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Angiotensin 2 Receptor Blocking AgentAka: Angiotensin Receptor Blocker, Losartan, Cozaar, Irbesartan, Avapro, Candesartan, Atacand, Eprosartan, Teveten, Telmisartan, Micardis, Valsartan, Diovan, Olmesartan, Benicar, Angiotensin Blocker

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  1. Indications
    1. Intolerance to ACE Inhibitor
    2. See ACE Inhibitor for indications
  2. Mechanism
    1. Renin-Angiotensin System
  3. Preparations
    1. Losartan (Cozaar)
      1. Start
        1. Normal: 50 mg PO qd (MAX 100 mg/day)
        2. Volume depleted: Start at 25 mg qd
      2. Takes 4-6 weeks to see peak effect
    2. Irbesartan (Avapro)
      1. Start 150 mg PO qd (max 300 mg/day)
    3. Candesartan (Atacand) 8 mg PO qd (maximum 32 mg/day)
    4. Eprosartan (Teveten) 400 mg PO qd (maximum 800 mg/day)
    5. Telmisartan (Micardis) 40 mg PO qd (maximum 80 mg/day)
    6. Valsartan (Diovan) 80 mg PO qd (maximum 320 mg/day)
    7. Olmesartan (Benicar) 20 mg PO qd (maximum 40 mg PO qd)
  4. Efficacy
    1. Proteinuria control is equivalent to ACE Inhibitors
      1. Kunz (2008) Ann Intern Med 148:30
    2. Not as effective as ACE Inhibitors in Myocardial Infarction prevention
      1. ARBs do not effect Angiotensin II type 2 receptors
      2. Results in less effect on fibrosis and blood flow
      3. Unlike ACE Inhibitors, ARBs don't effect nitric oxide
      4. (2005) Prescriber's Letter 12:31-2
    3. Reduces cardiovascular death, Cerebrovascular Accident and Myocardial Infarction risk
      1. Higher level cardiovascular protection than Atenolol
        1. However Atenolol is not the best Beta Blocker for cardiovascular disease prevention
      2. Dahlof (2002) Lancet 359:995
  5. References
    1. Burnier (2000) Lancet 355(9204):637
    2. Califf (2000) Am Heart J 139:S15
    3. Jacobsen (2001) {a 6854} 56(2):20

Losartan (C0126174)

Definition (CSP)antihypertensive agent; nonpeptide angiotension 1 subtype; angiotension 2 receptor antagonist/inhibitor.
Definition (MSH)An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Definition (NCI)The potassium salt form of losartan, a non-peptide angiotensin II antagonist with antihypertensive activity. Losartan potassium selectively and competitively blocks the binding of angiotensin II to the angiotensin I (AT1) receptor. Angiotensin II, formed from angiotensin I by angiotensin-converting enzyme (ACE), stimulates the adrenal cortex to synthesize and secrete aldosterone, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. Losartan potassium, by blocking the binding of angiotensin II to the AT 1 receptor, promotes vasodilatation and decreases the effects of aldosterone.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD019808
EnglishLosartan, LOSARTAN PREPARATION, lozartan
Spanishlosartan, losartano
Parent ConceptsAngiotensin Receptor Antagonists (C0815017), Antihypertensive Agents (C0003364), Biphenyl Compounds (C0005580), Imidazoles (C0020924), Tetrazoles (C0039703), Angiotensin II receptor antagonist (substance) (C0521942), [CV805] ANGIOTENSIN II INHIBITORS (C0973518)
SourcesAOD, CSP, MSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


valsartan (C0216784)

Definition (NCI)An orally active nonpeptide triazole-derived antagonist of angiotensin (AT) II with antihypertensive properties. Valsartan selectively and competitively blocks the binding of angiotensin II to the AT1 subtype receptor in vascular smooth muscle and the adrenal gland, preventing AT II-mediated vasoconstriction, aldosterone synthesis and secretion, and renal reabsorption of sodium, and resulting in vasodilation, increased excretion of sodium and water, a reduction in plasma volume, and a reduction in blood pressure.
Definition (PDQ)An orally active nonpeptide triazole-derived antagonist of angiotensin (AT) II with antihypertensive properties. Valsartan selectively and competitively blocks the binding of angiotensin II to the AT1 subtype receptor in vascular smooth muscle and the adrenal gland, preventing AT II-mediated vasoconstriction, aldosterone synthesis and secretion, and renal reabsorption of sodium, and resulting in vasodilation, increased excretion of sodium and water, a reduction in plasma volume, and a reduction in blood pressure. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=464172&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=464172&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C47781" NCI Thesaurus)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC081489
Englishvalsartan, VALSARTAN PREPARATION
Spanishvalsartan, valsartano
Parent ConceptsAngiotensin II receptor antagonist (substance) (C0521942), Tetrazoles (C0039703), Valine (C0042285), [CV805] ANGIOTENSIN II INHIBITORS (C0973518)
SourcesMSH, MTHSPL, NCI, NDFRT, PDQ, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


telmisartan (C0248719)

Definition (NCI)A benzimidazole derivative and a non-peptide angiotensin II receptor antagonist with antihypertensive property. Telmisartan selectively antagonizes angiotensin II binding to the AT1 subtype receptor, located in vascular smooth muscle and adrenal gland. The antagonism results in vasodilation and inhibits the angiotensin II-mediated aldosterone production, which in turn leading to a decrease in sodium and water as well as an increase in potassium excretion leading to a subsequent reduction in blood pressure.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC084178
Englishtelmisartan, TELMISARTAN PREPARATION
Spanishtelmisartan, telmisartano
Parent ConceptsAngiotensin II receptor antagonist (substance) (C0521942), Benzimidazoles (C0005050), Benzoates (C0005058), [CV805] ANGIOTENSIN II INHIBITORS (C0973518), Duplicate concept (C1274013)
SourcesMSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


eprosartan (C0287041)

Definition (NCI)A competitive and reversible angiotensin II receptor antagonist with anti-hypertensive property. Eprosartan blocks the binding of angiotensin II to the angiotensin (AT)1 receptor in vascular smooth muscle, thereby blocking the principal pressor action of angiotensin II on the renin-angiotensin system resulting in vascular dilatation. In addition, this agent blocks angiotensin II -induced stimulation of aldosterone synthesis and secretion by the adrenal cortex, cardiac contraction, renal resorption of sodium, activity of the sympathetic nervous system, and smooth muscle cell growth. Furthermore, eprosartan inhibits sympathetic norepinephrine production, thereby further reducing blood pressure.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC068373
Englisheprosartan, EPROSARTAN PREPARATION
Spanisheprosartan
Parent ConceptsAngiotensin II receptor antagonist (substance) (C0521942), Acrylates (C0001219), Imidazoles (C0020924), [CV805] ANGIOTENSIN II INHIBITORS (C0973518)
SourcesMSH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


irbesartan (C0288171)

Definition (CSP)antihypertensive; nonpeptide angiotension 1 subtype; angiotension 2 receptor antagonist.
Definition (NCI)A nonpeptide angiotensin II antagonist with antihypertensive activity. Irbesartan selectively and competitively blocks the binding of angiotensin II to the angiotensin I receptor. Angiotensin II stimulates aldosterone synthesis and secretion by adrenal cortex, which decreases the excretion of sodium and increases the excretion of potassium. Angiotensin II also acts as a vasoconstrictor in vascular smooth muscle. (NCI05)
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC081309
Englishirbesartan, IRBESARTAN PREPARATION
Spanishirbesartan, irbesartano
Parent ConceptsAntihypertensive Agents (C0003364), Angiotensin II receptor antagonist (substance) (C0521942), Biphenyl Compounds (C0005580), Tetrazoles (C0039703), [CV805] ANGIOTENSIN II INHIBITORS (C0973518)
SourcesCSP, MSH, MTHSPL, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Cozaar (C0591301)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHD019808
EnglishCozaar
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Avapro (C0595301)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC081309
EnglishAprovel, Avapro, BMS Brand of Irbesartan, Bristol Myers Brand of Irbesartan, Karvea, Sanofi Winthrop Brand of Irbesartan
SourcesMSH, MTH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


candesartan (C0717550)

Definition (NCI)A synthetic benzimidazole-carboxylate derivative and angiotensin II receptor antagonist with antihypertensive activity. Candesartan selectively competes with angiotensin II for the binding of the angiotensin II (AT1) receptor subtype 1 in vascular smooth muscle, thereby blocking angiotensin II-mediated vasoconstriction resulting in vascular dilatation. In addition, the antagonistic effect on AT1 in the adrenal gland, prevents angiotensin II-induced stimulation of aldosterone synthesis and secretion by the adrenal cortex. This blocks the effects of aldosterone leading to an increase in sodium excretion and water and eventually a reduction in plasma volume and blood pressure.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC081643
Englishcandesartan, CANDESARTAN PREPARATION
Spanishcandesartan, candesartano
Parent ConceptsAngiotensin II receptor antagonist (substance) (C0521942), CV 11974 (C0217087), [CV805] ANGIOTENSIN II INHIBITORS (C0973518)
SourcesMSH, MTH, NCI, NDFRT, RXNORM, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Atacand (C0718711)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC077793
EnglishAmias, Astra brand of candesartan cilexetil, AstraZeneca brand of candesartan cilexetil, Atacand, Blopress, Kenzen, Promed brand of candesartan cilexetil, Takeda brand of candesartan cilexetil
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Diovan (C0719949)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC081489
EnglishDiovan, Novartis brand of valsartan, Tareg
SourcesMSH, NCI, PDQ, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Micardis (C0721704)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC084178
EnglishAbbott brand of telmisartan, Boehringer Ingelheim brand of telmisartan, Micardis
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


Teveten (C0876891)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC068373
EnglishTeveten
SourcesMSH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)


olmesartan (C1098320)

Definition (NCI)A synthetic imidazole derivative and angiotensin II receptor antagonist with antihypertensive activity. Olmesartan selectively binds to the angiotensin type 1 (AT1) receptor subtype in vascular smooth muscle and adrenal gland, thereby competing with angiotensin II for binding to the AT1 receptor. This prevents angiotensin II-induced vasoconstriction and interferes with angiotensin II-mediated aldosterone secretion, thereby decreasing aldosterone production and preventing aldosterone-stimulated sodium retention and potassium excretion.
ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC437965
Englisholmesartan, OLMESARTAN PREPARATION, omesartan
Spanisholmesartan
Parent ConceptsAngiotensin II receptor antagonist (substance) (C0521942), [CV805] ANGIOTENSIN II INHIBITORS (C0973518), Unclassified Ingredients (C1372954)
SourcesMSH, MTH, NCI, NDFRT, SCTSPA, SNOMEDCT, USPMG, VANDF
Derived from the NIH UMLS (Unified Medical Language System)


Benicar (C1122245)

ConceptsOrganic Chemical (T109) , Pharmacologic Substance (T121)
MSHC097933
EnglishBenicar, Forest Brand of Olmesartan Medoxomil, Olmetec, Sankyo Brand of Olmesartan Medoxomil
SourcesMSH, MTH, NCI, RXNORM
Derived from the NIH UMLS (Unified Medical Language System)



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