Candesartan

drugbox
width=200

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IUPAC_name = 3-((2'-(2"H"-tetrazol-5-yl)
biphenyl-4-yl)methyl)-2-ethoxy-
3"H"-benzo [d] imidazole-4-carboxylic acid
CAS_number = 139481-59-7
ChemSpiderID = 2445
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: intestinal wall; candesartan: hepatic (CYP2C9)
elimination_half-life = 5.1–10.5 hours
excretion = Renal 33%, faecal 67%
pregnancy_category = D (Au)
legal_status = Rx-only
routes_of_administration = oral

Candesartan (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

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.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 | pmid = 13678868 | doi = 10.1016/S0140-6736(03)14282-1] 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.

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. [http://content.nejm.org/cgi/content/abstract/354/16/1685]

References

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]
* [http://www1.astrazeneca-us.com/pi/Atacand.pdf Prescribing Information for ATACAND]