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口服避孕药对甲泼尼龙药代动力学和药效学的影响。

Oral contraceptive effects on methylprednisolone pharmacokinetics and pharmacodynamics.

作者信息

Slayter K L, Ludwig E A, Lew K H, Middleton E, Ferry J J, Jusko W J

机构信息

Department of Pharmaceutics, State University of New York at Buffalo, NY 14260, USA.

出版信息

Clin Pharmacol Ther. 1996 Mar;59(3):312-21. doi: 10.1016/S0009-9236(96)80009-9.

Abstract

OBJECTIVE

Oral contraceptive (OC) steroids alter the disposition of numerous drugs, including corticosteroids. We investigated the pharmacokinetics and pharmacodynamics of methylprednisolone.

METHODS

Twelve women (six women used OC steroids and six women did not) received intravenous methylprednisolone (0.6 mg/kg ideal body weight). Methylprednisolone disposition was assessed from plasma concentrations. Pharmacodynamic parameters measured were plasma cortisol, whole blood histamine (reflecting basophils), and blood helper T lymphocytes.

RESULTS

Methylprednisolone clearance was significantly decreased in the women who used OC steroids (0.298 versus 0.447 L/hr/kg), resulting in a longer elimination half-life (2.20 versus 1.72 hours). With use of indirect response models, significant differences were observed with the cortisol and basophil responses. A larger value for the concentration that inhibits the zero-order production rate by 50% (0.37 versus 0.11 ng/ml) was observed in the women who used OC steroids for suppression of cortisol secretion, indicating less sensitivity to the suppressive effects of methylprednisolone. Greater net suppression of basophils was observed in the users of OC steroids (area under the response curve, 694 versus 401 ng x hr/ml). No differences were observed for helper T-cell responses.

CONCLUSION

OC steroids appear to inhibit methylprednisolone metabolism. However, mixed changes in several responses occur, indicating that women can probably receive similar doses of methylprednisolone irrespective of OC steroid use.

摘要

目的

口服避孕药(OC)类固醇会改变多种药物的处置情况,包括皮质类固醇。我们研究了甲泼尼龙的药代动力学和药效学。

方法

12名女性(6名使用OC类固醇,6名未使用)接受静脉注射甲泼尼龙(0.6mg/kg理想体重)。通过血浆浓度评估甲泼尼龙的处置情况。测量的药效学参数包括血浆皮质醇、全血组胺(反映嗜碱性粒细胞)和血液辅助性T淋巴细胞。

结果

使用OC类固醇的女性中甲泼尼龙清除率显著降低(0.298对0.447L/小时/千克),导致消除半衰期延长(2.20对1.72小时)。使用间接反应模型时,观察到皮质醇和嗜碱性粒细胞反应存在显著差异。在使用OC类固醇抑制皮质醇分泌的女性中,观察到抑制零级生成率50%的浓度值更大(0.37对0.11ng/ml),表明对甲泼尼龙的抑制作用敏感性较低。在使用OC类固醇的女性中观察到对嗜碱性粒细胞的净抑制作用更大(反应曲线下面积,694对401ng×小时/ml)。辅助性T细胞反应未观察到差异。

结论

OC类固醇似乎抑制甲泼尼龙代谢。然而,几种反应出现混合变化,表明无论是否使用OC类固醇,女性可能都能接受相似剂量的甲泼尼龙。

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