What is Tianeptine Sodium?
Chemically, tianeptine is a tricyclic compound structurally similar to classical tricyclic antidepressants (TCAs) like amitriptyline.
However, its pharmacological profile is distinctly different. The active pharmaceutical ingredient is formulated as its sodium salt (tianeptine sodium) to enhance solubility and bioavailability for oral administration.
It is prescribed for the treatment of major depressive disorder (MDD) and has shown efficacy in managing comorbid anxiety symptoms often associated with depression. Unlike many TCAs, it has a relatively low affinity for muscarinic, histaminergic, and adrenergic receptors, which accounts for its more favorable side-effect profile regarding anticholinergic effects like dry mouth, sedation, and cardiovascular issues.
Mechanism of Action: Beyond the Monoamine System
The early hypothesis that tianeptine enhances serotonin reuptake was based on observations in animal models. While this effect is documented, it does not fully explain its robust antidepressant and anxiolytic effects in humans. Contemporary understanding focuses on tianeptine's profound impact on glutamate, the brain's primary excitatory neurotransmitter, and its role in neuroplasticity.
Extensive preclinical studies demonstrate that tianeptine:
1.Modulates Glutamatergic Activity: It normalizes stress-induced alterations in glutamate transmission, particularly within the hippocampus and amygdala-key brain regions involved in emotion, memory, and stress response.
2.Restores Neuroplasticity: Chronic stress is known to cause neuronal atrophy and synaptic deficits in the hippocampus. Tianeptine has been shown to reverse these effects, promoting synaptic plasticity, increasing the density of dendritic spines, and facilitating neurogenesis. This effect is mediated through its interaction with the glutamatergic system, specifically by modulating NMDA and AMPA receptor trafficking and function.
3.Affects the HPA Axis: Tianeptine helps normalize hyperactivity of the hypothalamic-pituitary-adrenal (HPA) axis, a common feature in depression, thereby reducing the physiological impact of stress.
This multimodal mechanism, centering on the restoration of neuronal structure and function, aligns with the current neurotrophic and glutamatergic hypotheses of depression, explaining its efficacy where conventional SSRIs may fail or be poorly tolerated.
Indications and Target Population
Tianeptine sodium is primarily indicated for the treatment of Major Depressive Disorder (MDD) in adults. Its clinical profile makes it particularly suitable for specific patient subgroups:
1.Patients with Co-morbid Anxiety: Tianeptine exhibits notable anxiolytic properties, making it a valuable option for individuals whose depressive episodes are accompanied by significant anxiety, agitation, or irritability. This contrasts with some SSRIs that can initially exacerbate anxiety.
2.Patients Intolerant to SSRI Side Effects: Individuals who experience undesirable side effects from SSRIs or SNRIs-such as sexual dysfunction, emotional blunting, or severe initial agitation-may find tianeptine to be a better-tolerated alternative due to its different mechanism.
3.Elderly Patients: Due to its low anticholinergic burden and generally favorable cognitive profile (lacking significant sedation or memory impairment at therapeutic doses), tianeptine can be a considered choice for the elderly depressed population, who are more vulnerable to the side effects of traditional TCAs.
Important Contraindications and Warnings: Tianeptine is contraindicated in patients with a known hypersensitivity to the drug and should not be used concurrently with monoamine oxidase inhibitors (MAOIs). Crucially, it is not recommended for individuals with a history of substance use disorder. At high, supratherapeutic doses, tianeptine can act as an opioid receptor agonist (primarily at the μ-opioid receptor), leading to a potential for abuse, dependence, and severe withdrawal symptoms. This risk necessitates strict adherence to prescribed dosages and vigilant medical supervision.
How to get Tianeptine Sodium?
You can contact us. sales8@bpandabio.com Jennie
We Xi'an Herben Biological Technology Co., Ltd are professional supplier of Tianeptine Sodium in Xi'an from China.We supply high purity and good quality Tianeptine Sodium. You can check our COA certificate as below:
Tianeptine Sodium MOQ：
1:USA warehouse purchase directly, MOQ 100GRAM
2.China factory purchase :MOQ 50 GRAM
