Jansson R, Lindström B, Dahlberg P A
Clin Pharmacokinet. 1985 Sep-Oct;10(5):443-50. doi: 10.2165/00003088-198510050-00006.
The pharmacokinetics of methimazole following therapeutic doses were studied in healthy subjects, in thyrotoxic and hypothyroid patients before and after treatment to euthyroidism, and in patients with renal or hepatic insufficiency, using a highly sensitive gas chromatographic-mass spectrometric assay. Following intravenous administration of 10mg to healthy subjects, methimazole had an initial distribution half-life (t1/2 alpha) of 0.10 to 0.23 hours and an elimination half-life (t1/2 beta) of 4.9 to 5.7 hours. The absolute bioavailability after oral administration of 10mg methimazole in the fasting state was high, with a mean of 93%. The pharmacokinetic profiles showed small interindividual variations, although one of the hypothyroid patients had a rapid elimination half-life, in both the hypothyroid and euthyroid state (2.6 and 2.4 hours, respectively). The elimination rate was not enhanced in the thyrotoxic patients but was slightly prolonged in the hypothyroid patients. There was no influence of renal insufficiency, but a prolonged elimination half-life was observed in patients with hepatic failure, the prolongation being proportional to the degree of impairment. Thus, the pharmacokinetics of methimazole are relatively simple with small interindividual variations. In general, there are no pharmacokinetic reasons to adjust dosage in the treatment of thyrotoxicosis, except in the rare case of concomitant advanced hepatic insufficiency.
采用高灵敏度气相色谱 - 质谱分析法，在健康受试者、甲状腺毒症患者以及甲状腺功能减退患者治疗前、治疗至甲状腺功能正常后，还有肾功能或肝功能不全患者中，研究了治疗剂量甲巯咪唑的药代动力学。给健康受试者静脉注射10mg甲巯咪唑后，其初始分布半衰期（t1/2α）为0.10至0.23小时，消除半衰期（t1/2β）为4.9至5.7小时。空腹状态下口服10mg甲巯咪唑后的绝对生物利用度较高，平均为93%。药代动力学曲线显示个体间差异较小，尽管有一名甲状腺功能减退患者在甲状腺功能减退和甲状腺功能正常状态下的消除半衰期均较快（分别为2.6小时和2.4小时）。甲状腺毒症患者的消除速率未加快，但甲状腺功能减退患者的消除半衰期略有延长。肾功能不全对其无影响，但肝功能衰竭患者的消除半衰期延长，且延长程度与损害程度成正比。因此，甲巯咪唑的药代动力学相对简单，个体间差异较小。一般来说，除了罕见的伴有晚期肝功能不全的情况外，在治疗甲状腺毒症时没有药代动力学方面的理由调整剂量。
