Servier - Tianeptine Controversy: Difference between revisions
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==Mechanism of Action Controversy== | ==Mechanism of Action Controversy== | ||
Initially, Servier promoted tianeptine as having a unique mechanism of action, claiming it enhanced serotonin uptake—directly opposite to the mechanism of selective serotonin reuptake inhibitors (SSRIs). This purported mechanism challenged the monoamine hypothesis of depression, as both serotonin uptake inhibitors (classical tricyclic antidepressants) and this supposed serotonin uptake enhancer (tianeptine) showed antidepressant activity. | Initially, Servier promoted tianeptine as having a unique mechanism of action, claiming it enhanced serotonin uptake—directly opposite to the mechanism of selective serotonin reuptake inhibitors (SSRIs). This purported mechanism challenged the monoamine hypothesis of depression, as both serotonin uptake inhibitors (classical tricyclic antidepressants) and this supposed serotonin uptake enhancer (tianeptine) showed antidepressant activity. | ||
However, in 2014, researchers discovered that tianeptine actually functions as a full μ-opioid receptor (MOR) agonist, with EC50 values of 194±70 nM for human MOR and 641±120 nM for mouse MOR. It was also found to be a full δ-opioid receptor agonist, though with much lower potency, while showing no activity at κ-opioid receptors. This revelation significantly changed the understanding of tianeptine's mechanism of action and raised concerns about its potential for abuse. | However, in 2014, researchers discovered that tianeptine actually functions as a full μ-opioid receptor (MOR) agonist, with EC50 values of 194±70 nM for human MOR and 641±120 nM for mouse MOR. It was also found to be a full δ-opioid receptor agonist, though with much lower potency, while showing no activity at κ-opioid receptors. This revelation significantly changed the understanding of tianeptine's mechanism of action and raised concerns about its potential for abuse. | ||
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Despite being approved in France and other countries, tianeptine has never received FDA approval in the United States. The drug's μ-opioid receptor agonist properties give it a high abuse potential in large doses. Between 1989 and 2004, 141 cases of recreational use were identified in France, and an additional 45 cases between 2006 and 2011. | Despite being approved in France and other countries, tianeptine has never received FDA approval in the United States. The drug's μ-opioid receptor agonist properties give it a high abuse potential in large doses. Between 1989 and 2004, 141 cases of recreational use were identified in France, and an additional 45 cases between 2006 and 2011. | ||
In 2007, following problems with dependency, tianeptine's manufacturer Servier agreed to modify the drug's label at the request of the French Health Products Safety Agency. In 2001, Singapore restricted tianeptine prescribing to psychiatrists due to its recreational potential. | In 2007, following problems with dependency, tianeptine's manufacturer Servier agreed to modify the drug's label at the request of the French Health Products Safety Agency. This occurred after numerous cases of recreational use were identified in France between 1989 and 2004, indicating Servier was aware of the possibility that their initially proposed mechanism of action was wrong or at least incomplete. In 2001, Singapore restricted tianeptine prescribing to psychiatrists due to its recreational potential. | ||
==Current Status== | ==Current Status== | ||
Tianeptine is | Tianeptine is not approved by the FDA. | ||
==Consumer impact summary== | ==Consumer impact summary== | ||