Legler U F
Department of Endocrinology, University of Tuebingen, West Germany.
J Clin Endocrinol Metab. 1988 Jan;66(1):221-3. doi: 10.1210/jcem-66-1-221.
This study was undertaken to determine the effect of methimazole on the pharmacokinetics of iv prednisolone in patients with Graves' disease. Twenty women were studied, including eight with severe infiltrative ophthalmopathy who had taken methimazole and T4 for at least 4 months, six with severe infiltrative ophthalmopathy who had undergone subtotal thyroidectomy and, therefore, required no antithyroid treatment, and six age-matched normal women. All were euthyroid. Each women received 0.54 mg/kg prednisolone as an iv bolus dose. Plasma total and unbound prednisolone concentrations were measured at multiple times during a 10-h study period by high pressure liquid chromatography and equilibrium dialysis. The clearance of both total and unbound prednisolone was increased significantly in the women receiving methimazole therapy compared to values in both control groups. The volume of distribution at steady state was similar in all groups. These results suggest that patients receiving methimazole have enhanced prednisolone metabolism and, therefore, they may require higher prednisolone doses.
本研究旨在确定甲巯咪唑对格雷夫斯病患者静脉注射泼尼松龙药代动力学的影响。研究了20名女性，其中8名患有严重浸润性眼病，已服用甲巯咪唑和甲状腺素至少4个月；6名患有严重浸润性眼病，已接受甲状腺次全切除术，因此无需抗甲状腺治疗；以及6名年龄匹配的正常女性。所有患者甲状腺功能均正常。每位女性接受0.54mg/kg泼尼松龙静脉推注剂量。在10小时的研究期间，通过高压液相色谱法和平衡透析法多次测量血浆总泼尼松龙和游离泼尼松龙浓度。与两个对照组的值相比，接受甲巯咪唑治疗的女性中总泼尼松龙和游离泼尼松龙的清除率均显著增加。所有组的稳态分布容积相似。这些结果表明，接受甲巯咪唑治疗的患者泼尼松龙代谢增强，因此可能需要更高剂量的泼尼松龙。
