants, but are not supposed to be used long-term. Some side effects are tolerance or addiction to the drugs, poor memory while taking the drug and euphoria.

The effects of these sleep medications can last from 4 to more than 12 hours, depending on the drug and the dosage.

Some examples of them are:

  • Ativan (lorazepam)
  • Dalmane (flurazepam hydrochloride)
  • Halcion (triazolam)
  • Prosom (estazolam)
  • Restoril (temazepam)
  • Valium (diazepam)
  • Xanax (alprazolam)

Sleep-wake modifiers, or melatonin receptor agonists, such as Ramelteon (Rozerem) acts directly on the body’s sleep-wake cycle (circadian rhythm). Ramelteon binds specifically to melatonin receptors in the part of the brain that controls sleep to promote sleep. However, in doing so, it also switches on a hormone which inhibits or alters sex hormone production.

Ramelteon can affect hormone levels in the body, including sex hormones like testosterone and prolactin. This can results in a decreased interest in sex, problems getting pregnant, abnormal menstrual periods and leakage of milk from the nipples of a person who is not breastfeeding. It can also cause abnormal thoughts and behaviors such as worsening of depression, suicidal thoughts or actions, nightmares and hallucinations. It is another one of the complex behavior drugs.

Ramelteon should not be taken with or after a high-fat meal.

Expect the effects from this drug to last 4-6 hours.

Tricyclic antidepressants are sometimes used for insomnia as well as chronic pain and depression. Their side effects can be blurry vision, dry mouth, difficulty urinating and dizziness, among others. Examples of these drugs are:

  • Adapin (doxepin)
  • Aventyl (nortriptyline)
  • Elavil (amitriptyline)
  • Pamelor (nortriptyline)
  • Sinequan (doxepin)
  • Trazodone (desyrel)

Tricyclic antidepressants are not well studied for their effects on sleep.

The sedative-hypnotic drugs, or complex behavior drugs, are a class of different types of drugs that all have one scary thing in common: they can cause amnesia about complex behaviors such as eating, making phone calls and even driving while supposedly being asleep. They can also cause severe allergic reactions. As a result, they are required to have stronger warnings on the products’ labels Some of these sedative-hypnotic drugs are ones such as:

  • Ambien, Ambien CR (zolpidem tartrate), a selective GABA drug
  • Butisol sodium, a central nervous system depressant
  • Carbrital (pentobarbital and carbromal), a central nervous system depressant
  • Dalmane (flurazepam hydrochloride), a benzodiazepine
  • Doral (quazepam), a benzodiazepine
  • Halcion (triazolam), a benzodiazepine
  • Lunesta (eszopiclone), a nonbenzodiazepine hyponotic
  • Placidyl (ethchlorvynol), a nonbarbiturate hypnotic
  • Prosom (estazolam), a benzodiazepine
  • Restoril (temazepam), a benzodiazepine
  • Rozerem (ramelteon), a sleep-wake modifer
  • Seconal (secobarbital sodium), a central nervous system depressant
  • Sonata (zaleplon), a nonbarbiturate hypnotic

If Not a Sleep Medication for Insomnia, Then What Else?

First, see a doctor to rule out any thyroid, tumor or other significant medical condition which can be contributing to your insomnia.

After that, make changes in your dietary intake, lifestyle habits and exercise routines. Having a healthy gut can help you sleep better, too.

Nutritional therapy can have profound effects on your ability to sleep. If GERD keeps you up at night, review some of my suggestions for that on this page.

Protect Your Gut If You Take Insomnia Drugs

Taking any kind of sleep medication on a regular basis, unless you have a medical condition like epilepsy, is not using any of the drugs the way they were intended to be used.

If you find yourself desperate some night and you take an insomnia medication, please do what you can to protect your GI tract beforehand. Having a healthy gut will help to make the occasional sleep medication a non-event, just as it can make other occasional insults non-events.

Make sure you are eating real food. Make sure you are digesting your food properly and eliminating properly. Make sure you are repopulating the beneficial bacteria and yeasts in your gut on a regular basis with whole, raw, fermented foods and drinks and possibly probiotic supplements.

Most importantly, make sure that you do what you can to prevent yourself from being in that desperate mode of taking a sleep medication from happening again.

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