普萘洛尔对人体扑热息痛代谢的影响。
The effect of propranolol on paracetamol metabolism in man.
作者信息
Baraka O Z, Truman C A, Ford J M, Roberts C J
机构信息
Department of Medicine, Bristol Royal Infirmary.
出版信息
Br J Clin Pharmacol. 1990 Feb;29(2):261-4. doi: 10.1111/j.1365-2125.1990.tb03631.x.
Ten healthy volunteers were treated for 4 days with 160 mg propranolol HCl and placebo in random order. At the end of each treatment salivary antipyrine kinetics and the plasma kinetics and urinary excretion of paracetamol and its major metabolites were measured following a 1500 mg oral dose. Propranolol prolonged the half-life of antipyrine by 11 +/- 5% (mean +/- s.e. mean) and lowered its clearance by 14 +/- 3% (P less than 0.05). Propranolol increased the half-life of paracetamol by 25 +/- 12% (P less than 0.05) and lowered its clearance by 14 +/- 3% (P less than 0.05). Propranolol decreased the partial clearance of paracetamol to its cysteine and mercapturate derivatives by 16 +/- 3% (P less than 0.05) and 32 +/- 7% (P less than 0.05), respectively. The partial clearance to the glucuronide conjugate was decreased by 27 +/- 6% (P less than 0.05), whereas that to sulphate was not changed significantly. Propranolol inhibits paracetamol metabolism predominantly through inhibition of the oxidation and glucuronidation pathways.
10名健康志愿者以随机顺序接受了4天的治疗，分别给予160mg盐酸普萘洛尔和安慰剂。在每次治疗结束时，口服1500mg扑热息痛后，测量唾液中安替比林动力学、血浆动力学以及扑热息痛及其主要代谢产物的尿排泄情况。普萘洛尔使安替比林的半衰期延长了11±5%（平均值±标准误平均值），清除率降低了14±3%（P<0.05）。普萘洛尔使扑热息痛的半衰期延长了25±12%（P<0.05），清除率降低了14±3%（P<0.05）。普萘洛尔使扑热息痛向其半胱氨酸和巯基尿酸衍生物的部分清除率分别降低了16±3%（P<0.05）和32±7%（P<0.05）。向葡萄糖醛酸结合物的部分清除率降低了27±6%（P<0.05），而向硫酸盐的部分清除率无显著变化。普萘洛尔主要通过抑制氧化和葡萄糖醛酸化途径来抑制扑热息痛的代谢。
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