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14-September-2008 18:02:39 - Candesartan Candesartan Systematic IUPAC name 3-2'-2H-tetrazol-5-yl biphenyl-4-ylmethyl-2-ethoxy- 3H-benzodimidazole-4-carboxylic acid Identifiers CAS number 139481-59-7 ATC code C09CA06 PubChem 2541 DrugBank APRD00420 Chemical data Formula C24H20N6O3 Mol. mass 440.45 Pharmacokinetic data Bioavailability 15% candesartan cilexetil Metabolism Candesartan cilexetil: intestinal wall; candesartan: hepatic CYP2C9 Half life 5.1-10.5 hours Excretion Renal 33%, faecal 67% Therapeutic considerations Pregnancy cat. D Au Legal status ℞ Prescription only Routes oral Candesartan rINN pronounced /ˌkændɨˈsɑrtən/ is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. The prodrug candesartan cilexetil is marketed by AstraZeneca and Takeda Pharmaceuticals, commonly under the trade names Blopress, Atacand, Amias, and Ratacand. Contents 1 Clinical use 1.1 Indications 1.2 Combination with diuretic 2 Chemistry and pharmacokinetics 3 Randomized controlled trials 4 References 5 External links Clinical use Main article: Angiotensin II receptor antagonist Indications As with all angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study in the early 2000s demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure.1 Thus, while ACE inhibitors are still considered first-line therapy in heart failure, candesartan can be used in combination with an ACE to achieve improved mortality and morbidity vs. an ACE alone and additionally is an alternative in patients intolerant of ACE inhibitor therapy. Combination with diuretic Candesartan is also available in a combination formulation with a low dose thiazide diuretic, invariably hydrochlorothiazide, to achieve an additive antihypertensive effect. Candesartan/hydrochlorothiazide combination preparations are marketed under various trade names including Atacand HCT, Hytacand, Blopress Plus and Ratacand Plus. Candesartan cilexetil Candesartan cilexetil Chemistry and pharmacokinetics Candesartan is marketed as the cyclohexyl 1-hydroxyethyl carbonate cilexetil ester, known as candesartan cilexetil. Candesartan cilexetil is metabolised completely by esterases in the intestinal wall during absorption to the active candesartan moieity. The use of a prodrug form increases the bioavailability of candesartan. Despite this, absolute bioavailability is relatively poor at 15% candesartan cilexetil tablets to 40% candesartan cilexetil solution. Randomized controlled trials Over a period of four years, stage 1 hypertension developed in nearly two thirds of patients with untreated prehypertension the placebo group. Treatment of prehypertension with candesartan appeared to be well tolerated and reduced the risk of incident hypertension during the study period. Thus, treatment of prehypertension appears to be feasible.1 References ^ Pfeffer M, Swedberg K, Granger C, Held P, McMurray J, Michelson E, Olofsson B, Ostergren J, Yusuf S, Pocock S 2003. Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet 362 9386: 759-66. doi:10.1016/S0140-67360314282-1. PMID 13678868. External links Atacand web site or Atacand US, run by AstraZeneca Candesartan Prescribing Information for ATACAND v d e Agents acting on the renin-angiotensin system C09 ACE inhibitors Alacepril Benazepril Captopril Cilazapril Delapril Enalapril Fosinopril Imidapril Lisinopril Moexipril Perindopril Quinapril Ramipril Rentiapril Spirapril Temocapril Trandolapril Zofenopril Angiotensin II receptor antagonists AIIRA Azilsartan Candesartan Eprosartan Irbesartan Losartan Olmesartan Tasosartan Telmisartan Valsartan Renin inhibitors Aliskiren Remikiren Retrieved from http://en..org/wiki/Candesartan Categories: Angiotensin II receptor antagonists | Tetrazoles Views Article Discussion this page History Personal tools Log in / create account Navigation Main page Contents Featured content Current events Random article Search Go Search Interaction Community portal Recent changes Contact Donate to Help Toolbox What links here Related changes Upload file Special pages Printable version Permanent link Cite this page Languages Español Magyar Polski Português This page was last modified on 19 July 2008, at 14:22
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