Candesartan detailed information: Difference between revisions

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{{drugbox |
#REDIRECT [[Candesartan#Pharmacology]]
|width=200px
|image=Candesartan structure svg.png
|IUPAC_name = 3-((2'-(2''H''-tetrazol-5-yl)<br />biphenyl-4-yl)methyl)-2-ethoxy-<br />3''H''-benzo[d]imidazole-4-carboxylic acid
|CAS_number = 139481-59-7
| ATC_prefix = C09
| ATC_suffix = CA06
| PubChem = 2541
| DrugBank = APRD00420
| C=24 | H=20 | N=6 | O=3
|molecular_weight = 440.45
|bioavailability = 15% (candesartan cilexetil)
|metabolism = Candesartan cilexetil: [[intestine|intestinal wall]]; candesartan: [[hepatic]] ([[CYP2C9]])
|elimination_half-life = 5.1–10.5 hours
|excretion = [[Renal]] 33%, [[feces|faecal]] 67%
|pregnancy_category = D <small>([[Australia|Au]])</small>
|legal_status = Rx-only
|routes_of_administration = oral
}}
{{CMG}}
 
 
 
==[[Candesartan (patient information)|For patient information, click here]]==
 
'''Candesartan''' ([[International Nonproprietary Name|rINN]]) ({{pronEng|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'''.
 
==Clinical use==
{{dablink|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 [[death|mortality]] reduction benefits of candesartan therapy in [[congestive heart failure]].<ref name="Pfeffer2003">{{cite journal | author = Pfeffer M, Swedberg K, Granger C, Held P, McMurray J, Michelson E, Olofsson B, Ostergren J, Yusuf S, Pocock S | title = Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. | journal = Lancet | volume = 362 | issue = 9386 | pages = 759–66 | year = 2003 | id = PMID 13678868}}</ref> Thus, while [[ACE inhibitor]]s 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'''.
 
[[Image:Candesartan cilexetil.png|thumb|Candesartan cilexetil|150px|left]]
 
==Chemistry and pharmacokinetics==
Candesartan is marketed as the [[cyclohexane|cyclohexyl]] 1-[[hydroxy]][[ethyl]] [[carbonate]] (cilexetil) [[ester]], known as '''candesartan cilexetil'''. Candesartan cilexetil is metabolised completely by [[esteras]]es in the [[intestine|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.[http://content.nejm.org/cgi/content/abstract/354/16/1685]
 
==References==
{{reflist|2}}
 
==External links==
* [http://www.atacand.com/ Atacand web site] or [http://www.atacand-us.com/ Atacand US], run by [[AstraZeneca]]
* [http://www.meds-help.com/candesartan Candesartan]
 
 
{{Angiotensin II receptor antagonists}}
 
[[Category:angiotensin II receptor antagonists]]
[[Category:Tetrazoles]]
[[Category:Drugs]]
 
[[es:Candesartan]]
[[hu:Candesartan]]
[[pt:Candesartan]]
 
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Latest revision as of 23:26, 21 July 2014