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Angiotensin 2 Receptor Blocking Agent

Aka: Angiotensin 2 Receptor Blocking Agent, Angiotensin Receptor Blocker, Angiotensin Blocker, Losartan, Cozaar, Irbesartan, Avapro, Candesartan, Atacand, Eprosartan, Teveten, Telmisartan, Micardis, Valsartan, Diovan, Olmesartan, Benicar
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  1. Indications
    1. Intolerance to ACE Inhibitor
    2. See ACE Inhibitor for indications
  2. Contraindications
    1. See ACE Inhibitor for contraindications
  3. Mechanism
    1. Renin-Angiotensin System
  4. Preparations
    1. Losartan (Cozaar)
      1. Start: 50 mg orally daily or 25 mg daily if volume depleted (MAX 100 mg/day)
      2. Consider twice daily dosing
    2. Irbesartan (Avapro)
      1. Start 150 mg orally daily (max 300 mg/day)
    3. Candesartan (Atacand)
      1. Start 8 mg orally daily (maximum 32 mg/day)
    4. Eprosartan (Teveten)
      1. Start 400 mg orally daily (maximum 800 mg/day)
    5. Telmisartan (Micardis)
      1. Start 40 mg orally daily (maximum 80 mg/day)
    6. Valsartan (Diovan)
      1. Start 80 mg orally daily (maximum 320 mg/day)
    7. Olmesartan (Benicar)
      1. Start 20 mg orally daily (maximum 40 mg/day)
    8. Azilsartan (Edarbi)
      1. Start 40 mg orally daily (maximum 80 mg/day)
  5. Protocol: Equivalent dosing (switching between agents)
    1. Losartan (Cozaar) 100 mg daily or divided twice daily
    2. Irbesartan (Avapro) 300 mg daily
    3. Candesartan (Atacand) 16 mg daily
    4. Eprosartan (Teveten) 800 mg daily
    5. Telmisartan (Micardis) 40 mg daily
    6. Valsartan (Diovan) 160 mg daily
    7. Olmesartan (Benicar) 20 mg daily
    8. Azilsartan (Edarbi) 40 mg daily
  6. Efficacy
    1. Peak effect may require 4-6 weeks
    2. Proteinuria control is equivalent to ACE Inhibitors
      1. Kunz (2008) Ann Intern Med 148:30-48.
    3. 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
    4. Avoid in combination with ACE Inhibitors
      1. No advantage to combinations in Hypertension, vascular disease, Diabetes Mellitus and Coronary Artery Disease
      2. Moderate benefit of combination therapy in Congestive Heart Failure
      3. (2013) Prescr Lett 20(3): 13
    5. 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 359:995-1003
  7. References
    1. Burnier (2000) Lancet 355(9204):637-45
    2. Califf (2000) Am Heart J 139:S15-22
    3. Jacobsen (2001) Geriatrics 56(2):20-28
Medication Costs
Losartan Potassium (on 2/9/2012 at DrugStore.com)
Losartan Potassium 50mg Tablets #90 for $176.99 ($1.97/unit)
Losartan Potassium 25mg Tablets #90 for $125.99 ($1.40/unit)
Losartan Potassium 100mg Tablets #90 for $259.97 ($2.89/unit)
Losartan Potassium-HCTZ (on 2/9/2012 at DrugStore.com)
Losartan Potassium-HCTZ 30 50-12.5mg Tablets Bottle #1 for $69.99 ($69.99/unit)
Losartan Potassium-HCTZ 100-25mg Tablets #30 for $97.99 ($3.27/unit)
Losartan Potassium-HCTZ 100-12.5mg Tablets #30 for $95.99 ($3.20/unit)
Cozaar (on 2/9/2012 at DrugStore.com)
Cozaar 25mg Tablets #30 for $64.28 ($2.14/unit)
Cozaar 50mg Tablets #30 for $88.13 ($2.94/unit)
Avapro (on 2/9/2012 at DrugStore.com)
Avapro 75mg Tablets #30 for $95.91 ($3.20/unit)
Avapro 150mg Tablets #30 for $98.99 ($3.30/unit)
Avapro 300mg Tablets #30 for $119.99 ($4.00/unit)
Atacand (on 2/9/2012 at DrugStore.com)
Atacand 4mg Tablets #30 for $84.99 ($2.83/unit)
Atacand 8mg Tablets #30 for $77.99 ($2.60/unit)
Atacand 16mg Tablets #30 for $85.99 ($2.87/unit)
Atacand 32mg Tablets #30 for $111.99 ($3.73/unit)
Atacand HCT (on 2/9/2012 at DrugStore.com)
Atacand HCT 16-12.5mg Tablets #30 for $110.99 ($3.70/unit)
Atacand HCT 32-12.5mg Tablets #30 for $115.99 ($3.87/unit)
Atacand HCT 32-25mg Tablets #30 for $115.99 ($3.87/unit)
Teveten HCT (on 2/9/2012 at DrugStore.com)
Teveten HCT 600-12.5mg Tablets #30 for $120.99 ($4.03/unit)
Teveten HCT 600-25mg Tablets #30 for $109.98 ($3.67/unit)
Teveten (on 2/9/2012 at DrugStore.com)
Teveten 400mg Tablets #30 for $90.99 ($3.03/unit)
Teveten 600mg Tablets #30 for $109.99 ($3.67/unit)
Micardis (on 2/9/2012 at DrugStore.com)
Micardis 30 20mg Tablets Box #1 for $123.19 ($123.19/unit)
Micardis 30 40mg Tablets Box #1 for $123.99 ($123.99/unit)
Micardis 30 80mg Tablets Box #1 for $122.99 ($122.99/unit)
Micardis HCT (on 2/9/2012 at DrugStore.com)
Micardis HCT 30 80-25mg Tablets Box #1 for $123.99 ($123.99/unit)
Micardis HCT 30 40-12.5mg Tablets Box #1 for $123.99 ($123.99/unit)
Micardis HCT 30 80-12.5mg Tablets Box #1 for $122.00 ($122.00/unit)
Diovan HCT (on 2/9/2012 at DrugStore.com)
Diovan HCT 80-12.5mg Tablets #30 for $110.99 ($3.70/unit)
Diovan HCT 160-12.5mg Tablets #30 for $115.99 ($3.87/unit)
Diovan HCT 160-25mg Tablets #30 for $129.99 ($4.33/unit)
Diovan HCT 320-12.5mg Tablets #30 for $142.99 ($4.77/unit)
Diovan HCT 320-25mg Tablets #30 for $168.99 ($5.63/unit)
Diovan (on 2/9/2012 at DrugStore.com)
Diovan 80mg Tablets #30 for $100.99 ($3.37/unit)
Diovan 160mg Tablets #30 for $107.99 ($3.60/unit)
Diovan 320mg Tablets #30 for $131.99 ($4.40/unit)
Diovan 40mg Tablets #30 for $89.99 ($3.00/unit)
Benicar (on 2/9/2012 at DrugStore.com)
Benicar 5mg Tablets #30 for $78.99 ($2.63/unit)
Benicar 20mg Tablets #30 for $95.99 ($3.20/unit)
Benicar 40mg Tablets #30 for $134.99 ($4.50/unit)
Benicar HCT (on 2/9/2012 at DrugStore.com)
Benicar HCT 20-12.5mg Tablets #30 for $96.99 ($3.23/unit)
Benicar HCT 40-12.5mg Tablets #30 for $135.99 ($4.53/unit)
Benicar HCT 40-25mg Tablets #30 for $135.99 ($4.53/unit)
FPNotebook does not benefit financially from showing this medication data or their pharmacy links. This information is provided only to help medical providers and their patients see relative costs. Insurance plans negotiate lower medication prices with suppliers. Prices shown here are out of pocket, non-negotiated rates. See Needy Meds for financial assistance information.

Losartan (C0126174)

Definition (CHV) a drug used to treat hypertension
Definition (CHV) a drug used to treat hypertension
Definition (NCI) A drug used to treat high blood pressure. Losartan blocks the action of chemicals that make blood vessels constrict (get narrower). It is a type of angiotensin II receptor antagonist.
Definition (NCI) A drug used to treat high blood pressure. Cozaar blocks the action of chemicals that make blood vessels constrict (get narrower). It is a type of angiotensin II receptor antagonist.
Definition (MSH) An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Definition (CSP) antihypertensive agent; nonpeptide angiotension 1 subtype; angiotension 2 receptor antagonist/inhibitor.
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D019808
SnomedCT 373567002, 96309000
English losartan, Losartan, lozartan, 2-Butyl-4-chloro-1-((2'-(1H-etrazol-5-yl) (1,1'-biphenyl)-4-yl)methyl)-1H-imidazole-5-methanol, 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol, Losartan [Chemical/Ingredient], Losartan (product), Losartan (substance), LOSARTAN
Swedish Losartan
Czech losartan
Finnish Losartaani
Russian LOZARTAN, ЛОЗАРТАН
Japanese ロサルタン, ロザルタン
Croatian LOSARTAN
Spanish losartano, Losartán, Losartan, losartano (sustancia), losartán (producto), losartán (sustancia), losartán
Polish Losartan
French Losartane
German Losartan
Italian Losartan
Portuguese Losartano, Losartan
Sources
Derived from the NIH UMLS (Unified Medical Language System)


valsartan (C0216784)

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)
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C081489
SnomedCT 108581009, 386876001
English N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine, valsartan, L-Valine, N-(1-oxopentyl)-N-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, N-(p-(o-1H-Tetrazol-5-ylphenyl)benzyl)-N-valeryl-L-valine, valsartan (medication), VALSARTAN, valsartan [Chemical/Ingredient], Valsartan, Valsartan (product), Valsartan (substance)
Spanish valsartano, valsartano (sustancia), valsartán (producto), valsartán (sustancia), valsartán
Sources
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C084178
SnomedCT 318985000, 129487008, 387069000
English (1,1'-Biphenyl)-2-carboxylic acid, 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-, 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-(1,1'-biphenyl)-2-carboxylic acid, 4'-((4-Methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimidazolyl)methyl)-2-biphenylcarboxylic Acid, (1,1'-Biphenyl)-2-carboxylic Acid, 4'-((1,4'-dimethyl-2'-propyl(2,6'-bi-1H-benzimidazol)-1'-yl)methyl)-, telmisartan (medication), telmisartan, telmisartan [Chemical/Ingredient], TELMISARTAN, Telmisartan (product), Telmisartan (substance), Telmisartan
Spanish Telmisartan, telmisartano (sustancia), telmisartano, telmisartán (producto), telmisartán (sustancia), telmisartán
Sources
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C068373
SnomedCT 318990002, 396044005
English eprosartan, eprosartan [Chemical/Ingredient], Eprosartan (product), Eprosartan (substance), Eprosartan, 2-Thiophenepropanoic acid, alpha-((2-butyl-1-((4- carboxyphenyl)methyl)-lH-imidazol-5-yl)methylene)-, (E)-, EPROSARTAN
Spanish eprosartán (producto), eprosartán (sustancia), eprosartán
Sources
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)
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C081309
SnomedCT 108585000, 386877005
English 2-n-butyl-3-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)-1,3-diazaspiro(4,4)non-1-en-4-one, 1,3-Diazaspiro(4.4)non-1-en-4-one, 2-butyl-3-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, irbesartan, irbesartan (medication), IRBESARTAN, irbesartan [Chemical/Ingredient], Irbesartan, Irbesartan (product), Irbesartan (substance)
Spanish irbesartano (sustancia), irbesartano, irbesartán (producto), irbesartán (sustancia), irbesartán
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Cozaar (C0591301)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH D019808
English cozaar, Cozaar
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Avapro (C0595301)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C081309
English Aprovel, irbesartan (Avapro), avapro, aprovel, karvea, Karvea, Sanofi Winthrop Brand of Irbesartan, BMS Brand of Irbesartan, Bristol Myers Brand of Irbesartan, Avapro
Sources
Derived from the NIH UMLS (Unified Medical Language System)


candesartan (C0717550)

Definition (NCI) A synthetic, benzimidazole-derived angiotensin II receptor antagonist prodrug with antihypertensive activity. Candesartan selectively competes with angiotensin II for the binding of the angiotensin II receptor subtype 1 (AT1) in vascular smooth muscle, blocking angiotensin II-mediated vasoconstriction and inducing vasodilatation. In addition, antagonism of AT1 in the adrenal gland inhibits angiotensin II-stimulated aldosterone synthesis and secretion by the adrenal cortex; sodium and water excretion increase, followed by a reduction in plasma volume and blood pressure.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C081643
SnomedCT 108587008, 372512008
English 2-ethoxy-7-carboxy-1-(2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methylbenzimidazole, 1H-Benzimidazole-7-carboxylic acid, 2-ethoxy-1-((2'-(1H-tetrazol-5-yl)(1,1'-biphenyl)-4-yl)methyl)-, 2-Ethoxy-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-3H-benzoimidazole-4-carboxylic Acid, candesartan [Chemical/Ingredient], candesartan, Candesartan (product), Candesartan (substance), Candesartan, CANDESARTAN
Spanish candesartano (sustancia), candesartano, candesartán (producto), candesartán (sustancia), candesartán
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Atacand (C0718711)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C077793
English Atacand, Amias, atacand, blopress, Blopress, Astra brand of candesartan cilexetil, AstraZeneca brand of candesartan cilexetil, Kenzen, Promed brand of candesartan cilexetil, Takeda brand of candesartan cilexetil
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Diovan (C0719949)

Definition (CHV) brand name of a high blood pressure medication
Definition (CHV) brand name of a high blood pressure medication
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C081489
English Diovan, valsartan (Diovan), diovan, diovan [brand name], Novartis brand of valsartan, Tareg
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Micardis (C0721704)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C084178
English Micardis, telmisartan (Micardis), micardis, Boehringer Ingelheim brand of telmisartan, Abbott brand of telmisartan
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Teveten (C0876891)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C068373
English Teveten, teveten
Sources
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.
Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C437965
SnomedCT 385540001, 412259001
English olmesartan [Chemical/Ingredient], omesartan, Olmesartan (product), Olmesartan, Olmesartan (substance), OLMESARTAN, olmesartan, 4-(hydroxy-1-methylethyl)-2-propyl-1-((2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl)methyl)-1H-imidazole-5-carboxylic acid
Spanish olmesartán (producto), olmesartán, olmesartán (sustancia)
Sources
Derived from the NIH UMLS (Unified Medical Language System)


Benicar (C1122245)

Concepts Organic Chemical (T109) , Pharmacologic Substance (T121)
MSH C097933
English benicar, Forest Brand of Olmesartan Medoxomil, Olmetec, Sankyo Brand of Olmesartan Medoxomil, Benicar
Sources
Derived from the NIH UMLS (Unified Medical Language System)


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