PHARMACO KINETICS AND EFFECTS OF PROPRANOLOL IN TERMINAL UREMIC PATIENTS AND IN PATIENTS UNDERGOING REGULAR DIALYSIS TREATMENT
PHARMACO KINETICS AND EFFECTS OF PROPRANOLOL IN TERMINAL UREMIC PATIENTS AND IN PATIENTS UNDERGOING REGULAR DIALYSIS TREATMENT
复制标题
DOI：
10.2165/00003088-197601050-00004
复制
发表时间：
1976-01-01
影响因子：
4.5
通讯作者：
ET AL
中科院分区：
文献类型：
--
作者：
BIANCHETTI G;GRAZIANI G;ET AL
在慢性肾功能衰竭患者、接受常规透析治疗的患者和健康志愿者中，单次口服40 mg普萘洛尔后，测定其血液和血浆水平。在所有病例中均在1.5-3 h内观察到峰值水平。在慢性肾衰竭组中，普萘洛尔的血液和血浆峰浓度高2- 3倍（161 . ±. 41 ng/ml）比在透析患者中观察到的那些（47 . ±. 9 ng/ml）和健康志愿者（26 . ±. 1 ng/ml）。慢性肾功能衰竭患者的表观血浆清除率也显著降低。慢性肾功能衰竭患者建议减少肝脏提取。还发现，与透析后当天相比，在透析当天，常规透析患者的体循环可用剂量分数显著增加，表观血浆半衰期和分布容积也发生变化。未观察到透析器浸提普萘洛尔。在普萘洛尔连续治疗后定期透析的患者中也观察到普萘洛尔血药浓度的显著波动。普萘洛尔对血浆肾素活性的抑制作用与药物的消肿作用不完全相关。普萘洛尔应谨慎使用，在慢性肾功能衰竭低剂量。
Propranolol blood and plasma levels were measured after a single oral dose of 40 mg in patients with chronic renal failure, in patients undergoing regular dialysis treatment and in healthy volunteers. Peak levels were observed in all cases within 1.5-3 h. Peak blood and plasma concentrations of propranolol in the chronic renal failure group were 2- to 3-fold higher (161 .+-. 41 ng/ml) than those observed in the dialysis patients (47 .+-. 9 ng/ml) and in the healthy volunteers (26 .+-. 1 ng/ml). The apparent plasma clearance was also significantly reduced in the patients with chronic renal failure. A reduced hepatic extraction is suggested in chronic renal failure patients. A significant increase in the fraction of the dose available to the systemic circulation was also found, together with a modification of apparent plasma half-life and volume of distribution in regular dialysis patients during the dialysis day as compared with the after-dialysis day. No extraction of propranolol by the dialyzer was noticed. Marked fluctuations in propranolol blood concentrations were also observed in patients on regular dialysis following continuous propranolol treatment. The suppressive effect of propranolol on plasma renin activity did not fully correlate with the hypotensive effect of the drug. Propranolol should be used with great caution and at low doses in chronic renal failure.