Tianeptine is used for its antidepressant and anxiolytic properties and is a water-soluble nootropic. Tianeptine is an SSRE (which stands for selective serotonin reuptake enhancer), which differs from SSRIs, SNRIs and TCAs or even other monoaminergic modulating agents.
A quick overview: Tianeptine was discovered by The French Society of Medical Research and was patented in the 1960s. Since the late 1980s, it has been developed and marketed as an antidepressant known as Stablon by an French drug giant Servier. Tianeptine is sold in many places like Asia, Europe, and Latin America but not in the United States as it is not approved by the FDA. Tianeptine is also used for the treatment of asthma or irritable bowel syndrome, but as stated it is primarily used in the in the treatment of major depressive disorder. Tianeptine acts both as an anti-anxiety, non-sedating agent and a non-stimulating mood-brightener as well and as such users have said it is moderately useful in treating ADHD and OCD as well.
Tianeptine should be taken before a meal and should be taken orally as prescribed by a doctor. However users over at erowid have reported injecting Tianeptine with success as well. The normal dosage is usually 3 times daily, due to its short duration of action. In order to prevent an upset stomach while taking it, it should be taken with a glass of water. You should contact a physician for the correct dosage as it is condition dependent. There can be severe withdrawal symptoms that can be presented if discontinued right away so it is very important to consult a doctor before taking the medication (more on this below).
In 2014, it was discovered that Tianeptine is believed to contribute to anxiolytic properties because it works as a µ-opioid receptor agonist. Although Tianeptine does not have the high addictive potential (generally associated with many opioid drugs), it acts on µ-opioid receptors. This could also be the reason to the possible euphoric effects of Tianeptine that some users may experience at higher (recreational) doses.
Tianeptine works by modulating the action of the main excitatory neurotransmitter in the brain, which is glutamate. Stressful situations either causes too much or too little activity, which then leads to augment glutamates pathways. There is a degradation of nerve and brain tissue that leads to fluctuation in glutamatergic action. Depression is directly linked to neuroplasticity, which is the ability of the brain to adapt to new stimuli. The increase in neuroplasticity in the human brain contributes to the reduction in symptoms of depression. Tianeptine inhibits the body's harmful responses to stress by keeping glutamatergic pathways under control. This leads to increased neuroplasticity, which in turn allows the brain to handle anxiety and depression efficiently.
Tianeptine absorption when taken with food, can be delayed by half an hour but does not typically affect the total amount absorbed into the plasma. It is absorbed quite well orally, with a 99%(+/-28%) bioavailability. Oral administration is reduced when co-administered with alcohol. Tianeptine has a plasma half-life of 2.5 hours.
Tianeptine has been found to be effective in post-traumatic stress disorder and is as effective and safe as fluoxetine and moclobemide. It has also been found to be effective in treating depression in Parkinson's disease. There was a study conducted in Egypt in 2005, that demonstrated that Tianeptine was effective in men with erectile dysfunction and depression. There was also another study that was done in Spain in January 2007, that showed that Tianeptine is significantly effective in treating pain that is linked to fibromyalgia. Aside from its analgesic effect, Tianeptine also has an anticonvulsant effect as well. In regards to attention-deficit hyperactivity disorder or ADHD, Tianeptine has been shown to have efficacy with minimal side effects (references listed below).
One should avoid excess dosages of tianeptine. Other precautions must be taken if:
The general recommended dose for Tianeptine is 12.5 mg and should be taken 2-3 times in a day. It is important to divide the dosage of Tianeptine because of the exertion of its effects on shorter duration. It is recommended that individuals who plan to take Tianeptine must start out with a single or half tablet to in order to initially assess its effects. It is important to consult a physician for more accurate dosing instructions.
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