tianeptine and kratom - chi st. gabriel's health · low dose- recommended doses •nausea...
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Tianeptine and Kratom
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Objectives
Explain the history and origins of Tianeptine Describe the adverse effects
of Kratom use
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Tianeptine
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Tianeptine
Marketed as:•Stablon•Coaxil
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Tianeptine
Marketed in 15 European counties and 66 countries world wide
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Tianeptine
Online marketing- different“Boost working memory”“Improve mental clarify”
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Tianeptine
History•Discovered and patented in 1960s by the French society of medical research, but for many decades mechanism of action was unknown
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Tianeptine
Metabolism- β oxidation of side chain• 66% eliminated by kidneys• ½ life 2.5 hours• No adjustments in liver failure
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Tianeptine
Toxicity•Respiratory depression – death•Considered initially a rare, if not unheard of problem, as abuse of this medication was felt to be < 0.3%
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Tianeptine
Mechanism of Action•First reported mechanism of action was felt to be increased serotonin reuptake which was opposite of SSRI
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Tianeptine
In 2014 the article, “The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist” showed:• Mu activation was likely the initial molecular
event• Possible effects to delta receptor also• Indirectly modulates glutamate (excitatory)
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Tianeptine
“Our data are also in agreement with growing evidence regarding the importance of the opioid system in depression, anxiety and stress-related disorders.”
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Tianeptine
Tianeptine, an atypical pharmacological approach to depression
“A noteworthy fact is that tianeptine, despite its affinity for these receptors, did not cause tolerance, as it does not lose its efficacy after continued treatment, or physical dependence, as after suppression or administration of naloxone no withdrawal syndrome was observed. These two characteristics clearly differentiate tianeptine from the other opioids, such as morphine.”
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Tianeptine
Conflicts of Interest• C. Alamo has collaborated in studies on training and
information through presentations at scientific events for healthcare workers sponsored by Adamed, Exeltis, Janssen, Lundbeck, Normon, Otsuka, Pfizer, Sevier, Zambon.
• P. García-García works in the Medical Department of Exeltis Healthcare S.L.
• The other authors have no conflict of interests to declare.
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Tianeptine
Tianeptine: Why has it not been classified as a narcotic in Spain?
“In short, tianeptine is a drug new to Spain, but it is one that has raised numerous issues elsewhere for years. Compared to other antidepressants, it does not present any advantages with respect to either efficacy or convenience.”
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Tianeptine
Tianeptine, antidepressant with positive benefit/risk
Summary of letter= Calabozo does not know what he talking about
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Tianeptine
Reddit- the source of all knowledge• Tianeptine sodium- shorter acting 2.5 hours• Tianeptine sulfate- longer acting 7.5 hours
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Tianeptine
10-15 mg
50-60 mg
85-90 mg
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“Incredible mood enhancer”“Immediate antidepressant effect”
“Did not feel impaired”
“Sedation”“Impaired my ability to drive”
“Nodded off”“Vivid dreams”
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Tianeptine
Another post: “Tolerance is quick. Kills your ability to feel any other opioids, kills effectives of Kratom 100%”
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Tianeptine
Low dose- recommended doses• Nausea• Constipation• Headache• Dizziness
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Tianeptine
High dose- when misused• May mimic opioid OD- Naloxone effective• Tolerance common• NAS after delivery
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Tianeptine
Withdrawal•Really indistinguishable from opioids
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Tianeptine
Use of Buprenorphine-Naloxone in the Treatment of Tianeptine Use Disorder
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Kratom
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Kratom
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Kratom
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Kratom
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Kratom
• DEA - Mitragyna speciose (Rubiaceae family)• Indigenous to Thailand, Malaysia, Myanmar,
Papua New Guinea, others
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Kratom
History• Tree indigenous to Asia• Used in religious practices
and by workers for mild stimulation
• Member of the coffee family• At times in history used to
help taper people off of opioids
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Kratom
• Formulations• Leaves• Powder• Pills• Leaves• Liquid extract/tinctures
• Route• Drink• Chew leaves• Smoke• Ingest pills
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Kratom
•Adverse Effects• Dry mouth• Nausea• Weight loss• Constipation• Seizure
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•Hepatic injury•QT prolongation•Tolerance•Withdrawal
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Kratom
•Withdrawal•Similar to opioid withdrawal•Starts at about 6-12 hours•Lasts about 2-3 days
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References
• Gassaway MM, Rives ML, Kruegel AC, Javitch JA, Sames D. The atypical antidepressant and neurorestorative agent tianeptine is a μ-opioid receptor agonist. Transl Psychiatry. 2014;4(7):e411. Published 2014 Jul 15. doi:10.1038/tp.2014.30
• Alamo C, Garcia-Garcia P, Lopez-Munoz F, Zaragoza C. Tianeptine, an atypical pharmacological approach to depression. Journal of Psychiatry and Mental Health, 2019-07-01, Volume 12, Issue 3, Pages 170-186, Copyright © 2019
Calabozo B, Molina V, Uribe F. Tianeptine: Why has it not been classified as a narcotic in Spain? Journal of Psychiatry and Mental Health, 2016-07-01, Volume 9, Issue 3, Pages 176-177, Copyright © 2016Garcia-Garcia P. Tianeptine, antidepressant with positive benefit/risk. Journal of Psychiatry and Mental Health, 2016-10-01, Volume 9, Issue 4, Pages 234-235, Copyright © 2016Trowbridge P, Walley AY. Use of buprenorphine-naloxone in the treatment of tianeptine use disorder. J Addict Med. 2019 Jul/Aug; 13(4):331-333.
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