Lebel M, Grose J H, Lacourcière Y
L'Hôtel-Dieu de Québec, Canada.
Am J Hypertens. 1991 Sep;4(9):740-4. doi: 10.1093/ajh/4.9.740.
Cromakalim, a novel potassium channel-activating drug, was administered for a 3-day period in eight untreated hospitalized patients with established hypertension. The fixed and single dose of 1.5 mg/day produced a significant reduction in systolic and diastolic blood pressure with a small increase in heart rate. Glomerular filtration rate was unchanged and effective renal plasma flow was slightly increased with a concomitant small decrease in filtration fraction and in renal vascular resistance. No significant change was observed in urinary prostaglandin (PG)E2, PGF2 alpha, and thromboxane B2, while 6-keto-PGF1 alpha (the stable metabolite of prostacyclin) rose from 189 +/- 6 to 368 +/- 115 ng/day. The renal excretion of 6-keto-PGF1 alpha correlates with the modification observed in renal plasma flow, suggesting a compensatory role for prostacylin in preserving renal hemodynamics during antihypertensive therapy with cromakalim.
新型钾通道激活药物克罗卡林，对8例未经治疗的高血压住院患者进行了为期3天的给药。固定单剂量为1.5毫克/天，可显著降低收缩压和舒张压，心率略有增加。肾小球滤过率未变，有效肾血浆流量略有增加，同时滤过分数和肾血管阻力略有下降。尿前列腺素（PG）E2、PGF2α和血栓素B2未见明显变化，而6-酮-PGF1α（前列环素的稳定代谢产物）从189±6纳克/天升至368±115纳克/天。6-酮-PGF1α的肾排泄与肾血浆流量的变化相关，提示前列环素在克罗卡林降压治疗期间维持肾血流动力学方面具有代偿作用。
