Hydroxytryptophan: Uses, Benefits, Side Effects, Safety Profile, Absorption and Elimination

It is sold in the United States as a sleep aid, although used as complementary and alternative medicine therapy for depression and as an appetite suppressant.

5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid precursor for serotonin and melatonin biosynthesis in the brain, with an antidepressant, anxiolytic, sleep, and weight loss benefits, but with a few caveats.

Currently, depression is hypothetically described as caused by having low serotonin levels in the brain, although we still don’t understand exactly what causes depression.

5-HTP in supplement form is extracted from the Griffonia simplicifolia plant, an African shrub. Hydroxytryptophan cannot be converted to kynurenine and easily crosses the blood-brain barrier.

Only 3% of oral l-tryptophan is converted to serotonin, while more than 70% of oral 5-HTP is converted. 5-HTP causes an increase in endorphins and catecholamines; equipotency with serotonin and tricyclic reuptake inhibitors; Advantages: less expensive, better tolerated, fewer and milder side effects.

Hydroxytryptophan, the molecular intermediate between l-tryptophan and serotonin, is readily absorbed when taken orally and easily crosses the blood-brain barrier. Increase serotonin.

It also increases endorphins and is at least as effective as pharmaceuticals used to prevent migraine headaches, but much safer and better tolerated—dosage of 200 to 600 mg.

5-Hydroxytryptophan (5-HT) acts on G-protein-coupled receptors in the gastrointestinal tract to modulate intestinal motility in a pro / or antipropulsive manner, depending on the G-protein-coupled receptor subtype and its anatomical location.


Using hydroxytryptophan for insomnia

It’s not normal to struggle to fall asleep and wake up in the morning feeling more tired than when you went to bed. Hydroxytryptophan targets sleep problems from all angles, including limbic system repair, hormone levels, and circadian rhythm retraining.

Several small studies have indicated some improvement in subjective and objective sleep quality after 5-HTP administration. For example, a study using a 200 mg dose demonstrated an increase in REM sleep.

Despite initial evidence suggesting that it could be a valuable treatment for insomnia, the research studies have been small in number and have shared methodological limitations. Additional work replicating these findings would allow for greater certainty in the effectiveness of 5-HTP.

Using hydroxytryptophan for panic and anxiety attacks

In human clinical trials, 5-HTP herbal extracts increased gamma-aminobutyric acid (GABA) receptor agonists or increased gamma-aminobutyric acid levels entirely, promoting sensation relaxation and anxiety reduction.

Using hydroxytryptophan for night terrors in children

Children 3-10 years old who suffer from night terrors every night had a reduction of 93.5% after taking a supplement of 2 mg/kg each night before going to bed for a month.

Using hydroxytryptophan to reduce appetite and achieve weight loss

Carbohydrates increase serotonin levels in the brain, so increasing serotonin levels, such as 5-HTP supplementation, can mitigate carbohydrate cravings and appetite, helping sustain dietary interventions and loss of weight.

In small clinical trials, 5-HTP supplementation in obese women produced no changes in mood but decreased food intake and weight loss.

In the obesity and weight loss intervention studies, up to 900 mg or 8 mg/kg of body weight of 5-HTP was used safely for two weeks, although side effects of nausea and vomiting were reported.

Use of hydroxytryptophan for successful dietary intervention in type II diabetes

In a 2-week clinical trial involving 25 overweight, diabetic subjects without dietary restrictions, subjects receiving 5-HTP had reduced caloric, carbohydrate, and fat intake compared to placebo.

Hydroxytryptophan benefits

Hydroxytryptophan bridges neurotoxic tryptophan metabolites. Tryptophan can be converted to kynurenic acid and quinolinic acid, implicated in psychiatric disorders such as schizophrenia, anxiety, depression, and attention deficit hyperactivity disorder. Like most medications, the administration of Deanxit can cause adverse effects, although they do not occur in all patients.

These conversions occur more in individuals with inflammation, which may link inflammation and psychiatric or neurological disorders.

5-HTP is not directly converted to neurotoxic metabolites, but high serotonin levels can cause a reaction that increases these metabolites.

Side Effects and Safety Profile of Hydroxytryptophan

The starting dose for the treatment of insomnia is usually 100 mg to 300 mg before bedtime. Case studies have indicated that higher doses are associated with vivid nightmares during sleep.

Additional reported side effects include nausea and headaches. There is direct and indirect evidence of potential heart valve damage or disease in rare cases.

Acute serotonin syndrome if combined with selective serotonin reuptake inhibitors (SSRIs) or monoamine oxidase inhibitors (MAOIs) and vomiting and nausea when combined with carbidopa.

Because 5-HTP has not been thoroughly studied in clinical settings, possible side effects and interactions with other medications are not well understood.

Eosinophilia myalgia syndrome (EMS) is a disease that causes severe and disabling muscle pain, skin symptoms, and other neurotoxic reactions that have affected more than 1,500 people and caused at least 38 deaths.

The Food and Drug Administration estimated that there are 10 cases of eosinophilia-myalgia syndrome associated with 5-HTP worldwide. No new cases of supplement-related eosinophilia-myalgia syndrome have been reported since 1990.

Hydroxytryptophan absorption and elimination

5-HTP is rapidly absorbed in the upper intestine, with 50% of 5-HTP absorbed within 1.5 hours. The elimination of 5-HTP is also rapid, with 50% interested in 2 hours.

Due to the rapid pharmacokinetics of 5-HTP, slow administration of 5-HTP may be more beneficial in maintaining serotonin levels in the brain. About 70% of ingested 5-HTP is found in the bloodstream.

Patients taking 5-hydroxytryptophan have severely decreased levels of cytochrome P450 expression.