A revolutionary supplement for insomnia
A revolutionary supplement for insomnia
By – Dr Michael K Maraist
Insomnia is a very common disorder, affecting millions of people around the world at any given time. The incidence of insomnia is estimated to be as high as 30%. This is well demonstrated in the fact that Consumer Reports reported that in 2005, US pharmacies filled 43 million prescriptions for treatment of insomnia, with a price tag of $2.7billion.
Primary insomnia was determined to be the diagnosis in 12% of the studied population in a cross-sectional study of nearly 1000 patients who complained of sleep difficulties. While this is a complex issue, one of the key features in these patients is the heightened arousal state, where the threshold for waking is lowered (i.e. they are extremely “light sleepers”). The goal of any hypnotic medication in treating such problems is to raise that threshold and attempt to allow the patient to experience a deeper stage of sleep, so that they feel well-rested in the morning upon arising.
There are a multitude of targets that these medications attempt to modulate in order to achieve these effects within the brain. Most prescription medications which are approved by the FDA for use in treating insomnia target a system in the brain referred to as GABA. GABA (gamma amino-butryic acid) can be thought of as a sleep-promoting neurotransmitter. Neurotransmitters are chemicals that act within the central nervous system (brain and spinal cord) to cause a change in function and/or behavior. Prescription medications (such as Xanax, Valium, Ativan, and Restoril) which enhance the activity at GABA receptors in the brain increase the effects of GABA which is normally present. One of the problems with use of the GABA receptor as a target is the development of side effects as well as tolerance (i.e. medications that target the GABA receptor may lose their efficacy over time).
Other neurotransmitter targets which can be modulated to enhance sleep include the serotonin system, the histamine system, the glycine system, melatonin receptor activation, as well as modulation of adenosine levels and activity in the brain. Many of these systems are rather complicated but we will briefly touch on each of these systems.
Serotonin receptors are numerous within the brain (over 14 unique receptors have been identified within the CNS) and have many, complex functions. This system is modulated by the neurotransmitter serotonin. The serotonin system is one of the most complex neurotransmitter systems discovered thus far but is thought to be important in effects of mood regulation (i.e depression) as well as sleep and wake regulation. Many prescription medications which are used off-label to promote sleep (ex. Trazodone) are felt to be beneficial in promoting sleep due to their effects on the serotonin system within the brain. Tryptophan is an amino acid which is converted to serotonin and also serves as a precursor for melatonin and has the potential to be effective in promoting sleep by modulating the serotonin system similarly to trazodone.
The histamine system is another neurotransmitter system that can be altered to affect sleep and wake systems within the brain. Many of the over-the-counter sleep aids contain an antihistamine such as diphenhydramine (active component in Benadryl). These medications may give the consumer a sense of sleepiness after consumption, but clinical studies have failed to show any significant improvement in sleep duration and/or sleep quality. However, these drugs have been shown to impair next-day performance with concentration-related tasks.
Glycine is a unique system in the central nervous system which can also be targeted to enhance sleep. The two sleep-promoting neurotransmitters which are most-widely distributed in the central nervous system are GABA and glycine. The effects of glycine are to increase relaxation and enhance sleep by causing a generalized decrease in the activity in muscles throughout the body, thereby enhancing relaxation and promoting sleep.
Melatonin has been marketed for years for sleep-promoting effects. It is extremely important in regulating the circadian rhythm (the “sleep clock”) within all mammals to regulate normal sleep. At physiological doses (the amount of melatonin that is normally produced by the brain), sleepiness does not occur as an effect. However, in higher doses, melatonin has been shown to shorten the time that it takes to fall asleep (decreases the sleep latency). Tryptophan, also serves as a precursor to melatonin production.
Adenosine is a chemical within the body (referred to as a neuromodulator) which is extremely widely spread and has multiple end results depending on the characteristics of the receptor to which it binds. In the brain, adenosine levels have been show to increase during periods of wake. This appears to be a signal in the brain that leads to a cascade of events ultimately leading to sleep onset. The effects of chemicals referred to as adenosine agonists (drugs which bind to adenosine receptors and “act” like normal adenosine) have been shown to enhance sleep.
Tranquilo is a natural supplement which contains phenibut, hops, passion flower, tryptophan, valerian root, and mulungu. The combination of these ingredients acts on many of the neurotransmitter systems listed above to enhance sleep and relaxation.
Phenibut is actually a derivative of naturally-occurring GABA. It has been used in Russia since the 1960s as an approved treatment for post-traumatic stress disorder, anxiety, and as a nootropic drug. Nootropics have the potential to enhance memory and function of the central nervous system. Phenibut has been shown in studies to reduce stress and fear response, improve immune function as well as to enhance learning. Its effects on sleep are GABA-mediated and this is described in detail above.
Hops (Humulus lupulus) is most widely known for its use in breweries to flavor beer. However, it also has been shown to have a potential benefit in treatment of insomnia. It is most frequently used in combination with valerian root and the combination has been studied and shown to enhance sleep, when measured using certain parameters. The actual effects within the central nervous system from a chemical perspective are unclear but there have been some suggestions that the mechanism of action rests in modulating melatonin and serotonin pathways.
Passion flower (passiflora incarnata) is derived from a species of plant that is found in South America, China, New Guinea, and in the US. The actions of the extracts from this plant have been shown to act via GABA systems. Studies have demonstrated benefit in treating anxiety, stress, depression, menopausal symptoms and even as an anti-spasmotic agent.
Tryptophan is an essential amino acid that serves as a precursor to several neurotransmitters and also as a precursor to production of melatonin. The functions of these neurotransmitters are vast but many of these may assist with creating a feeling of calmness and may ease depressive symptoms. Melatonin is an important neurohormone which is a key factor in regulating sleep and wake cycles, marketed independently for years as a natural hypnotic agent.
Valerian root, particularly in combination with hops has been shown to be effective in a study looking at 30 healthy volunteers at blocking the effects of caffeine. Caffeine works to block the effects of adenosine. Adenosine, as stated above, actually acts to improve sleep quality. Scientific studies on valerian root have shown evidence of improved sleep quality with no significant side effects. It has been used for thousands of years for its effects on insomnia, even dating back to ancient Greek and Roman times. While more studies are needed to discern the exact effects the valerian root has on sleep systems, it appears to primarily work by altering adenosine activity.
Mulungu, erythrina mulungu, is a Brazilian plant that has been shown in animal studies to block the effects of toxins that were administered to induce seizures. The mechanism of action is theorized to be due to effects on the glycine system. The herb extract has been shown to also shorten sleep latency and increase total sleep time in the subjects studied.
Tranquilo is a unique natural supplement which combines the effects of each of these individual components, allowing multiple targets to improve sleep quality-melatonin, GABA, adenosine, glycine, and serotonin. Furthermore, the formula allows the possibility for improvement symptoms of anxiety, depression and menopausal symptoms.
Dr. Maraist is board-certified in both neurology and sleep medicine. He completed his undergraduate work, medical school training, residency, and sleep medicine fellowship at the University of Florida in Gainesville, Florida.
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