Regardless of the quality and length of average sleep per person, one thing is clear: a persistent lack of sleep can have devastating consequences for the human body and its mental and physical health. Thousands of life-threatening human errors occur every day due to a lack of adequate and normal sleep. But not only are dangerous end states associated with these disorders, but also our emotional world, our mental ability to “get through the day” and cope with challenges at work, learning skills, and relationship management – A great deal of life is influenced by sleep and lack of sleep. Insomniacs experience a variety of ways to alleviate the problem, from sleeping pills, exercise, optimal nutrition, yoga, and meditation, or complementary medicine.

Problems with regularity and quality of sleep have become a real epidemic in the last 50 years. Whoever, he above medical solutions generate the following phenomena:

• Development of dependence and mobility of the body mainly in solutions of opioid-based sedatives.
• These solutions come with a wide range of severe side effects that do not encourage consumers to start treatment.
• Sometimes these solutions ease the problem slightly but in an ineffective way.

CBD emerged as the “Solution of the century” to sleep disorders.

Sleep & the endocannabinoid system

Our body produces endocannabinoids using the endocannabinoid system – a system that contributes to maintaining the balance in the neural transport system (homeostasis). Today, scientists prove that there are situations in which the body stops producing enough endocannabinoids and it needs or can use external sources, such as hemp cannabis = phytocannabinoids. Numerous studies have already shown that CBD use achieves greater sleep cycles relative to not using it.

Researchers have begun to examine the medical potential of CBD in connection with many sleep disorders such as:

• Daydreaming and falling asleep during the day.

• Obstructive apnea.

• Rapid eye movement [REM] sleep cycle disorders.

• Nightmares as a result of Post-Traumatic Stress Disorder (PTSD) and decreased sleep quality and time as a result of chronic pain.

In addition to the importance of easy and equally quick anaesthetics is the quality of sleep itself, and its duration. Because of the way CBD stimulates the entire endocannabinoid system, it can regulate the way you sleep, allowing for continuous and prolonged sleep cycles.

• Potential Effects of Cannabidiol as a Wake-Promoting Agent.
• Clinical endocannabinoid deficiency (CECD): can this concept explain the therapeutic benefits of cannabis in migraine, fibromyalgia, irritable bowel syndrome, and other treatment-resistant conditions?
• Endocannabinoid Signaling Regulates Sleep Stability.

How does CBD Treats Sleep Disorders?

In recent decades, an idea has been tested that the neurotransmitter – Adenosine messenger plays an important role in monitoring the body’s sleep mechanism. Numerous studies have shown that adenosine agonists facilitate sedation and antagonists of adenosine have stimulation activity and make it difficult to fall asleep. The neural messengers – Adenosine and Thymidine are released from nerve cells in the brain, bind to A1 & A2 receptors corresponding in other nerve cells, thus activating mechanisms for natural relaxation and deep sleep.

The adenosine A1 receptor is ubiquitous throughout the entire body.

This receptor has an inhibitory function on most of the tissues in which it is expressed. In the brain, it slows metabolic activity by a combination of actions. Presynaptically, it reduces synaptic vesicle release while post synaptically it has been found to stabilize the magnesium on the NMDA receptor.

What is the role of CBD in preventing sleep disturbances?

Members of the Equilibrative Nucleoside Transporter (ENT) Family (TC# 2.A.57) are transport proteins that are specific to nucleosides and nucleobases and are part of the major facilitator superfamily. They generally possess 6 to10, transmembrane segments (TMSs) and are 300-600 amino acid residues in length.

ENTs function in nucleoside and nucleobase uptake for salvage pathways of nucleotide synthesis and, of adenosine available to cell surface receptors, mammalian ENTs additionally influence physiological processes ranging from cardiovascular activity to neurotransmission.

The adenosine receptors (or P1 receptors) are a class of purinergic G protein-coupled receptors with adenosine as the endogenous ligand. There are four known types of adenosine receptors in humans: A1, A2A, A2B, and A3; each is encoded by a different gene.

Adenosine A2A Receptor

The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors produces the stimulating effects of coffee, tea, and chocolate.

Each type of adenosine receptor has different functions, although with some overlap. For instance, both A1 receptors and A2A play roles in the heart, regulating myocardial oxygen consumption and coronary blood flow, while the A2A receptor also has broader anti-inflammatory effects throughout the body. These two receptors also have important roles in the brain regulating the release of other neurotransmitters such as dopamine [DA] and glutamate [Glu], while the A2B and A3 receptors are located mainly peripherally and are involved in processes such as inflammation and immune responses.

Most older compounds acting on adenosine receptors are nonselective, with the endogenous agonist adenosine being used in hospitals as a treatment for severe tachycardia (rapid heartbeat), and acting directly to slow the heart through action on all four adenosine receptors in heart tissue as well as producing a sedative effect through action on A1 and A2A receptors in the brain. Xanthine derivatives such as caffeine and theophylline act as non-selective antagonists at A1 and A2A receptors in both heart and brain and so have the opposite effect to adenosine, producing a stimulant effect and rapid heart rate. These compounds also act as phosphodiesterase inhibitors, which produce additional anti-inflammatory effects, and make them medically useful for the treatment of conditions such as asthma. Newer adenosine receptor agonists and antagonists are much more potent and subtype-selective and have allowed extensive research into the effects of blocking or stimulating the individual adenosine receptor subtypes, which is now resulting in a new generation of more selective drugs with many potential medical uses.

The plant-derived cannabinoids Δ-9-tetrahydrocannabinol (THC) and cannabidiol (CBD) both have immunosuppressive effects; although some effects of THC are mediated by the CB2 receptor, CB2 binds CBD weakly. In examining the effects of THC and CBD on microglial [MG] proliferation, a recent study has found that these compounds potently inhibit [3H]thymidine incorporation into a murine microglial cell line with no effect on the cell cycle. Treatment with THC and CBD decreased [3H]thymidine uptake into microglia, with IC50 values that match inhibition of [3H]thymidine incorporation into DNA. CBD and, less potently, THC decreased uptake of [3H]adenosine to a similar extent as [3H]thymidine in both murine microglia and RAW264.7 macrophages. Binding studies confirm that CBD binds to the equilibrative nucleoside transporter 1 [ENT-1] with a Ki < 250 nM. Because adenosine agonists have anti-inflammatory & sedative effects, and because uptake of adenosine is a primary mechanism of terminating adenosine signalling, scientists study the hypothesis that CBD is immunosuppressive & sedative because it enhances endogenous adenosine signalling. In vivo treatment with a low dose of CBD decreases TNFα production in lipopolysaccharide [LPS] -treated mice; this effect is reversed with an A2A adenosine receptor antagonist and abolished in A2A receptor knockout mice. These studies demonstrate that CBD can enhance adenosine signalling through inhibition of uptake and provide a non-cannabinoid receptor mechanism by which CBD can decrease inflammation.

CBD inhibits the adenosine transporter protein = ENT-1, allowing new adenosine molecules to bind adenosine receptors in the brain & body, strengthening sedation and sleep. Thus, adenosine activity increases, and its effect on sleep increases. The sedation is easy and fast, the insomnia is prevented and the awakening is fast, with the feeling of “filling batteries” – as proper sleep should be. Dozens of studies point to the relationship between CBD and improving and treating sleep problems. That means a lot for many people that are giving up addictive sleeping pills with severe side effects that impair function and alertness the day after.

CBD as a treatment for Insomnia

Persistent insomnia can exist as a result of several medical and psychiatric factors, incorrect sleep habits, substances that have a stimulating effect, or various biological factors (allergies). Insomnia develops in many people who are in high emotional stress, anxiety, or amid traumatic events. CBD’s known ability as an anti-anxiety can benefit insomnia sufferers. Many report the feeling of relaxation & sedation that CBD can induce throughout the body. Whether insomnia is caused by allergy, hormonal system problems, various neurological conditions, or chronic pain – cannabidiol can be a significant part of the path to a long-term solution.

Effects of acute systemic administration of cannabidiol on sleep-wake cycle in rats.

Insomnia that accompanies Epilepsy

In a preliminary study conducted between 1972 and 1980 in the United States, CBD or a placebo drug were given to 15 volunteers with epilepsy who also suffer from chronic insomnia. Seven of the eight subjects who received CBD reported a marked improvement in quality and sleep and its duration, with the group receiving the placebo drug, did not reporting any improvement.

Hypnotic and antiepileptic effects of cannabidiol.

The relationship between anxiety and sleep and how both are treated by CBD

In the Western world, anxiety is considered a multi-systemic physical and mental disorder that affects the lives of millions. Anxiety appears as a disease in changing many components of the patients’ lives, such as interpersonal contraction and social relationships, completion of professional tasks at work, and a regular sleep cycle.

Anxiety can cause a constant feeling of fatigue that comes in a place of actual sleep and when sleep does not “fill the batteries” and does not “drain the waste” – the already high level of anxiety and mental stress – increases, and so on in an endless circle. CBD helps regulate the endocannabinoid system but is also active and plays an important role in maintaining the nervous system integrity: CBD inhibits the removal (uptake) of the sedating nerve messenger adenosine. All of this makes CBD with great potential to treat anxiety and, as a result, optimally restore sleep mechanisms.

Effectiveness of Cannabidiol Oil for Pediatric Anxiety and Insomnia as Part of Posttraumatic Stress Disorder: A Case Report

CBD as a treatment of sleep disorders derived from chronic pain

Recent studies have continued to reveal the relationship between CBD use and chronic pain soothing. The anti-inflammatory feature of CBD is also associated with soothing pain. In many cases, insomnia comes from chronic pain that impairs continuous sleep and makes the nights restless and at the same time exhausting. CBD will weaken the pain and inflammation in case it is the source. It will give the body’s systems the ability to rebalance and “refill batteries” through quality sleep. Many CBD consumers who came to use it due to chronic pain reported an improvement in the sleep cycle as a result of its use. Why wouldn’t it work the other way around?

CBD as a treatment of sleep problems due to the use of THC

Many cannabis consumers are familiar with the sometimes-sedative effect that marijuana consumption has created for recreational use. Some people have to stay away from cannabis use, certainly not as daily use. Over time, marijuana strains were “divided” into two mains: “stimulating” and “soothing” varieties. Stimulating varieties have been recommended for use in the morning and during the day and sedating varieties for use in the evening and before bedtime. Interestingly, Indica “strains” contain more than 0.5% w/w of the relaxing monoterpene Myrcene while Sativa “strains” contain much less of that terpene.

Today it is known that the relaxing “varieties” are CBD-rich & CBN-rich varieties.

• Effect of Delta-9-tetrahydrocannabinol and cannabidiol on nocturnal sleep and early-morning behaviour in young adults.

• Hypnotic like effects of cannabidiol in the rat.

• Endocannabinoid modulation of cortical up-states and NREM sleep.

Useful Information:

Because CBD acts on the sleep mechanism as a whole it is not a “sleeping pill” of the familiar type that acts almost immediately and its effect expires after a given time. Much anecdotal evidence suggests that CBD begins to affect the sleep mechanism only after several days of continuous use and at a regular low dose. There are many reports of people whose sleep has improved due to the use of CBD but they do not take it at all before bed but in the morning or during the day! It takes a few hours for CBD molecules to be absorbed from the intestine, pass through the liver and reach their numerous protein targets in the human body.