Marino M R, Vachharajani N N
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 18543, USA.
Clin Pharmacokinet. 2001;40(8):605-14. doi: 10.2165/00003088-200140080-00004.
Irbesartan is an angiotensin II receptor antagonist indicated for the treatment of patients with hypertension. Although irbesartan does not require biotransformation for its pharmacological activity, it does undergo metabolism via the cytochrome P450 (CYP) 2C9 isoenzyme and negligible metabolism by the CYP3A4 isoenzyme. The long term treatment of patients with hypertension is generally required for effective management of the disease, and the use of concurrent medications is usually inevitable. This paper reviews the drug and food interaction trials involving irbesartan that have been conducted to date. Based on the available literature, no significant interactions have been identified between irbesartan and hydrochlorothiazide, nifedipine, simvastatin, tolbutamide, warfarin, magnesium and aluminum hydroxides, digoxin or food. Fluconazole did increase the steady-state peak plasma concentration (by 19%) and area under the concentration-time curve (by 63%) of irbesartan, but these increases are not likely to be clinically significant. In summary, irbesartan has demonstrated minimal potential for drug or food interactions in trials conducted to date.
厄贝沙坦是一种血管紧张素II受体拮抗剂，用于治疗高血压患者。尽管厄贝沙坦的药理活性不需要生物转化，但它确实会通过细胞色素P450（CYP）2C9同工酶进行代谢，而通过CYP3A4同工酶的代谢可忽略不计。高血压患者通常需要长期治疗才能有效控制病情，同时使用其他药物通常不可避免。本文综述了迄今为止进行的涉及厄贝沙坦的药物和食物相互作用试验。根据现有文献，未发现厄贝沙坦与氢氯噻嗪、硝苯地平、辛伐他汀、甲苯磺丁脲、华法林、氢氧化镁和氢氧化铝、地高辛或食物之间存在显著相互作用。氟康唑确实会使厄贝沙坦的稳态血药峰浓度（升高19%）和浓度-时间曲线下面积（升高63%）增加，但这些增加在临床上可能不具有显著意义。总之，在迄今为止进行的试验中，厄贝沙坦显示出药物或食物相互作用的可能性极小。
