Candesartan

Abstract

Candesartan cilexetil is the prodrug of candesartan, an angiotensin II receptor antagonist. Candesartan binds selectively and non-competitively to the angiotensin II receptor type 1, thus preventing the actions of angiotensin II. Clinical trials have demonstrated its efficacy at a dose range of 2 to 32 mg once daily in hypertension of all grades, heart failure, in reducing urinary albumin excretion in diabetes mellitus and in coexisting hypertension and renal failure. Pharmacokinetic properties of candesartan cilexetil in elderly patients are not significantly different from those in younger individuals. Hepatic impairment does not change pharmacokinetics of candesartan cilexetil at doses up to 12 mg/day. No dose adjustment is necessary in patients with mild or moderate renal impairment. Tolerability of candesartan cilexetil is not much different from that of placebo. All adverse events are usually of mild to moderate severity and not dose-related. The most common adverse events were headache, upper respiratory tract infection, back pain, and dizziness. The incidence of these adverse effects, as well as of cough, was similar in patients treated with candesartan cilexetil or placebo. The incidence of adverse events in long-term trials was not different from that in short-term trials. Tolerability of candesartan cilexetil does not differ with either age or gender.

A Systematic Comparison of the Properties of Clinically Used Angiotensin II Type 1 Receptor Antagonists

“…Antagonism of AT1R by various ARBs has also been tested in vivo in humans, mostly healthy volunteers, and, similar to the above animal studies, this was largely done for ANGinduced blood pressure elevations. Following the original study with losartan (Christen et al, 1991), such studies have been performed with candesartan (Delacretaz et al, 1995;Ogihara et al, 1995;Belz et al, 1997Belz et al, , 2000Malerczyk et al, 1998;Fuchs et al, 2000;Gleiter et al, 2004), irbesartan (Belz et al, 1999Maillard et al, 1999;Mazzolai et al, 1999), losartan (Munafo et al, 1992;Belz et al, 1997Belz et al, , 1999Belz et al, , 2000Maillard et al, 1999;Mazzolai et al, 1999;Fuchs et al, 2000;Gleiter et al, 2004), telmisartan Stangier et al, 2001), and valsartan (Müller et al, 1994;Morgan et al, 1997;Belz et al, 1999Belz et al, , 2000Maillard et al, 1999;Mazzolai et al, 1999).…”

Evaluation of Adherence Should Become an Integral Part of Assessment of Patients With Apparently Treatment-Resistant Hypertension

“…[80][81][82] Table 3 summarizes the pharmacokinetic characteristics of the most frequently used antihypertensive drugs belonging to the 5 main classes. [83][84][85][86][87][88][89][90][91][92][93] Drug monitoring may also be influenced by preanalytical errors. False-negative results might be because of nonspecific drug adsorption on the plastic tube or separator gel used or to drug instability at higher temperature or sensitivity to light as described for nifedipine.…”

Is Blockade of the Renin-angiotensin System Able to Reverse the Structural and Functional Remodeling of the Left Ventricle in Severe Aortic Stenosis?

“…Clinical assessment and echocardiography at the end of treatment were done 2 days after discontinuation of treatment and, therefore, any acute effects of candesartan were probably missed. The dose of candesartan, 16 mg per day, should have been sufficient, 35 although a larger dose was used in the CHARM trial of heart failure with preserved EF. 36 Interestingly, the CHARM-Preserved trial and other large controlled trials have consistently failed to show benefits from RAS inhibition in heart failure with normal EF.…”