What Happens in the Brain with Drug-Free Sleep Aids?
Share
Trouble sleeping, but afraid of potent prescription sleeping pills? You're definitely not alone. People are so scared of waking up groggy or foggy after taking conventional sedatives. What most of us really want is what is known as restorative sleep; i.e,. That deep, high-quality kind that makes you feel refreshed and ready for the day. In this article, we will take a more in-depth look at how these "drug-free" sleep aids actually work in the brain, how they differ from traditional sedatives, and how a well-designed formula like Defined Sleep harnesses this science to help you sleep better naturally.
To find out more about our science-backed CBD-sleep station at DefinedSleep.com
What Does It Mean for Sleep Aids to Be Drug-Free?
What's the Difference Between Drug-Free, Natural Sleep Supplements and Non-Sedative Sleep Supplements?
"Drug-free" usually means that the supplement is free of potent prescription sedatives (such as benzodiazepines) and OTC antihistamines. "Natural" can be defined as substances that come from plants or other non-synthetic sources. "Non-sedative" means that the goal is to allow your brain to reach the right stages in the sleep cycle (deep/REM) and sleep soundly without feeling groggy the next morning. But be careful because even if something is natural, it can still be a sedative that can cause dependency- that's a big difference.
Are CBD and terpenes considered to be drug-free or pharmacological?
While CBD (cannabidiol) and terpenes (aromatic plant compounds) are natural, plant-based, and non-intoxicating, they do interact with our body's biological systems (such as the endocannabinoid system); therefore, they have pharmacological properties. As a matter of fact, CBD is the active component of the FDA-approved drug Epidiolex to treat children with severe forms of intractable epilepsy. Importantly, the formula used in Defined Sleep is THC-free and melatonin-free, and is designed to support sleep architecture as opposed to just sedating.
Again, why do we get the annoying sluggishness or dependency of some of the "natural" aids?
Because they are acting on the same brain pathways as the sedative drugs, for example, with some herbal sleep aids, you may get increased levels of the neurotransmitter, gamma amino butyric acid (GABA), causing you to fall asleep more quickly, but for many sedatives cause you to spend less time in deep and REM cycles, causing you to wake up feeling fuzzy. It is the gap between falling asleep and actually sleeping well.
The non-sedative design of Defined Sleep
What Is Deep Sleep and REM Sleep, and How Does the Brain Regulate Sleep?
What are the mechanisms for falling asleep and maintaining sleep in the brain?
Multiple areas of the brain are involved in the regulation of sleep. The hypothalamus, particularly a small region known as the ventrolateral preoptic nucleus, helps you to quiet down your arousal systems so that your brain will be able to wind down. Meanwhile, your brainstem and your reticular activating system are hard at work, keeping you awake. But in order to fall asleep, you have to reduce arousal, decrease your stress hormones such as cortisol, and allow your brain to transition into its natural sleep state.
What goes on in the brain during restorative (slow wave and REM) sleep?
The problem with many sedatives is that even though they may try to help you sleep longer by putting you to sleep, they tend not to provide the very stages that your brain needs the most: deep and REM sleep. You may be spending eight hours in bed, but if the sleep stages that are supposed to be restorative are too low, you're still going to wake up tired and foggy.
Why do sedative drugs suppress these stages?
Although most sedatives frequently increase total sleep time due to their ability to induce unconsciousness, they tend to deteriorate slow wave sleep (SWS) or REM sleep, or break down sleep architecture. You may be asleep longer, but in the wrong modes that your brain needs to be in to do any good. Hence, why you can wake up even when you have had some sleep, but still feel tired and/or still foggy.
What's the Difference Between Sleep Aids and Cognitive Sleep Support?
How do prescription sedatives (e.g., benzodiazepines, hypnotics) affect the brain?
Drugs such as benzodiazepines act at GABA-A nerve receptors and enhance inhibitory neurotransmission (i.e., lowering brain activity). They lower your arousal level and make you drowsy.
Why is the Sedation not Restoration?
Because proper sleep health isn't simply hours in bed, it's the right cycles (deep + REM), with minimal interruptions, and leaves you feeling refreshed when you wake up.
What common OTC Sleep Aids (i.e., antihistamines, melatonin) do, and where do they fall short?
Antihistamines work by blocking histamine receptors, and they do induce a drowsy effect. Still, they do not improve deep or REM sleep - some antihistamines actually decrease deep and REM sleep as much as prescription sleeping drugs do. Melatonin is a hormone that regulates the onset of sleep. Production is responsible for signaling to your body that it is nighttime vs. daytime and encourages sleep onset, but does not ensure restorative sleep architecture. Some "natural" sleep aids induce drowsiness without good sleep. In fact, a recent study by the American Heart Association found that long-term use of melatonin is linked to significant adverse health effects.
Why is the Sedation not Restoration?
Proper health isn't simply how many hours you spend lying down, but ensuring that your brain spends sufficient time in the phases where deep sleep + REM occur. Sedation can result in "forced" sleep, but this is not the same as restorative sleep.
How Can CBD and Terpenes Equip Us to Sleep Better Without Being Sedated?
What is the Endocannabinoid System, and how is it related to sleep regulation?
The human body also produces cannabinoids (called endocannabinoids) in the same way as the cannabis plant. Arousal, stress, sleep-wake, and processing are all mediated through these endocannabinoids and the receptors that they bind to (CB1, CB2). CBD is also able to interact with the ECS (albeit not in the same way that THC does) and can induce sleep by triggering calming and stress-modulating (anti-anxiety) circuits, and by increasing deep and REM sleep.
How do CBD & Tepenes, and ECS receptors and sleep centers interact?
CBD has the power to regulate the CB1/CB2 indirectly, reduce cortisol and anxiety, and help our nervous system shift to rest. Terpenes, such as linalool or β-caryophyllene, may either directly or indirectly influence other types of neural pathways (GABA, adenosine, CB2) or indirectly influence ECS and brain stem activity. The goal of the bundle approach, CBD+Terpenes, is to aid in increasing deep and REM stages.
What does research say about CBD and its effect on deep and REM sleep?
A placebo-controlled double-blind, randomized, crossover trial (125 adults with insomnia) demonstrated that the treatment of a 300mg dose of CBD + terpene preparation increased the average percentage of night in the rapid-wave sleep stage as well as REM sleep. Some individuals averaged 2x as much deep and REM sleep relative to the placebo control over a period of 30 days. The clinical trials are DOI registered as NCT05233761. These findings suggest that the use of CBD + a terpene combination may offer the ability to optimize restorative sleep and not simply help you fall asleep.
What Neural Pathways Do Drug-Free Sleep Aids Interfere With?
How CBD alters Sleep Neurochemistry (e.g., Gaspar et al, 2019). Nervous system neurotransmitters in the brain are essential for many of our bodily functions, including regulating our sleep.
CBD seems to act on anxiety by modulating the serotonin (5-HT1A) receptor, acts on cortisol (HPA axis modulation), and may affect adenosine signalling (which promotes sleep), as well as indirect support for the gamma neurotransmitter (GABA). (MDPI)
What are the brain areas that the terpenes (linalool or β-myrcene) will affect?
- Linalool (from lavender): Anxiolytic, Sedative Activity in animals. Modulation of glutamate and gamma-aminobutyric acid (GABA) receptors
- β-myrcene (hops/lemongrass) Muscle relaxant, Sedative Activity in animals
- β-caryophyllene (hops/lemongrass) Selective CB2 receptor binding (animals) activity OModulation of stress/inflammation
These compounds are beneficial to help the brain transition from an excited state to a restoration state without heavy sedation.
How is this similar to the effects of traditional sedatives on the hippocampus and other parts of the brain crucial for regulating the sleep-wake cycle, attention, and alertness, etc?
Traditional sedatives blunt memory formation from the hippocampus, diminish the amplitude of slow waves, suppress REM, and may fragment sleep. By contrast, a properly composed CBD/terpene supplement would gently support the naturally occurring neural pathways that catalyze both deep and REM sleep, instead of overriding them.
Are The Effects of Drug-Free Sleep Aids Measurable in Real Life?
What do users of wearable devices (such as Oura and WHOOP) report while taking CBD-based sleep aids?
Whereas large controlled datasets are not available, many people who have used CBD/terpene aids report increased time in the "deep and REM sleep" phases when wearables are used, as well as less sleep fragmentation. The trial for Defined Sleep was done with a tracker placed on the wrist to measure SWS+REM objectively. (JCMS, PubMed)
Are improvements experienced immediately or accumulated over time?
Improvements in deep and REM sleep were observed immediately and continued over time. The treatment period in the trial lasted 4 weeks, and participants with low baseline SWS+REM or those with a diurnal sleeping habit (assumed that they are working at night, i.e., shift workers) were especially responsive to the treatment with CBD + terpenes.
Can drug-free aids help those with insomnia, menopause symptoms, or sleep disorders caused by work schedules?
The trial was focused on participants with insomnia, and demonstrated a significant benefit in those with low baseline SWS+REM and day-sleepers. While no particular trials have been done specifically for menopause or shift-worker disorder, the model suggested by the action of CBD + terpenes (support deep/REM rather than sedation) indicates that it might be helpful. As always, see your healthcare professional.
Is CBD Safe: How Does It Interact with or Affect Natural Sleeping Aids?
Can CBD interact with other drugs?
Yes. While CBD is well-tolerated, it can interact with certain medicines, including anticoagulants, anti-convulsants, and some drugs that are metabolized by the liver. Always check to see if any of the medications that you are taking interact with CBD by talking to your doctor or using an online drug interaction checker.
Are there patient populations who should talk to their doctor before attempting the drug-free solutions?
People with severe medical conditions, those taking multiple drugs, or people with a liver problem should consult their doctor before trying CBD. Also, be sure to use third-party tested products.
What are the most essential criteria in determining third-party testing & purity certificates?
Look for:
- THC-free confirmation
- Certificate of analysis (COA) indicating the amount of CBD present and the absence of harmful contaminants
- Batch and transparency from the brand -
What would make a good non-sedative sleep aid?
If you use sleep-tracking technology, what metrics should you follow to see if your sleep aid helps you??
Effective aids could help you:
- Fall asleep faster (decreased latency)...this is what all sedatives do
- Increased total sleep time
- Increases the deep (slow-wave) and REM sleeping times.
- Wake up, alert, no morning fog.
The Defined Sleep trial, with the measurement of the percentage of night in SWS+REM, has seen some quantifiable improvements.
What clinical trial design will provide valid evidence?
Quality trials are: double-blind, placebo-controlled, randomised, cross-over (where practicable), and use objective sleep recording (e.g., actigraphy). The trial for Defined sleep meets all these criteria. (ClinicalTrials). The vast majority of published clinical trials on CBD have not been conducted to this high level of rigor.
Should you make a routine out of using these products or use them as needed?
As with any sleep aid, consistency works. Use it as needed before you go to sleep while at the same time maintaining good sleep hygiene (same time at bed every night, low light, no screens). Use supplements on top of good sleeping habits, and not instead of sleep.
FAQs
Q: Is CBD A Sedative?
A: No. It is not a knock-out sedative; it promotes deeper stages of sleep and the calming down of the nervous system.
Q: Can I take a sleeping pill every night?
A: Yes, so long as no contraindication exists and the proper formula has been selected, and if always carefully checked with a health care practitioner
Q: Is There a Build-up/Build-down Effect?
A: Build-up effect or tolerance does not occur with Defined Sleep.
Willing to get restful sleep again, without tranquilizers, melatonin, or morning brain fog - Explore the Defined Sleep difference: Science-backed, plant-based, and clinically supported.
Where Can You Go To Learn More About Sleep Science and Safe Natural Alternatives?
What are other drug-free strategies that are beneficial to deep sleep?
In addition to the supplements, exercise, sleep routine, light exposure (bright early and dim late), cool bedroom, little caffeine/alcohol, mindfulness/relaxation before going to sleep.
Are doctors reluctant to prescribe ECS-friendly supplements?
Pharmacists, sleep experts, and integrative physicians who are aware of the ECS and non-sedative options are starting to be more open to using well-designed CBD/terpene formulas, especially after other sedative options have failed, or where the patient wants less fogginess upon waking up.
Tired of feeling dependent and groggy the next day, then try using natural methods to help give you deep, restorative sleep without the dependency? Unscrew the science-supported strength of natural cannabinoids and terpenes.