Putting the efficacy of candesartan cilexetil into perspective: a review of new comparative data.
Candesartan is one of the first angiotensin II receptor antagonists (AIIRAs) to be developed. It binds tightly to and dissociates slowly from the angiotensin subtype 1 (AT1) receptor in vitro. These binding characteristics differ from those of losartan, which demonstrates lower affinity and faster dissociation from the AT1 receptor. Candesartan causes long-lasting antagonism of the vascular contractile response to angiotensin II compared with irbesartan, losartan or the active metabolite of losartan - EXP-3174. While there are relatively few distinctions that can be made between the AIIRAs in terms of their pharmacokinetic profiles, the antagonistic potency of candesartan cilexetil at the AT1 receptor over 24 h clearly differentiates it from other members of its class. These differences are reflected in the antihypertensive efficacy and duration of action of candesartan in clinical trials.
Mallion
J M
JM
CHU Hôpital Michallon, Médecine Interne et Cardiologie, Grenoble, France.
Badguet
J P
JP
D000804:Angiotensin II / Q000037:antagonists & inhibitors; D057911:Angiotensin Receptor Antagonists; D000818:Animals; D000959:Antihypertensive Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D001562:Benzimidazoles / Q000494:pharmacology* / Q000627:therapeutic use*; D001713:Biphenyl Compounds / Q000494:pharmacology* / Q000627:therapeutic use*; D001794:Blood Pressure / Q000187:drug effects; D002417:Cattle; D002531:Cerebellum / Q000187:drug effects; D002940:Circadian Rhythm; D005260:Female; D006321:Heart / Q000187:drug effects; D006801:Humans; D006973:Hypertension / Q000188:drug therapy*; D066298:In Vitro Techniques; D000077405:Irbesartan; D007700:Kinetics; D019808:Losartan / Q000494:pharmacology / Q000627:therapeutic use; D008297:Male; D008875:Middle Aged; D011355:Prodrugs; D011817:Rabbits; D016032:Randomized Controlled Trials as Topic; D011945:Receptors, Angiotensin / Q000502:physiology; D012083:Renin / Q000187:drug effects / Q000502:physiology; D013777:Tetrazoles / Q000494:pharmacology / Q000627:therapeutic use; D013997:Time Factors
D057911:Angiotensin Receptor Antagonists; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D001713:Biphenyl Compounds; D011355:Prodrugs; D011945:Receptors, Angiotensin; D013777:Tetrazoles; D000804:Angiotensin II; D012083:Renin; D000077405:Irbesartan; D019808:Losartan; C077793:candesartan cilexetil; C081643:candesartan