Campbell B C, Shepherd A N, Reid J L
Br J Clin Pharmacol. 1982 Feb;13(2):213-7. doi: 10.1111/j.1365-2125.1982.tb01359.x.
1 The effects of the orally active angiotensin converting enzyme inhibitor, captopril, were examined in 15 patients with mild or moderate essential hypertension. 2 Following initial dosing with captopril 25 mg, there was a significant fall in supine and erect blood pressure in 2 h and lasting for 6 h. There was no significant alteration of heart rate. No reduction was seen in plasma noradrenaline concentration. Maximum inhibition of plasma converting enzyme activity occurred 60 min post-dosing. 3 There was a strong positive correlation between blood pressure reduction and converting enzyme inhibition. The magnitude of the blood pressure reduction and converting enzyme inhibition following initial dosing was reflected in subsequent success with captopril monotherapy during a 12 week follow-up period. 4 It was also found that patients who did not achieve adequate blood pressure control on captopril in doses of 50 mg three times daily or less still were not controlled on a dose of 150 mg three times daily without the addition of a diuretic. 5 The risks of renal and marrow toxicity from captopril may be reduced by administering only low doses with the addition, where necessary, of a thiazide diuretic.
对15例轻度或中度原发性高血压患者进行了口服活性血管紧张素转换酶抑制剂卡托普利的效果研究。
初始给予卡托普利25毫克后,仰卧位和直立位血压在2小时内显著下降,并持续6小时。心率无明显变化。血浆去甲肾上腺素浓度未见降低。给药后60分钟出现血浆转换酶活性的最大抑制。
血压降低与转换酶抑制之间存在强正相关。初始给药后血压降低和转换酶抑制的程度反映在随后12周随访期内卡托普利单药治疗的成功情况。
还发现,每日三次服用50毫克或更低剂量卡托普利未能实现充分血压控制的患者,在不添加利尿剂的情况下,每日三次服用150毫克剂量时仍未得到控制。
通过仅给予低剂量卡托普利,并在必要时添加噻嗪类利尿剂,可降低卡托普利导致肾毒性和骨髓毒性的风险。