Azilsartan medoxomil is a prodrug that is rapidly converted to the active moiety, azilsartan, which selectively antagonize the effects of angiotensin II by blocking its binding to the AT1 receptor in multiple tissues. Angiotensin II is the principal pressor agent of the renin-angiotensin system, with effects that include vasoconstriction, stimulation of synthesis and release of aldosterone, cardiac stimulation, and renal reabsorption of sodium.
藥動學
Bioavailability: ~60% , Protein binding: > 99%; primarily to serum albumin. Metabolism: Gut: prodrug hydrolyzed to active metabolite (azilsartan ); Hepatic: primarily via CYP2C9 to inactive metabolites. Excretion: Feces (~55%); urine (~42%, 15% as unchanged drug). Elimination half-life: approximately 11 hours.
禁忌症
Hypersensitivity to the active substance or to any of the excipients; pregnancy; Do not co-administer aliskiren with azilsartan in patients with diabetes.
懷孕分類
D [FDA]
哺乳分類
Infant risk cannot be ruled out. [MDX]
副作用
Dizziness, diarrhea, hypotension.
劑量和給藥方法
80 mg ORALLY once daily; consider a starting dose of 40 mg ORALLY once daily for patients receiving high doses of diuretics