Clinical Information

Venlafaxine is a serotonin and norepinephrine reuptake inhibitor approved for treatment of major depression, anxiety and panic disorders, and social phobias. It is also used for bipolar disorder, bulimia, post-traumatic stress, obsessive behavior, and attention-deficit disorder. Venlafaxine is converted by CYP2D6 to the active metabolite, O-desmethylvenlafaxine. The therapeutic range for venlafaxine includes measurement if O-desmethylvenlafaxine; optimal response is seen when combined concentrations of parent and metabolite are between 195 and 400 ng/mL. Venlafaxine is significantly affected by reduced hepatic function, but only slightly by reduced renal function.

Average elimination half-lives are 5 hours for venlafaxine and 10 hours for O-desmethylvenlafaxine, which are much shorter than many other antidepressants. For this reason, extended release formulations are available. Time to peak serum concentration is 2 hours for the regular product and 8 hours for the extended release product. Common toxicities are mild, including drowsiness, dizziness, nausea, and headache.