Aneptinex
Aneptinex Uses, Dosage, Side Effects, Food Interaction and all others data.
Aneptinex is a drug used primarily in the treatment of major depressive disorder and has been studied in the treatment of irritable bowel syndrome (IBS) . Structurally, it is classified as a tricyclic antidepressant (TCA), however, it possesses different pharmacological properties than typical tricyclic antidepressants .
Aneptinex was discovered and patented by The French Society of Medical Research in the 1960s . Currently, tianeptine is approved in France and manufactured and marketed by Laboratories Servier SA; it is also marketed in several other European countries under the trade name “Coaxil” as well as in Asia (including Singapore) and Latin America as “Stablon” and “Tatinol” but it is not available in Australia, Canada, New Zealand, the U.K. or the U.S.
Analyses in large-scale epidemiologic surveys have shown that the anxiety disorders are widely comorbid with major depression. This makes antidepressant with anxiolytic properties particularly unique and attractive .
| Trade Name | Aneptinex |
| Generic | Tianeptine |
| Tianeptine Other Names | Tianeptina, Tianeptine |
| Type | |
| Formula | C21H25ClN2O4S |
| Weight | Average: 436.952 Monoisotopic: 436.122355695 |
| Protein binding | 95% bound to plasma protein . |
| Groups | Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | Hungary, Poland, Slovakia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aneptinex is an atypical tricyclic antidepressant with antidepressant and anxiolytic effects primarily used to treat major depressive disorder.
Used primarily in the treatment of major depressive disorder and anxiety . It is currently being studied for fibromyalgia pain treatment .
Aneptinex is also used to associated treatment for these conditions: Major Depressive Disorder (MDD)
How Aneptinex works
Recent studies suggest that tianeptine acts as a full agonist at the mu-type opioid receptor (MOR) , . The mu opioid receptors are currently being studied as effective targets for antidepressant therapies . It is believed that the clinical effects of tianeptine are owed to its modulation of these receptors . In addition to its actions on the opioid receptor, previous studies have owed its action to its effect on the serotonin receptor , , dopamine (D2/3) receptors , and glutamate receptors , , as discussed below:
Aneptinex has challenged the monoaminergic hypothesis of depression, as well as the widely supported monoaminergic mechanisms whereby the action of most known antidepressants have been explained . Specifically, this drug is thought to persistently alter glutamate receptor bursting of the hippocampal CA3 commissural associational synapse . Current research suggests that tianeptine produces its antidepressant effects through the modulation of glutamate receptor activity (for example, AMPA receptors and NMDA receptors) and affect the release of brain-derived neurotrophic factor (BDNF), which impacts neural plasticity . More recent studies by support the role of tianeptine in the modulation of glutaminergic activity in the amygdala, the emotional region of the brain associated with memories .
Aneptinex reduces the hypothalamic-pituitary-adrenal response to stress, and thus prevents stress-related behavioral issues . In rodents, the stress of acute restraint increases extracellular levels of glutamate in the basolateral amygdala an effect that was inhibited by tianeptine . Interestingly, the SSRI fluoxetine increased extracellular glutamate levels in the basolateral amygdala regardless of stress conditions. These data demonstrate that the mechanism of action of tianeptine is distinct from SSRIs and support the hypothesis that the mechanism of action of tianeptine relates to alteration of glutaminergic activity in the amygdala and the hippocampus .
In addition to the above mechanisms, tianeptine is a unique antidepressant and anxiolytic medication that stimulates the uptake of serotonin (5-hydroxytryptamine; 5-HT), and 5-hydroxyindoleacetic acid (5-HIAA) in brain tissue .
Although the monoaminergic neurotransmitters serotonin (5-HT), noradrenaline (NA) and dopamine (DA) are proven to be related to the occurrence of depressive disorders, it is now recognized that monoamine deficits are not sufficient to explain the mechanism of action of antidepressant medications .
Toxicity
There are several published case reports of tianeptine intoxication and death . An overdose of tianeptine can lead to opiod-like effects and lead to respiratory failure and death, due to its direct effect on the mu opioid receptor . In addition, cardiotoxicity can result from an overdose of this medication .
Food Interaction
- Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of tianeptine.
- Exercise caution with St. John's Wort. This herb induces CYP3A metabolism, which may reduce serum levels of tianeptine.
Volume of Distribution
0.8 L/kg (0.77 +/- 0.31 L/kg)
Elimination Route
Well absorbed, approximately 99% bioavailability .
Half Life
Approximately 2.5 h
Clearance
Rapidly cleared by the kidneys .
Elimination Route
Eliminated with bile as glucuronide and glutamine conjugates .
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