Zeeh J, Fuchs L, Bergmann W, Antonin K H, Degel F, Bieck P, Platt D
Chair of Internal Medicine and Gerontology, University Erlangen-Nürnberg, Germany.
Eur J Clin Pharmacol. 1996;49(5):387-91. doi: 10.1007/BF00203783.
The pharmacokinetics of brofaromine, a selective inhibitor of monoamine oxidase A, was evaluated in 12 frail elderly patients (66-92 y) and 12 healthy volunteers (20-35 y).
Quantitative liver function tests were performed to show whether brofaromine elimination in the elderly could be predicted from noninvasive assessment of CYP1A2 activity (caffeine clearance) or liver plasma flow (sorbitol clearance).
In the elderly the AUC of brofaromine was significantly increased (e.g. for the 75 mg dose 43.2 vs 19.9 mumol*h.l-1, clearance was reduced (5.0 vs. 11.8 l.h-1), the volume of distribution was smaller (130 vs. 230 l), and the half-life was slightly increased (19.0 vs. 14.2 h). No significant correlation was observed between hepatic plasma flow and brofaromine clearance (r = 0.41, P = 0.05), whereas CYP1A2 activity and brofaromine clearance were tightly correlated (r = 0.94, P < 0.0001).
Caffeine clearance, a simple, noninvasive test of CYP1A2 activity, is predictive of brofaromine clearance.
在12名体弱老年患者（66 - 92岁）和12名健康志愿者（20 - 35岁）中评估单胺氧化酶A选择性抑制剂溴法罗明的药代动力学。
进行定量肝功能测试，以表明能否通过对CYP1A2活性（咖啡因清除率）或肝血浆流量（山梨醇清除率）的非侵入性评估来预测老年人中溴法罗明的清除情况。
在老年人中，溴法罗明的AUC显著增加（例如，75毫克剂量时为43.2对19.9微摩尔·小时·升⁻¹），清除率降低（5.0对11.8升·小时⁻¹），分布容积较小（130对230升），半衰期略有增加（19.0对14.2小时）。肝血浆流量与溴法罗明清除率之间未观察到显著相关性（r = 0.41，P = 0.05），而CYP1A2活性与溴法罗明清除率紧密相关（r = 0.94，P < 0.0001）。
咖啡因清除率，一种简单的CYP1A2活性非侵入性测试，可预测溴法罗明清除率。
