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Antagonists at the AT1 receptor (sartans)

The sartans used in the treatment of essential hypertension are mainly active in their own right and produce competitive antagonism of angiotensin acting at the AT1 receptor. However, two members of the group (candesartan cilexitil and olmesartan medoxomil) are prodrugs and one (losartan potassium) is metabolised to form a derivative that acts as an insurmountable antagonist.

A table of the pharmacokinetic properties of sartans is available for reference purposes.