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Comment · Thu, September 18, 2014 · Ceretropic

Tianeptine abuse: a case report (2014)

What they were answering

Bateau55 · 0 points

Tianeptine's ability to augment AMPA and NMDA receptor function actually makes it's opiate effects more addicting, literally doing the opposite of classic anti-addiction drugs like DXM and Memantine, or the opiates used for curbing opiate addiction, Methadone and Tramadol. Surprised that this interaction isn't mentioned more when discussing it.

AMPA and NMDA receptor function are essential for creating most of the negative side effects of addictive substances (i.e. addiction, tolerance, withdrawal effects, conditioned fear, place preference etc.), and blockade of the receptors inhibits the negative aspects of these substances while augmentation of these receptors augments these negative effects.

u/MisterYouAreSoDumb · Ceretropic

It is an NMDA/AMPA modulator, not an agonist. It normalizes the current between the AMPA and NMDA receptors. There is no evidence that it exacerbates tolerance, side effects, or addictiveness to opioids. In fact, there is evidence of the opposite.

Tianeptine reduces morphine antinociceptive tolerance and physical dependence

The combination of tianeptine with morphine significantly reduced the development of morphine antinociceptive tolerance and suppressed the incidence of naloxone-precipitated withdrawal symptoms. We conclude that tianeptine is an effective inhibitor of morphine-induced antinociceptive tolerance and physical dependence in mice. Our results would imply that comedication with tianeptine and morphine might benefit those who need long-term morphine treatment.

Analysis of the side effects of tianeptine.

Tianeptine does not induce sedation and thus does not disturb the recovery of active life. It does not induce anticholinergic effects (dry mouth, constipation, etc.), even in elderly subjects. It is devoid of heart and blood pressure side effects including postural hypotension tachycardia, ECG abnormalities, and especially atrioventricular or intraventricular conduction disorders. Moreover, tianeptine does not disturb the hematologic, renal, hepatic parameters, even in alcoholic patients in the detoxification period. It does not induce physical or psychological signs of dependence when discontinued, even in alcoholic patients or drug addicts. No abuse of tianeptine and no tolerance were noted in detoxified opiate addicts.

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