Tianeptine: An Atypical Antidepressant with Multimodal Pharmacology

Bailey, Sarah; Almatroudi, Abdulrahman Mohammed I; Kouris, Andreas

doi:10.2174/2211556006666170525154616

Cited by 5 publications

(10 citation statements)

References 110 publications

(151 reference statements)

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“…Tianeptine (1, Figure 1), marketed under the name Stablon, is considered an atypical antidepressant with multimodal pharmacology. 1 It is atypical because the first hypothesis for its antidepressant activity involves binding to the serotonin reuptake transporter (SERT) and stimulating serotonin reuptake. 2 Later, it was shown that tianeptine also modulates the glutamatergic system, showing effects on neuroplasticity in the hippocampus and amygdala.…”

Section: Introductionmentioning

confidence: 99%

Tianeptine Esters Derivatives: A Study of Protein-Drug Interaction Performed by Fluorescence Quenching and Molecular Docking

Soares

Ceschi

Franceschini

et al. 2019

J. Braz. Chem. Soc.

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The nature of binding between bovine serum albumin (BSA) and the antidepressant tianeptine and a new series of esters derivatives were studied in this paper. The interactions with BSA were investigated by UV-Vis and fluorescence spectroscopy at three different temperatures. The fluorescence quenching experiments showed that BSA interactions with tianeptine could be dynamic while to its esters a static mechanism was observed. The results showed that tianeptine quenches the intrinsic fluorescence of BSA more efficiently than its esters due to the presence of the free acid portion. The number of binding sites determined by fluorescence spectroscopy is approximately equal to 1 indicating that there is one binding site between BSA tianeptine esters, but the presence of a second interaction site for tianeptine at higher temperatures could be not ruled out. Molecular docking calculations point out a strong affinity of tianeptine and its esters to the site IIA of protein, supporting the hypothesis of a static quenching mechanism.

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Section: Introductionmentioning

confidence: 99%

Tianeptine Esters Derivatives: A Study of Protein-Drug Interaction Performed by Fluorescence Quenching and Molecular Docking

Soares

Ceschi

Franceschini

et al. 2019

J. Braz. Chem. Soc.

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“…En relación con estos hallazgos, la modulación que ejerce tianeptina sobre la transmisión sináptica glutamatérgica parece ser la hipótesis actual que explica su eficacia terapéutica. Además, sus características neurobiológicas parecen implicar una interacción dinámica entre los numerosos sistemas de neurotransmisión no monoaminérgica y su capacidad de restaurar la neuroplasticidad normal en regiones límbicas, así como para regular al alza la neurogénesis en el hipocampo, mecanismos que mediarían sus beneficios procognitivos 54,55 .…”

Section: Eficacia De Los Antidepresivos Para El Tratamiento Del Deter...unclassified

Efectos del tratamiento antidepresivo en la cognición de pacientes con enfermedad de Alzheimer

García‐Alberca¹

2024

KRANION

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La depresión es una manifestación que se observa con frecuencia durante el curso clínico de la enfermedad de Alzheimer (EA). Su presencia oscila entre la aparición de síntomas depresivos y el desarrollo, menos habitual, de un episodio depresivo mayor. Aunque la relación etiopatogénica entre ambas entidades no está todavía suficientemente clara, se admite que comparten algunas bases neurobiológicas comunes. Es bien conocido que las alteraciones cognitivas constituyen un síntoma nuclear de los trastornos depresivos no asociados a un proceso demencial y que la depresión que coexiste con la EA ocasiona importantes consecuencias negativas y se ha asociado, a su vez, con un deterioro cognitivo más rápido. En la práctica clínica el uso de antidepresivos es habitual para tratar la depresión en la EA, pero una gran parte de los individuos no responden al tratamiento farmacológico. Por este motivo, en la actualidad existen líneas de investigación que han avanzado hasta el desarrollo de nuevos fármacos que constituyen prometedoras opciones terapéuticas que cuentan, además de su efecto antidepresivo, con el potencial de mejorar la función cognitiva en pacientes con EA.

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“…In partial agreement, an analysis by Bailey et al that reviewed all accessible tianeptine clinical trial data reported that tianeptine is effective as an antidepressant, allowing for improved functionality compared to standard first-line antidepressant medications. However, it also acknowledged tianeptine's potential for abuse and dependence when ingested at high doses due to its mu-opioid receptor agonist effects [8]. While studies agree that tianeptine, at its therapeutic dose, is effective at treating depression, its opioid-like characteristics can induce euphoria at high enough doses [8].…”

Section: Tianeptinementioning

confidence: 99%

“…However, it also acknowledged tianeptine's potential for abuse and dependence when ingested at high doses due to its mu-opioid receptor agonist effects [8]. While studies agree that tianeptine, at its therapeutic dose, is effective at treating depression, its opioid-like characteristics can induce euphoria at high enough doses [8]. In countries where tianeptine is prescribed to treat depression, 25 to 50-mg daily doses are standard.…”

Section: Tianeptinementioning

confidence: 99%

“…The serotonin reuptake transporter (SERT) is a target of many standard first-line pharmacologic treatments for MDD, including SSRIs and SNRIs. While these drugs increase the concentration of 5-HT in the synaptic cleft by inhibiting its reuptake at SERT, it is postulated that tianeptine's mechanism is the complete opposite-that it instead stimulates serotonin reuptake due to the presence of a specific amino acid in its side chain [5,8]. More recent studies employing advanced technology have contradicted this theory, demonstrating that the drug exhibits low affinity for 5-HT transporters and does not exert significant effects on 5-HT neurotransmission [4,11].…”

Section: Serotonergic Mechanismsmentioning

confidence: 99%

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Tianeptine, an Antidepressant with Opioid Agonist Effects: Pharmacology and Abuse Potential, a Narrative Review

Edinoff,

Sall,

Beckman

et al. 2023

Pain Ther

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Tianeptine is an antidepressant drug approved for the treatment of major depressive disorder in countries other than the US. It is classified as an atypical tricyclic antidepressant and has shown potential benefits in addressing anxiety and irritable bowel disease. However, it is important to note that tianeptine is not approved for any use by the United States Federal Drug Administration (FDA). Despite its lack of approval by the FDA, tianeptine has been distributed online and at small retail locations. The term “gas station drugs” refers to a wide range of substances typically available for purchase from gas stations, corner stores, bodegas, mini marts, smoke shops, and the Internet. These substances may be produced commercially by drug manufacturers or in clandestine laboratories to mimic the effects of more well-known illicit/controlled substances such as marijuana, cocaine, opioids, etc. Tianeptine has made its way to convenience stores and gas station shelves, branded as “Zaza” and “Tianna Red.” It can also be obtained online from independent vendors without a prescription. Misuse of tianeptine can lead to euphoric, opioid-like highs with the potential for chronic users to develop dependence and tolerance. Overdose and use in suicide attempts have also been documented. This manuscript is a narrative review, highlighting the dangers of tianeptine and other gas station drugs and underscoring the urgent need to regulate these substances.

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Tianeptine: An Atypical Antidepressant with Multimodal Pharmacology

Cited by 5 publications

References 110 publications

Tianeptine Esters Derivatives: A Study of Protein-Drug Interaction Performed by Fluorescence Quenching and Molecular Docking

Tianeptine Esters Derivatives: A Study of Protein-Drug Interaction Performed by Fluorescence Quenching and Molecular Docking

Efectos del tratamiento antidepresivo en la cognición de pacientes con enfermedad de Alzheimer

Tianeptine, an Antidepressant with Opioid Agonist Effects: Pharmacology and Abuse Potential, a Narrative Review

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