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Candesartan

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Candesartan
File:Candesartan.svg
Systematic (IUPAC) name
2-ethoxy-1-({4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl}methyl)-1H-1,3-benzodiazole-7-carboxylic acid
Clinical data
Trade names Atacand
AHFS/Drugs.com monograph
MedlinePlus a601033
  • AU: D
  • (Prescription only)
oral
Pharmacokinetic data
Bioavailability 15% (candesartan cilexetil)
Metabolism Candesartan cilexetil: intestinal wall; candesartan: hepatic (CYP2C9)
Half-life 9 hours
Excretion Renal 33%, faecal 67%
Identifiers
139481-59-7 7pxY
C09CA06
PubChem CID 2541
IUPHAR ligand 587
DrugBank DB00796 7pxY
ChemSpider 2445 7pxY
UNII S8Q36MD2XX 7pxY
KEGG D00626 7pxN
ChEBI CHEBI:3347 7pxY
ChEMBL CHEMBL1016 7pxY
Chemical data
Formula C24H20N6O3
440.45 g/mol
 14pxN (what is this?)  (verify)

Candesartan (rINN) /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. It is available in generic form.[1]

Clinical use

As with other angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Results from the CHARM study (early 2000s) demonstrated the morbidity and mortality reduction benefits of candesartan therapy in congestive heart failure.[2] 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.

Prehypertension

In a four-year randomized controlled trial, candesartan was compared to placebo to see whether it could prevent or postpone the development of full-blown hypertension in people with so-called prehypertension. During the first two years of the trial, half of participants were given candesartan, and the others received placebo; candesartan reduced the risk of developing hypertension by nearly two-thirds during this period. In the last two years of the study, all participants were switched to placebo. By the end of the study, candesartan had significantly reduced the risk of hypertension, by more than 15%. Serious side effects were actually more common among participants receiving placebo than in those given candesartan.[3]

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, Advantec and Ratacand Plus.

Chemistry and pharmacology

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). Its IC50 is 15 µg/kg.

See also

References

  1. ^ http://www.sandoz.com/cs/www.sandoz.com-v4/assets/media/shared/documents/Candesartan_PR.pdf
  2. ^ 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. doi:10.1016/S0140-6736(03)14282-1. 
  3. ^ Julius S, Nesbitt SD, Egan BM et al. (July 2006). "Feasibility of treating prehypertension with an angiotensin-receptor blocker". New England Journal of Medicine 354 (16): 1685–97. PMID 16537662. doi:10.1056/NEJMoa060838. 

External links