Oral sarpogrelate can improve endothelial dysfunction as effectively as oral cilostazol, with fewer headaches, in active young male smokers

Abstract

Sarpogrelate and cilostazol are two commonly used adjunctive antiplatelet agents that also can be used to improve endothelial dysfunction. We compared the effects of sarpogrelate and cilostazol on endothelial dysfunction in active male smokers with flow-mediated dilatation (FMD). We enrolled and compared baseline and follow-up FMD in 20 young male smokers without any known cardiovascular diseases. Two participants who were initially medicated with cilostazol dropped out because of severe headache after taking medication. However, they continued the other experiment with sarpogrelate medication. Baseline endothelium-dependent dilatation (EDD) after reactive hyperemia was 7.5 % ± 1.9 % and endothelium-independent dilatation (EID) after sublingual administration of nitroglycerin was 13.3 % ± 3.4 %. After a 2-week treatment of cilostazol, follow-up EDD significantly increased (7.7 % ± 1.9 to 8.8 ± 2.0 %, P = 0.016), but follow-up EID changed insignificantly (13.2 % ± 3.5 to 12.5 % ± 3.9 %, P = 0.350). With the sarpogrelate treatment, follow-up EDD was significantly increased (7.4 % ± 1.9 % to 8.8 % ± 1.9 %, P = 0.021), but follow-up EID was similar (13.5 % ± 3.5 to 14.0 % ± 3.2 %, P = 0.427). There was no clinical significance between the two groups on follow-up EDD and EID (P = 0.984 and 0.212, respectively). However, the mean score of intensity of headache was significantly higher in the cilostazol group than in the sarpogrelate group (3.8 % ± 2.5 % vs 1.4 % ± 2.2 %, P = 0.005). EDD showed a similar significant increase with 2-week treatment of cilostazol and sarpogrelate. However, intensity of headaches was significantly higher in the cilostazol group.

Multiple-Dose Study to Evaluate Pharmacokinetics, Pharmacodynamics, and Safety in Healthy Subjects: A Comparison of Controlled-Release Sarpogrelate and Immediate-Release Sarpogrelate

“…Sarpogrelate is also effective in improving ischemic symptoms such as ulcers, cold feeling in the limbs, and sharp pains, without causing headache and facial flushing, which are common adverse events (AEs) in other antiplatelet agents [11,12] .…”

The Effect of Cilostazol on Endothelial Function as Assessed by Flow-Mediated Dilation in Patients with Coronary Artery Disease

“…Three reports 16–18) investigating younger smokers found that 2 weeks of cilostazol treatment resulted in FMD improvement. These studies 16–18) indicated that younger smokers are more likely to respond to cilostazol treatment.…”

“…Three reports 16–18) investigating younger smokers found that 2 weeks of cilostazol treatment resulted in FMD improvement. These studies 16–18) indicated that younger smokers are more likely to respond to cilostazol treatment. One report 19) examined patients with silent cerebral lacunar infarction and hypercholesterolemia who received a combination of probucol and cilostazol for four weeks, and found that treatment resulted in FMD improvement.…”

Effect of sarpogrelate treatment on the prognosis after endovascular therapy for critical limb ischemia

“…Sarpogrelate is a 5-HT 2 antagonist and is now clinically approved for symptomatic PAD in Japan. Although its mechanisms of action are not yet fully understood, previous reports showed that sarpogrelate reduces platelet aggregation [19, 20], improves endothelial function [21, 22], and enhances peripheral circulation [23, 24]. In addition, some clinical trials have demonstrated its favorable effects on cardiovascular diseases [25] and skin ulcers [26], as well as intermittent claudication [27].…”