Sarpogrelate Hydrochloride, a Selective 5-HT2A Antagonist, Improves Vascular Function in Patients With Peripheral Arterial Disease

Peripheral arterial disease (PAD) is 1 of the major manifestations of atherosclerosis. PAD is associated with endothelial dysfunction. Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, has been widely used as an anti-platelet agent for the treatment of PAD. There is no information on whether endothelial function is improved after initiation of sarpogrelate treatment in patients with PAD. The purpose of this study was to evaluate the effects of sarpogrelate on endothelial function in patients with PAD. We divided PAD patients into 2 groups: those treated with sarpogrelate at a dose of 100 mg 3 times per day orally for 12 weeks (sarpogrelate group, n = 10), and those who remained on conventional therapy (control group, n = 11). Forearm blood flow (FBF) and leg blood flow (LBF) responses to reactive hyperemia (RH) and sublingual administration of nitroglycerin (NTG) were measured using strain-gauge plethysmography. After 12 weeks of sarpogrelate administration, FBF and LBF responses during RH showed significant increases from 13.2 +/- 1.7 to 18.1 +/- 2.2 mL/min per 100 mL tissue (P < 0.01) and from 8.2 +/- 0.9 to 14.2 +/- 2.1 mL/min per 100 mL tissue (P < 0.05), respectively. Sarpogrelate-induced augmentation of FBF and LBF responses to RH was maintained at 24 weeks. No change was observed in the control group at each follow-up time point. The changes in FBF and LBF after sublingual NTG were similar during follow-up periods in the 2 groups. These findings suggest that long-term oral administration of sarpogrelate improves vascular function in patients with PAD.