Description

Tianeptine

 

• Chemical name (IUPAC):  7-[(3-chloro-6,11-dihydro-6-methyl-5,5-dioxydibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid

• Common name:  Tianeptine (acid form)

• CAS number:  66981-73-5

• Molecular formula:  C₂₁H₂₅ClN₂O₄S

• Molar mass:  436.95 g/mol

• Purity (HPLC):  ≥ 99.41%

• Appearance:  White to almost white crystalline powder.

• Packaging: 1000mg of molecule in sealed  string aluminum pouch.

Tianeptine in Acid Form (Tianeptine Acid) – Substance and Application Profile

Tianeptine is  an atypical antidepressant  with a unique, multifaceted mechanism of action. Structurally classified as a tricyclic psychoactive compound, it differs significantly pharmacologically from classic drugs in this group. Initially, it was believed to act primarily by  enhancing serotonin reuptake , but contemporary research indicates that its primary therapeutic effects result from  modulation of the glutamatergic system  and  agonist action on μ-opioid receptors (MOR) .

Tianeptine in its acid form (7-[(3-chloro-6-methyl-5,5-dioxido-6,11-dihydrodibenzo[c,f][1,2]thiazepin-11-yl)amino]heptanoic acid) is the basic, free form of the compound, before conversion to salts (e.g., sodium or sulfate). It is characterized by  high affinity for plasma proteins  (approximately 95%) and  a short half-life  of approximately 2.5 hours. It is rapidly metabolized in the liver, mainly by β-oxidation of the heptanoic acid side chain, to active metabolites (MC5).

---

🧪  Mechanism of Action and Therapeutic Applications

The main mechanism of tianeptine’s antidepressant and anxiolytic effects is related to its influence on  synaptic plasticity  and  modulation of the glutamatergic system . It alleviates the effects of chronic stress by normalizing the function of the hypothalamic-pituitary-adrenal (HPA) axis and counteracting stress-related changes in brain regions such as the hippocampus and amygdala.

Its action as  a μ-opioid receptor (MOR) agonist is also crucial . This property accounts not only for part of the therapeutic effect but also for  the potential for abuse  and  dependence , particularly at doses significantly above therapeutic levels (25-50 mg/day). Action at the MOR leads to indirect stimulation of the dopaminergic reward system, which can induce euphoria.

Main Medical Applications:

• Treatment of major depressive disorder (MDD):  Efficacy confirmed in clinical trials, comparable to SSRIs (e.g. fluoxetine) and TCAs (e.g. amitriptyline), with a more  favorable side effect profile  (lower risk of dry mouth, constipation, circulatory system burden).

• Treatment of anxiety disorders,  including generalized anxiety disorder and panic disorder.

• Treatment of irritable bowel syndrome (IBS)  and  bronchial asthma  (due to the modulation of free serotonin levels in plasma).

• Supporting the detoxification process in opioid dependence  – see section below.

---

⚕️  Potential Use in Opioid Detoxification

The MOR agonist action of tianeptine allows  it to alleviate withdrawal symptoms  following discontinuation of so-called “hard opioids” (e.g., heroin, fentanyl). Its short duration of action and receptor affinity allow for theoretical use in  maintenance or substitution therapy , analogous to methadone or buprenorphine.

⚠️  IMPORTANT WARNING:  It is important to emphasize that this is  an unapproved (off-label) use  and carries  significant risk . Tianeptine itself has  a high potential for addiction . Attempting to self-medicate or detox without the close supervision of a psychiatric or addiction specialist will likely lead to  a transition from one addiction to another , often with a more severe course. Reports from poison control centers in the US indicate a sharp increase in cases of severe poisoning and deaths associated with the abuse of tianeptine purchased as a “dietary supplement.”

---

📊  Comparison of Tianeptine with Selected Antidepressant Medicinal Products

The table below provides a comparative overview of tianeptine and other classes of antidepressants.

---

🌍 Preparaty Zawierające Tianeptynę (Nazwy Handlowe i Kraje)

Tianeptyna jest dostępna na rynkach farmaceutycznych wielu krajów pod różnymi nazwami handlowymi, głównie w formie soli sodowej. Oto lista przykładowych preparatów:

---

⚠️ Bezpieczeństwo, Działania Niepożądane i Status Prawny

Działania niepożądane przy dawkach terapeutycznych są generalnie łagodne i obejmują: nudności, bóle brzucha, zawroty głowy, ból głowy, bezsenność lub senność. Przy dawkach nadużywanych (nawet 100-krotnie wyższych niż terapeutyczne) występują: euforia, sedacja, depresja oddechowa, tachykatdia, drgawki, śpiączka, a nawet zgon. Zespół abstynencyjny jest bardzo silny i przypomina zespół odstawienny opioidów: lęk, pobudzenie, bezsenność, bóle mięśni, biegunka, wymioty.

Status prawny tianeptyny jest złożony i zależy od kraju:

• W Polsce: Tianeptyna nie jest zarejestrowana jako produkt leczniczy. Jej status prawny jest niejednoznaczny. Nie figuruje na wykazie substancji kontrolowanych ustawy o przeciwdziałaniu narkomanii, jednak podlegać może regulacjom ustawy – Prawo farmaceutyczne. Sprzedaż jej w formie “odczynnika” lub “suplementu” jest prawnie wątpliwa i obarczona wysokim ryzykiem.

• Na świecie: Jest lekiem na receptę w wielu krajach (np. Francja, Hiszpania, Brazylia). W USA nie jest zatwierdzona przez FDA, a w kilku stanach (m.in. Alabama, Michigan) została wpisana na listę substancji kontrolowanych Schedule I/II z powodu nadużyć. Podobne restrykcje wprowadzono m.in. we Włoszech.

---

📚 Podsumowanie i Podstawy Naukowe

Tianeptine is a pharmacologically intriguing molecule whose mechanism of action goes beyond the classic “monoaminergic hypothesis” of depression. Its ability to modulate glutamate and act on opioid receptors offers a unique therapeutic approach, but it also carries  a significant potential for abuse and severe dependence .

• Gubinelli, F. et al. (2023).  Analysis of Tianeptine in Dietary Supplements . Nutraceuticals. – Documents uncontrolled sales, dose variability, and risks associated with “Tianeptine” products.

• Velagapudi, AK et al. (2024).  What is tianeptine…  – A detailed review of the management of tianeptine poisoning and withdrawal based on data from poison control centers.

• Gichinga, MG et al. (2023).  Tianeptine, an Antidepressant with Opioid Agonist Effects  – An excellent narrative review summarizing the pharmacology, epidemiology of abuse, and dangers of tianeptine.

• Alamo, C. et al. (2019).  Tianeptine, an atypical pharmacological approach to depression  – An in-depth analysis of the pharmacological mechanism of action and place of tianeptine in the treatment of depression.

 

Legal Notice:

Nonsensia Lab specializes in the production of chemical reagents for professional use. All reagents offered are labeled as not for human consumption. The above description is a scientific study of the molecule being sold and does not constitute medical advice.