Michigan is officially the first state in the nation to outlaw a substance that medical professionals say is adding fuel to the fire that is the opioid crisis — formally banning a drug known as Tianeptine.
First prescribed as an opiate-like antidepressant in Europe as early as the 1950s, Tianeptine is commonly abused in the United States because it’s easily modified and easily accessible. The drug is sold under trade names such as Coaxil or Stablon and also marketed as a stress relief supplement, which can be purchased effortlessly online in most other states.
In recommended doses, Tianeptine does not make the user feel high and does seem to treat depression differently than other antidepressants available. Serious problems arise, however, when the substance is taken in excess and modified to have stronger effects.
According to Grand Valley State University professor of Biomedicine Babasola Fateye, users can modify the structure of this substance so that it can be snorted, injected or even vaped.
On most websites, Tianeptine is presented as a mood-enhancing, anxiety-reducing, focus-improving supplement in a capsule form. Scroll down a bit further, though, and you’ll see the fine print.
Nootropics.com, a widely-utilized online source for Tianeptine, includes a warning below the product which reads:
“Tianeptine may have opiate-like withdrawal symptoms and shows potential for abuse. Ensure that usage is gradually reduced with care, and if ever in doubt, consult a qualified medical professional. If you have ever been addicted to opioids, Tianeptine may have an immediate addictive effect.”
More and more recently, opiate addicts all over the country are realizing that Tianeptine is a cheap, federally legal loophole that will give them the fix their looking for. The longer these products stay available for anyone to purchase, the more the problem continues to grow.
The opiate-like effects of the drug are appealing to users, but causing alarm to Michigan state officials, particularly those in the Midland area, where police say the community is gripped by the impact of Tianeptine use, which causes withdrawal symptoms that can be painful and violent. The Associated Press reported in March 2018 that the Midland and Saginaw areas saw drastic spikes in Tianeptine sodium related deaths in the previous year.
In February 2018, Midland substance abuse recovery coach Alyssa Wood testified before the Senate Judiciary Committee on how her addiction to Tianeptine sodium affected her while she was weaning herself off heroin. According to Wood, coming off heroin was easy compared to the withdrawals she experienced from Tianeptine.
“I could not get out of bed, go to work, have a normal, functioning day without (Tianeptine) in my life,” Wood said in the hearing. “I am convinced that it is the next epidemic.”
Michigan State Police legislative liaison Sgt. Matthew Williams believes that though Tianeptine could have medical benefits down the line, the excessive consumption of the drug is a serious issue for local communities.
“Because the bill ranks the drug as Schedule II and not Schedule I, Michigan residents could legally use Tianeptine in the event that it is ever approved by the FDA,” Williams said.
Williams says the bill aims to effectively stomp out all legal manufacture, distribution and possession of Tianeptine sodium in Michigan.
Tianeptine is an antidepressant agent with a novel neurochemical profile. It increases serotonin (5-hydroxytryptamine; 5-HT) uptake in the brain (in contrast with most antidepressant agents) and reduces stress-induced atrophy of neuronal dendrites. Like the selective serotonin reuptake inhibitors (SSRIs) and in contrast with most tricyclic antidepressant agents, tianeptine does not appear to be associated with adverse cognitive, psychomotor, sleep, cardiovascular or bodyweight effects and has a low propensity for abuse. Tianeptine has a comparatively favourable pharmacokinetic profile. It is not subject to first-pass hepatic metabolism, has high bioavailability and limited distribution, and is rapidly eliminated. While this offers advantages for tianeptine over the tricyclic antidepressant agents in terms of dose titration, treatment changes and potential drug interactions, its rapid elimination makes adherence to dosage schedules more important. Tianeptine differs from most antidepressants in that it is not primarily metabolised by the hepatic cytochrome P450 system, indicating less likelihood of drug-drug interactions; this is of particular interest for elderly patients. Tianeptine, in dosages of 25 to 50 mg/day, has been investigated in patients with major depression, depressed bipolar disorder, dysthymia or adjustment disorder. It has equivalent antidepressant efficacy to several classical antidepressant agents (amitriptyline, clomipramine, imipramine, mianserin) and the SSRIs fluoxetine (in most patients), paroxetine and sertraline. Comparison with maprotiline indicated superior efficacy for tianeptine but dothiepin appeared superior in another study. Extended treatment with tianeptine decreases the incidence of relapse/recurrence of depression. Tianeptine appears to be as effective as fluoxetine, sertraline, amitriptyline, clomipramine and mianserin and more effective than maprotiline in improving associated anxiety in patients with depressive disorders. Depression and anxiety symptoms in alcohol dependant patients also respond well to tianeptine. The adverse effects associated with tianeptine are similar in many respects to those of the SSRIs and minimal in comparison with the tricyclic antidepressants. The most common adverse effects are nausea, constipation, abdominal pain, headache, dizziness and changes in dreaming. Anticholinergic effects occur less often with tianeptine than with tricyclic agents. Hepatoxicity is rare. The dosage should be decreased in elderly patients and those with severe renal failure, but adjustment is not necessary in patients with alcoholism or hepatic impairment, or those undergoing haemodialysis.
CONCLUSIONS:The antidepressant efficacy and favourable tolerability and pharmacokinetic profiles of tianeptine in patients with depression, including those with associated anxiety, have been proven; the data indicate that it may have additional potential in specific subgroups of depressed patients such as the elderly and those with chronic alcoholism.