5-HTP

Can Melatonin and 5-HTP Improve Your Sleep?

Posted by

1


An estimated 40 percent of Americans are sleep deprived, according to the documentary “Sleepless in America,” with many getting less than five hours of sleep per night.

Melatonin Levels

Story at-a-glance

  • Melatonin significantly reduced or prevented jet lag when taken close to the target bedtime at the destination
  • Melatonin may decrease the time it takes to fall asleep and improve total sleep time and quality
  • Your body produces 5-HTP (5-hydroxytryptophan) from the amino acid tryptophan
  • 5-HTP works in your brain and central nervous system by promoting the production of the neurotransmitter serotonin, and thereby may help boost mood and enhance sleep

There are many reasons for this, from intentionally staying up late to watch TV or surf the web to health problems (like pain) that keep you awake.

Millions of Americans struggle to fall asleep each night, including about 10 percent who suffer from chronic insomnia. This latter condition involves difficulty falling asleep and staying asleep, as well as waking up too early in the morning.

In many cases, making changes to your sleep-hygiene routine and lifestyle, such as exercising more and avoiding exposure to blue light at night, can significantly improve your sleep.

However, if you feel like you’ve tried virtually everything and you’re still struggling to get a restful night’s sleep, it might be time to consider two natural supplements, melatonin and 5-hydroxytryptophan (5-HTP).

Why Melatonin Is Important for Sound Sleep

Your brain typically starts secreting the hormone melatonin around 9 or 10 p.m., which makes you sleepy. These regularly occurring secretions help regulate your sleep cycle as well as provide other important health benefits, including helping to prevent cancer.

Melatonin acts as a marker of your circadian phase or biological timing. In a nutshell, this hormone influences what time of day or night your body thinks it is, regardless of what time the clock on the wall displays.

Melatonin is produced by a pea-sized gland in the middle of your brain called the pineal gland.

In a normal night’s sleep, your melatonin levels stay elevated for about 12 hours. Then, as the sun rises, your pineal gland reduces your production of melatonin, and the levels in your blood decrease until they’re hardly measurable at all.

When your circadian rhythms are disrupted, such as from shift work, jet lag or nighttime light exposure, your body produces less melatonin.

Melatonin deficiency may come with some profound biological disadvantages, such as higher levels of inflammation, a weakened immune system, and an increased risk of cancer.

Who May Benefit From Melatonin Supplements?

It is best to encourage your body to produce its own melatonin. Your pineal gland produces melatonin roughly in approximation to the contrast of bright sun exposure in the day and complete darkness at night.

If you are in darkness all day long, it can’t appreciate the difference and will not optimize your melatonin production.

So one of the best ways to increase your melatonin production naturally is to get exposure to bright sunlight during the day and sleep in complete blackness at night. Supplementation may be beneficial in some cases, particularly if your circadian rhythm is off (such as from jet lag).

In a Cochrane review that analyzed 10 randomized trials, melatonin significantly reduced or prevented jet lag when taken close to the target bedtime at the destination.

The researchers recommended melatonin for adult travelers flying across five or more time zones, particularly in the eastern direction, and, if necessary, for those flying across two to four time zones.1

A recent review published in the French journal Annales Pharmaceutiques Françaises further revealed the importance of melatonin in regulating the body’s internal clock for optimal sleep:2

“The internal or biological clock which is located in the suprachiasmatic nuclei of the anterior hypothalamus is controlled by clock genes and environmental factors which are able to synchronize the clock to 24h.

Rhythm desynchronization (shiftwork and nightwork, transmeridian flights, aging, some psychiatric diseases, blindness, intake of some drugs … ) occurs when the internal clock does no longer work in harmony with the astronomical time i.e. our watch.

The circadian system consists of three major elements, which are the clock, the retinohypothalamic tract and melatonin which is secreted by the pineal gland and considered as the arrow of the clock.

Both light and melatonin present a phase response curve useful for the treatment of sleep circadian disorders.”

More Is Not Typically Better With Melatonin Supplementation

As for dosage, the researchers noted, “Daily doses of melatonin between 0.5 and 5 mg [milligrams] are similarly effective, except that people fall asleep faster and sleep better after 5 mg than 0.5 mg. Doses above 5 mg appear to be no more effective.”

In a study looking into the use of melatonin for primary sleep disorders, the supplement also appeared safe and effective, working to decrease the time it takes to fall asleep and improve total sleep time and quality.3

Keep in mind that only a very small dose is required — typically 0.25 mg or 0.5 mg to start with, and you can adjust it up from there.

Taking higher doses, such as 3 mg, can sometimes make you more wakeful instead of sleepier, so adjust your dose carefully and, ideally, under the guidance of a holistic health care practitioner.

In addition, melatonin supplementation may be most effective in people with low melatonin levels. If your levels are optimized, you may not experience additional sleep benefits from added supplementation.

Melatonin’s Link to Diabetes Risk

About one-third of people are thought to carry a gene variant to melatonin receptor 1B (MTNR1B), which increases the risk of developing type 2 diabetes.

A new study from researchers at Lund University in Sweden has now revealed that the effect of melatonin is stronger in carriers of this genetic variant, and this may be responsible for the increased diabetes risk.4

The study involved 23 carriers of the genetic variant and 22 non-carriers. Both groups received 4 mg of melatonin at bedtime for three months. The variant carriers had lowered insulin secretion and significantly higher blood sugar levels after melatonin supplementation.

Similar results were first demonstrated in lab-cultured beta cells and mice, which showed melatonin causes insulin-producing cells to reduce insulin release via signaling from MTNR1B melatonin receptor proteins.

Mice with disrupted MTNR1B receptors produced more insulin, but in people with the aforementioned genetic variant, the amount of MTNR1B protein on insulin-producing cells is increased.

Since the cells then become more sensitive to melatonin, they produce less insulin, leading to higher blood sugar levels. As reported by Medical News Today:5

“Senior investigator Dr. Hindrik Mulder, a professor specializing in molecular metabolism at Lund’s Diabetes Center, says their findings could explain why the risk of developing type 2 diabetes is higher in people who work overnight or who have sleeping disorders.”

What Is 5-HTP and How Does It Affect Sleep?

Your body produces 5-HTP (5-hydroxytryptophan) from the amino acid tryptophan (found in foods like poultry, eggs and cheese).

However, eating tryptophan-rich foods is not likely to significantly increase your 5-HTP levels, so 5-HTP supplements (which are made from extracts of the seeds of the African tree Griffonia simplicifolia) are sometimes used.

The chemical 5-HTP works in your brain and central nervous system by promoting the production of the neurotransmitter serotonin, and thereby may help boost mood and enhance sleep.

In one study, an amino acid preparation containing both GABA (a calming neurotransmitter) and 5-HTP reduced time to fall asleep, increased the duration of sleep and improved sleep quality.6 Further, as noted by the University of Maryland Medical Center:7

“In one study, people who took 5-HTP went to sleep quicker and slept more deeply than those who took a placebo. Researchers recommend 200 to 400 mg at night to stimulate serotonin, but it may take six to 12 weeks to be fully effective.”

There may be some beneficial “side effects” to 5-HTP as well. Research suggests the supplement naturally reduces appetite and food intake (including reduced carbohydrate consumption) and is associated with significant weight loss.8

Another study found 5-HTP led to significant improvements in symptoms of fibromyalgia as well, with only mild and transient side effects reported.9 The anti-depressant properties of 5-HTP are also of interest, and preliminary research suggests it may work as well as certain antidepressants in people with mild to moderate depression.10

Try Natural Sleep Aids Before Sleeping Pills

Natural sleep aids work with your body’s natural circadian rhythm to help you get truly restful sleep. This is not the case with prescription sleeping pills. A study in 2012 revealed that people who take sleeping pills are not only at higher risk (by 35 percent) for certain cancers, but they are also nearly four times as likely to die as people who don’t take them. The list of health risks from sleeping pills includes:

  • Higher risk of death, including from accidents
  • Increased risk of cancer
  • Increased insulin resistance, food cravings, weight gain and diabetes
  • Complete amnesia, even from events that occurred during the day
  • Depression, confusion, disorientation, and hallucinations

Research involving data from more than 10,500 people who received drugs for poor sleep (including benzodiazepines) also showed that “as predicted, patients prescribed any hypnotic had substantially elevated hazards of dying compared to those prescribed no hypnotics.”

The association held true even when patients with poor health were taken into account — and even if the patients took fewer than 18 pills in a year.11 In “The Dark Side of Sleeping Pills,” an e-book by one of the study’s researchers, Dr. Daniel Kripke, it’s explained:12

“The patients who took sleeping pills died 4.6 times as often during follow-ups averaging 2.5 years. Patients who took higher doses (averaging over 132 pills per year) died 5.3 times as often. It seems quite likely that the sleeping pills were causing early death for many of the patients …

Theoretically, there could be confounding factors or biases in the selection of patients which caused these deaths without involving sleeping pills. We can only say that we found almost no evidence of such biases … If sleeping pills cause even a small portion of the excess deaths and cancers associated with their use, they are too dangerous to use.”

Try This First for Better Sleep Starting Tonight

If you need more sleep, I suggest you read through my full set of 33 healthy sleep guidelines for details on proper sleep hygiene, but to start, consider implementing the following changes. If you’ve tried these steps and are still having trouble sleeping, you may want to consider melatonin or 5-HTP.

•Avoid watching TV or using your computer in the evening, at least an hour or so before going to bed. These devices emit blue light, which tricks your brain into thinking it’s still daytime. Normally, your brain starts secreting melatonin between 9 and 10 p.m., and these devices emit light that may stifle that process. Even the American Medical Association (AMA) now states:13

” … [N]ighttime electric light can disrupt circadian rhythms in humans and documents the rapidly advancing understanding from basic science of how disruption of circadian rhythmicity affects aspects of physiology with direct links to human health, such as cell cycle regulation, DNA damage response, and metabolism.”

•Make sure you get BRIGHT sun exposure regularly. Your pineal gland produces melatonin roughly in approximation to the contrast of bright sun exposure in the day and complete darkness at night. If you are in darkness all day long, it can’t appreciate the difference and will not optimize your melatonin production.

•Sleep in complete darkness, or as close to it as possible. The slightest bit of light in your bedroom can disrupt your body’s clock and your pineal gland’s melatonin production. Even the tiniest glow from your clock radio could be interfering with your sleep, so cover your radio up at night or get rid of it altogether.

Move all electrical devices at least 3 feet away from your bed. You may want to cover your windows with drapes or blackout shades. If this isn’t possible, wear an eye mask.

•Install a low-wattage yellow, orange, or red light bulb if you need a source of light for navigation at night. Light in these bandwidths does not shut down melatonin production in the way that white and blue bandwidth light does. Salt lamps are handy for this purpose. You can also download a free application called f.lux that automatically dims your monitor or screens14 or use blue-light-blocking glasses.

•Keep the temperature in your bedroom no higher than 70 degrees F. Many people keep their homes too warm (particularly their upstairs bedrooms). Studies show that the optimal room temperature for sleep is between 60 to 68 degrees F.

•Take a hot bath 90 to 120 minutes before bedtime. This increases your core body temperature, and when you get out of the bath it abruptly drops, signaling your body that you are ready to sleep.

•Avoid using loud alarm clocks. Being jolted awake each morning can be very stressful. If you are regularly getting enough sleep, you might not even need an alarm.

•Get some sun in the morning, if possible. Your circadian system needs bright light to reset itself. Ten to 15 minutes of morning sunlight will send a strong message to your internal clock that day has arrived, making it less likely to be confused by weaker light signals during the night. More sunlight exposure is required as you age.

•Be mindful of electromagnetic fields (EMFs) in your bedroom. EMFs can disrupt your pineal gland and its melatonin production, and may have other negative biological effects as well. A gauss meter is required if you want to measure EMF levels in various areas of your home. Ideally, you should turn off any wireless router while you are sleeping. You don’t need the Internet on when you are asleep.

5-HTP: Prozac’s True Alternative

Posted by

0


5-HTP (otherwise known as 5-hydroxytryptophan or Oxitriptan) is the less well known cousin of serotonin (5-HT), one of the most important brain neurotransmitters.

5HTP vs. Tryptophan

L-Tryptophan is first converted to 5-HTP in nerve cells by a vitamin B3 dependent enzyme, and then 5-HTP is converted to 5-HT by a vitamin B6 dependent enzyme. Yet thanks to modern science, we can now take preformed 5-HTP, with many consequent advantages.

5-HTP passes through the blood brain barrier into the brain far more easily than Tryptophan, and getting Tryptophan through the blood brain barrier is the main bottleneck, which in many people leads to inadequate brain serotonin levels.

Also, 5-HTP is not used to make proteins in the body, while tryptophan is, so there isn’t competition by cells outside the brain for 5-HTP, as there is for the body’s scare Tryptophan supplies.

The body often uses Tryptophan to make vitamin B3, at a very high cost of 60mg L-Tryptophan to make just 1mg B3! However 5-HTP is not wasted to make vitamin B3.

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. Because of this, L-Tryptophan supplementation especially in chronically stressed people should be kept to 1 gram (1000 mg.) per day or less, because the stress hormone- cortisol activates pyrrolase.

The work of HM van Praag, SN Young and others over the last 20 years, shows that serotonin is a key brain neurotransmitter involved in mood regulation (anti-anxiety and antidepressant) and impulse control (inhibits aggression and obsessive compulsive disorders [OCD], pain control and sleep).

Serotonin is also the precursor for our pineal gland’s production of melatonin. Human clinical studies show that 5-HTP is a far more efficient increaser of brain serotonin than L-Tryptophan. Furthermore, when 5-HTP has been compared to Tryptophan in human studies, 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.

Unlike Tryptophan, 5-HTP has been shown to increase brain dopamine and noradrenaline activity. These are two key mood and alertness regulating neurotransmitters, and whentyrosine, the amino-acid precursor for brain dopamine/noradrenaline is given along with 5-HTP, the effect is even more powerful.

5HTP vs. Prozac

In a society that has made the serotonin-selective re-uptake inhibitor (SSRI) drugs such as Prozac the gold standard of managing the serotonin-deficiency syndrome, even though the Poeldinger study showed 5-HTP to be superior to it, it is worth noting that a study reported by Risch and Nemeroff demonstrates, that even those successfully treated with SSRIs (ignoring their frequent and sometimes serious side-effects) are still dependent upon their brains’ producing adequate serotonin from either Tryptophan or 5-HTP.

SSRIs work by conserving existing brain serotonin supplies by keeping more serotonin in the synaptic gap between neurons. They achieve this through preventing enzymatic degradation of synaptic serotonin. SSRIs do not enhance serotonin production. Risch and Nemeroff state;

“…depressed patients were treated with low-Tryptophan diets that were supplemented with high doses of neutral amino acids [which compete with Tryptophan for transport through the blood-brain barrier]… Remitted depressed subjects receiving serotonergic antidepressants (e.g. fluoxetine [Prozac], fluvoxamine) who were challenged with low-Tryptophan diet supplemented with neutral amino acids promptly relapsed into severe clinical depression. When the Tryptophan supplementation was provided, the patients promptly recovered…”

The many successful published studies using 5-HTP show that 5-HTP, by naturally elevating brain serotonin, can alleviate the serotonin-deficiency syndrome without any help from SSRI drugs. Yet the study related by Risch and Nemeroff eloquently shows that the success of SSRI drugs is crucially dependent upon the brain producing adequate serotonin (from either Tryptophan or 5-HTP), and that brain serotonin production is the controlling or rate-limiting variable underlying the apparent success of SSRIs. It appears that the more logical and economically sound choice to alleviate conditions that result from the serotonin deficiency syndrome is 5-HTP, the immediate precursor of the deficient substance.

Conclusion

Van Praag’s and Young’s work suggests that 5-HTP is more likely to be effective for those suffering an anxious, agitated, aggressive, irritable depression and is rarely effective for those suffering from a severe, vegetative, total “blahs” type depression.

5-HTP may also be helpful in some cases of compulsive carbohydrate overeating, alcohol addiction and compulsive gambling (specific forms of OCD), as well as for insomnia.

Side effects of 5-HTP are occasional gastrointestinal upset, hypomania and euphoria. Even though 5-HTP is a natural substance normally made by the brain, without medical supervision prudence suggests limiting daily dosage to 100 mg. to 200 mg., a dose shown to be effective in human clinical studies.

Research also shows that both tryptophan, and even more so 5-HTP, increase the activity of MAO inhibitor drugs, tricyclic antidepressants and selective serotonin inhibitor (SSRI) drugs, such as Prozac, Paxil and Zoloft. Therefore L-Tryptophan and especially 5-HTP, should only be used by anyone taking any of these drugs ONLY with their prescribing physician’s consent and supervision.