Säkö S, Sotaniemi E A, Anttila M
Eur J Drug Metab Pharmacokinet. 1986 Apr-Jun;11(2):81-6. doi: 10.1007/BF03189831.
The role of liver drug metabolism on blood pressure (BP) response to a lipophilic (propranolol) and hydrophilic (sotalol) beta blocker in thirty hypertensive patients was studied. Ten patient treated with diuretics were classified according to plasma antipyrine clearance rate as rapid and slow metabolizers. They were first treated for one month with propranolol and then for one month with sotalol at equivalent dosage. Four patients, classified as rapid drug metabolizers had a better response to sotalol, 139 (SD 13)/92 (SD 6) mmHg, than to propranolol, 164 (21)/104 (10) mmHg. For the other six patients, with slow drug metabolism, the response to propranolol, 142 (8)/95 (8) mmHg was equal to sotalol, 143 (19)/93 (8) mmHg. Twenty patients were randomly divided into two groups. The patients in these groups were similar as to sex, age, body mass index, BP and rate of drug metabolism. The subjects in the first group were treated with propranolol and diuretic and those in the second with sotalol and diuretic. The BP response was equal in both groups, propranolol 147 (14)/96 (7) mmHg and sotalol 143 (12)/95 (9) mmHg after two years' follow-up. The rate of drug metabolism must be considered when evaluating response to lipophilic but not to hydrophilic beta blocker.
研究了肝脏药物代谢对30例高血压患者血压(BP)对亲脂性(普萘洛尔)和亲水性(索他洛尔)β受体阻滞剂反应的作用。10例接受利尿剂治疗的患者根据血浆安替比林清除率分为快速代谢者和缓慢代谢者。他们首先接受普萘洛尔治疗1个月,然后接受等效剂量的索他洛尔治疗1个月。4例被归类为快速药物代谢者对索他洛尔的反应更好,为139(标准差13)/92(标准差6)mmHg,而对普萘洛尔的反应为164(21)/104(10)mmHg。对于其他6例药物代谢缓慢的患者,对普萘洛尔的反应为142(8)/95(8)mmHg,与索他洛尔的反应143(19)/93(8)mmHg相当。20例患者被随机分为两组。这些组中的患者在性别、年龄、体重指数、血压和药物代谢率方面相似。第一组患者接受普萘洛尔和利尿剂治疗,第二组患者接受索他洛尔和利尿剂治疗。两年随访后,两组的血压反应相当,普萘洛尔为147(14)/96(7)mmHg,索他洛尔为143(12)/95(9)mmHg。在评估对亲脂性β受体阻滞剂而非亲水性β受体阻滞剂的反应时,必须考虑药物代谢率。