Ookawara S, Tabei K, Sakurai T, Sakairi Y, Furuya H, Asano Y
Department of Medicine, Jichi Medical School, Tochigi-ken, Japan.
Eur J Clin Pharmacol. 1996;51(2):149-51. doi: 10.1007/s002280050176.
Nafamostat mesilate, a potent protease inhibitor, is widely used for the treatment of pancreatitis, disseminated intravascular coagulation and as an anticoagulant in haemodialysis. However, hyperkalaemia associated with nafamostat mesilate has been reported. It is thought to be due to decreased urinary potassium excretion, of the drug suppression of aldosterone secretion, and a direct inhibitory action on the apical Na+ conductance in collecting ducts. We have seen two cases of nafamostat mesilate associated-hyperkalaemia, which indicated that extrarenal potassium imbalance might play a role in inducing hyperkalaemia.
To examine the effect of nafamostat mesilate on potassium transport in erythrocytes in vitro, 86RbCl uptake was measured in red blood cells from eight healthy volunteers.
Nafamostat mesilate and a metabolite, 6-amidino-2-naphthol, at concentrations of 10(-4) and 10(-3) M, respectively, significantly, suppressed potassium influx whilst another metabolite, p-guanidino-benzoic acid, had no effect. The inhibitory action of nafamostat mesilate was not affected by various inhibitors.
Nafamostat mesilate and its metabolite, 6-amidino-2-naphthol, suppressed potassium influx in erythrocytes by inhibition of a Na-K ATPase dependent pathway, which was not inhibited by amiloride, barium, nor by frusemide (furosemide).
甲磺酸萘莫司他是一种强效蛋白酶抑制剂,广泛用于治疗胰腺炎、弥散性血管内凝血,以及在血液透析中用作抗凝剂。然而,已有报道称甲磺酸萘莫司他会导致高钾血症。其原因被认为是尿钾排泄减少,这是由于该药物抑制醛固酮分泌,以及对集合管顶端钠电导有直接抑制作用。我们遇到了两例与甲磺酸萘莫司他相关的高钾血症病例,这表明肾外钾失衡可能在诱发高钾血症中起作用。
为了在体外研究甲磺酸萘莫司他对红细胞钾转运的影响,我们测量了8名健康志愿者红细胞对86RbCl的摄取。
甲磺酸萘莫司他及其一种代谢产物6-脒基-2-萘酚,浓度分别为10(-4)和10(-3) M时,均显著抑制钾内流,而另一种代谢产物对胍基苯甲酸则无此作用。甲磺酸萘莫司他的抑制作用不受各种抑制剂的影响。
甲磺酸萘莫司他及其代谢产物6-脒基-2-萘酚通过抑制钠钾ATP酶依赖性途径抑制红细胞钾内流,该途径不受阿米洛利、钡或呋塞米(速尿)的抑制。