Ruoxinlin Toludesvenlafaxine Hydrochloride Sustained-release Tablets

1. Indications and Usage
Major Depressive Disorder (MDD): Treatment of adult patients with major depressive disorder.
Efficacy: Demonstrated improvement in depressive symptoms, including anhedonia, psychomotor retardation, cognitive impairment, and fatigue.
2. Dosage and Administration
Route of Administration: Oral administration ONLY.
Recommended Dosage: 40 mg to 160 mg once daily.
Critical Administration Instructions:
Titration: Starting dose is 40 mg once daily. Based on individual response, the dose may be increased to 80 mg within one week. The maximum dose should not exceed 160 mg once daily.
Timing: Take at a relatively fixed time each day, with or without food.
Swallowing: Tablets must be swallowed whole; do not crush, chew, or dissolve.
Discontinuation: Do not stop abruptly. Taper the dose gradually to avoid discontinuation symptoms.
3. Mechanism of Action
Dual Reuptake Inhibition: Toludesvenlafaxine is an enantiomerically enriched compound that inhibits the reuptake of 5-hydroxytryptamine (5-HT) and norepinephrine (NE).
Active Metabolite: It is rapidly hydrolyzed in vivo to its active metabolite, O-desmethylvenlafaxine (ODV), which acts as a potent and selective 5-HT and NE reuptake inhibitor.
Neurotransmission: This mechanism enhances central nervous system 5-HT and NE neurotransmission, leading to antidepressant effects.
4. Safety and Warnings
Suicidal Ideation: Antidepressants increase the risk of suicidal thinking and behavior in children, adolescents, and young adults (≤24 years) during short-term use.
Serotonin Syndrome: Risk increases when used with other serotonergic drugs (e.g., triptans, tricyclics, other SSRIs/SNRIs).
MAOI Interaction: Contraindicated with Monoamine Oxidase Inhibitors (MAOIs). At least 7 days must pass after stopping toludesvenlafaxine before starting an MAOI, and at least 14 days after stopping an MAOI before starting toludesvenlafaxine.
Cardiovascular Monitoring: Monitor for increases in blood pressure and heart rate.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Nausea, dizziness, dry mouth, somnolence, and headache.
Clinical Research Highlights: Phase 3 randomized, double-blind, placebo-controlled trials confirmed its efficacy in treating MDD. Discontinuation of treatment due to adverse reactions occurred in 5.75% of treated patients.
6. Drug Interactions
CYP Enzymes: Toludesvenlafaxine is primarily metabolized via ester hydrolysis by carboxylesterase 2 (CES2). It does not significantly inhibit or induce major CYP450 enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, 3A4).
Drug-Drug Interactions: The risk of CYP-mediated drug-drug interactions is low.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Toludesvenlafaxine Hydrochloride.
Appearance: White or off-white film-coated tablets.
Packaging: Aluminum-plastic blister packaging.
Storage: Store at controlled room temperature (20°C to 25°C); protect from moisture.