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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.

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1 Clinical use
- 1.1 Indications
- 1.2 Combination with diuretic
2 Chemistry and pharmacokinetics
3 Randomized controlled trials
4 References

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

^ 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.

v • d • e Agents acting on the renin-angiotensin system (C09)
ACE inhibitors	Benazepril • Captopril • Enalapril • Fosinopril • Lisinopril • Perindopril • Quinapril • Ramipril • Spirapril • Trandolapril
Angiotensin II receptor antagonists (AIIRA)	Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan
Renin inhibitors	Aliskiren • Remikiren

Category: Angiotensin II receptor antagonists

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.