Azilsartan is a synthetic antagonist of the Angiotensin II receptor. It has an effective concentration of 1-100 nM and an IC50 of 2.6 nM on the human Angiotensin II type-1 receptor1. The antihypertensive effects of azilsartan are dose-related. A 32-mg dose of azilsartan decreases the maximal constrictive effect of Angiotensin II by approximately 90% when the drug reaches peak plasma concentration. The estimated bioavailability of Azilsartan is 60% and it is not affected by food. Azilsartan is primarily metabolized by CYP 2C9. Its two main metabolites are M-1 and M-2. These metabolites have a low affinity towards the AT receptor and have no substantial pharmacological effect. Renal clearance of azilsartan is approximated to 2.3 ml/minute. Most of the product is eliminated in the feces (55%) and in the urine (42%) while the rest remains unchanged. Many clinical trials have shown a beneficial effect of Azilsartan on the lowering of blood pressure. The most common side effect of Azilsartan is diarrhea occurring in 2% of patients receiving 80-mg dose. Other possible adverse effects are nausea, muscle spasm, cough and dizziness2.
