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Statements

Subject Item
n2:DB00796
rdf:type
n3:Drug
n3:description
Candesartan is an angiotensin-receptor blocker (ARB) that may be used alone or with other agents to treat hypertension. It is administered orally as the prodrug, candesartan cilexetil, which is rapidly converted to its active metabolite, candesartan, during absorption in the gastrointestinal tract. Candesartan lowers blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); it competes with angiotensin II for binding to the type-1 angiotensin II receptor (AT1) subtype and prevents the blood pressure increasing effects of angiotensin II. Unlike angiotensin-converting enzyme (ACE) inhibitors, ARBs do not have the adverse effect of dry cough. Candesartan may be used to treat hypertension, isolated systolic hypertension, left ventricular hypertrophy and diabetic nephropathy. It may also be used as an alternative agent for the treatment of heart failure, systolic dysfunction, myocardial infarction and coronary artery disease.
n3:dosage
n29:271B64A5-363D-11E5-9242-09173F13E4C5 n29:271B64A2-363D-11E5-9242-09173F13E4C5 n29:271B64A3-363D-11E5-9242-09173F13E4C5 n29:271B64A4-363D-11E5-9242-09173F13E4C5
n3:generalReferences
# Pfeffer MA, Swedberg K, Granger CB, Held P, McMurray JJ, Michelson EL, Olofsson B, Ostergren J, Yusuf S, Pocock S: Effects of candesartan on mortality and morbidity in patients with chronic heart failure: the CHARM-Overall programme. Lancet. 2003 Sep 6;362(9386):759-66. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/13678868 # Mendis B, Page SR: Candesartan: widening indications for this angiotensin II receptor blocker? Expert Opin Pharmacother. 2009 Aug;10(12):1995-2007. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19563275 # Baguet JP, Barone-Rochette G, Neuder Y: Candesartan cilexetil in the treatment of chronic heart failure. Vasc Health Risk Manag. 2009;5(1):257-64. Epub 2009 Apr 8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/19436650 # Bader, M. (2004). Renin-angiotensin-aldosterone system. In S. Offermanns, & W. Rosenthal (Eds.). _Encyclopedic reference of molecular pharmacology_ (pp. 810-814). Berlin, Germany: Springer. # Stanfield, C.L., & Germann, W.J. (2008). _Principles of human physiology_ (3 ^rd^ ed.). San Francisco, CA: Pearson Education, Inc.
n3:group
approved
n3:halfLife
Approximately 9 hours.
n3:indication
May be used as a first line agent to treat uncomplicated hypertension, isolated systolic hypertension and left ventricular hypertrophy. May be used as a first line agent to delay progression of diabetic nephropathy. Candesartan may be also used as a second line agent in the treatment of congestive heart failure, systolic dysfunction, myocardial infarction and coronary artery disease in those intolerant of ACE inhibitors.
n3:manufacturer
n10:271B6495-363D-11E5-9242-09173F13E4C5
owl:sameAs
n28:DB00796 n33:DB00796
dcterms:title
Candesartan
adms:identifier
n7:3347 n8:2445 n9:50240609 n11:587 n12:587 n13:DB00796 n14:0186-0004-31 n15:PA448765 n16:C07468 n17:D00626 n18:2541 n19:46508342 n34:Candesartan
n3:mechanismOfAction
Candesartan selectively blocks the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. This inhibits the AT1-mediated vasoconstrictive and aldosterone-secreting effects of angiotensin II and results in an overall decrease in blood pressure. Candesartan is greater than 10,000 times more selective for AT1 than AT2. Inhibition of aldosterone secretion may increase sodium and water excretion while decreasing potassium excretion.
n3:packager
n10:271B6493-363D-11E5-9242-09173F13E4C5 n10:271B6494-363D-11E5-9242-09173F13E4C5 n10:271B6491-363D-11E5-9242-09173F13E4C5 n10:271B6492-363D-11E5-9242-09173F13E4C5 n10:271B648F-363D-11E5-9242-09173F13E4C5 n10:271B6490-363D-11E5-9242-09173F13E4C5 n10:271B648D-363D-11E5-9242-09173F13E4C5 n10:271B648E-363D-11E5-9242-09173F13E4C5
n3:patent
n26:5534534 n26:2083305 n26:2040955 n26:5705517
n3:routeOfElimination
When candesartan is administered orally, about 26% of the dose is excreted unchanged in urine. Candesartan is mainly excreted unchanged in urine and feces (via bile).
n3:synonym
CV-11974 Blopress Candesartan cilexetil 2-Ethoxy-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-benzimidazole-7-carboxylic acid 2-Ethoxy-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4ethyl]}-1H-benzimidazole-7-carboxylic acid 2-Ethoxy-1-(P-(O-1H-tetrazol-5-ylphenyl)benzyl)-7-benzimidazolecarboxylic acid
n3:toxicity
No lethality was observed in acute toxicity studies in mice, rats and dogs given single oral doses of up to 2000 mg/kg of candesartan cilexetil or in rats given single oral doses of up to 2000 mg/kg of candesartan cilexetil in combination with 1000 mg/kg of hydrochlorothiazide. In mice given single oral doses of the primary metabolite, candesartan, the minimum lethal dose was greater than 1000 mg/kg but less than 2000 mg/kg.
n3:volumeOfDistribution
* 0.13 L/kg
n30:hasAHFSCode
n31:24-32-08
n3:foodInteraction
Take without regard to meals. Administer on a regular basis, at about the same time each day.
n3:mixture
n20:271B648C-363D-11E5-9242-09173F13E4C5
n3:proteinBinding
Candesartan is highly bound to plasma proteins (>99%) and does not penetrate red blood cells.
n3:synthesisReference
Marina Etinger, Boris Fedotev, Ben-Zion Dolitzky, "Preparation of candesartan cilexetil." U.S. Patent US20050131037, issued June 16, 2005.
n24:hasConcept
n25:M0217705
foaf:page
n23:candesartan.html n35:candesar.htm
n3:IUPAC-Name
n5:271B64AA-363D-11E5-9242-09173F13E4C5
n3:InChI
n5:271B64B0-363D-11E5-9242-09173F13E4C5
n3:Molecular-Formula
n5:271B64AF-363D-11E5-9242-09173F13E4C5
n3:Molecular-Weight
n5:271B64AC-363D-11E5-9242-09173F13E4C5
n3:Monoisotopic-Weight
n5:271B64AD-363D-11E5-9242-09173F13E4C5
n3:SMILES
n5:271B64AE-363D-11E5-9242-09173F13E4C5
n3:Water-Solubility
n5:271B64A8-363D-11E5-9242-09173F13E4C5
n3:logP
n5:271B64A9-363D-11E5-9242-09173F13E4C5 n5:271B64C0-363D-11E5-9242-09173F13E4C5 n5:271B64A6-363D-11E5-9242-09173F13E4C5
n3:logS
n5:271B64A7-363D-11E5-9242-09173F13E4C5
n30:hasATCCode
n32:C09CA06
n3:H-Bond-Acceptor-Count
n5:271B64B6-363D-11E5-9242-09173F13E4C5
n3:H-Bond-Donor-Count
n5:271B64B7-363D-11E5-9242-09173F13E4C5
n3:InChIKey
n5:271B64B1-363D-11E5-9242-09173F13E4C5
n3:Polar-Surface-Area--PSA-
n5:271B64B2-363D-11E5-9242-09173F13E4C5
n3:Polarizability
n5:271B64B4-363D-11E5-9242-09173F13E4C5
n3:Refractivity
n5:271B64B3-363D-11E5-9242-09173F13E4C5
n3:Rotatable-Bond-Count
n5:271B64B5-363D-11E5-9242-09173F13E4C5
n3:absorption
Following administration of the candesartan cilexetil prodrug, the absolute bioavailability of candesartan was estimated to be 15%. Food with a high fat content has no affect on the bioavailability of candesartan from candesartan cilexetil.
n3:affectedOrganism
Humans and other mammals
n3:casRegistryNumber
139481-59-7
n3:category
n3:clearance
* 0.37 mL/min/kg
n3:containedIn
n4:271B6496-363D-11E5-9242-09173F13E4C5 n4:271B64A0-363D-11E5-9242-09173F13E4C5 n4:271B64A1-363D-11E5-9242-09173F13E4C5 n4:271B649E-363D-11E5-9242-09173F13E4C5 n4:271B649F-363D-11E5-9242-09173F13E4C5 n4:271B649C-363D-11E5-9242-09173F13E4C5 n4:271B649D-363D-11E5-9242-09173F13E4C5 n4:271B649A-363D-11E5-9242-09173F13E4C5 n4:271B649B-363D-11E5-9242-09173F13E4C5 n4:271B6498-363D-11E5-9242-09173F13E4C5 n4:271B6499-363D-11E5-9242-09173F13E4C5 n4:271B6497-363D-11E5-9242-09173F13E4C5
n3:Bioavailability
n5:271B64BC-363D-11E5-9242-09173F13E4C5
n3:Ghose-Filter
n5:271B64BE-363D-11E5-9242-09173F13E4C5
n3:MDDR-Like-Rule
n5:271B64BF-363D-11E5-9242-09173F13E4C5
n3:Number-of-Rings
n5:271B64BB-363D-11E5-9242-09173F13E4C5
n3:Physiological-Charge
n5:271B64BA-363D-11E5-9242-09173F13E4C5
n3:Rule-of-Five
n5:271B64BD-363D-11E5-9242-09173F13E4C5
n3:Traditional-IUPAC-Name
n5:271B64AB-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-acidic-
n5:271B64B8-363D-11E5-9242-09173F13E4C5
n3:pKa--strongest-basic-
n5:271B64B9-363D-11E5-9242-09173F13E4C5