About: Losartan     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : http://linked.opendata.cz/ontology/drugbank/Drug, within Data Space : linked.opendata.cz associated with source document(s)

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http://linked.open...gbank/description
  • Losartan is an angiotensin-receptor blocker (ARB) that may be used alone or with other agents to treat hypertension. Losartan and its longer acting metabolite, E-3174, lower blood pressure by antagonizing the renin-angiotensin-aldosterone system (RAAS); they compete 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. Losartan 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 systolic dysfunction, myocardial infarction, coronary artery disease, and heart failure. (en)
http://linked.open...y/drugbank/dosage
http://linked.open...generalReferences
  • # Dahlof B, Devereux RB, Kjeldsen SE, Julius S, Beevers G, de Faire U, Fyhrquist F, Ibsen H, Kristiansson K, Lederballe-Pedersen O, Lindholm LH, Nieminen MS, Omvik P, Oparil S, Wedel H: Cardiovascular morbidity and mortality in the Losartan Intervention For Endpoint reduction in hypertension study (LIFE): a randomised trial against atenolol. Lancet. 2002 Mar 23;359(9311):995-1003. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/11937178 # Guo ZX, Qiu MC: [Losartan downregulates the expression of transforming growth factor beta type I and type II receptors in kidney of diabetic rat] Zhonghua Nei Ke Za Zhi. 2003 Jun;42(6):403-8. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/12895325 # Habashi JP, Judge DP, Holm TM, Cohn RD, Loeys BL, Cooper TK, Myers L, Klein EC, Liu G, Calvi C, Podowski M, Neptune ER, Halushka MK, Bedja D, Gabrielson K, Rifkin DB, Carta L, Ramirez F, Huso DL, Dietz HC: Losartan, an AT1 antagonist, prevents aortic aneurysm in a mouse model of Marfan syndrome. Science. 2006 Apr 7;312(5770):117-21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/16601194 # Bader, M. (2004). Renin-angiotensin-aldosterone system. In S. Offermanns, & W. Rosenthal (Eds.). _Encyclopedic reference of molecular pharmacology_ (pp. 810-814). Berlin, Germany: Springer. # Sica, D.A., Gehr, T.W.B., & Ghosh, S. (2005). Clinical pharmacokinetics of losartan. _Clinical Pharmacokinetics, 44_(8), 797-814. "PMID: 16029066":http://www.ncbi.nlm.nih.gov/pubmed/16029066 # Stanfield, C.L., & Germann, W.J. (2008). _Principles of human physiology_ (3 ^rd^ ed.). San Francisco, CA: Pearson Education, Inc. # FDA label (en)
http://linked.open...gy/drugbank/group
  • approved (en)
http://linked.open...drugbank/halfLife
  • The terminal t<sub>1/2</sub> of losartan is 2 hours. The active metabolite has a half-life of 6-9 hours. (en)
http://linked.open...ugbank/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. Losartan 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. (en)
http://linked.open...bank/manufacturer
sameAs
Title
  • Losartan (en)
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http://linked.open...mechanismOfAction
  • Losartan competitively inhibits the binding of angiotensin II to AT1 in many tissues including vascular smooth muscle and the adrenal glands. Losartan is metabolized to its active metabolite, E-3174, which is 10 to 40 times more potent than losartan and acts as a non-competitive AT1 antagonist. Inhibition of angiotensin II binding to AT1 inhibits its AT1-mediated vasoconstrictive and aldosterone-secreting effects and results in decreased vascular resistance and blood pressure. Losartan is 1,000 times more selective for AT1 than AT2. Inhibition of aldosterone secretion may increase sodium and water excretion while decreasing potassium excretion. Losartan is effective for reducing blood pressure and may be used to treat essential hypertension, left ventricular hypertrophy and diabetic nephropathy. (en)
http://linked.open...drugbank/packager
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http://linked.open...outeOfElimination
  • Following oral administration of losartan, 35% of the dose is recovered in the urine and about 60% in the feces. Following an intravenous dose, 45% is recovered in the urine and 50% in the feces. (en)
http://linked.open.../drugbank/synonym
  • Losartan (en)
  • DuP 89 (en)
  • 2-N-Butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl]imidazole (en)
  • (2-Butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanol (en)
http://linked.open...drugbank/toxicity
  • Hypotension and tachycardia; Bradycardia could occur from parasympathetic (vagal) stimulation, LD<sub>50</sub>= 1000 mg/kg (orally in rat) (en)
http://linked.open...umeOfDistribution
  • * 34 L [losartan, healthy subjects] * 12 L [active metabolite, healthy subjects] (en)
http://linked.open.../drug/hasAHFSCode
http://linked.open...k/foodInteraction
  • Take without regard to meals. Take at same time each day. Food delays absorption, but does not affect the extent of absorption. (en)
http://linked.open.../drugbank/mixture
http://linked.open...nk/proteinBinding
  • 99.7% protein bound, primarily to albumin (en)
http://linked.open...ogy/drugbank/salt
  • (en)
http://linked.open...ynthesisReference
  • Gordon C. Campbell, Jr., Anil M. Dwivedi, Dorothy A. Levorse, James A. McCauley, Krishnaswamy S. Raghavan, "Polymorphs of losartan and the process for the preparation of form II of losartan." U.S. Patent US5608075, issued May, 1994. (en)
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http://linked.open...atable-Bond-Count
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