Azilsartan (EDARBI): A New Angiotensin Receptor Blocker (ARB) for Hypertension

Approved by the FDA for Marketing in the USA

Randa Hilal-Dandan

Disclosures

AccessMedicine from McGraw-Hill 

In This Article

Pharmacokinetics

Azilsartan medoxomil is a prodrug supplied in 40 mg and 80 mg tablets. The recommended dose of azilsartan medoxomil is 80 mg tablet taken orally once a day (a starting dose of 40 mg once daily should be considered in patients using high dose diuretics).[2] Following oral administration, azilsartan medoxomil is hydrolyzed in the GI tract to its active metabolite, azilsartan. The oral bioavailabilty of azilsartan is ~60% and it is not affected by the presence of food. Azilsartan is almost completely bound to plasma proteins (>99%), mainly serum albumin. Peak plasma concentrations (Cmax) are achieved within 1.5 - 3 hours. Steady-state levels are achieved in 5 days. Azilsartan is metabolized mostly via CYP2C9 into two inactive metabolites. The main metabolite, referred to as M-II, is formed by O-dealkylation; and the minor metabolite, referred to as M-I, is formed by decarboxylation. The elimination t1/2 is 11 hours.[2] Elimination of the drug is via feces (55%) and urine (42%). About 15% of the dose is eliminated as unchanged azilsartan in urine. Renal clearance is 2.3 ml/min. In rats, azilsartan crosses the blood brain barrier and placental barrier.[2]

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