一个痛风的临床案例AClinicalCaseforGout.PDF

一个痛风的临床案例 A Clinical Case for Gout 关于下市促尿酸排泄药苯溴马隆 About the withdrawal uricosuric agent Benzbromarone (BBR) by Tom Hsiung, B.S. Pharm 患者信息 Patient Information 年龄Age: approximately 30 yrs 性别 Gender: male 诊断 Diagonise: Gout 处方 Rx: • Benzbromarone （苯溴马隆）, 剂量未知 治疗策略Treatment Approach 痛风的治疗包括三方面: • Treating the acute attack （治疗急性发作）; • Lowering excess stores of urate to prevent flares of gouty arthritis and to prevent tissue deposition of urate crystals; （降尿酸治疗） • Providing prophylaxis to prevent acute flares. （预防急性发作） 注意：过往的资料描述到必须等到痛风急性关节炎完全缓解数周后，才能开 始降尿酸治疗（否则，降尿酸治疗会加重或者延长痛风急性关节炎 [扰乱循 环中的尿酸水平] ）。而2012的ACR痛风指南则专门提到，可以在痛风急性 关节炎发作期间开始降尿酸治疗，前提是已经开始有效地抗炎管理。 降尿酸治疗Lowering Uric Acid Level Therapy 治疗目标Therapeutic Goal : 6 mg/dL (360 umol/L) • Allopurinol (别嘌醇), 降低尿酸的生成; • Uricosuric agents （促尿酸排泄药）,抑制肾小管对尿 酸的重吸收; • Pegloticase （尿酸酶）, 催化尿酸氧化为尿囊素. Risk for anaphylaxis is higher if serum uric acid level >6 mg/dL; G6PD-deficiency (pharmacogenetics). 药物动力学以及药效学 Pharmacokinetics and Pharmacodynamics Benzabromarone (BBR/苯溴马隆) is a uricosuric agent which was first marketed for the management of gout in 1976. BBR lowers serum urate concentrations by reducing the reabsorption of uric acid from the renal tubules ( inhibition of apical transporter proteins GLUT9 and URAT1). BBR was withdrawn from use in many countries after being associated with 11 cases of fatal hepatotoxicity from 1994 to 2003 (dose- dependent). 药物动力学以及药效学 Pharmacokinetics and Pharmacodynamics 肝酶CYP2C9 BBR 6-OH-BBR （6-羟基苯溴马隆） (Hepatotoxicity/ 肝毒性) 肝酶CYP2C9 Metabolite 1 （代谢物1 ） (Pharmacologics/ Metabolite 2 发挥药效) （代谢物2 ） 药物基因学 Pharmacogenetics 肝酶