Quick Comparison

B-ComplexTianeptine
Half-LifeWater-soluble; excreted daily (except B12 which is stored)2.5-3 hours (tianeptine), 7-8 hours (active metabolite MC5)
Typical DosageStandard: A quality B-complex providing 25-100 mg of B1, B2, B3, B5, B6, plus 400-800 mcg folate (as methylfolate) and 500-1000 mcg B12 (as methylcobalamin). Methylated forms preferred for B9 and B12 (folate → methylfolate, B12 → methylcobalamin). Take in the morning — B vitamins can be mildly energizing.Prescription dose: 12.5 mg three times daily (Stablon). Extended-release: 25 mg once daily (Tianeurax). Do not exceed prescribed doses — abuse potential at higher doses due to opioid activity.
AdministrationOral (capsules, tablets, sublingual). Methylated forms preferred for B9 and B12. Take with breakfast.Oral (tablets). Immediate-release (12.5 mg TID) or extended-release (25 mg QD).
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Mechanism of Action

B-Complex

Each B vitamin serves specific neurological functions: B1 (thiamine) — cofactor for transketolase (pentose phosphate pathway), pyruvate dehydrogenase, and alpha-ketoglutarate dehydrogenase; essential for glucose metabolism and ATP production in neurons. B2 (riboflavin) — precursor to FAD/FMN, cofactors for Complex I and II of the electron transport chain, and glutathione reductase. B3 (niacin/niacinamide) — precursor to NAD+/NADPH via the salvage pathway; NAD+ is substrate for sirtuins, PARP, and 400+ dehydrogenases. B5 (pantothenic acid) — component of coenzyme A, required for acetylcholine synthesis via choline acetyltransferase and for fatty acid oxidation. B6 (pyridoxine) — cofactor for AADC (5-HTP to serotonin, L-DOPA to dopamine), GABA synthesis (GAD), and homocysteine metabolism. B9 (folate) — tetrahydrofolate donates methyl groups for dTMP and purine synthesis, and for homocysteine remethylation. B12 (cobalamin) — cofactor for methionine synthase (myelin maintenance) and methylmalonyl-CoA mutase.

Tianeptine

Tianeptine is a full agonist at mu-opioid (MOR) and delta-opioid (DOR) receptors, mediating both its antidepressant/anxiolytic effects and abuse potential at high doses. Paradoxically, it enhances serotonin reuptake via SERT—opposite to SSRIs—yet still produces antidepressant effects, possibly through opioid-mediated mood regulation. Tianeptine modulates glutamatergic signaling by reversing stress-induced downregulation of AMPA receptor subunits (GluA1/GluA2) and restoring synaptic plasticity. In the hippocampus and amygdala, it prevents stress-induced dendritic atrophy, spine loss, and CA3 pyramidal cell damage—likely through opioid receptor activation and downstream HPA axis effects. It increases BDNF levels and promotes neurogenesis. The combination of opioid agonism, glutamate normalization, and neuroplasticity enhancement underlies its unique profile.

Risks & Safety

B-Complex

Common

Bright yellow urine (harmless — riboflavin excretion), mild nausea.

Serious

Very safe at standard doses. B6 can cause peripheral neuropathy at >200 mg daily for extended periods.

Rare

Flushing from niacin (B3) if non-flush form is not used.

Tianeptine

Common

Nausea, constipation, abdominal pain, headache, dizziness, dry mouth.

Serious

Opioid-like effects at high doses (euphoria, dependence, respiratory depression). Withdrawal syndrome with abrupt cessation after chronic high-dose use. Abuse and overdose deaths reported.

Rare

Hepatotoxicity, skin reactions.

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