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5-HTP & Ecstasy
Ecstasy is a recreational drug that is also a borderline therapeutic drug. Following the euphoric high it produces, it is known to plunge its users into a deep low. Some take 5 HTP to even out this “come down”. Find out why 5 HTP works in this way and what dangers may arise from concurrent use of 5 HTP and Ecstasy.
5 HTP is commonly sold as an over-the-counter dietary supplement. It is a naturally occurring amino acid which, although rare in food crops, is usually extracted from the seeds of a West African plant, Griffonia simplicifolia.
In the body, 5 HTP is the intermediate product in the synthesis of serotonin, an important neurotransmitter in the brain. It is made from L-tryptophan, an essential amino acid.
While L-tryptophan is also available as a supplement, 5 HTP supplements are better at increasing serotonin levels. This is because tryptophan, unlike 5 HTP, competes with other amino acids to cross the blood-brain barrier.
The sole role of 5 HTP in the brain is to be converted to serotonin. This reaction is catalyzed by 5 HTP decarboxylase and vitamin B6.
Therefore, 5 HTP can be used to treat any condition that can be improved by increasing serotonin levels.
Since serotonin controls mood, sleep and appetite, 5 HTP supplements are recommended as antidepressants, sleep aids and appetite suppressants. This means that they can be used to treat depression and anxiety disorders, insomnia and sleep disorders as well as obesity and weight gain.
Ecstasy is the street name for 3, 4-methylenedioxy-N-methylamphetamine or MDMA.
The key effects of Ecstasy are euphoria, diminished anxiety and reduced inhibition. Although Ecstasy is illegal in most countries, it has been used before in treating psychiatric disorders and similar conditions like PTSD (post-traumatic stress disorder).
In fact, some experts still advocate the therapeutic effects of Ecstasy and current efforts are in place to determine if the benefits of the drug outweighs its risks.
Recreational use of Ecstasy can cause subjective changes in perception and consciousness. Some of the effects reported by Ecstasy users are:
After the effects of Ecstasy has worn off, users will experience a crash characterized by the following symptoms:
Most of these side effects of Ecstasy use are caused by prolonged effect of serotonin in the brain and the body as well as the depletion of serotonin after Ecstasy has cleared from the system.
Depression is the most common presentation of Ecstasy crash and it is caused by low levels of serotonin.
Therefore, many Ecstasy users try to alleviate depression by ingesting tryptophan and 5 HTP supplements which can increase serotonin production in the brain.
Ecstasy has a complex effect in the body. In the brain, it causes excitation by releasing dopamine, norepinephrine and serotonin. It also binds to 5 HT2A, a serotonin receptor, as well as alpha-2 adrenergic receptor.
In the endocrine system, Ecstasy triggers the release of oxytocin, prolactin, vasopressin and some other hormones.
Ecstasy overdose causes serotonin syndrome and psychosis resulting from over-stimulation of the brain.
The major symptoms of Ecstasy overdose include:
Besides overdose, other serious adverse effects of Ecstasy user as hyponatremia and hyperthermia.
Hyponatremia is the more common of the two although hypernatremia is the more difficult to treat. Both side effects can quickly lead to death.
Hyponatremia means low sodium levels in the blood. It is caused by drinking too much water as Ecstasy uses try to avoid dehydration from hyperactivity. It can also result from the action of Ecstasy on the pituitary gland.
When Ecstasy induces the release of vasopressin from the pituitary gland, this antidiuretic hormone causes water retention in the kidneys and volume of urine can significantly fall. The water retention from the kidneys is usually accompanied by salt retention but the hyperactivity following Ecstasy use drives out salt through the skin by excessive sweating.
Hyperthermia is an even more pressing adverse effect of Ecstasy use. As the core temperature of the body begins to rise, multiple organs start shutting off.
Hyperthermia after Ecstasy use is often caused by serotonin syndrome as the brain becomes flooded with the neurotransmitter.
Most of the psychoactive effects of Ecstasy are due to changes the drug makes to serotonin pathway.
Different studies have shown that Ecstasy works by increasing the release of serotonin into the synapses between neurons. In fact, the effect SSRIs (selective serotonin reuptake inhibitors) have on Ecstasy suggests that serotonin release is necessary for most of the effects of the psychoactive drug.
The serotonin released in the brain also binds to serotonin receptors known to trigger the release of some of the neurotransmitters and neurohormones that contribute to the effect of Ecstasy.
For example, drugs that block 5 HT1A serotonin receptors reduce the effects Ecstasy has on social behavior. Because 5 HT1A receptors promote the release of oxytocin, blocking them reduce the amount of the hormone released following Ecstasy ingestion.
High doses or repeated intake of Ecstasy may make lasting changes to the serotonergic system. Such changes include reduced production of serotonin in the brain, reduced production of enzymes needed in serotonin synthesis and other factors needed for this synthesis.
All of these effects mean that while Ecstasy reduces serotonin transmission, it does not affect serotonin neurons.
However, this can cause depression in Ecstasy users even when the psychoactive drug is no longer taken.
The neurological damage caused by Ecstasy is believed to be due to dopamine release (triggered by serotonin) or a neurotoxic metabolite of Ecstasy.
To reduce the neurotoxic effect of Ecstasy on the serotonin pathway, antioxidants such as vitamins A, C and E, minerals such as zinc and selenium and B vitamins are sometimes recommended.
SSRIs can also help reduce the permanent damage caused by Ecstasy by blocking dopamine or Ecstasy metabolite from entering the transporter responsible for serotonin reuptake. Therefore, SSRIs and Ecstasy inhibit each other in the brain, and although, the combination of both drugs can cause serotonin syndrome, this is rarely the case.
MAOIs, on the other hand, have a higher tendency to cause serotonin syndrome and do not provide comparable benefits as SSRIs.
However, serotonin release is not the whole story about Ecstasy.
Drugs that also increase the release of serotonin do not produce the same effects as Ecstasy. Therefore, other neurotransmitter pathways (especially dopamine and norepinephrine) must be involved in the actions of Ecstasy.
Increased serotonin level has been shown to protect the brain from neurological damage caused by neurotoxic factors released after the ingestion of Ecstasy.
Since 5 HTP supplements are the simplest, safest and quickest means of increasing serotonin levels, they are usually taken before or after Ecstasy.
While the use of 5 HTP in this way is not officially recommended mostly because Ecstasy is largely an illegal drug and 5 HTP is a dietary supplement, such combination is actually a common advice given to Ecstasy users.
5 HTP can smoothen the “come-down” effects of Ecstasy. When taken before Ecstasy, it provides the needed serotonin to make up for the level used up during Ecstasy high.
Therefore, besides preventing Ecstasy-induced depression, 5 HTP supplement can also help prevent insomnia, panic attacks and anxiety disorders. It also protects the nerve cells from the neurotoxic effects of Ecstasy.
The usual preloading dose of 5 HTP is 200 mg. 100 mg of vitamin B6 is also recommended since the vitamin is a cofactor for the enzyme that converts 5 HTP to serotonin in the brain.
Others may add 1000 mg of vitamin C which is an antioxidant that can also protect nerve cells from the oxidative damage due to the superoxide free radicals released as the brain metabolizes Ecstasy.
100 mg of magnesium, a muscle relaxant, may also be added to prevent trisma (clenching jaw) and bruxia (grinding teeth), two peculiar symptoms associated with Ecstasy use.
Users who take 5 HTP with Ecstasy find that both drugs are well tolerated.
Of course, there is potential for serotonin syndrome especially when 5 HTP is taken before Ecstasy. This may happen because both drugs increase serotonin concentration.
However, reports of serotonin toxicity following combination of 5 HTP and Ecstasy are rare. Even then care should be taken especially because there is no guaranteed way to predict who might experience serotonin syndrome with this combination.
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