5-Hydroxytrytophan (5-HTP) - Natural, alternative SSRI (Selective Serotonin Reuptake Inhibitor)
Clinical trials show that the herbal extract 5-HTP is a safe, effective way to boost brain SEROTONIN levels
SSRI’s drugs enhance brain levels of the neurotransmitter SEROTONIN, used to carry signals / pass messages between neurons (nerve cells). SEROTONIN is usually taken back into the secreting neuron from the synaptic gap between neurons, but SSRI drugs selectively block reuptake of SEROTONIN to make it more available for passing messages.
SSRIs are used to treat:
- Anxiety
- Depression
- Stress
- Panic disorder
- OCD
- Bulimia
- Hot flashes
- Premature ejaculation
- And more
5-HTP (a seed extract of the West African plant Griffonia simplicifolia readily available OTC at reasonable cost) has been shown to produce results equal to or better than those of synthetic drugs. Used in problems arising from SEROTONIN or MELATONIN deficiency and has been used for decades in Europe as an approved and effective treatment for a wide range of health problems, including depression, fibromyalgia, sleep problems (including insomnia), binge eating, pain, obsessive compulsive behavior, chronic headaches, weight loss, and other medical complaints.
5-HTP is the precursor to SEROTONIN – usually produced by the body from tryptophan (a food amino acid) via a vitamin B3-dependent enzyme ( tryptophan hydroxylase)
5-HTP for SEROTONIN – Against Depression
5-HTP for SEROTONIN – Aid for Weight-loss
The body can convert SEROTONIN to the hormone MELATONIN – responsible for setting your biological clock and helping you sleep.
Tryptophan from food is metabolized from 5-HTP to SEROTONIN to MELATONIN
Tryptophan is a naturally occurring amino acid found in certain foods (especially protein) required by the human body for the production of SEROTONIN and MELATONIN.
Tryptophan is an essential amino acid. Meaning it must be eaten, since the body cannot make it; L-tryptophan is also obtainable by prescription
Tryptophan Conversions | |
| Conversions | Details |
| Tryptophan Via Tryptophan hydroxylase(vitamin B3-dependent enzyme*) ▼ | Mainly converted in intestines; B3 shortage reduces 5-HTP, SEROTONIN, MELATONIN production |
| 5-HTP Via 5-HTP decarboxylase (vitamin B6 dependent enzymeHowever, too much B6 can convert 5-HTP to SEROTONIN before it reaches the brain **) ▼ | B6 shortage reduces SEROTONIN / MELATONIN production |
| SEROTONIN Via SEROTONIN n-acetyl transferase (NAT) ▼ | Alleviates:depression, hunger, OCD’s, Migraine, Fibromyalgia pain; |
| N-acetyl SEROTONIN (NAS) | |
| Via Hydroxy-indole-O-methyltransferase (HIOMT) + SAMe (Donates a methyl group molecule to HIOMT ) SAMe – And Other Methyl Donor Molecules (vitamin B6, B12, and folate dependent) ▼ | |
| MELATONIN | Aids Sleep; Potent antioxidant; |
* The body often uses Tryptophan to make vitamin B3, at a very high cost of 60 mg L-Tryptophan to make just 1 mg B3.
** Extremely high amounts of vitamin B6 can cause 5-HTP to convert into SEROTONIN before it reaches the brain. Consequently, this raises blood SEROTONIN levels
- 5-HTP can pass the blood brain barrier, whereas 5-HTP can pass the blood brain barrier, whereas SEROTONIN is too large a molecule. Thus it is desireable that some 5-HTP enters the brain before conversion, which may not happen if B6 is available to excess. As to how much B6 is too much is debateable, but is conservatively in the 5-10 mg range. SEROTONIN is too large a molecule. Thus it is desireable that some 5-HTP enters the brain before conversion, which may not happen if B6 is available to excess. How much B6 is too much is debateable, but is conservatively in the 5-10 mg range.
- Experiments with monkeys and rats found that ample amounts of B6 (Even to the point of “moderate excess”) increased production of brain SEROTONIN from 5-HTP by up to 60%. (Dakshinamurti et al, 1990; Hartvig et al, 1995)
Conversely, however, a notable rat study found that rats with vitamin B6 deficiency produced very little SEROTONIN in the rat brain. Dakshinamurti et al, 1976
5-HTP can be taken as a supplement to increase brain’s levels of the hormones:
- SEROTONIN – to help alleviate:Depression, anxiety, hunger, OCD’s, Migraine, Fibromyalgia pain;
- MELATONIN – help with: Insomnia, also a powerful antioxidant in the body;
Advantages of 5-HTP over tryptophan supplementation
- 5-HTP more easily passes blood brain barrier (BBB). For many people, getting tryptophan through the blood brain barrier is the main bottleneck leading to inadequate brain SEROTONIN levels. 5-HTP passes through the BBB into the brain far more easily than tryptophan.
- Less competition / more efficient. Unlike tryptophan, 5-HTP is not used to make proteins in the body, so there is no competition for 5-HTP by cells outside the brain, as there is for the body’s scarce tryptophan supplies. Human clinical studies show that 5-HTP is far more efficient at increasing brain SEROTONIN levels than L-tryptophan.
- More effective against depression. 5-HTP has been a far more successful antidepressant, even when the Tryptophan dosage used is 10 to 15 times higher than the 5-HTP dosage. Also, relapses back into depression are more common with Tryptophan than with 5-HTP.
- Not toxic to liver (especially when under stress). L-Tryptophan can be broken down in the liver by pyrrolase, an enzyme that converts Tryptophan to kynurenine and its metabolites, which can be mildly liver toxic at high levels. 5-HTP is not metabolized through this pathway. The stress hormone, CORTISOL, activates pyrrolase, such that any L-Tryptophan supplementation should be kept to under 1 gram (1000 mg.),especially in those who are chronically stressed.
- 5-HTP also increases mood /alertness neurotransmitters. Unlike Tryptophan, 5-HTP has been shown to increase brain dopamine and noradrenaline activity. These are two key mood and alertness regulating neurotransmitters, and when tyrosine, the amino-acid precursor for brain dopamine/ noradrenaline is given along with 5-HTP, the effect is even more powerful.
Health benefits of supplementing 5-HTP
5-HTP for MELATONIN - To treat insomnia and other sleeping disorders
MELATONIN is the body’s natural “Sleeping Pill”
- MELATONIN regulates our sleep-wake cycle and helps us fall asleep – Low MELATONIN levels can cause sleep-onset insomnia. Research studies show that supplementing with 5-HTP may have positive effects on sleep patterns.
- The pineal gland (“Third Eye”) – a small organ within the brain, sometimes called the “third eye” that “sees” more deeply and truly than the other two. Stimulated by darkness and inhibited by light, the pineal gland produces small amounts of MELATONIN from SEROTONIN during the day and larger amounts at night. MELATONIN produced is also stored in the pineal gland.
- How does the body utilize MELATONIN to control sleep? – the pineal gland uses MELATONIN as a “messenger” to other systems.
5-HTP supplementation is preferable to MELATONIN for insomnia
- 5-HTP improves the quality of sleep – instead of feeling tired, worn out, and “hungover” people taking 5-HTP feel vibrant, well rested, and ready to take on the challenges of the day. When we sleep more deeply and dream more efficiently, we wake in the morning with our physical and psychological “batteries”fully charged.
- 5-HTP provides the quickest, most effective, and most consistent overall results in treating insomnia – People who use MELATONINas a sleep sedative may find that switching from MELATONIN to 5-HTP will make it easier to fall asleep and to stay asleep. They will also enjoy healthy and memorable dream periods, and wake up without the morning grogginess that some people experience with MELATONIN.
- 5-HTP directly triggers production and release of MELATONIN irrespective of how much light is present – by by-passing the brain’s light-regulation system that controls MELATONIN secretion.5-HTP results in the increased production of neurotransmitters such as SEROTONIN and NOREPINEPHRINE that stimulate the noradrenergic receptors in the brain. This stimulation directly triggers the production and release of MELATONIN.The higher level of circulating MELATONIN helps you to fall and stay asleep better.
Obtain the broader benefits from increased SEROTONIN l evels – which are not increased by taking MELATONIN alone (MELATONIN does not enhance SEROTONIN functions).
The effects of 5-HTP on MELATONIN depend on:
- How much 5-HTP you take
- Time of day 5-HTP is taken
5-HTP increases REM sleep significantly (typically by about 25%) while simultaneously increasing deep sleep stages 3, and 4 (without increasing total sleep time) – making sleep more restful and rejuvenating. 5-HTP accomplishes this by shortening the amount of time you spend in sleep stages 1 and 2, which in some ways are the least important stages of the cycle. The higher the dose, the more time spent in REM – In most cases, the lower dosage is adequate. Higher doses may lead to a greater number of disturbing dreams and nightmares due to abnormally prolonged REM sleep. It can also lead to mild nausea.
5-HTP is also useful in the treatment of sleep disorders other than insomnia – indicated by clinical studies.
5-HTP for SEROTONIN to treat depression
5-HTP comparable to popular SSRIs / antidepressants. Double-blind studies of depression sufferers have compared 5-HTP to many of the popular SSRIs and tricyclic antidepressants, showing consistent results as good, if not better, but with much milder side-effects. Since the early 1970s, at least 15 studies involving 511 subjects have evaluated the clinical effects of 5-HTP on depression. Overall, study results showed a significant improvement in 56% of the subjects.
In one study 59 depressed patients were given 150-300 mg of 5-HTP /day. Astoundingly, 40 of the patients (68%) showed a favorable response, and most within one week.
Several small studies have compared 5-HTP to standard antidepressants. The best was a 6-week study of 63 people given either 5-HTP (100 mg 3 times daily) or an antidepressant in the Prozac family (fluvoxamine, 50 mg 3 times / day). Researchers found equal benefit between the supplement and the drug. However, 5-HTP caused fewer and less severe side effects.
Studies show that the beta endorphins (the “feel good” hormones) are significantly increased after consumption of 200 mg. of 5-HTP / day by patients with severe depression.
Indoleamine Hypothesis – i.e. Depression is caused by SEROTONIN deficiency – Accumulated evidence supports the indoleamine hypothesis of depression, which suggests that major depression results from a deficiency of available SEROTONIN or inefficient SEROTONIN.
Among the evidence supporting this hypothesis is:
- The effectiveness of SSRIs on depression.
- A study found that the brains of the teenagers who committed suicide had about 1.7 times the total amount of SEROTONIN 2-A receptors (abbreviated as 5-HT2A) in the frontal cortex (important in mood and decision making, among other roles) and the hippocampus (an area important in mood, learning, and memory). In addition, the gene signal for the SEROTONIN 2-A receptors was increased in the same regions. The receptor labeling method clearly indicated that SEROTONIN 2-A receptors were higher in the teenagers who committed suicide, and suggested that a particular cell type in a deep layer of the cortex was most affected.
- Evidence of reduced levels of 5-hydroxyindolacetic (5-HIAA) acid, a SEROTONIN metabolite, in the cerebral spinal fluid of depressed patients. Manuel Tancer, M.D. and Charles R. Schuster, Ph.D.
5-HTP for SEROTONIN to aid weight loss
As an appetite Suppressant. Brain SEROTONIN levels control feelings of fullness after we eat. Weight gain has been linked to a SEROTONIN deficiency in the brain.
- A shortage of SEROTONIN, means the brain doesn’t tell us to stop eating – ultimately leading to obesity.
- Weight loss products such as Redux and Fenfluramine (of the Phen-Fen diet) work similarly to anti-depressants such as Prozac and Zoloft, by increasing SEROTONIN levels – by using a SEROTONIN reuptake inhibiting mechanism.
SEROTONIN has also been found to effect the body’s percentage of diet-induced heat production thermogenesis) -a certain amount of food consumed is immediately converted to heat. Evidence indicates that the level of diet-induced thermogenesis is what determines whether a person is likely to be overweight, since food energy not converted to heat is stored as fat.
A meal may stimulate an increase in heat production:
- Up to a 40% in lean people
- or 10% or less in obese people.
Studies using 5-HTP for weight loss
- 5-HTP supplementation enabled overweight individuals to adhere to dietary recommendations and achieved significant weight loss in a 12-week double-blind study – 20 overweight women were randomly assigned to receive either 5-HTP (300 mg three times/day) or a placebo.No diet was prescribed during the first 6 weeks; the women were placed on a 1200 calorie diet for the second 6 weeks. The women who took the placebo lost 2.28 lbs, while the women who took the 5-HTP lost 10.34 lbs.
5-HTP appeared to promote weight loss by promoting a feeling of satiety and a reduction in carbohydrate intake thus reducing calories consumed – it appeared that the women in the control group had difficulty adhering to the diet, whereas 90% of the 5-HTP group reported having no problem maintaining the diet. Cangiano C et al
- 5-HTP supplementation for 5 weeks reduced calorie intake and promoted weight loss in women who otherwise made no conscious effort to lose weight –The women achieved a weight-loss averaging 3lb during the five-week period. Cangiano C et al, University of Rome, Italy.
- A 1989 study showed 200 mg of 5-HTP increases the MELATONIN levels in the body nearly 200% – this is significant because in a 12-week rodent study, rats given MELATONIN experienced reductions in body weight, visceral fat, plasma leptin and plasma insulin levels. Schwarz, Young, and Brown,Kyurenine and SEROTONIN Pathways Progress in Tryptophan Research. Advances in Experimental Medicine and Biology, 1989.
- In a 12-week study of 5-HTP supplementation, an average 6lbs was lost in the first 6 weeks and an additional average of about 8lbs was lost in the second 6 weeks – 300 mg of 5-HTP was given before each meal. It was realized that decrease in appetite was the most likely reason for the weight loss. The side effect to the 300 mg three times / day dosage was that 70% of the patients felt nauseous during the first six weeks, but none of the patients reported nausea by the second six weeks.
- Animal studies – have shown that administering 5-HTP literally turns off hunger and the craving for food.
How to supplement 5-HTP
Where to find 5-HTP ?
5-HTP is readily available in stores as an extract from the seeds of Griffonia Simplicifolia (a West African plant ). Note that since 5-HTP cannot be patented, drug companies have no interest in promoting this natural compound.
How much 5-HTP to take?
The typical recommendation is 50 – 100mg 5-HTP three times / day spaced apart – Start with 50mg and build up to minimize side effects.
(Some supporting studies used doses of 5-HTP in the range of 300-900mg /day – for reducing pain in migraines, fibromyalgia, reducing appetite and promoting sleep).
If after 4 weeks at 100 mg 5-HTP three times /day the desired results are not achieved, then increase the dosage to 200 mg three times / day.
(Up to 300 mg 5-HTP three times /day has been well tolerated. However, do not exceed 900 mg per day. Mild nausea is sometimes reported at higher doses, but is generally temporary).
When to take 5-HTP?
For most problems: | 5-HTP can be taken any time of day. |
For weight loss: | To act as a natural appetite suppressant and reduce the craving for carbohydrates, take 5-HTP on an empty stomach 20-30 minutes before each meal. |
For insomnia: | Take 100 to 300 mg 5-HTP, 30-45 minutes before retiring. Start with the lower dose for 3 days, then consider increasing the dose if results are unsatisfactory. |
5-HTP will not be effective without B vitamins
Conversion enzymes require B3, B6 and B12 – Take a daily B-complex supplement -either of:
- A whole food green drink – containing a daily sufficiency of B vitamins
- B complex supplement – in particular, B12 deficiency seems to be a common factor in those experiencing insomnia
Vitamin B12 (Cobalamin) – “The energy vitamin”
Side Effects of 5-HTP?
Minor gastrointestinal discomfort, including nausea – Human studies at doses of 400mg /day of 5-HTP find no serious side effects, and only about 20% incidence of mild, transitory side effects.
Toxicity of 5-HTP?
Animal studies show the first signs of 5-HTP toxicity at ~1000mg (scaled for human bodyweight), with diarrhea a common side effect. Death is first noted in dogs around the human equivalent of 10,000 mg.
Studies at 800-900mg /day in humans have never been found life threatening or otherwise having serious side-effects. Many mild side effects at these dosages have been found, but after the dosage is decreased, they go away.
Nutritional Support for Brain and Nervous System | |
What | Comments |
| Vitamin B Complex (especially Vitamins B3, B6 and B12) andmagnesium;St John’s Wort, Tyrosine (poultry, almonds, avocados, bananas dairy products, lima beans, pumpkin, seeds sesame seeds), Ginger, Marine Oil and Flax Seed Oil | B3 and B6 aid SEROTONIN synthesis.However, note that Vitamin B6 taken in doses > 5mg causes 5-HTP to be converted into SEROTONINbefore it passes into the brain – Since SEROTONIN does not pass the blood-brain barrier as easily as 5-HTP does, this effect is undesirable. |
| Water | 6-8 glasses per day with 1/4 tsp sea or Himalayan salt per qt. |
| Ginkgo Biloba | To improve brain circulation (E.g. Dr. Schulze’s Brain Circulation Improver) |
| Tryptophan-rich foodsProtein: turkey, chicken, fish, pheasant, partridge, cottage cheese, eggs, nuts, milk, cheese.Non-Protein: bananas, wheat germ, avocados, and the legumes (beans, peas, pulses, soy) | Naturally boost SEROTONIN levels.Tryptophan is such a large molecule, other more easily absorbed amino acids in protein actively compete with it to cross the blood-brain barrier. In order to divert them, and encourage the uptake of tryptophan it is helpful to eat starchy foods, such as brown rice, whole meal bread, oatmeal and jacket potatoes, alongside the protein foods. |
| Reduce caffeine and alcohol and OMIT aspartame, sucralose and soda from your diet | |
References
Cangiano C et al, Eating behavior and adherence to dietary prescriptions in obese adult subjects treated with 5-hydroxytryptophan, 3rd Department of Internal Medicine, University of Rome, La Sapienza, Italy
Dakshinamurti K, Sharma SK, Bonke D. (1990) Influence of B vitamins on binding properties of serotonin receptors in the CNS of rats. Klin Wochenschr;68:142-145.
Dakshinamurti K, LeBlancq WD, Herchl R, Havlicek V. (1976) Nonparallel changes, in brain monoamines of pyridoxine deficient growing rats. Exp Brain Res.;26:355-366.
Hartvig P, Lindner KJ, Bjurling P, Langstrom B, Tedroff J. (1995) Pyridoxine effect on synthesis rate of serotonin in the monkey brain measured with positron emission tomography. J Neural Trans ;102:91-97.
Manuel Tancer, M.D. and Charles R. Schuster, Ph.D., SEROTONIN and dopamine system interactions in the reinforcing properties of psychostimulants: A research strategy; Clinical Research Division on Substance Abuse Department of Pyschiatry and Behavioral Neurosciences, Wayne State University School of Medicine
