Kamal Mohamed A, Jusko William J
Department of Pharmaceutical Sciences, School of Pharmacy and Pharmaceutical Sciences, University at Buffalo, NY 14260, USA.
J Clin Pharmacol. 2004 Sep;44(9):1034-45. doi: 10.1177/0091270004267808.
Systemic lupus erythematosus is an autoimmune disease primarily affecting women. Currently, systemic lupus erythematosus therapy is suboptimal due to adverse effects of immunosuppressants, particularly corticosteroids. This study determines the single effects of prednisolone, dehydroepiandrosterone, bromocriptine, tamoxifen, mycophenolic acid, 2-chloro-2'-deoxyadenosine, azathioprine, and chloroquine on lectin-stimulated proliferation of human T lymphocytes, as well as determining whether there are interactions in the joint effects of prednisolone and these agents. The T lymphocytes from the whole blood of 10 middle-aged women were stimulated by phytohemagglutinin and cultured with varying drug concentrations. The Hill function was used to evaluate single-drug response data. Isobolograms were constructed to qualitatively analyze interactions. Parametric analysis based on competitive and noncompetitive interaction models was further applied to quantify the joint interactions and predict steroid-sparing potential. The surface interaction parameter (psi) estimated from parametric analysis was in concordance with isobolographic inspection for all interactions studied. All interactions favored the noncompetitive model. Results suggest that dehydroepiandrosterone is additive in its effect with prednisolone, whereas tamoxifen interacts synergistically, both providing steroid-sparing effects. Novel immuno-suppressants such as mycophenolic acid may still provide added pharmacologic benefit during therapy despite a slight antagonistic interaction with prednisolone. These studies help rationalize actual or potential use of other drugs with prednisolone in the treatment of systemic lupus erythematosus.
系统性红斑狼疮是一种主要影响女性的自身免疫性疾病。目前,由于免疫抑制剂尤其是皮质类固醇的不良反应,系统性红斑狼疮的治疗效果并不理想。本研究确定了泼尼松龙、脱氢表雄酮、溴隐亭、他莫昔芬、霉酚酸、2-氯-2'-脱氧腺苷、硫唑嘌呤和氯喹对凝集素刺激的人T淋巴细胞增殖的单一作用,以及确定泼尼松龙与这些药物联合作用时是否存在相互作用。用植物血凝素刺激10名中年女性全血中的T淋巴细胞,并在不同药物浓度下进行培养。采用希尔函数评估单药反应数据。构建等效线图以定性分析相互作用。进一步应用基于竞争性和非竞争性相互作用模型的参数分析来量化联合相互作用并预测激素节省潜力。从参数分析估计的表面相互作用参数(psi)与所有研究相互作用的等效线图检查结果一致。所有相互作用均支持非竞争性模型。结果表明,脱氢表雄酮与泼尼松龙的作用具有相加性,而他莫昔芬具有协同相互作用,两者均具有激素节省作用。新型免疫抑制剂如霉酚酸尽管与泼尼松龙有轻微的拮抗相互作用,但在治疗期间仍可能提供额外的药理益处。这些研究有助于使泼尼松龙与其他药物在系统性红斑狼疮治疗中的实际或潜在用途更加合理。