Vortioxetine (Trintellix)

Vortioxetine (Trintellix) is an antidepressant with many actions (also termed a multimodal antidepressant). In addition to being a serotonin reuptake inhibitor, Vortioxetine has numerous effects at other receptor sites which work together in complex and poorly understood ways to produce an antidepressant effect.

RECEPTOR PROFILE:

  • SERT Inhibition (serotonin reuptake inhibition)
  • 5HT1A Full Agonist
  • 5HT1B Partial Agonist
  • 5HT1D Antagonist
  • 5HT3 Antagonist
  • 5HT7 Antagonist

ROUTE OF ADMINISTRATION: Oral

 

HALF-LIFE: 66 hours

 

TIME TO STEADY STATE: 2 weeks

 

PEAK IN PLASMA: 7-11 hours

 

PLASMA PROTEIN BOUND: 98%

 

METABOLISM: Hepatic; Phase I+II; CYP2D6; Inactive metabolites

 

HEPATIC IMPAIRMENT (HI): No dose adjustment for mild/moderate HI

 

RENAL IMPAIRMENT (RI): No dose adjustment needed

 

FOOD or FAST (PO)? Either

 

STARTING DOSE:

~10mg PO daily (18-65 years old)

~5mg PO daily (>65 years old)

 

TARGET DOSING RANGE: 5-20mg / day

 

BEST TIME TO DOSE: Morning after a meal or night

 

HOW TO DOSE:
>>Start 5mg-10mg per day and increase dose by 5mg after two (2) weeks based on response and tolerability.

>>Max dose typically 20mg/day 

 

PREGNANCY: N/A*

 

BREASTFEEDING: N/A* 

 

NOTABLE SIDE EFFECTS: 

  • Nausea (Dose dependent;usually first few weeks)

 

WHEN SIDE EFFECTS OCCUR: 

  • Hold for 3 days and restart at half the dose

 

NOTABLE INTERACTIONS:

  • Avoid with MAOIs
  • If switching from or to an MAOI, washout is 2 weeks
  • Not an inducer/inhibitor of CYP450
  • If given with 2D6 Inhibitors (paroxetine, fluoxetine), AUC is doubled
  • May reduce effects of triptans used for migraines (via 5HT1D antagonism)

 

FDA INDICATIONS:
1) Major depressive disorder 

*Not enough information

 

ADDITIONAL INFORMATION

  • Some evidence that vortioxetine improves cognitive symptoms of depression
  • Minimal to no sexual dysfunction at dosages of 5mg-10mg
    • Dosages of 20mg/day showed similar sexual side effects as duloxetine 60mg/day
  • Minimal to no withdrawal syndrome (due to long half-life)
  • Minimal to no effects on body weight
  • No clinically meaningful QT changes after 14 days of 40mg/day 

References

  1. Schatzberg, A. F., & DeBattista, C. (2015). Manual of clinical psychopharmacology. Washington, DC: American Psychiatric Publishing.
  2. Schatzberg, A. F., & Nemeroff, C. B. (2017). The American Psychiatric Association Publishing textbook of psychopharmacology. Arlington, VA: American Psychiatric Association Publishing.
  3. Stahl, S. M. (2013). Stahl’s essential psychopharmacology: Neuroscientific basis and practical applications (4th ed.). New York, NY, US: Cambridge University Press.