Kempin S J, Jackson C W, Edwards C C
Antimicrob Agents Chemother. 1977 Oct;12(4):451-4. doi: 10.1128/AAC.12.4.451.
Pentamidine isethionate is a trypanocidal drug used for the treatment of Pneumocystis carinii pneumonitis. Hematological complications have occasionally been reported and include anemia, leukopenia, and thrombocytopenia. We report here several qualitative abnormalities of in vitro platelet function and coagulation that have not been described previously. Platelets were exposed in vitro to concentrations of pentamidine isethionate ranging from 0.5 to 100 mug/ml of platelet-rich plasma. Clot retraction, platelet adhesiveness to glass beads, and platelet aggregation (adenosine 5'-diphosphate [ADP], thrombin, epinephrine, collagen, and ristocetin) were inhibited in a dose-dependent fashion. The addition of pentamidine isethionate after aggregation had been initiated with ADP reversed both primary and, to a lesser degree, secondary aggregation. Platelet factor 3 availability and serotonin uptake and release (using collagen as the releasing agent) were not inhibited. Serotonin release with 10(-4) M ADP was slightly inhibited. Pentamidine isethionate prolonged the thrombin time of plasma at concentrations of 5 mug/ml and greater. The prothrombin time was prolonged at concentrations greater than 10 mug/ml of plasma. The inhibition of aggregation was reversed by washing and resuspension in plasma or by the addition of calcium or magnesium ions.
戊烷脒异硫氰酸盐是一种用于治疗卡氏肺孢子虫肺炎的杀锥虫药物。偶尔有血液学并发症的报道，包括贫血、白细胞减少和血小板减少。我们在此报告了几种以前未描述过的体外血小板功能和凝血的定性异常情况。将血小板在体外暴露于富含血小板血浆中浓度范围为0.5至100微克/毫升的戊烷脒异硫氰酸盐。凝块回缩、血小板对玻璃珠的黏附性以及血小板聚集（腺苷5'-二磷酸[ADP]、凝血酶、肾上腺素、胶原和瑞斯托菌素）均呈剂量依赖性受到抑制。在用ADP引发聚集后加入戊烷脒异硫氰酸盐可逆转初级聚集，并在较小程度上逆转次级聚集。血小板因子3的可用性以及5-羟色胺的摄取和释放（使用胶原作为释放剂）未受到抑制。用10(-4)M ADP诱导的5-羟色胺释放略有抑制。戊烷脒异硫氰酸盐在血浆浓度为5微克/毫升及更高时可延长血浆的凝血酶时间。在血浆浓度大于10微克/毫升时，凝血酶原时间延长。通过在血浆中洗涤和重悬或加入钙或镁离子可逆转聚集的抑制作用。
