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Chemical Compound Review

BISOPROLOL     1-(propan-2-ylamino)-3-[4-(2- propan-2...

Synonyms: Cardicor, Emconcor, Bisocor, Detensiel, Euradal, ...
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Disease relevance of BISOPROLOL


Psychiatry related information on BISOPROLOL


High impact information on BISOPROLOL

  • The effect of bisoprolol on perioperative mortality and myocardial infarction in high-risk patients undergoing vascular surgery. Dutch Echocardiographic Cardiac Risk Evaluation Applying Stress Echocardiography Study Group [1].
  • This effect was blocked by both the specific beta 1 blocker bisoprolol and the peptide P0-beta [11].
  • METHODS AND RESULTS: In 557 patients studied, bisoprolol significantly reduced heart rate (-16.3+/-15.3 versus -1.6+/-13.4 bpm, respectively; P<.001) compared with placebo at 2 months after inclusion in the study [12].
  • CONCLUSIONS: Preservation of left ventricular function appears to play a key role in the bisoprolol-induced beneficial effects on prognosis in heart failure [12].
  • The competition by (+/-)bisoprolol (beta 1-selective antagonist) and ICI 118,551 (beta 2-selective antagonist) for [125I](-)iodocyanopindolol binding sites in coronary artery resulted in nonlinear Hofstee plots (beta 1:beta 2 = 90%:10%) [13].

Chemical compound and disease context of BISOPROLOL


Biological context of BISOPROLOL


Anatomical context of BISOPROLOL

  • Furthermore, catecholamine-induced increases in lymphocyte subsets could be inhibited by pretreatment with the nonselective beta-adrenoceptor antagonist propranolol, but not by the beta1-selective antagonist bisoprolol [21].
  • Blood samples were collected for the determination of thyroid hormones and TSH concentration during L-T4 therapy and after 3 and 6 months of associated L-T4 plus bisoprolol therapy [22].
  • Bisoprolol prolongs significantly sinus cycle length, corrected sinus node recovery time, AH interval, cycle length inducing AV-node block, effective and functional refractory periods of the AV-node [23].
  • The different action on local vascular resistance in the brachial artery territory could be interpreted as the expression of the high beta 1 selectivity of bisoprolol leaving the vascular beta 2 receptors unopposed, whereas non-selective propranolol acts on both beta-adrenoceptor subtypes [20].
  • The study examines intrinsic activity, beta-adrenoceptor-G-protein coupling and beta(1)-selectivity of nebivolol and bisoprolol in human ventricular myocardium [24].

Associations of BISOPROLOL with other chemical compounds


Gene context of BISOPROLOL

  • CYP2D6 metabolized bisoprolol stereoselectively (R > S), whereas the metabolism of bisoprolol by CYP3A4 was not stereoselective [28].
  • In contrast, CYP2D6 genotype did not affect plasma concentrations of bisoprolol and the extent of its beta-adrenergic inhibition [29].
  • Therefore, the species difference in the R/S ratio of metabolic clearance for the oxidation of bisoprolol enantiomers (dog > human) is mainly due to the species difference in the stereoselectivity of one of the cytochrome P450 subfamilies (CYP3A) [30].
  • The relation between CLcr and the CL/F of bisoprolol was not altered by the CYP2D6 and CYP2C19 genotypes, gender, or age [31].
  • They also decreased the in vivo heart beating frequency of mice pretreated with bisoprolol (a beta1-adrenergic receptor antagonist) for 4 min after injection [32].

Analytical, diagnostic and therapeutic context of BISOPROLOL


  1. The effect of bisoprolol on perioperative mortality and myocardial infarction in high-risk patients undergoing vascular surgery. Dutch Echocardiographic Cardiac Risk Evaluation Applying Stress Echocardiography Study Group. Poldermans, D., Boersma, E., Bax, J.J., Thomson, I.R., van de Ven, L.L., Blankensteijn, J.D., Baars, H.F., Yo, T.I., Trocino, G., Vigna, C., Roelandt, J.R., van Urk, H. N. Engl. J. Med. (1999) [Pubmed]
  2. A multifactorial trial design to assess combination therapy in hypertension. Treatment with bisoprolol and hydrochlorothiazide. Frishman, W.H., Bryzinski, B.S., Coulson, L.R., DeQuattro, V.L., Vlachakis, N.D., Mroczek, W.J., Dukart, G., Goldberg, J.D., Alemayehu, D., Koury, K. Arch. Intern. Med. (1994) [Pubmed]
  3. Medical treatment to reduce total ischemic burden: total ischemic burden bisoprolol study (TIBBS), a multicenter trial comparing bisoprolol and nifedipine. The TIBBS Investigators. von Arnim, T. J. Am. Coll. Cardiol. (1995) [Pubmed]
  4. Long-term effects of beta-adrenergic blocking agent treatment on hemodynamic function and left ventricular remodeling in rats with experimental myocardial infarction: importance of timing of treatment and infarct size. Hu, K., Gaudron, P., Ertl, G. J. Am. Coll. Cardiol. (1998) [Pubmed]
  5. Comparison of the effects of two doses of bisoprolol on exercise tolerance in exercise-induced stable angina pectoris. de Muinck, E., Wagner, G., vd Ven, L.L., Lie, K.I. Eur. Heart J. (1987) [Pubmed]
  6. Bisoprolol-induced rapid eye movement sleep behavior disorder. Iranzo, A., Santamaria, J. Am. J. Med. (1999) [Pubmed]
  7. Predictors of medical events in patients enrolled in the cardiac insufficiency bisoprolol study (CIBIS): a study of the interactions between beta-blocker therapy and occurrence of critical events using analysis of competitive risks. Funck-Brentano, C., Lancar, R., Le Heuzey, J.Y., Lardoux, H., Soubrié, C., Lechat, P. Am. Heart J. (2000) [Pubmed]
  8. Comparative effects of bisoprolol and nitrendipine on exercise capacity in hypertensive patients with regular physical activity. Brion, R., Carré, F., Verdier, J.C., Poncelet, P., Douard, H., Page, E., Amoretti, R., Gauthier, J., Ducardonnet, A., Gressin, V., Dubanchet, A. J. Cardiovasc. Pharmacol. (2000) [Pubmed]
  9. Comparison of bisoprolol and diazepam in the treatment of cardiac neurosis. Fogari, R., Zoppi, A., Corradi, L., Pasotti, C., Malamani, G.D., Gradnik, R., Bokor, D., Gala, C. Cardiovascular drugs and therapy / sponsored by the International Society of Cardiovascular Pharmacotherapy. (1992) [Pubmed]
  10. Impact of antihypertensive treatment on quality of life: comparison between bisoprolol and bendrofluazide. Vanmolkot, F.H., de Hoon, J.N., van de Ven, L.L., Van Bortel, L.M. Journal of human hypertension. (1999) [Pubmed]
  11. Molecular mimicry between the immunodominant ribosomal protein P0 of Trypanosoma cruzi and a functional epitope on the human beta 1-adrenergic receptor. Ferrari, I., Levin, M.J., Wallukat, G., Elies, R., Lebesgue, D., Chiale, P., Elizari, M., Rosenbaum, M., Hoebeke, J. J. Exp. Med. (1995) [Pubmed]
  12. Prognostic value of bisoprolol-induced hemodynamic effects in heart failure during the Cardiac Insufficiency BIsoprolol Study (CIBIS). Lechat, P., Escolano, S., Golmard, J.L., Lardoux, H., Witchitz, S., Henneman, J.A., Maisch, B., Hetzel, M., Jaillon, P., Boissel, J.P., Mallet, A. Circulation (1997) [Pubmed]
  13. Characteristics of adrenoceptors and [3H]nitrendipine receptors of porcine vascular smooth muscle: differences between coronary artery and aorta. Nishimura, J., Kanaide, H., Nakamura, M. Circ. Res. (1987) [Pubmed]
  14. Long-term beta-blocker treatment prevents chronic creatine kinase and lactate dehydrogenase system changes in rat hearts after myocardial infarction. Laser, A., Neubauer, S., Tian, R., Hu, K., Gaudron, P., Ingwall, J.S., Ertl, G. J. Am. Coll. Cardiol. (1996) [Pubmed]
  15. A comparison of once daily bisoprolol, 5 and 10 mg, and atenolol 100 mg in the treatment of angina pectoris. Maltz, M.B., Dymond, D.S., Nathan, A.W., Camm, A.J. Eur. Heart J. (1987) [Pubmed]
  16. Comparison of bisoprolol with nifedipine for treatment of essential hypertension in the elderly: comparative double-blind trial. Amabile, G., Serradimigni, A. Eur. Heart J. (1987) [Pubmed]
  17. Maintenance of sinus rhythm after electrical cardioversion of persistent atrial fibrillation; sotalol vs bisoprolol. Plewan, A., Lehmann, G., Ndrepepa, G., Schreieck, J., Alt, E.U., Schömig, A., Schmitt, C. Eur. Heart J. (2001) [Pubmed]
  18. Efficacy and safety of bisoprolol and atenolol in patients with mild to moderate hypertension: a double-blind, parallel group international multicentre study. Lithell, H., Selinus, I., Hosie, J., Frithz, G., Weiner, L. Eur. Heart J. (1987) [Pubmed]
  19. The single dose pharmacokinetics of bisoprolol (10 mg) in renal insufficiency: the clinical significance of balanced clearance. Payton, C.D., Fox, J.G., Pauleau, N.F., Boulton-Jones, J.M., Ioannides, C., Johnston, A., Thomas, P. Eur. Heart J. (1987) [Pubmed]
  20. Effects of bisoprolol on local vascular resistance. Bailliart, O., Kedra, A.W., Bonnin, P., Savin, E., Martineaud, J.P. Eur. Heart J. (1987) [Pubmed]
  21. Catecholamines modulate human NK cell circulation and function via spleen-independent beta 2-adrenergic mechanisms. Schedlowski, M., Hosch, W., Oberbeck, R., Benschop, R.J., Jacobs, R., Raab, H.R., Schmidt, R.E. J. Immunol. (1996) [Pubmed]
  22. Control of adrenergic overactivity by beta-blockade improves the quality of life in patients receiving long term suppressive therapy with levothyroxine. Biondi, B., Fazio, S., Carella, C., Sabatini, D., Amato, G., Cittadini, A., Bellastella, A., Lombardi, G., Saccà, L. J. Clin. Endocrinol. Metab. (1994) [Pubmed]
  23. Electrophysiological effects of bisoprolol. Proclemer, A., Gradnik, R., Savonitto, S., Feruglio, G.A. Eur. Heart J. (1987) [Pubmed]
  24. Characterization of beta(1)-selectivity, adrenoceptor-G(s)-protein interaction and inverse agonism of nebivolol in human myocardium. Maack, C., Tyroller, S., Schnabel, P., Cremers, B., Dabew, E., Südkamp, M., Böhm, M. Br. J. Pharmacol. (2001) [Pubmed]
  25. Etiology and response to drug treatment in heart failure. Follath, F., Cleland, J.G., Klein, W., Murphy, R. J. Am. Coll. Cardiol. (1998) [Pubmed]
  26. Circadian activity of the endogenous fibrinolytic system in stable coronary artery disease: effects of beta-adrenoreceptor blockers and angiotensin-converting enzyme inhibitors. Sayer, J.W., Gutteridge, C., Syndercombe-Court, D., Wilkinson, P., Timmis, A.D. J. Am. Coll. Cardiol. (1998) [Pubmed]
  27. Bisoprolol improves perfusion of ischaemic myocardium in anaesthetized pigs. Sassen, L.M., den Boer, M.O., Rensen, R.J., Saxena, P.R., Verdouw, P.D. Br. J. Pharmacol. (1988) [Pubmed]
  28. Pharmacokinetics and metabolism of bisoprolol enantiomers in humans. Horikiri, Y., Suzuki, T., Mizobe, M. Journal of pharmaceutical sciences. (1998) [Pubmed]
  29. Influence of CYP2D6 genotype on metoprolol plasma concentration and beta-adrenergic inhibition during long-term treatment: a comparison with bisoprolol. Nozawa, T., Taguchi, M., Tahara, K., Hashimoto, Y., Igarashi, N., Nonomura, M., Kato, B., Igawa, A., Inoue, H. J. Cardiovasc. Pharmacol. (2005) [Pubmed]
  30. Stereoselective metabolism of bisoprolol enantiomers in dogs and humans. Horikiri, Y., Suzuki, T., Mizobe, M. Life Sci. (1998) [Pubmed]
  31. Pharmacokinetic variability of routinely administered bisoprolol in middle-aged and elderly Japanese patients. Taguchi, M., Nozawa, T., Igawa, A., Inoue, H., Takesono, C., Tahara, K., Hashimoto, Y. Biol. Pharm. Bull. (2005) [Pubmed]
  32. scFv single chain antibody variable fragment as inverse agonist of the beta2-adrenergic receptor. Peter, J.C., Eftekhari, P., Billiald, P., Wallukat, G., Hoebeke, J. J. Biol. Chem. (2003) [Pubmed]
  33. Efficacy of once daily bisoprolol in stable angina pectoris: an objective comparison with atenolol and long term follow-up. Kohli, R.S., Khurmi, N.S., Kardash, M.M., Hughes, L.O., Lahiri, A., Raftery, E.B. Eur. Heart J. (1985) [Pubmed]
  34. Heart rate variability and ischaemia in patients with coronary heart disease and stable angina pectoris; influence of drug therapy and prognostic value. TIBBS Investigators Group. Total Ischemic Burden Bisoprolol Study. Weber, F., Schneider, H., von Arnim, T., Urbaszek, W. Eur. Heart J. (1999) [Pubmed]
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