Tianeptine
Tianeptine. An atypical antidepressant that, unusually, acts as an efficacious agonist at the µ-opioid receptor (and a low-potency full δ-opioid… Oral half-life 2.5 h.
An atypical antidepressant that, unusually, acts as an efficacious agonist at the µ-opioid receptor (and a low-potency full δ-opioid agonist) — now understood to underlie both its mood effects and its abuse liability ("gas station heroin"). It also modulates glutamatergic transmission and reverses stress-induced hippocampal remodeling. At supratherapeutic doses the opioid agonism produces euphoria, tolerance, dependence, and a classic opioid withdrawal syndrome.
PubChem CID 68870 (free acid; marketed sodium salt ≈459 g/mol). PK: Salvadori 1990 (PMID:2341111) verbatim eliminated "with a half-life of 2.5 +/- 1.1 h". Inactive at KOR per the same paper. PK: THE ROW CARRIED A CITATION AND NOTHING ELSE, SO EVERY PARAMETER WAS A SILENT DEFAULT — while the cited abstract states three of them verbatim. THE OBVIOUS ONE IS A TRAP: "total clearance and volume of distribution of tianeptine were 230 +/- 59 ml.min-1 and 0.47 +/- 0.14 l.kg-1" is a steady-state volume from a study with a genuine distribution phase ("the mean distribution half-life being about 0.7 h"), and storing it would assert a clearance a third below that same abstract own figure. THE COHERENT ONE-COMPARTMENT VOLUME WAS ALREADY IN THIS RECORD REFERENCES — "the apparent volume of distribution being about 0.8 L/kg (0.77 +/- 0.31 L/kg)" — and lands within eight percent. Bioavailability is verbatim at 99 percent from a real intravenous arm, so class 6 is decided rather than assumed. The absorption rate is BACK-DERIVED to reproduce a verbatim peak time of 0.94 h and is flagged as such. THE COST IS STATED: preserving exposure puts the peak around 177 ng/mL against a verbatim 334, and the volume that fixes the peak breaks exposure by half — though that abstract never states its dose, so the comparison is indicative rather than decisive. A SOFT CAVEAT ON THE EFFECT COMPARTMENT: its approximation is reasoned from a neutral lipophilic opioid, while tianeptine is an ANION at physiological pH with far poorer passive brain entry, so the stored rate probably overstates the speed.
Pharmacokinetics
- Oral — t½ 2.5 h · F 99% · ka 2.7 h⁻¹ · Vd 53.9 L
Sources: PMID:2341111, PMID:25026323, PMID:3180120