What is Tianeptine? (Tianeptine Sodium Sulfate Salt)
Tianeptine, also known as Stablon, is a medication mainly used in the treatment of major depressive disorder. It has also been used to treat irritable bowel syndrome and asthma. Tianeptine has antidepressant and anti-anxiety properties. To buy Tianeptine, you must know about this product.
Tianeptine is a drug that is used as an antidepressant. It is a racemic mixture of two tricyclic synthetic chemical compounds, which are aromatics, carboxylic acids, and amines. Tianeptine is therapeutically effective by modulating glutamatergic synapses.
Tianeptine has a variety of effects on the body, including improved motivation, suppression of anxiety, cognitive euphoria, tune-up, rejuvenation, and cognitive fatigue.
Health Effects of Tianeptine:
- Tianeptine improves depressive symptoms.
- Tianeptine decreases anxiety, stress, and symptoms of Stress.
- Tianeptine benefits memory and learning.
- Tianeptine is an Anti-inflammatory.
- Tianeptine decreases pain.
- Tianeptine helps treat Irritable Bowel Syndrome.
- Tianeptine reduces asthma.
An increasing number of different antidepressants are currently available for treating depression. Nevertheless, resistance to therapy is observed in individual cases. Among other things, these patients can be treated with neuroleptics. Tianeptine (Stablon) can also be used in these cases.
A combination of antidepressants and Tianeptine (Stablon) is ultimately effective and significantly reduces the Hamilton Depression Score. A combination of antidepressants and Tianeptine (Stablon) appears to be an effective new therapy option for severe depression.
Tianeptine is approved in Germany for the treatment of mild, moderate and severe depression. It can also be used off-label for the treatment of anxiety disorders and obsessive-compulsive disorders since there are indications of the effectiveness of Tianeptine in the treatment of these.
The efficacy was checked in two placebo-controlled studies using the values in the Montgomery-Åsberg Depression Scale (MADRS). In both studies, Tianeptine was significantly more effective than placebo. Efficiency compared to amitriptyline (50 to 100 mg / day), clomipramine (100 to 200 mg / day), dothiepin (150 to 225 mg / day), imipramine (100 to 200 mg / day), maprotilin (75 mg / Day) and Mianserin (30 to 80 mg / day) was also verified in studies.
In a dosage of 25 to 50 mg / day, Tianeptine proved to be on a par with the tri- and tetracyclic antidepressants with regard to the antidepressant and anxiolytic effects.
A five-study meta-analysis examined efficacy (MADRS scores) compared to SSRI . Tianeptine was also as effective in severely depressed patients as the comparative SSRIs fluoxetine, paroxetine, and sertraline.
Mechanism of Action
Pharmacodynamics (effects in the body): Tianeptine is a partial agonist of the μ-opioid receptor with atypical effects. The substance has a modulating effect on glutameric NMDA and AMPA receptors and appears to prevent or reverse stress-related changes in the hippocampus and prefrontal cortex.
Tianeptine also increases the reuptake of serotonin from the synaptic cleft in parts of the brain, at least in the initial phase of treatment, and increases the extracellular dopamine concentration in the nucleus accumbens of the forebrain.
Therefore, in the past, it was referred to as a serotonin reuptake enhancer ( SRE ) as opposed to the serotonin reuptake inhibitors ( SSRIs ) . It is unclear how these serotonergic and dopaminergic effects are triggered since Tianeptine itself has no affinity for serotonergic and dopaminergic receptors, or the serotonin and dopamine transporters. One explanation could be the involvement of the A1 adenosine receptors.
Pharmacokinetics (metabolism in the body):
The maximum plasma level is reached after one hour. The plasma half-life is 1.4-3.6 hours. The active metabolite MC5 has a half-life of 7.6 hours, which means that a steady state level occurs within a week. Tianeptine is not subject to any recognizable first-pass metabolism. Intake with meal delays the absorption time by half an hour, the bioavailability is reduced by 25 percent.
Side Effects of Tianeptine
Known side effects that may occur are:
Common (less than 1 in 10, but more than 1 in 100 people) anorexia (eating disorders), nightmares, insomnia, drowsiness, drowsiness, headache, circulatory collapse, tremors, limited eyesight, hot flushes, fast or unnatural palpitations, chest pain, breathing difficulties, dry mouth, Indigestion, abdominal pain, nausea, vomiting, flatulence, diarrhea, heartburn, back pain, muscle pain, weakness, feeling of a lump in your throat.
Uncommon (less than 1 in 100 but more than 1 in 1,000 people) itching, hives (rash).
Rare (less than 1 in 1,000 but more than 1 in 10,000 people treated) with drug abuse and addiction, especially in patients under 50 years of age, alcohol or drug abuse history.
Frequency not known Suicide and suicidal behavior.
Compared to other tricyclics, Tianeptine was statistically significantly less likely to have autonomic and CNS side effects, gastrointestinal disorders, an increase in weight and heart rate or tremor, according to the meta-study. Sexual dysfunction was less common compared to SSRI, but the dry mouth was more common than with fluoxetine treatment. Compared to paroxetine, it was significantly more tolerable.
Structure and stereoisomerism of Tianeptine
Tianeptine has a central, seven-membered heterocyclic ring and has structural similarities with the benzodiazepines. Structurally, but not in terms of its effects, Tianeptine is classified as a tricyclic antidepressant. Tianeptine is chiral and contains a stereo center, so there are two enantiomers :
- (R)-7-[(3-Chlor-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-yl)amino]heptansäure-S,S-dioxid [= (R)-Form] und
- (S)-7-[(3-Chlor-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-yl)amino]heptansäure-S,S-dioxid [= (S)-Form].
The drug Tianeptine is used as a racemate [1: 1 mixture of ( R ) -form and ( S ) -form]. It is known that the ( R ) and the ( S ) form act differently; in animal experiments, the (-) – enantiomer alone significantly reduced effects that were provoked by administered serotonin.