Geffner D L, Sladek J, Hershman J M
Endocrine Section, Wadsworth Veterans Administration Medical Center, Los Angeles, CA 90073.
Drugs Exp Clin Res. 1990;16(4):167-73.
The pharmacokinetics of atenolol and the effect of the drug on the clinical and laboratory features of hyperthyroidism were studied in 23 patients with hyperthyroidism. In the hyperthyroid state, the time to peak plasma concentration (Tmax) occurred significantly earlier, the elimination half-life was significantly shorter, and the areas under the curve were also significantly less compared to the euthyroid state, but there was no significant difference in peak plasma concentrations (Cmax) between these states. Administration of atenolol once daily resulted in marked clinical improvement in 2 to 4 weeks. The clinical index of thyrotoxic symptoms and signs decreased from 23.2 +/- 10.8 to 8.4 +/- 5.3 (p less than 0.005). Pulse similarly decreased significantly from 93.9 +/- 15.7 to 77.8 +/- 10.5. In contrast to the marked clinical improvement, there was no change in any of the serum concentrations of thyroid hormones T4, free T4, T3 and free T3 at the time of maximal clinical effect compared to pretreatment values. These data show that the beneficial effect of atenolol in hyperthyroidism is not due to changes in thyroid hormone metabolism.
对23例甲状腺功能亢进患者研究了阿替洛尔的药代动力学及其对甲状腺功能亢进临床和实验室特征的影响。与甲状腺功能正常状态相比，在甲状腺功能亢进状态下，血浆浓度达峰时间（Tmax）显著提前，消除半衰期显著缩短，曲线下面积也显著减小，但这些状态下的血浆峰浓度（Cmax）无显著差异。每日一次给予阿替洛尔，2至4周后临床症状明显改善。甲状腺毒症症状和体征的临床指数从23.2±10.8降至8.4±5.3（p<0.005）。脉搏同样从93.9±15.7显著降至77.8±10.5。与显著的临床改善形成对比的是，在达到最大临床疗效时，与治疗前值相比，甲状腺激素T4、游离T4、T3和游离T3的血清浓度均无变化。这些数据表明，阿替洛尔对甲状腺功能亢进的有益作用并非由于甲状腺激素代谢的改变。
