Candesartan detailed information
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| Candesartan detailed information
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| 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 | |
| ATC code | C09 |
| PubChem | |
| DrugBank | |
| 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 |
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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.
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.[3]
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.
External links
- Atacand web site or Atacand US, run by AstraZeneca
- Candesartan
Agents acting on the renin-angiotensin system (C09) | |
|---|---|
| ACE inhibitors | Benazepril • Captopril • Delapril • Enalapril • Fosinopril • Imidapril • Lisinopril • Moexipril • Perindopril • Quinapril • Ramipril • Spirapril • Temocapril • Trandolapril • Zofenopril |
| Angiotensin II receptor antagonists (AIIRA) | Candesartan • Eprosartan • Irbesartan • Losartan • Olmesartan • Tasosartan • Telmisartan • Valsartan |
| Renin inhibitors | Aliskiren • Remikiren |
Acknowledgement and Attribution Regarding Sources of Content
Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .
