a Department of Cardiology and Cardiovascular Pathophysiology , Hospital and University of Perugia , Perugia , Italy.
b Department of Internal Medicine , Hospital of Assisi , Assisi , Italy.
Expert Opin Drug Metab Toxicol. 2018 May;14(5):533-541. doi: 10.1080/17425255.2018.1468435. Epub 2018 May 10.
Fimasartan is the ninth and latest Angiotensin Receptor Blockers for the treatment of hypertension. Fimasartan is a derivative of losartan in which the imidazole ring has been replaced. It provides a selective type 1 angiotensin II receptor antagonist effect with noncompetitive, in surmountable binding. Fimasartan is rapidly absorbed following oral administration with an oral bioavailability of 18.6 ± 7.2%. Fimasartan is relatively stable in terms of metabolism and more than 90% of circulating fimasartan moieties in the plasma are in the parent form; fecal elimination and biliary excretion are the predominant elimination pathways of fimasartan. Areas covered: We reviewed data from clinical trials that investigated safety and efficacy of fimasartan in hypertension. Expert opinion: Fimasartan proved good efficacy in blood pressure reduction. In large clinical studies,fimasartan showed an excellent safety profile and when combined with hydrochlorothiazide oram lodipine, it showed a better effect on controlling blood pressure than monotherapy. Fimasartan 60-120 mg once daily has also shown an antihypertensive effect over 24-h. Moreover, preclinical studies demonstrated organ-protecting effects of fimasartan. These results make fimasartan an attractive candidate for the treatment of hypertension. However, it remains to test the benefit of using fimasartan on clinical outcomes.
法米沙坦是治疗高血压的第九种也是最新的血管紧张素受体阻滞剂。法米沙坦是氯沙坦的衍生物，其中咪唑环已被取代。它提供了一种选择性的 1 型血管紧张素 II 受体拮抗剂作用，具有非竞争性、不可逾越的结合。法米沙坦口服后迅速吸收，口服生物利用度为 18.6±7.2%。法米沙坦在代谢方面相对稳定，在血浆中循环的法米沙坦部分中超过 90%以母体形式存在；粪便消除和胆汁排泄是法米沙坦的主要消除途径。涵盖领域：我们回顾了临床试验的数据，这些试验研究了法米沙坦在高血压中的安全性和疗效。专家意见：法米沙坦在降低血压方面证明了良好的疗效。在大型临床研究中，法米沙坦显示出极好的安全性，当与氢氯噻嗪或氨氯地平联合使用时，其控制血压的效果优于单药治疗。法米沙坦 60-120mg 每日一次也显示出 24 小时的降压作用。此外，临床前研究表明法米沙坦具有器官保护作用。这些结果使法米沙坦成为治疗高血压的一个有吸引力的候选药物。然而，仍需检验使用法米沙坦对临床结局的益处。
