Erbler H C, Wernze H, Hilfenhaus M
Eur J Clin Pharmacol. 1976 Feb 6;9(4):253-7. doi: 10.1007/BF00561657.
Canrenone was administered in doses of 2 x 82 mg and 2 x 164 mg per day over a period of 10 days to diabetic patients without cardiovascular, liver or kidney involvement. Aldosterone excretion and plasma aldosterone increased only slightly during both regimes. There was a clear-cut increase in aldosterone excretion only after discontinuation of canrenone. Excretion of sodium, potassium and fluid was not significantly changed either during or after treatment. The lack of effect of canrenone on the kidney was in contrast to the significant decrease in serum sodium and increase in serum potassium, and the significant, dose-dependent rise in plasma renin activity following canrenone administration. The increased plasma renin activity persisted for some days after discontinuation of canrenone. It is suggested that canrenone primarily exerted its effect in the distal part of the large intestine where ionic movements are most affected by aldosterone. The disproportionately slight increase in plasma aldosterone concentration and aldosterone excretion, in spite of the greatly elevated plasma renin activity and serum potassium level, is considered to be due to a direct inhibitory effect of canrenone on aldosterone production in the adrenals.
对无心血管、肝脏或肾脏病变的糖尿病患者,以每天2×82毫克和2×164毫克的剂量给予坎利酮,持续10天。在两种给药方案期间,醛固酮排泄和血浆醛固酮仅略有增加。仅在停用坎利酮后,醛固酮排泄才有明显增加。治疗期间及治疗后,钠、钾和液体的排泄均无显著变化。坎利酮对肾脏无作用,这与血清钠显著降低、血清钾升高以及坎利酮给药后血浆肾素活性显著的剂量依赖性升高形成对比。停用坎利酮后,血浆肾素活性仍持续升高数天。提示坎利酮主要在大肠远端发挥作用,在该处离子运动受醛固酮影响最大。尽管血浆肾素活性和血清钾水平大幅升高,但血浆醛固酮浓度和醛固酮排泄的增加却不成比例地轻微,这被认为是由于坎利酮对肾上腺醛固酮生成有直接抑制作用。