vortioxetine TRINTELLIX
Class: Multimodal AntidepressantFDA Indications: MDD
Off-Label Use: GAD, Cognitive Symptoms Associated With Depression, Geriatric Depression
Prescribing
Forms: 5, 10, 20mg tabletDose Range: 10-20 mg/day
Starting: Start 10 mg qd; can ↓ to 5 mg once daily or ↑ to 20 mg qd depending on patient response; maximum recommended dose generally 20 mg qd
Stopping: Because of long t½, taper is not necessary
Precautions
Contraindications: Concomitant use of MAOIsSerious Side Effects: Serotonin syndrome; ↑ risk of SI in children and young adults; may impair platelet aggregation; SIADH
Side Effects: nausea (26% @ 10mg, versus 9% placebo), constipation
Pharmacodynamics
1° MOA: Selective serotonin reuptake inhibitor2° MOA:
- antagonism @ 5HT1D
- antagonism @ 5HT3A
- antagonism @ 5HT7
- partial agonism @ 5HT1B
- agonism @ presynaptic somatodendritic 5HT1A autoreceptors
- agonism @ postsynaptic 5HT1ARs
Target: SERT, 5HT1A, 5HT1B, 5HT1D, 5HT3, 5HT7,
Pharmacokinetics
t½: 66° TMAX: 7°Substrate of: 2D6; 2B6, 2C9, 2C19, 3A4
Inhibits: ∅ ; Induces: ∅
Active Metabolites: ∅
DDIs
- - DO NOT CO-PRESCRIBE WITH MAOIs (need a 14-21 day washout period)
- - 2D6 inhibitors can ↑ serum levels; 2D6 inducers can ↓ serum levels
Misc
- - unique multimodal mechanism of action
- - most studies suggest clinically meaningful advantage in terms of tolerability over other serotonergic agents
- - incidence of sexual side-effects appears particularly low
- - well tolerated in the elderly
- - no weight gain
- - growing evidence of possible cognitive benefits; appears to ↑ frontal cortical activity in a pattern that differs from SSRIs/SNRIs
Special Populations
Category C—No controlled studies in humans.
There are no clinical data regarding the effect on lactation and nursing
No dose adjustment necessary
Renal impairment does not affect clearance.
Hepatic impairment does not affect clearance.
References
Trintellix Package InsertApplied Clinical Pharmacokinetics And Pharmacodynamics Of Psychopharmacological Agents
Concise Guide To Drug Interaction Principles For Medical Practice
Foye's Principles Of Medicinal Chemistry
The Clinical Pharmacokinetics Of Lu AA21004 And Its Major Metabolite In Healthy Young Volunteers
New Generation Multi-modal Antidepressants: Focus On Vortioxetine For Major Depressive Disorder
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