Wiersinga W M, Fabius A J, Touber J L
Acta Endocrinol (Copenh). 1977 Nov;86(3):522-32. doi: 10.1530/acta.0.0860522.
Studies were undertaken to elucidate whether orphenadrine influences thyroid function. Seven volunteers were given orphenadrine in weekly increasing dosage up to 300 mg per day; in 5 patients chronically treated with 300 mg orphenadrine daily the drug was gradually discontinued. No changes were found in PBI, RT3U, TT3 and TSH during or after orphenadrine medication; also TSH- and TT3-responses to 200 microgram TRH iv were not influenced by the drug. Orphenadrine medication increased serum thyroxine values (P less than 0.001) as measured with the competitive protein binding (CPB) technique, but did not influence serum thyroxine values measured by radioimmunoassay. Orphenadrine added to serum in vitro in the Murphy-Pattee assay did not increase thyroxine values; two out of eight tested metabolites however did. It is concluded that orphenadrine in a dosage up to 300 mg per day does not influence thyroid function. It increases serum thyroxine levels as measured by the competitive protein binding technique of Murphy and Pattee. This is due to an in vitro competition between ethanol-extractable orphenadrine metabolites and thyroxine for binding sites on the thyroxine binding globulin.
开展了多项研究以阐明奥芬那君是否会影响甲状腺功能。7名志愿者接受奥芬那君治疗,每周剂量递增,直至每日300毫克;5名长期每日服用300毫克奥芬那君的患者逐渐停药。在服用奥芬那君期间及之后,未发现蛋白结合碘(PBI)、反三碘甲状腺原氨酸摄取率(RT3U)、总三碘甲状腺原氨酸(TT3)和促甲状腺激素(TSH)有变化;药物对静脉注射200微克促甲状腺激素释放激素(TRH)后的TSH和TT3反应也无影响。采用竞争性蛋白结合(CPB)技术测定时,奥芬那君治疗可使血清甲状腺素值升高(P<0.001),但采用放射免疫测定法时对血清甲状腺素值无影响。在墨菲-帕蒂试验中,体外向血清中添加奥芬那君不会使甲状腺素值升高;然而,所检测的8种代谢物中有2种会使甲状腺素值升高。得出的结论是,每日剂量达300毫克的奥芬那君不会影响甲状腺功能。采用墨菲和帕蒂的竞争性蛋白结合技术测定时,它会使血清甲状腺素水平升高。这是由于可乙醇提取的奥芬那君代谢物与甲状腺素在甲状腺素结合球蛋白上的结合位点存在体外竞争。