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Candesartan



Candesartan
Systematic (IUPAC) name
3-((2'-(2H-tetrazol-5-yl)
biphenyl-4-yl)methyl)-2-ethoxy-
3H-benzo[d]imidazole-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.

Additional recommended knowledge

Contents

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.[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.[1]

References

  1. ^ 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. PMID 13678868.
 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Candesartan". A list of authors is available in Wikipedia.
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