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== | ||
Revision as of 10:00, 24 March 2025
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Tianeptine is a drug marketed as an antidepressant by the french company Servier. Tianeptine has opioid like effects, leading to potential dependence and addiction.
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.
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.
Regulatory Issues and Abuse Potential
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. 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
Tianeptine is not approved by the FDA.
Consumer impact summary
Despite not being FDA-approved for any medical use, tianeptine is widely available in gas stations, convenience stores, and online retailers under misleading marketing. This accessibility creates a false impression of safety and legitimacy2. Users are often unaware of the true nature of what they're consuming, with products frequently containing doses far exceeding therapeutic levels used in countries where tianeptine is prescribed legally—up to 3000mg compared to the 12.5-50mg therapeutic range.
Tianeptine has become increasingly problematic in the United States, where it is sold as an unregulated supplement under names like "Tianaa" and "Zaza". These products have been linked to severe addiction, with poison control center cases involving tianeptine exposure increasing from 11 total cases between 2000 and 2013 to 151 cases in 2020 alone.
The FDA has issued multiple warnings about tianeptine, stating it is "not approved by the FDA for any medical use" and warning consumers about "dangerous and unproven claims that tianeptine can improve brain function and treat anxiety, depression, pain, opioid use disorder, and other conditions".
Several U.S. states have banned tianeptine, including Kentucky, where Democratic Governor Andy Beshear signed an emergency order banning it in March 2023, using legislation originally created to ban fentanyl analogs.
See also