Andriulli A, Arrigoni A, Gindro T, Karbowiak I, Buzzetti G, Armanini D
Divisione di Gastroenterologia, Ospedale San Giovanni Battista Molinette, Torino, Italia.
Digestion. 1989;44(3):155-62. doi: 10.1159/000199905.
Plasma levels of canrenone and androgen receptor-active materials (ARM) were determined during long-term oral K-canrenoate or spironolactone therapy in cirrhotics with chronic recurrent ascites. Mean plasma canrenone level was approximately 3 times higher under K-canrenoate than under spironolactone treatment; moreover, the levels were not dose related. Either type of treatment did not affect plasma aldosterone and testosterone concentrations. Plasma ARM during K-canrenoate treatment did not change, whereas in the spironolactone group a 3-fold increase of ARM occurred (p less than 0.05). No dose-related effect was evident with the latter treatment. The lower incidence of gynecomastia in the K-canrenoate group was not correlated with values of plasma canrenone or ARM (p greater than 0.05). Our study questions the traditional view that the mode of action of spironolactone is via its metabolite canrenone. The two antialdosterone drugs, although equally effective in clearing ascites from cirrhotics, appear to act through partially different metabolites. The lower incidence of antiandrogenic or estrogen-like side effects during K-canrenoate seems to be related to metabolites other than canrenone itself.
在对患有慢性复发性腹水的肝硬化患者进行长期口服钾坎利酸钾或螺内酯治疗期间，测定了血浆中坎利酮以及雄激素受体活性物质（ARM）的水平。在钾坎利酸钾治疗下，血浆坎利酮平均水平约为螺内酯治疗下的3倍；此外，这些水平与剂量无关。两种治疗方式均未影响血浆醛固酮和睾酮浓度。在钾坎利酸钾治疗期间，血浆ARM未发生变化，而在螺内酯组中，ARM出现了3倍的升高（p小于0.05）。后一种治疗方式未显示出明显的剂量相关效应。钾坎利酸钾组中男性乳房发育发生率较低与血浆坎利酮或ARM值无关（p大于0.05）。我们的研究对传统观点即螺内酯的作用方式是通过其代谢产物坎利酮提出了质疑。这两种抗醛固酮药物虽然在清除肝硬化患者腹水方面同样有效，但似乎是通过部分不同的代谢产物起作用。钾坎利酸钾治疗期间抗雄激素或雌激素样副作用发生率较低似乎与坎利酮本身以外的代谢产物有关。
