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Chemical Compound Review

Aprovel     2-butyl-3-[[4-[2-(2H- tetrazol-5...

Synonyms: Avalide, Irbetan, Avapro, IRBESARTIN, Irbesarran, ...
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Disease relevance of Avapro


Psychiatry related information on Avapro


High impact information on Avapro

  • The average blood pressure during the course of the study was 144/83 mm Hg in the placebo group, 143/83 mm Hg in the 150-mg group, and 141/83 mm Hg in the 300-mg group (P=0.004 for the comparison of systolic blood pressure between the placebo group and the combined irbesartan groups) [7].
  • The effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes [7].
  • Hemodynamic effects of the angiotensin II receptor antagonist irbesartan in patients with cirrhosis and portal hypertension [2].
  • In these patients, baseline plasma renin (P < 0.002) and cystatin C (P < 0.001) levels were higher, and creatinine clearance (P < 0.02), serum sodium (P < 0.01), and albumin (P < 0.05) were lower than in patients who tolerated irbesartan [2].
  • RESULTS: Irbesartan reduced the hepatic venous pressure gradient by 12.2% +/- 6.6% (P < 0.05) and mean arterial pressure by 5.3% +/- 4.0% in 13 of 18 verum patients [2].

Chemical compound and disease context of Avapro


Biological context of Avapro


Anatomical context of Avapro

  • In addition, superoxide levels and monocyte-binding capacity were also significantly reduced in coronary artery disease patients receiving irbesartan [15].
  • In the peri-infarct cortex, irbesartan treatment decreased the number of apoptotic cells on day 3 and attenuated the invasion of activated microg-lia and macrophages on days 3 and 7 after ischemia [18].
  • Irbesartan pretreatment completely abolished the ischemia-induced c-Fos expression in the hippocampus [19].
  • Treatment with irbesartan can substantially improve the activity and production of these enzymes in skin fibroblasts [12].
  • The AT1 receptor antagonist irbesartan was continuously infused intracerebroventricularly using osmotic minipumps over a 5-day period before and for 3 or 7 days after middle cerebral artery occlusion (MCAO) for 90 minutes [18].

Associations of Avapro with other chemical compounds


Gene context of Avapro

  • Only IRB reduced serum IL-6 and hsCRP levels significantly compared with baseline (p < 0.01), whereas ENAL did not (hsCRP p < 0.02 IRB vs. ENAL, p < 0.01 IRB vs. ENAL) [13].
  • RESULTS: Both treatment regimens enhanced serum IL-10 levels (IRB p < 0.001, ENAL p < 0.03) and reduced serum MMP-9 protein (IRB p < 0.001, ENAL p < 0.05) and MMP-9 activity (IRB p < 0.005, ENAL p < 0.05) [13].
  • The Ang II type 1 (AT1)-receptor blocker irbesartan completely blocked DNA synthesis, migration, MAPK activation, and c-fos induction by Ang II in VSMCs [24].
  • Both the angiotensinogen 235 T-allele (P = 0.02) and the AT1-receptor 1166 AC genotype responded with the greatest reduction in LVM when treated with irbesartan (-0.1 +/- 19 g/m2 for AA and -18 +/- 30 g/m2 for AC, P = 0.02), independent of blood pressure reduction [25].
  • RESULTS: The diastolic blood pressure (DBP) response differed in relation to the CYP2C9 genotype in patients given irbesartan: the reduction in patients with genotype CYP2C9*1/CYP2C9*1 (n = 33) was 7.5% and that with CYP2C9*1/CYP2C9*2 (n = 12) was 14.4% ( P= 0.036) [26].

Analytical, diagnostic and therapeutic context of Avapro


  1. Renoprotective effect of the angiotensin-receptor antagonist irbesartan in patients with nephropathy due to type 2 diabetes. Lewis, E.J., Hunsicker, L.G., Clarke, W.R., Berl, T., Pohl, M.A., Lewis, J.B., Ritz, E., Atkins, R.C., Rohde, R., Raz, I. N. Engl. J. Med. (2001) [Pubmed]
  2. Hemodynamic effects of the angiotensin II receptor antagonist irbesartan in patients with cirrhosis and portal hypertension. Schepke, M., Werner, E., Biecker, E., Schiedermaier, P., Heller, J., Neef, M., Stoffel-Wagner, B., Hofer, U., Caselmann, W.H., Sauerbruch, T. Gastroenterology (2001) [Pubmed]
  3. Angiotensin AT1 receptor inhibition. Effects on hypertrophic remodeling and ACE expression in rats with pressure-overload hypertrophy due to ascending aortic stenosis. Weinberg, E.O., Lee, M.A., Weigner, M., Lindpaintner, K., Bishop, S.P., Benedict, C.R., Ho, K.K., Douglas, P.S., Chafizadeh, E., Lorell, B.H. Circulation (1997) [Pubmed]
  4. Headache in mild-to-moderate hypertension and its reduction by irbesartan therapy. Hansson, L., Smith, D.H., Reeves, R., Lapuerta, P. Arch. Intern. Med. (2000) [Pubmed]
  5. Effect of irbesartan monotherapy compared with ACE inhibitors and calcium-channel blockers on patient compliance in essential hypertension patients: A multicenter, open-labeled, three-armed study. Koylan, N., Acarturk, E., Canberk, A., Caglar, N., Caglar, S., Erdine, S., Guneri, S., Ilerigelen, B., Kabakci, G., Onder, R., Sagkan, O., Buyukozturk, K. Blood Press. (2005) [Pubmed]
  6. Treatment of diabetic nephropathy with angiotensin II receptor antagonist. Lewis, E.J., Lewis, J.B. Clin. Exp. Nephrol. (2003) [Pubmed]
  7. The effect of irbesartan on the development of diabetic nephropathy in patients with type 2 diabetes. Parving, H.H., Lehnert, H., Bröchner-Mortensen, J., Gomis, R., Andersen, S., Arner, P. N. Engl. J. Med. (2001) [Pubmed]
  8. Dose-related beneficial long-term hemodynamic and clinical efficacy of irbesartan in heart failure. Havranek, E.P., Thomas, I., Smith, W.B., Ponce, G.A., Bilsker, M., Munger, M.A., Wolf, R.A. J. Am. Coll. Cardiol. (1999) [Pubmed]
  9. Cardiac fibrosis occurs early and involves endothelin and AT-1 receptors in hypertension due to endogenous angiotensin II. Seccia, T.M., Belloni, A.S., Kreutz, R., Paul, M., Nussdorfer, G.G., Pessina, A.C., Rossi, G.P. J. Am. Coll. Cardiol. (2003) [Pubmed]
  10. The antiproteinuric effect of angiotensin antagonism in human IgA nephropathy is potentiated by indomethacin. Perico, N., Remuzzi, A., Sangalli, F., Azzollini, N., Mister, M., Ruggenenti, P., Remuzzi, G. J. Am. Soc. Nephrol. (1998) [Pubmed]
  11. Preserving cardiac function in the hypertensive patient: why renal parameters hold the key. Montalescot, G., Collet, J.P. Eur. Heart J. (2005) [Pubmed]
  12. Effects of irbesartan on intracellular antioxidant enzyme expression and activity in adolescents and young adults with early diabetic angiopathy. Chiarelli, F., Di Marzio, D., Santilli, F., Mohn, A., Blasetti, A., Cipollone, F., Mezzetti, A., Verrotti, A. Diabetes Care (2005) [Pubmed]
  13. Comparative effects of AT1-antagonism and angiotensin-converting enzyme inhibition on markers of inflammation and platelet aggregation in patients with coronary artery disease. Schieffer, B., Bünte, C., Witte, J., Hoeper, K., Böger, R.H., Schwedhelm, E., Drexler, H. J. Am. Coll. Cardiol. (2004) [Pubmed]
  14. The paradox of the low-renin state in diabetic nephropathy. Price, D.A., Porter, L.E., Gordon, M., Fisher, N.D., De'Oliveira, J.M., Laffel, L.M., Passan, D.R., Williams, G.H., Hollenberg, N.K. J. Am. Soc. Nephrol. (1999) [Pubmed]
  15. Irbesartan, an angiotensin type 1 receptor inhibitor, regulates the vascular oxidative state in patients with coronary artery disease. Khan, B.V., Navalkar, S., Khan, Q.A., Rahman, S.T., Parthasarathy, S. J. Am. Coll. Cardiol. (2001) [Pubmed]
  16. The pharmacokinetics of irbesartan in renal failure and maintenance hemodialysis. Sica, D.A., Marino, M.R., Hammett, J.L., Ferreira, I., Gehr, T.W., Ford, N.F. Clin. Pharmacol. Ther. (1997) [Pubmed]
  17. Short-term and sustained renal effects of angiotensin II receptor blockade in healthy subjects. Burnier, M., Hagman, M., Nussberger, J., Biollaz, J., Armagnac, C., Brouard, R., Weber, B., Brunner, H.R. Hypertension (1995) [Pubmed]
  18. Sustained blockade of brain AT1 receptors before and after focal cerebral ischemia alleviates neurologic deficits and reduces neuronal injury, apoptosis, and inflammatory responses in the rat. Lou, M., Blume, A., Zhao, Y., Gohlke, P., Deuschl, G., Herdegen, T., Culman, J. J. Cereb. Blood Flow Metab. (2004) [Pubmed]
  19. Blockade of central angiotensin AT(1) receptors improves neurological outcome and reduces expression of AP-1 transcription factors after focal brain ischemia in rats. Dai, W.J., Funk, A., Herdegen, T., Unger, T., Culman, J. Stroke (1999) [Pubmed]
  20. Improved islet morphology after blockade of the renin- angiotensin system in the ZDF rat. Tikellis, C., Wookey, P.J., Candido, R., Andrikopoulos, S., Thomas, M.C., Cooper, M.E. Diabetes (2004) [Pubmed]
  21. Opposing effects of angiotensin II on muscle and renal blood flow under euglycemic conditions. Fliser, D., Dikow, R., Demukaj, S., Ritz, E. J. Am. Soc. Nephrol. (2000) [Pubmed]
  22. Time course and extent of angiotensin II antagonism after irbesartan, losartan, and valsartan in humans assessed by angiotensin II dose response and radioligand receptor assay. Belz, G.G., Butzer, R., Kober, S., Mang, C., Mutschler, E. Clin. Pharmacol. Ther. (1999) [Pubmed]
  23. Angiotensin II receptor blockade in normotensive subjects: A direct comparison of three AT1 receptor antagonists. Mazzolai, L., Maillard, M., Rossat, J., Nussberger, J., Brunner, H.R., Burnier, M. Hypertension (1999) [Pubmed]
  24. Central role of the MAPK pathway in ang II-mediated DNA synthesis and migration in rat vascular smooth muscle cells. Xi, X.P., Graf, K., Goetze, S., Fleck, E., Hsueh, W.A., Law, R.E. Arterioscler. Thromb. Vasc. Biol. (1999) [Pubmed]
  25. Polymorphisms in the angiotensinogen and angiotensin II type 1 receptor gene are related to change in left ventricular mass during antihypertensive treatment: results from the Swedish Irbesartan Left Ventricular Hypertrophy Investigation versus Atenolol (SILVHIA) trial. Kurland, L., Melhus, H., Karlsson, J., Kahan, T., Malmqvist, K., Ohman, P., Nyström, F., Hägg, A., Lind, L. J. Hypertens. (2002) [Pubmed]
  26. The CYP2C9 genotype predicts the blood pressure response to irbesartan: results from the Swedish Irbesartan Left Ventricular Hypertrophy Investigation vs Atenolol (SILVHIA) trial. Hallberg, P., Karlsson, J., Kurland, L., Lind, L., Kahan, T., Malmqvist, K., Ohman, K.P., Nyström, F., Melhus, H. J. Hypertens. (2002) [Pubmed]
  27. Irbesartan, an angiotensin type 1 receptor inhibitor, regulates markers of inflammation in patients with premature atherosclerosis. Navalkar, S., Parthasarathy, S., Santanam, N., Khan, B.V. J. Am. Coll. Cardiol. (2001) [Pubmed]
  28. Effect of irbesartan on nitrotyrosine generation in non-hypertensive diabetic patients. Ceriello, A., Assaloni, R., Da Ros, R., Maier, A., Quagliaro, L., Piconi, L., Esposito, K., Giugliano, D. Diabetologia (2004) [Pubmed]
  29. Pre-treatment with Irbesartan attenuates left atrial stunning after electrical cardioversion of atrial fibrillation. Dagres, N., Karatasakis, G., Panou, F., Athanassopoulos, G., Maounis, T., Tsougos, E., Kourea, K., Malakos, I., Kremastinos, D.T., Cokkinos, D.V. Eur. Heart J. (2006) [Pubmed]
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