SLEEP AIDS (written by dinoiii):
Catnip
BASIC MOA: Nepetalactone isomers are the actives here, somewhat like (BUT NOT EXACTLY) the active ingredients in valerian and mild sedatives.
EVIDENCE-BASED EFFICACY: A few poorly-controlled studies suggest multiple administrations throughout the day to be an effective dosing pattern which does have the potential to decrease compliance.
FORMS & DOSAGES: 2-4 grams taken in a titrated up matter to assess tolerance and avoid the potential for groggy "morning-after" feeling.
POTENTIAL SIDE EFFECTS/INTERACTIONS: None reported to date.
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Kava
BASIC MAO/Chemistry: Extracts of Kava root contain both lipophilic and hydrophilic components. The active components are referred to as kavalactones or kavapyrones. The active enolides + dienolides are thought to be kawain (kavain), methysticin (+ its dihydro active metabolite), and to a lesser extent, yangonin. These active byproducts are hypothesized to do a number of things in the central nervous system (CNS). While it is generally argued to have a MOA unknown, theories have emerged and gained support around this substance. In vitro, kavalactones have been shown to readily bind GABA-A receptors located in the hypothalamus and amygdala, areas thought to be largely responsible for emotion and memory rather than cognition and movement. KAVA may also increase the number of GABA-binding sites. Other suggested mechanisms include reduced excitatory neurotransmission by decreasing the release of glutamate, inhibition of norepinephrine uptake, reversible MAO-B inhibition, or dopamine antagonism. KAVA has also been shown to have mild anticonvulsant properties in animals, possibly involving voltage-dependent sodium channels. There have been reported analgesic effects in humans with animal data suggesting opioid receptors NOT be involved - therefore the jury is still out as to how this effect is seen.
EVEIDENCE-BASED EFFICACY: This substance has undergone several true well-conducted placebo-controlled trials in Europe and the United States for the treatment of anxiety. Most show significant improvements in anxiety symptoms in patients with moderate to severe anxiety within 8 weeks after starting treatment.
One study in particular put the supp head-to-head with a leading drug of an equivalent class:
KAVA vs. Oxazepam (a benzodiazepine) yielded similar reductions in anxiolytic effects BUT fewer adverse effects were seen in the KAVA group.
FORMS & DOASGES: Unfortunately, KAVA appears to have a slow onset of action for treatment of anxiety (which can extend to similar efficacious results in sedative-promoting effects, at which time many users may give up on the supp attributing their stoppage to its not "working"), most patients only responding after 4-8 weeks of therapy.
POTENTIAL SIDE EFFECTS/INTERACTIONS: Dinoiii's EXTREME CAUTIONARY WARNING: One of the kavalactones, kavain, has in-vitro COX-inhibitory activity and the potential for antiplatelet and anti-inflammatory effects needs further study.
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Chamomile
BASIC MOA: For purposes of sleep, you may desire to opt for the German/Hungarian variety (there is a Roman variety almost indistinguishable, but alas falls in a different genus and species.).They have tried to isolate the single most active substance in chamomile, with apigenin and other flavones, chamazulene, and a-bisabolol often identified. But most studies have concluded that a whole herb extract is better than any individual phytochemicals. Outside of its insomnia therapy use, chamomile finds use as an anti-inflammatory as well - VERY comparable, if not better than hydrocortsione!
EVIDENCE-BASED EFFICACY: One study shows induction of a deep sleep in 10 out of 12 cardiac catheterization patients, but otherwise data on a larger scale remains unfortunately deficient.
FORMS & DOSAGES: Two or three 250mg caps three times per day is what were used in the studies which makes for an exhaustive dosing protocol to follow. If you can keep up with it, however, then by all means.
POTENTIAL SIDE EFFECTS/INTERACTIONS: None reported, however, cross-reactions may be seen in anyone allergic to ragweed, celery, or aster-family herbs. Again, this is yet another one that should be avoided with NSAIDs, fish oil, vitamin E and other blood thinners due to a coumadin-like property. Minor allergic reactions have been discussed alongside nausea but dosing to induce these symptoms is highly unlikely in most people.
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Valerian
BASIC MOA: The Greeks, beginning with Hippocrates, used valerian roots (translated as phu based on its pugnant smell beneath the surface - i.e. - the root which held the medicinal properties) to help them fall asleep, an application that still holds up under scientific scrutiny. We know conclusively that valerian sedates, quiets the CNS, and minimizes muscle spasms - just like pharmaceutical tranquilizers. After a few thousand years of study, though, we still don't know why. At first, researchers referred to just two phytochemical classes - valeoptriates and the bornyl esters as contributing to 100% of the active properties, now we know there are at least several more - valeranone and the kessyl esters. Another example of the whole herb being better than the sum of its parts.
EVIDENCE-BASED EFFICACY: Combined with St. John's Wort, Valerian bested diazepam (Valium) in a 2-week trial involving 100 people being treated for anxiety. A different double-blind coupled Valerian with hops (see above) showing superiority to triazolam (Halcion), another benzodiazepine, for relieving sleep disorders. When I mention superiority here, the results on efficacy were not what contributed to that dubbing - as efficacy was NOT statistically significant in its difference. However, the safety (i.e. - less side effects associated with the non-habit-forming supplements) profile is what allows for superior rating.
FORMS & DOSAGES: About 300-500 mg of standardized extract before bedtime. 1, 425-2,780 mg of non-standardized supplement for insomnia relief before bed.
POTENTIAL SIDE EFFECTS/INTERACTIONS: Hepatotoxicity (liver toxicity) has been reported in a few multi-herb preparation formulas. It remains unclear as to whether this side effect is evident with Valerian alone. A compound called scullcap is usually the culprit I think - because the more hepatotoxic herb germander is often mistakenly harvested as scullcap. Furthermore, reports on 50 cases of overdose with a combination preparation containing hyoscine, cyproheptadine, and valerian indicated the expected symptoms of cyproheptadine and hyoscine toxicity, but no signs of hepatotoxicity developed in the short or long term.
Mild, transient stomach upset as well as nausea and vomiting have been reported anecdotally. Large doses may be associated with decreased intestinal motility - perhaps offsetting some of the appetite stimulating effects of hops when used in combo.
Valerian has also been reported to cause headache, excitability, insomnia, uneasiness, ataxia, and hypothermia, although the level of adverse effects reported in clinical trials has not been greater than for a placebo. Short-term mild impairments in vigilance, concentration, and processing time for complex thoughts, as well as mild fatigue, have been reported in trials (lasting for several hours), although residual sedative effects appear to be less pronounced than those for benzos (i.e. - no hangover drowsiness). The problem is that preliminary evidence suggests that valerian is non-sedating in recommended doses. With higher dosing protocols, the evolution of this "hangover" effect cannot be excluded. Chronic high-dose actually leads to a similar "Valerian withdrawl" similar to that seen with benzos. Delirium, ameliorated by benzos, was reported in a single patient undergoing withdrawl from high-dose valerian. Dizziness and headache have been reported rarely in human studies. Anecdotally, some people may develop a "paradoxical reaction" leading to nervousness or excitability.
Sleep Aids
Melatonin: ++ (long-term use)
Catnip: +
Kava: +++ , – (w/ NSAIDs, fish oil, Vit E)
Chamomile: ++ , – (w/ NSAIDs, fish oil, Vit E)
Valerian: +++ (high dose, short-term, proper taper), + (low dose, short term, proper taper), – (high dose, long-term, proper taper), – (high dose, short-term, abrupt cessation), – (w/ various interacting agents listed above)
