Homeida M M, Ali H M, Arbab B M, Harron D W
Department of Medicine, University of Khartoum, Sudan.
Br J Clin Pharmacol. 1987 Sep;24(3):393-6. doi: 10.1111/j.1365-2125.1987.tb03187.x.
Eight Sudanese patients with hepatosplenic schistosomiasis and seven Sudanese controls were administered a single oral dose of long acting (LA), propranolol 160 mg; blood propranolol levels were measured at regular intervals for 12 h using g.l.c. In patients with hepatosplenic schistosomiasis, propranolol blood concentrations were greater (P less than 0.05) at all time intervals, Cmax 63.5 (29-143) ng ml-1 (median and range) than controls Cmax 23 (12-37) ng ml-1. Median AUC0-12 was also greater (P less than 0.05) (533 and 218 ng ml-1 h respectively), tmax were not significantly different. In patients and controls prior to treatment, standing heart rate (77.5 (60-110), 72 (68-74) beats min-1) systolic (120 (105-150), 110 (100-120) mm Hg) and diastolic blood pressure (75 (60-90), 70 (60-80) mm Hg) were not significantly different. However following propranolol administration a reduction (P less than 0.05) occurred in both systolic (median 20 mm Hg) and diastolic (median 12.5 mm Hg) blood pressure in the patients compared with controls. Heart rate was reduced by a median of 10 beats min-1 in both groups. These observations indicate that propranolol bioavailability in patients with hepatosplenic schistosomiasis is increased possibly due to reduced presystemic extraction.
对8例患有肝脾血吸虫病的苏丹患者和7名苏丹对照者单次口服160mg长效普萘洛尔;使用气相色谱法在12小时内定期测量血中普萘洛尔水平。在患有肝脾血吸虫病的患者中,在所有时间间隔内,普萘洛尔血药浓度均更高(P<0.05),Cmax为63.5(29 - 143)ng/ml(中位数和范围),而对照者的Cmax为23(12 - 37)ng/ml。中位数AUC0 - 12也更高(P<0.05)(分别为533和218 ng/ml·h),tmax无显著差异。在治疗前,患者和对照者的静息心率(77.5(60 - 110),72(68 - 74)次/分钟)、收缩压(120(105 - 150),110(100 - 120)mmHg)和舒张压(75(60 - 90),70(60 - 80)mmHg)无显著差异。然而,与对照者相比,服用普萘洛尔后患者的收缩压(中位数20mmHg)和舒张压(中位数12.5mmHg)均出现降低(P<0.05)。两组的心率中位数均降低了10次/分钟。这些观察结果表明,肝脾血吸虫病患者中普萘洛尔的生物利用度增加,可能是由于首过消除减少所致。