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Find out what supplements help insomnia
Prescription sleep medications are not without their side effects. For example, recent evidences have confirmed that benzodiazepines can raise the risk of dementia in old age. In contrast, most studies find certain natural supplements to be effective and safe in the treatment of insomnia. These natural supplements include herbs, B vitamins, amino acids and natural chemicals produced in the brain. Read on to find out which supplements can help your insomnia and how they induce sleep.
by Brad Chase
Valerian is a flowering plant that has been used as a sedative herb in traditional medicine for centuries. Even today, it is the most popular of the sedative herbs.
Valerian is also used to treat stress, anxiety and tension headaches in traditional medicine. Researchers have investigated its benefits for those suffering from these conditions as well as in the treatment of muscle spasms, epilepsy and ADHD (attention deficit hyperactivity disorder).
This herb contains a number of phytochemicals with potential sedative properties including alkaloids, volatile oil, free amino acids and even GABA.
GABA or gamma aminobutyric acid is a naturally occurring amino acid. However, it is more commonly regarded as a neurotransmitter.
In the central nervous system, GABA is the chief inhibitory neurotransmitter. It blocks neuronal activity in certain brain cells especially those belonging to the sleep centers. Therefore, it can produce a calming effect and induce sedation.
However, the GABA content of valerian is unlikely to contribute to the sedative effect of the herb because GABA does not cross the blood-brain barrier. Instead, the GABA utilized by the central nervous system is mostly synthesized in the brain.
Studies show that certain phytochemicals in valerian increase GABA levels in the brain and also increase GABA activity by binding to GABA-A receptors.
Not all studies investigating the effectiveness of valerian in the treatment of insomnia produced positive results. However, there is sufficient evidence from positive results, reviews, meta-analyses and general practice to support the use of valerian as a sedative herb.
In fact, valerian is regarded as a drug, and not a dietary supplement, in some European countries where it is available as an over-the-counter insomnia remedy.
Valerian can be used alone or in combination with herbs such as kava, hops and passionflower.
Kava or kava kava is a Pacific plant notable for its sedative and anesthetic properties. While the roots of the plant are used to prepare different types of medicinal drinks in Polynesian cultures, the leaves and stems are also included in kava supplements.
The chief bioactive phytochemicals in kava are known as kavalactones.
Kavalactones act on the central nervous system to improve cognition, mood, dreaming and sedation. They are also known for their muscle relaxant, anxiolytic and numbing effects.
Kavalactones improves mood and can reduce depression not by affecting serotonin levels but by increasing dopamine levels and enhancing the activities of noradrenaline.
The sedative effect of kavalactones derive from their ability to increase GABA-A receptor activity. Scientists believe that kava affects GABA receptors in a novel way that makes it effective even in the presence of drugs that block those receptors.
Studies show that the medicinal effects of kava last long after its ingestion. Therefore, while kava promotes deep, satisfying, dreamless sleep, it may still cause drowsiness the morning after.
There have been concerns regarding the side effects of kava especially liver toxicity. However, all evidence indicates that the herb does not cause liver damage on its own. Reports of this side effect have been linked to alcohol intake and possible contaminants in the herbal supplement.
Hop is the traditional remedy prepared from the flowers of Humulus lupulus. Besides its use as a medicinal herb, hop is also commonly added to beer to give it a bitter taste and a tangy flavor.
Hop is a folkloric remedy for insomnia and anxiety. Its inclusion in beers is believed to be responsible for some of the sedative effects of this type of alcoholic drinks. In fact, one study found that the optimal dose of hop is the concentration in which it is present in beers.
Rather than directly increase GABA levels in the brain, the phytochemicals in hop enhance GABA activity.
Therefore, hop is an excellent complement to sedative herbs that raise the concentration of GABA in the brain.
There are only a few studies done on hop but the available evidence suggests that the herb can improve the quality of sleep. However, a number of studies have investigated the benefits of combining hop with valerian.
One such study, published in 2009 in the journal, Planta Medica, found that the combination of hop and valerian is effective in the treatment of caffeine-induced insomnia.
Some studies also show that valerian-hop combinations are effective and safer alternatives to prescription sleep medications.
The sedative effects of passionflower is milder than those of valerian and kava. Therefore, it is a gentler sedative herb and commonly combined with these herbs.
The leaves, flowers and stems of passionflower are used to prepare the herb although the most popular forms are teas and infusions made from the dried leaves as well as its tincture.
Passionflower promotes sedation by stimulating the release of GABA in the body. In the brain, this neurotransmitter reduces brain activity and, therefore, induces sedation. Elsewhere, GABA relaxes the muscles. Overall, it has a calming effect.
There are a number of bioactive phytochemicals in passionflower but is unclear whether the herb’s sedative effect is due to one phytochemical or a combination of them.
The flavonoids and alkaloids in passionflower were once believed to be responsible for the herb’s sedative properties. However, recent studies indicate that the amino acid content of passionflower may also contribute by directly increasing GABA levels.
One of these amino acids, alanine, is a precursor in the synthesis of GABA in the central nervous system.
Besides raising GABA concentration in the brain, there is evidence to suggest that some of the flavonoids in passionflower can also increase GABA activity at GABA-A receptors.
Studies show that passionflower (Passiflora incarnata and not other species such as P. edulis) is an effective sedative and anxiolytic. In fact, one study showed that low doses of passionflower extract can reduce anxiety without inducing sleep.
At therapeutic doses, passionflower can relieve insomnia and improve the quality of sleep especially when combined with valerian, hops and/or kava.
Chamomile is one of the sedative herbs traditionally used to relieve anxiety and help insomnia.
The use of chamomile tea as a sedative and anxiolytic drink is supported by a number of clinical trials and meta-analyses including a 2011 review published in the journal, European Neuropsychopharmacology.
Studies show that certain phytochemicals in chamomile have high affinity for GABA receptors and promote relaxation and sedation through this ability.
Chamomile is not recommended for pregnant women because it can trigger uterine contractions. The National Institutes of Health also recommends that nursing mothers avoid chamomile.
Lemon balm is another sedative herb commonly consumed as a tea. It has a mild sedative effect and a significant anxiolytic property.
The sedative and anxiolytic properties of lemon balm are linked to one of its phytochemicals, rosmarinic acid. This natural antioxidant inhibits the enzyme, GABA transaminase. Therefore, it prolongs the actions of GABA in the brain.
Besides directly increasing GABA levels, lemon balm can also improve mood and reduce stress.
All of these beneficial medicinal effects can help provide relief for people with insomnia.
Because most sedative drugs and herbs target GABA and its receptors, some health experts recommend simply taking GABA supplements to treat insomnia and anxiety.
However, oral GABA supplements do not necessarily lead to increased GABA levels in the central nervous system. For one, GABA does not cross the blood-brain barrier in appreciable amounts. Rather, it is synthesized in the brain from amino acids such as glutamate.
On the other hand, there are studies that have reported the calming effect of GABA after the ingestion of oral GABA supplement.
To support this result is the observation that the blood-brain barrier does not effectively shield certain parts of the brain.
One of these exposed areas is known as periventricular nucleus, a part of the hypothalamus.
Since the hypothalamus controls sleep and the circadian cycle, it is possible that oral GABA supplements may induce sedation and increase GABA levels in this part of the brain. However, the periventricular nucleus has only been reached by GABA injections.
Furthermore, there is evidence that certain GABA formulations may pass through the blood-brain barrier by tweaking the drug delivery mechanisms.
Specifically, supplements made from niacin and phenylated GABA act as prodrugs and can cross into the brain. Once across the blood-brain barrier, these supplements split into niacin and GABA, two natural supplements proven to help insomnia.
L-tryptophan is an essential amino acid that serves as the precursor for a number of important compounds including niacin, serotonin and melatonin.
This means that tryptophan is a starter molecule in the syntheses of different supplements that can improve mood and sleep. Therefore, it is commonly recommended to help insomnia.
On one hand, tryptophan can increase niacin level. On the other hand, it can be used to make serotonin and then melatonin. While the second pathway has a more profound effect on sleep, it is the minor pathway.
Therefore, serotonin and melatonin supplements are sometimes preferred because they are likely to produce better results. Serotonin also has the added benefit of relieving depression, a cause of insomnia.
Melatonin supplement does not always work for insomnia. This is because melatonin is not the direct sleep trigger that it is advertised to be. It is simply a part of the sleep equation.
In addition, melatonin is released only when it is dark. Therefore, its release is linked to the normal sleep-wake cycle. Studies show that melatonin supplements produce the best results for night shift workers and those experiencing jet lag.
When magnesium deficiency causes muscle spasm and periodic limb movement especially at night, it disrupts sleep by leading to frequent arousal during the night. Therefore, magnesium supplementation can improve insomnia by relieving these involuntary muscle movements.
However, magnesium can also directly improve sleep through its effect on nerve conduction.
Magnesium is known to reduce neuronal conduction and produce a “calming” effect in the brain. This action is strong enough to increase slow wave or “deep” sleep. In fact, one of the side effects of magnesium supplementation is vivid dreaming.
Different studies have proven that magnesium can improve both the quality of sleep as well as the sleep-wake cycle. These positive effects were demonstrated in infants, adults and the elderly.
In addition, magnesium has been shown to increase the production of melatonin.
B vitamins may not be classified as sedative supplements but they can aid sleep.
These vitamins can help insomnia by correcting certain vitamin deficiencies that cause insomnia; by serving as cofactors in the synthesis of serotonin, GABA and melatonin; and by relieving conditions that may disrupt sleep.
The table below summarizes the benefits of B vitamins in the treatment of insomnia.
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Moderex, a natural remedy for anxiety and insomnia, contains natural neurotransmitters that have been shown to help combat anxiety and insomina.