Divoll M, Abernethy D R, Ameer B, Greenblatt D J
Clin Pharmacol Ther. 1982 Feb;31(2):151-6. doi: 10.1038/clpt.1982.24.
Thirty-two healthy men and women, 23 to 78 yr old, received single 650-mg intravenous doses of acetaminophen and the drug's kinetics were determined from multiple plasma samples drawn over the next 8 to 12 hr. Acetaminophen elimination half-life averaged 2.7 hr (range, 1.9 to 4.3 hr) and was not related to age or sex. Volume of distribution (corrected for weight) was larger in men than in women (0.99 and 0.86 l/kg) and declined with age in both sexes. This probably reflects increased fat per kilogram body weight in women and in the elderly, together with incomplete distribution of this nonlipophilic drug into body fat. Acetaminophen clearance tended to decline with age in both sexes, but differences were of borderline significance. On the basis of kinetics data alone, adjustment of acetaminophen dosage for the elderly is generally not necessary.
32名年龄在23至78岁之间的健康男性和女性接受了单次650毫克对乙酰氨基酚静脉注射剂量,然后在接下来的8至12小时内从多个血浆样本中测定该药物的动力学。对乙酰氨基酚的消除半衰期平均为2.7小时(范围为1.9至4.3小时),与年龄或性别无关。分布容积(校正体重后)男性大于女性(分别为0.99和0.86升/千克),且在两性中均随年龄下降。这可能反映出女性和老年人每千克体重的脂肪增加,以及这种非亲脂性药物在体内脂肪中的分布不完全。对乙酰氨基酚的清除率在两性中均倾向于随年龄下降,但差异具有临界显著性。仅根据动力学数据,一般无需为老年人调整对乙酰氨基酚的剂量。