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盐酸沙格雷酯,一种选择性5-HT2A拮抗剂,可改善外周动脉疾病患者的血管功能。

Sarpogrelate hydrochloride, a selective 5-HT2A antagonist, improves vascular function in patients with peripheral arterial disease.

作者信息

Miyazaki Masanori, Higashi Yukihito, Goto Chikara, Chayama Kazuaki, Yoshizumi Masao, Sanada Hiroaki, Orihashi Kazumasa, Sueda Taijiro

机构信息

Department of Surgery, Hiroshima University Graduate School of Biomedical Sciences, Hiroshima, Japan.

出版信息

J Cardiovasc Pharmacol. 2007 Apr;49(4):221-7. doi: 10.1097/FJC.0b013e3180325af3.

DOI:10.1097/FJC.0b013e3180325af3
PMID:17438407
Abstract

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.

摘要

外周动脉疾病(PAD)是动脉粥样硬化的主要表现之一。PAD与内皮功能障碍相关。盐酸沙格雷酯是一种选择性5-HT2A拮抗剂,已被广泛用作抗血小板药物治疗PAD。关于PAD患者开始使用沙格雷酯治疗后内皮功能是否改善尚无相关信息。本研究的目的是评估沙格雷酯对PAD患者内皮功能的影响。我们将PAD患者分为两组:一组患者每天口服100 mg沙格雷酯,每日3次,持续12周(沙格雷酯组,n = 10);另一组患者继续接受常规治疗(对照组,n = 11)。使用应变片体积描记法测量前臂血流量(FBF)和腿部血流量(LBF)对反应性充血(RH)和舌下含服硝酸甘油(NTG)后的反应。沙格雷酯给药12周后,RH期间的FBF和LBF反应显著增加,分别从每100 mL组织13.2±1.7 mL/min增加到18.1±2.2 mL/min(P < 0.01)和从每100 mL组织8.2±0.9 mL/min增加到14.2±2.1 mL/min(P < 0.05)。沙格雷酯引起的FBF和LBF对RH反应的增强在24周时得以维持。对照组在每个随访时间点均未观察到变化。两组随访期间舌下含服NTG后FBF和LBF的变化相似。这些发现表明,长期口服沙格雷酯可改善PAD患者的血管功能。

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