Coaxil (Tianeptine)
Tianeptine, often sold as a medication under the brand name Coaxil and Stablon, stands apart from conventional antidepressants due to its unique properties and mechanism of action.
Developed by French researchers in the 1960s, Tianeptine offers a departure from the classical treatment of depression in multiple ways - much due to its unique pharmacological profile.
What is Coaxil?
Coaxil, containing the active substance Tianeptine, works through a multifaceted mechanism of action that immediately sets it apart from the most common antidepressants. Initially, it was characterized as a selective serotonin reuptake enhancer (SSRE), although later it was decided that it is more similar to classical tricyclic antidepressants (TCA) in the way it affects serotonin receptors.
The unique part about Tianeptine is its atypical properties, including its role as a μ-opioid receptor (MOR) full agonist and its impact on glutamatergic, neurotrophic, and neuroplastic pathways.
Tianeptine's interaction with Mu opioid receptors may contribute to its role in dopamine release and modulation of glutamatergic mechanisms, which can help explain its antidepressant and anxiolytic effects, as well as its ability to improve somatic symptoms.
Common Uses
Tianeptine is primarily prescribed for the treatment of depression and various anxiety disorders. However, its use is somewhat controversial, as it is not approved by regulatory agencies in many countries, including the United States. It is mainly prescribed as a treatment in Eastern European countries.
While several scientific studies have proven its effectiveness in treating depressive disorder, companies developing a Tianeptine-based medication in the US have halted the process on multiple occasions.
This occurred most recently in October 2023, when Tonix Pharmaceuticals disclosed that it had stopped the advancement of Tianeptine as a standalone treatment for major depressive disorder following unsatisfactory outcomes in phase-2 clinical trials.
Banned in Parts of the US
Another controversial part about Tianeptine is the significant abuse potential. Despite its antidepressant properties, Tianeptine has faced regulatory hurdles in the United States. The Drug Enforcement Administration (DEA) has classified Tianeptine as a Schedule II controlled substance, highlighting its potential for abuse.
More than 7 states have banned the sale and distribution of Tianeptine due to reports of abuse and addiction. Before this, the medication was sold over-the-counter across many parts of the country, with information about its potential misuse have been spreading on social media during the last decade.
Where is Coaxil Used?
- Bulgaria
- Czech Republic
- Estonia
- Hungary
- Lithuania
- Latvia
- Poland
- Romania
- Russia
- Slovakia
- Ukraine
Side Effects
Like any medication, Tianeptine can cause side effects. However, it is not related to any sexual side effects, like many first-line antidepressants such as Sertraline or Paroxetine. On the other hand, it may frequently lead to weight gain.
Common side effects also include nausea, dizziness, drowsiness, and constipation. It can make the person taking it more agitated and irritable. Hot flashes, palpitations, tremors, and blurred vision may occur in 0,1-1% of all its users.
More serious side effects, such as respiratory depression and cardiac abnormalities, have also been reported, especially at high doses or in cases of misuse.
Rare side effects include hepatitis, hypomania, and protracted muscle aches.
Contraindications
The only absolute contraindication for Tianeptine is previously-known hypersensitivity or severe allergic reactions to Tianeptine or any similar medication.
Individuals with a history of substance abuse should most likely avoid the medication, as it may lead to misuse. Those with poor adherence to their treatment regimen may also present a challenge when taking Tianeptine since the medication has to be taken 3 times a day. This is unlike most other antidepressants, which only need to be taken once.
Last update: February 20, 2024
Disclaimer: The information provided is intended for general informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult with a qualified healthcare provider, such as a physician, before starting any new treatment or making changes to your existing treatment plan. Individual responses to treatment may vary, and a healthcare professional can provide personalized guidance based on your specific needs and circumstances. If you are experiencing severe or persistent symptoms of disease or mental illness, seek immediate medical attention.