Vortioxetine (Trintellix)

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. To review antidepressant mechanisms, enroll in the Neuropsychopharmacology Course.

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.