The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Micardis     2-[4-[[4-methyl-6-(1- methylbenzoimidazol-2...

Synonyms: Kinzal, Kinzalmono, Pritor, Targit, Telmisartan, ...
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.

Disease relevance of Micardis


Psychiatry related information on Micardis


High impact information on Micardis


Chemical compound and disease context of Micardis

  • Moreover, the identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma modulating ability suggests new opportunities for developing third-generation ARBs and PPARgamma activators, with enhanced potential for treating hypertension, diabetes and the metabolic syndrome [10].
  • Up to one-third of patients with hypertension initially responsive to telmisartan 40 or 80 mg/day in a 4-year study required the eventual addition of HCTZ 12.5 or 25 mg/day and/or another agent to maintain BP control [11].
  • OBJECTIVE: To assess the antihypertensive efficacy and safety of the novel AT1 receptor antagonist, telmisartan, compared with that of enalapril in elderly patients with mild to moderate hypertension [12].
  • METHODS: We studied 70 subjects (32 men and 38 women) aged 47.6 +/- 12.2 (mean +/- SD) years, with mild to moderate essential hypertension; they were randomly assigned to receive monotherapy with either telmisartan (80 mg) or valsartan (160 mg), in the form of a single daily tablet upon awakening [13].
  • When administered at dosages of 40 to 160 mg once daily to patients with mild to moderate hypertension, telmisartan significantly reduced systolic and diastolic BP compared with placebo and was at least as effective as atenolol 50 or 100 mg and lisinopril 10 to 40 mg [4].

Biological context of Micardis


Anatomical context of Micardis


Associations of Micardis with other chemical compounds

  • The dual inhibition of angiotensin II function by telmisartan - AT1R blockade and downregulation - would contribute to more complete inhibition of the renin-angiotensin system [15].
  • PATIENTS AND METHODS: A 2-4-week single-blind placebo run-in was followed by randomization of 1039 patients (age 36-84 years) with ISH [seated SBP 150-179 mmHg and seated diastolic blood pressure (DBP) < 90 mmHg] to once-daily double-blind treatment with telmisartan 20, 40 or 80 mg, HCTZ 12.5 mg, or placebo [18].
  • The concentrations that reduced the enhancement by 50% (IC50 values, expressed as -log mol/l +/- SEM) were 9.05 +/- 0.16 losartan, 10.28 +/- 0.20 telmisartan and 9.20 +/- 0.23 irbesartan [19].
  • Mean changes in supine systolic blood pressure were -22.1 mmHg for telmisartan and -20.1 mmHg for enalapril (P = 0.350) [12].
  • The trough : peak ratio and the smoothness index were slightly higher in systolic, but similar in diastolic blood pressure, for telmisartan as compared to valsartan [13].

Gene context of Micardis

  • Taken together, our in vitro data show that the insurmountable antagonism of telmisartan is due at least in part to its very slow dissociation from AT1 receptors [20].
  • In the present study, we have characterized the contribution of organic anion transporting polypeptide (OATP) isoforms to the hepatic uptake of telmisartan by isolated rat hepatocytes, human cryopreserved hepatocytes, and human transporter-expressing cells [21].
  • To identify which human OATP transporters are important for the hepatic uptake of telmisartan, the uptake assay was carried out using OATP1B1- and OATP1B3-expressing human embryonic kidney 293 cells and cryopreserved human hepatocytes [21].
  • AT1-R signaling blockade with telmisartan inhibited various inflammatory mechanisms including macrophage infiltration and upregulation of VEGF, intercellular adhesion molecule-1 (ICAM-1), MCP-1, and IL-6 in the retinal pigment epithelium-choroid complex [22].
  • Our data demonstrate that the effects of ANG II on collagen secretion and production in adult rat cardiac fibroblasts in culture are AT1-receptor mediated since they were abolished by the specific AT1-receptor antagonist telmisartan but not by the specific AT2-receptor antagonist P-186 [23].

Analytical, diagnostic and therapeutic context of Micardis


  1. Molecular Characterization of New Selective Peroxisome Proliferator-Activated Receptor {gamma} Modulators With Angiotensin Receptor Blocking Activity. Schupp, M., Clemenz, M., Gineste, R., Witt, H., Janke, J., Helleboid, S., Hennuyer, N., Ruiz, P., Unger, T., Staels, B., Kintscher, U. Diabetes (2005) [Pubmed]
  2. Insulin-sensitizing effects of telmisartan: implications for treating insulin-resistant hypertension and cardiovascular disease. Pershadsingh, H.A., Kurtz, T.W. Diabetes Care (2004) [Pubmed]
  3. Telmisartan: a review of its use in the management of hypertension. Battershill, A.J., Scott, L.J. Drugs (2006) [Pubmed]
  4. Telmisartan. McClellan, K.J., Markham, A. Drugs (1998) [Pubmed]
  5. Angiotensin II receptor blockade in TGR(mREN2)27: effects of renin-angiotensin-system gene expression and cardiovascular functions. Böhm, M., Lee, M., Kreutz, R., Kim, S., Schinke, M., Djavidani, B., Wagner, J., Kaling, M., Wienen, W., Bader, M. J. Hypertens. (1995) [Pubmed]
  6. Angiotensin II Receptor Blockers Downsize Adipocytes in Spontaneously Type 2 Diabetic Rats With Visceral Fat Obesity. Mori, Y., Itoh, Y., Tajima, N. Am. J. Hypertens. (2007) [Pubmed]
  7. Inhibition of angiotensin I-converting enzyme induces radioprotection by preserving murine hematopoietic short-term reconstituting cells. Charrier, S., Michaud, A., Badaoui, S., Giroux, S., Ezan, E., Sainteny, F., Corvol, P., Vainchenker, W. Blood (2004) [Pubmed]
  8. Telmisartan inhibits AGE-induced C-reactive protein production through downregulation of the receptor for AGE via peroxisome proliferator-activated receptor-gamma activation. Yoshida, T., Yamagishi, S., Nakamura, K., Matsui, T., Imaizumi, T., Takeuchi, M., Koga, H., Ueno, T., Sata, M. Diabetologia (2006) [Pubmed]
  9. Telmisartan inhibits beta2-integrin MAC-1 expression in human T-lymphocytes. Link, A., Lenz, M., Legner, D., Böhm, M., Nickenig, G. J. Hypertens. (2006) [Pubmed]
  10. Antidiabetic mechanisms of angiotensin-converting enzyme inhibitors and angiotensin II receptor antagonists: beyond the renin-angiotensin system. Kurtz, T.W., Pravenec, M. J. Hypertens. (2004) [Pubmed]
  11. Telmisartan/hydrochlorothiazide: in the treatment of essential hypertension. Fenton, C., Keating, G.M., Scott, L.J. Drugs (2003) [Pubmed]
  12. Efficacy and safety of telmisartan, a selective AT1 receptor antagonist, compared with enalapril in elderly patients with primary hypertension. TEES Study Group. Karlberg, B.E., Lins, L.E., Hermansson, K. J. Hypertens. (1999) [Pubmed]
  13. Effects of telmisartan 80 mg and valsartan 160 mg on ambulatory blood pressure in patients with essential hypertension. Calvo, C., Hermida, R.C., Ayala, D.E., Ruilope, L.M. J. Hypertens. (2004) [Pubmed]
  14. Neuroprotective Effects of Angiotensin II Type 1 Receptor (AT1R) Blocker, Telmisartan, via Modulating AT1R and AT2R Signaling in Retinal Inflammation. Kurihara, T., Ozawa, Y., Shinoda, K., Nagai, N., Inoue, M., Oike, Y., Tsubota, K., Ishida, S., Okano, H. Invest. Ophthalmol. Vis. Sci. (2006) [Pubmed]
  15. Telmisartan downregulates angiotensin II type 1 receptor through activation of peroxisome proliferator-activated receptor gamma. Imayama, I., Ichiki, T., Inanaga, K., Ohtsubo, H., Fukuyama, K., Ono, H., Hashiguchi, Y., Sunagawa, K. Cardiovasc. Res. (2006) [Pubmed]
  16. Angiotensin type 1 receptor antagonists induce human in-vitro adipogenesis through peroxisome proliferator-activated receptor-gamma activation. Janke, J., Schupp, M., Engeli, S., Gorzelniak, K., Boschmann, M., Sauma, L., Nystrom, F.H., Jordan, J., Luft, F.C., Sharma, A.M. J. Hypertens. (2006) [Pubmed]
  17. Suppression of ocular inflammation in endotoxin-induced uveitis by blocking the angiotensin II type 1 receptor. Nagai, N., Oike, Y., Noda, K., Urano, T., Kubota, Y., Ozawa, Y., Shinoda, H., Koto, T., Shinoda, K., Inoue, M., Tsubota, K., Yamashiro, K., Suda, T., Ishida, S. Invest. Ophthalmol. Vis. Sci. (2005) [Pubmed]
  18. Angiotensin II receptor antagonist telmisartan in isolated systolic hypertension (ARAMIS) study: efficacy and safety of telmisartan 20, 40 or 80 mg versus hydrochlorothiazide 12.5 mg or placebo. Manolis, A.J., Reid, J.L., de Zeeuw, D., Murphy, M.B., Seewaldt-Becker, E., Köster, J. J. Hypertens. (2004) [Pubmed]
  19. Sympatholytic properties of several AT1-receptor antagonists in the isolated rabbit thoracic aorta. Nap, A., Balt, J.C., Pfaffendorf, M., Van Zwieten, P.A. J. Hypertens. (2002) [Pubmed]
  20. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. Maillard, M.P., Perregaux, C., Centeno, C., Stangier, J., Wienen, W., Brunner, H.R., Burnier, M. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  21. Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Ishiguro, N., Maeda, K., Kishimoto, W., Saito, A., Harada, A., Ebner, T., Roth, W., Igarashi, T., Sugiyama, Y. Drug Metab. Dispos. (2006) [Pubmed]
  22. Angiotensin II Type 1 Receptor-Mediated Inflammation Is Required for Choroidal Neovascularization. Nagai, N., Oike, Y., Izumi-Nagai, K., Urano, T., Kubota, Y., Noda, K., Ozawa, Y., Inoue, M., Tsubota, K., Suda, T., Ishida, S. Arterioscler. Thromb. Vasc. Biol. (2006) [Pubmed]
  23. Induction of cardiac fibrosis by angiotensin II. Lijnen, P.J., Petrov, V.V., Fagard, R.H. Methods and findings in experimental and clinical pharmacology. (2000) [Pubmed]
  24. The prospective, randomized investigation of the safety and efficacy of telmisartan versus ramipril using ambulatory blood pressure monitoring (PRISMA I). Williams, B., Gosse, P., Lowe, L., Harper, R. J. Hypertens. (2006) [Pubmed]
  25. Selective suppression of pathologic, but not physiologic, retinal neovascularization by blocking the angiotensin II type 1 receptor. Nagai, N., Noda, K., Urano, T., Kubota, Y., Shinoda, H., Koto, T., Shinoda, K., Inoue, M., Shiomi, T., Ikeda, E., Tsubota, K., Suda, T., Oike, Y., Ishida, S. Invest. Ophthalmol. Vis. Sci. (2005) [Pubmed]
  26. Inhibition of angiotensin II-induced facilitation of sympathetic neurotransmission in the pithed rat: a comparison between losartan, irbesartan, telmisartan, and captopril. Balt, J.C., Mathy, M.J., Pfaffendorf, M., van Zwieten, P.A. J. Hypertens. (2001) [Pubmed]
WikiGenes - Universities