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tianeptine

N06AX14

Forms & Strengths

Oral tablets: 12.5 mg sodium salt
Oral tablets: 12.5 mg or 30 mg extended-release (sodium salt)
Oral tablets: 20 mg (tianeptine sulfate)

Adult Dosing

Major depressive disorder: 12.5 mg orally three times daily before meals
Maximum recommended dose: 37.5 mg daily
Renal impairment (severe, CrCl < 30 mL/min): Maximum 12.5 mg twice daily
Hepatic impairment: No specific dosage adjustment required

Pediatric Dosing

Safety and efficacy in pediatric patients under 18 years have not been established
Use in children and adolescents is not recommended

Indications

Treatment of major depressive episodes in adults
Anxiety associated with depression (off-label or regional approval variations)

Mechanism of Action

Atypical tricyclic structure acting as a full agonist at $\mu$-opioid receptors
Enhances extracellular serotonin reuptake in the cortex and hippocampus (inverse to typical SSRIs)
Modulates glutamate transmission and prevents stress-induced dendritic atrophy

Contraindications

Hypersensitivity to tianeptine or any excipients
Concurrent use with monoamine oxidase inhibitors (MAOIs) due to risk of hypertensive crisis and serotonin syndrome
Children under 18 years of age

Adverse Reactions

Insomnia, nightmares, drowsiness, dizziness
Dry mouth, constipation, abdominal pain, nausea, vomiting
Tachycardia, extrasystoles, chest pain
High potential for abuse, dependence, and severe withdrawal syndrome with misuse

Drug Interactions

MAOIs: Fatal or severe hypertensive crises and serotonin syndrome; require a 14-day washout period
Central nervous system depressants (alcohol, opioids, sedatives): Enhanced sedation and respiratory depression risk
No significant CYP450 enzyme-mediated interactions identified in clinical studies

Curated Content: Needs Vetting Before Put to Clinical Use