Calvo R, Carlos R, Erill S
Clin Pharmacol Ther. 1980 Feb;27(2):179-83. doi: 10.1038/clpt.1980.27.
Procaine hydrolysis in vitro has been studied in whole blood, plasma, and washed erythrocytes. Esterase activity was higher in whole blood than in either diluted plasma or resuspended erythrocytes. Eserine and echothiophate specifically inhibited plasma procaine esterase activity, while acetazolamide blocked hydrolysis of procaine by washed erythrocytes. Kinetic studies in whole blood also identified 2 different enzymes. Procaine esterase activity associated with red blood cells was not impaired in patients with renal failure or hepatic cirrhosis, but procaine half-life (t 1/2) in whole blood of normal subjects was longer after 250 mg acetazolamide.
已在全血、血浆和洗涤过的红细胞中对普鲁卡因的体外水解进行了研究。全血中的酯酶活性高于稀释血浆或重悬红细胞中的酯酶活性。毒扁豆碱和依可碘酯特异性抑制血浆普鲁卡因酯酶活性，而乙酰唑胺可阻断洗涤过的红细胞对普鲁卡因的水解。全血中的动力学研究还鉴定出两种不同的酶。肾衰竭或肝硬化患者红细胞相关的普鲁卡因酯酶活性未受损，但在正常受试者全血中，给予250mg乙酰唑胺后，普鲁卡因半衰期（t1/2）延长。
