Brunner Hans R, Laeis Petra
Division of Hypertension and Vascular Medicine, Centre Hospitalier Universitaire Vaudois, Lausanne, Switzerland.
J Hypertens Suppl. 2003 May;21(2):S43-6. doi: 10.1097/00004872-200305002-00008.
Olmesartan medoxomil is a new angiotensin-II receptor antagonist for the treatment of hypertension. Olmesartan medoxomil is a pro-drug that is de-esterified to the active metabolite, olmesartan. Olmesartan has a dual method of elimination, with about 60% eliminated by the liver and the remainder by the kidney. In situations of impaired renal or hepatic function, the alternative excretion pathway can compensate for the compromised one. Olmesartan is not metabolized by the cytochrome P450 enzyme system and therefore has a low potential for metabolic drug interactions, a feature that may be of importance when treating patients on multiple drug regimens, such as the elderly. Olmesartan is well tolerated and has an excellent safety profile that is comparable to that of placebo. In addition, olmesartan provides 24-h blood pressure control with a once-daily dosing. In head-to-head studies, olmesartan delivered superior blood pressure reduction when compared with other angiotensin-II receptor antagonists at their recommended doses.
奥美沙坦酯是一种用于治疗高血压的新型血管紧张素II受体拮抗剂。奥美沙坦酯是一种前体药物，经去酯化后成为活性代谢产物奥美沙坦。奥美沙坦有双重消除途径，约60%经肝脏消除，其余经肾脏消除。在肾功能或肝功能受损的情况下，替代排泄途径可补偿受损的途径。奥美沙坦不通过细胞色素P450酶系统代谢，因此发生代谢性药物相互作用的可能性较低，这一特性在治疗采用多种药物治疗方案的患者（如老年人）时可能很重要。奥美沙坦耐受性良好，具有与安慰剂相当的出色安全性。此外，奥美沙坦每日给药一次即可实现24小时血压控制。在头对头研究中，与其他血管紧张素II受体拮抗剂按推荐剂量给药相比，奥美沙坦能更有效地降低血压。
