How Do Sleeping Pills Work? MOA And Usage

Last Updated: December 19, 2019

Authored by Nena Messina, Ph.D.

Sleep medications induce sleep through a mechanism that affects one’s central nervous system. There are several types of sleep medications – barbiturates, benzodiazepines, non-benzodiazepines, melatonin, antihistamines, etc. categorized according to their strength, ingredients and the mechanism of action. For instance, barbiturates are a type of medication for a sleep disorder that creates a mild sedative effect by lowering neurotransmission levels. Benzodiazepines are fast-acting sleeping pills that have a mechanism which makes a substantial impact on GABA receptors of the brain to give a quick sedative effect. This article discusses the usage and mechanism of action of different types of sleep medication, with an in-depth look into sleeping pills for children, sleeping pills side effects, recreational use of these drugs, and their addictive properties.

How Taking Sleeping Pills Works

All kinds of sleeping aids, including sleeping pills for kids, have a mechanism of action that impacts the user’s brain to induce drowsiness.

Mild sleep medications such as antihistamine drugs cause drowsiness as a side effect of their mechanism of action. The sleepiness is caused by blocking histamine, an organic nitrogenous compound. Prescription sleeping pills are stronger in their mechanism of action and are used to treat chronic insomnia. They affect the GABA receptors in the brain, inducing a kind of relaxing drowsiness that causes sleep. As for the mechanism of action of sleep cycle modifiers like Rozerem, they directly impact the circadian rhythm of the body that is simply known as the natural body clock by working on the hypothalamus.

What Sleep Aids Are Used For

Due to their nature of giving a temporary relaxing and sedative effect through their mechanism of action, sleep medications are used to treat a variety of disorders as mentioned below.

Sleeping Pills for Insomnia

This is the most common use of sleep medication. Some sleep medication helps the user fall asleep (Rozerem, Halcion, Sonata, Ambien), some helps them stay asleep (Silenor), and some deliver both results (Estazolam, Restoril, Ambien CR, Belsomra) depending on the active ingredient in sleeping pills. For example, Ambien’s active ingredient is Zolpidem Tartrate, that has a mechanism of action which impacts the GABA receptors to induce a sedative effect on the user quickly.

young man with insomnia

Sleeping Pills for Anxiety

Benzodiazepines such as Xanax and Valium are commonly referred to as the best sleeping pills for flights since their mechanism of action delivers a quick relief for anxiety due to their sedative and hypnotic effects to calm down an agitated person.

Note that it may be illegal to bring some of such medications on board. Check the laws and regulations of the destination location as well as the transporting company’s rules. Make sure to have a prescription on hand.

For Alcohol Withdrawal

One of the common symptoms of alcohol withdrawal is agitation and losing sleep. Studies show that close to 58% of those who are experiencing alcohol withdrawal have insomnia. Do sleeping pills work for this particular kind of insomnia due to the mechanism of action of sleep aids that also have addictive properties? Yes. However, due to the mechanism of action of sedative-hypnotic drugs, it should always be done as a part of a treatment plan, including therapy and lifestyle changes. Otherwise, there is the risk of developing another addiction.

Sleeping Pills for Depression

Insomnia or the inability to sleep is a known symptom of depression. Sleep aids are used as a way to quickly decrease the symptoms that negatively affect health, while other methods of psychotherapy are used to treat the more ingrained issue of depression. These drugs are also used to treating other psychiatric disorders such as PTSD.

How Long Sleeping Pills Take To Kick In

The duration that it takes for sleep aids to start taking effect depends on several factors including the type of the pill, the mechanism of action, the weight, age, and the metabolism of the user, what food they have consumed before taking the drug, how long have they gone with no sleep before taking the drug, etc.

senior woman taking sleeping pills

For a natural sleeping aid like melatonin, it usually takes up to 30 minutes since that is the time it takes for melatonin to reach a maximum concentration in the blood. If a user is constantly wondering why they took sleeping pills still can’t sleep, it may be because they have built a tolerance for the drug and should consult a doctor before they increase the dose.

How to Use Sleep Aids

Sleep aids should be taken about 30 minutes before bedtime, ideally on an empty stomach for best results. They are most effective when the user allows enough time – at least 8 hours – to sleep after taking them. Taking sleeping pills and staying awake may lead to feeling groggy and weak on the body. For this reason, it is better not to use them the night before one needs waking up early. Due to the mechanism of action in sleep aids, there is a huge chance of users starting to feel dependent on this medication.

Using Sleep Medication for Children

Inability to fall asleep or stay asleep is a frequent issue in children as well, hence the widespread use of sleeping aid for kids. Currently, there are no specific prescription sleeping pills for babies or children to treat childhood insomnia. They are usually given either antihistamine drugs such as Benadryl and Nytol or mile hypnotic sleep medication such as Ambien.

Due to their intense mechanism of action that directly affects the central nervous system of the body, this medication, even the sleep medication for children over the counter should always be given sparingly and with caution. Same concerns apply to use sleeping aids during pregnancy and while breastfeeding. While some sleep medications such as Ambien and Tylenol are considered safe during pregnancy, it is always recommended to follow the guidance of a physician.

a body taking sleeping pills

Recreational Use of Sleeping Pills

The quick relaxing and sedative effect given by certain sleeping pill ingredients and their mechanism of action has led to people taking sleeping pills recreationally. Recreational use of these medications is considered to be an abuse and may lead to legal consequences as well as health adverse reactions!

Sleep aids like Ambien, Lunesta, and Valium are common ingredients in drug cocktails, a mix of substances meant to give an intense “high” to the user that has the potential to be extremely damaging to the body, and even cause fatal situations. Another dangerous practice is mixing sleeping pills and wine or other alcoholic beverages.

Addiction to Sleep Medication and Rehabilitation

Prescription sleep aids such as benzodiazepines are not recommended to use continuously for over two weeks due to their highly addictive properties. This happens due to the natural process of the human body building a tolerance for the drug over time which makes the user increase the prescribed dose assuming that the current doses of sleeping pills don’t work. After continuing high doses of sedative medications, the user starts experiencing withdrawal symptoms if they stop using. As for how to treat addiction to sleep medication, it includes a treatment plan including detoxing, therapy, and inpatient care with medical attention. Detoxing from sedative-hypnotic drugs can be dangerous if done without the supervision of medical staff. There are well-reputed rehab places that provide these services while providing counseling for any underlying issues that may have led to addiction.

Page Sources

  1. Leonie Fricke-Oerkermann, Julia Plück, Michael Schredl, Kathrin Heinz, Alexander Mitschke, Alfred Wiater, and Gerd Lehmkuhl. Prevalence and Course of Sleep Problems in Childhood. Sleep. 2007 Oct 1; 30(10): 1371–1377.

Published on: September 17th, 2019

Updated on: December 19th, 2019

About Author

Nena Messina, Ph.D.

Nena Messina is a specialist in drug-related domestic violence. She devoted her life to the study of the connection between crime, mental health, and substance abuse. Apart from her work as management at addiction center, Nena regularly takes part in the educational program as a lecturer.


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