Clinical Information

Duloxetine is an antidepressant of the serotonin-norepinephrine reuptake inhibitor class. It is effective in treating symptoms of depression, including physical pain associated with depression; other uses include therapy of neuropathic pain, fibromyalgia, and urinary stress incontinence. Duloxetine also inhibits serotonin uptake in human platelets, and may be associated with potentiation of bleeding.

Duloxetine undergoes extensive hepatic biotransformation to numerous inactive metabolites. The drug is metabolized by CYP1A2 and CYP2D6, with moderate potential for drug interactions (duloxetine is both a substrate and a moderate inhibitor of CYP2D6). The mean elimination half-life is 12.5 hours with steady-state concentrations occurring in about 3 days. Specimens for therapeutic monitoring should be drawn immediately before the next scheduled dose (ie, trough).

Duloxetine is not recommended for patients with hepatic impairment, substantial alcohol use, or chronic liver disease. Use in patients with renal disease significantly increases exposure to duloxetine due to decreased elimination. Patients with mild-to-moderate renal dysfunction should be monitored closely; use of duloxetine is not recommended in end-stage renal disease.