Differences among angiotensin II type 1 receptor blockers: characteristics of candesartan cilexetil.
Several angiotensin II type 1 (AT1) receptor blockers are now available for the treatment of hypertension. Although the agents in this class all act by blocking the AT1-receptor, they differ in their pharmacokinetics and binding characteristics. One of the newest AT1-receptor blockers, candesartan cilexetil, is administered in an inactive form and is rapidly and completely converted to the active drug, candesartan, during gastrointestinal absorption. In vitro studies have shown that candesartan has the highest receptor affinity of all the available AT1-receptor blockers and is not displaced from the receptor by high concentrations of angiotensin II. The tight and long-lasting binding of candesartan to the AT1-receptor provides effective blockade of the negative cardiovascular effects of angiotensin II.
Unger
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Institute of Pharmacology, Christian-Albrechts University, Kiel, Germany.
D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000378:metabolism*; D001562:Benzimidazoles / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D001682:Biological Availability; D001713:Biphenyl Compounds / Q000378:metabolism* / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007408:Intestinal Absorption; D044140:Receptor, Angiotensin, Type 1; D044139:Receptor, Angiotensin, Type 2; D011945:Receptors, Angiotensin / Q000378:metabolism; D013777:Tetrazoles
D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D044140:Receptor, Angiotensin, Type 1; D044139:Receptor, Angiotensin, Type 2; D011945:Receptors, Angiotensin; D013777:Tetrazoles; C077793:candesartan cilexetil