Lorcaserin Extended-Release Tablets and Valvulopathy

Regurgitant cardiac valvular disease, primarily affecting the mitral and/or aortic valves, has been reported in patients who took serotonergic drugs with 5-HT2B receptor agonist activity. The etiology is thought to involve activation of 5-HT2B receptors on cardiac interstitial cells. At therapeutic concentrations, lorcaserin is selective for 5-HT2C receptors relative to 5-HT2B receptors, thus it is not known if lorcaserin can cause valvulopathy. In clinical trials of one year duration, 2.4% of patients receiving lorcaserin and 2.0% of patients receiving placebo developed echocardiographic criteria for valvular regurgitation at one year (mild or greater aortic regurgitation and/or moderate or greater mitral regurgitation). None of these patients was symptomatic. Lorcaserin has not been studied in patients with congestive heart failure or hemodynamically-significant valvular heart disease. Preliminary data suggest that 5-HT2B receptors may be overexpressed in congestive heart failure. Therapy with lorcaserin should be administered cautiously in patients with congestive heart failure or preexisting valvulopathy. Patients who develop signs and symptoms of valvular heart disease such as dizziness, fatigue, weakness, dyspnea, edema, or arrhythmia during treatment with lorcaserin should seek prompt medical attention. Discontinuation of lorcaserin should be considered.