Tianeptine: a public health risk

Tianeptine is an atypical tricyclic antidepressant used in Europe, Asia (it was developed in the USSR in the 1960s), and Latin America. It also has μ-opioid receptor agonist activity. It is not approved for use in the US. see https://www.cdc.gov/mmwr/volumes/67/wr/mm6730a2.htm?s_cid=mm6730a2_w ​

Details:

--the CDC analyzed poison control center calls for tianeptine during 2000-2017, a total of 218 calls, 52% being for tianeptine-only exposure

--from 2000-2013, there were a total of 11 calls, which then increased from 5 in 2014, to 38 in 2015, to 83 in 2016, and 81 in 2017

--91% of the calls were from health care providers

Results:

--55% of people had intentional exposure, 84% by ingestion/7% parenteral/2%inhalation

--57% of the calls were for those 21-40 yo

--most common problems were: neurologic (48%; mostly agitation, drowsiness, confusion), cardiovascular (33%; mostly tachycardia, high blood pressure), and GI (11%; mostly nausea); also some effects mimicked opioid toxicity or withdrawal

--44% were treated, evaluated and released from the ED, 24% were admitted to a critical care unit

--there were 29 withdrawal-related calls, mostly for agitation (33%), nausea (33%), vomiting (19%), tachycardia (19%), hypertension (14%), diarrhea (10%), tremor (10%) and diaphoresis (10%)

--there have been 2 deaths reported in Texas, and 2 more not reported through the National Poison Data System

--treatment included benzodiazepines (57%), fluids (38%), and antiemetics (19%)

--tianeptine, if not taken alone, is most commonly taken with phenibut (a GABA receptor agonist, mostly acting on GABA-B receptors, similar to baclofen; is available in the US, and can be used to treat anxiety, insomnia, depression, stuttering, vestibular disorders, memory enhancement, and PTSD). tianeptine​ is also taken with ethanol, benzos, and opioids

--outcomes tended to be more major (eg, requiring treatment; sometimes life-threatening or resulting in residual disability or disfigurement) when tianeptine​ was used with other substances

--reporting by regions in the US: South (35%), West (25%), Midwest (22%), Northeast (19%)

--82% male, 18% female

Commentary:

--In the country Georgia, tianeptine was withdrawn from the market in 2010. in Russia and Armenia, it was classified as a controlled substance in 2010, and in Ukraine in 2011

--though not FDA-aproved, it is available on-line in the US as a dietary supplement or research chemical

--online discussion forums note the euphoregenic effects of tianeptine, and the combo of tianeptine and phenibut have an enhanced effect. this combo was the most reported combo

--a report like this is helpful in revealing trends but very likely understates the problem by being limited to poison center calls, a voluntary system for reporting by health providers

--and the overall clinical data (length of stay, treatment response, sequelae) was pretty limited in this database

so, yet another potentially harmful substance increasingly around. a prior blog reference kratom, also a  μ-opioid receptor agonist​, with several reported deaths. (see http://gmodestmedblogs.blogspot.com/2016/01/2-blogs-in-1-kratom-and-repeated-opioid.html  )

 my concerns are:

--as mentioned in a recent blog, the cost of prescription opioids in the community has increased because of some effective programs in limiting these prescriptions, with the unfortunate (though anticipated) effect of leading people to cheaper but more dangerous drugs

--there is much easier access to tianeptine (and kratom) over the regular internet, and access to everything in the dark web. and these new drugs will keep on appearing and be at least one step ahead of us

--and, it really does not seem that there is an easy solution.  the underlying issues leading to this epidemic of substance use disorders need to be dealt with: people need reasonable housing, food access, education, rewarding jobs, clean environments, health care, a functional and responsive political system, and a sense of hope for the future....

As per Virchow in 1879: "Don't crowd diseases (epidemics) point everywhere to deficiencies of society?"

geoff​

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