The Preclinical and Clinical Effects of Vilazodone for the Treatment of Major Depressive Disorder

Figures & data

Table 1. Vilazodone pharmocological and clinical properties.

Dose	10–40 mg/day
Mechanism
Receptor action	5-HT1A receptor partial agonist
Absorption
Tmax	3.7–5.3 h
Peak plasma concentration	156 ng/ml
T1/2, hour	20–24 h
Absolute bioavailability (with food)	Bioavailability from 22 to 72%
Food effect	AUC0-24 h increased from 147 to 160% with high fat meals and 64 to 85% with light meals
Distribution
% Protein binding	96–99%
Metabolism
Pathways	CYP: primarily by the hepatic CYP450 3A4 enzyme system and secondarily by CYP2C19, CYP2D6 Non-CYP: mediated by carboxylesterases
Excretion	1% urine unchanged drug in urine 2% unchanged drug in feces
Safety
Common adverse effects (>10%)	Diarrhea, nausea, headache
Pregnancy	Category C