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Chemical Compound Review

Presolol     1-[4-(2- methoxyethyl)phenoxy]-3- (propan-2...

Synonyms: Spesicor, Spesikor, Betaloc, Betalok, Lopressor, ...
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Disease relevance of metoprolol


Psychiatry related information on metoprolol


High impact information on metoprolol

  • As compared with metoprolol therapy, electrophysiologically guided antiarrhythmic drug therapy did not improve the overall outcome of patients with sustained ventricular tachyarrhythmias [3].
  • The incidence of symptomatic arrhythmia and sudden death combined was virtually the same in the two groups with inducible arrhythmia after two years of observation (electrophysiologically guided therapy vs. metoprolol therapy, 46 percent vs. 48 percent) [3].
  • At the end of the follow-up period, the patients in the weight-reduction group had lost an average of 8.3 kg, and their blood pressure had decreased by an average of 14/13 mm Hg, as compared with 12/8 mm Hg in the metoprolol group and 9/4 mm Hg in the placebo group [1].
  • The changes in thickness of the interventricular septum and the left ventricular mass in the weight-reduction group were also greater than those in the metoprolol group [1].
  • However, there were 17 cases of ventricular fibrillation in the placebo group (697 patients) and only 6 in the metoprolol group (698 patients, P less than 0.05) [2].

Chemical compound and disease context of metoprolol


Biological context of metoprolol


Anatomical context of metoprolol

  • Specific binding in the presence of 10(-5) M metoprolol was reduced approximately 75% for both arterioles and myocytes [20].
  • Immediately after thrombotic occlusion of the left anterior descending coronary artery, the cardioselective beta-blocking agent metoprolol was given intravenously at a dose of 0.5 mg/kg infused over 10 min [21].
  • Additionally, patients treated with metoprolol had an increased percentage of T cells, natural killer cells, and increased interleukin-2 receptor density upon stimulation with concanavalin A [22].
  • CONCLUSIONS: It appears that patients with dilated cardiomyopathy who are treated with metoprolol have enhancement of cell-mediated immunity and improvement of T-cell function; these improvements are correlated to improvement in ejection fraction [22].
  • At branching sites in the thoracic aorta, immunoglobulin G incorporation and endothelial cell replication were significantly greater in untreated monkeys than in metoprolol-treated monkeys (p less than 0.01 for both analyses); no differences existed at nonbranch sites [23].

Associations of metoprolol with other chemical compounds

  • The frequency rates of responders (diastolic blood pressure, less than or equal to 95 mm Hg) in the metoprolol group and the hydrochlorothiazide group were 50% and 47% after four weeks and 65% and 61% after eight weeks, respectively [24].
  • On the other hand, alpha-blocker phentolamine and beta 1-blocker metoprolol did not abolish the stimulation of AdC in PST by ISO [25].
  • MEASUREMENTS AND MAIN RESULTS: Resting systolic blood pressure measured without drug therapy was lowered markedly after exercise conditioning on placebo (146 to 135 mm Hg) and on metoprolol (144 to 133 mm Hg) (P less than 0.05), but not on propranolol (no change) [26].
  • Carvedilol at 50 to 100 mg/d produced reductions in exercise heart rate that were similar to metoprolol at 125 to 150 mg/d, indicating comparable degrees of beta-blockade [17].
  • METHODS AND RESULTS: Fifteen patients with New York Heart Association class III-IV CHF secondary to dilated cardiomyopathy were titrated to a minimum dose of metoprolol 25 mg BID on a background therapy of digoxin, diuretic, and angiotensin-converting enzyme inhibitors [22].

Gene context of metoprolol

  • Significant interaction between the nonprescription antihistamine diphenhydramine and the CYP2D6 substrate metoprolol in healthy men with high or low CYP2D6 activity [27].
  • This index correlated with the 4'-hydroxylation of S-mephenytoin (rs = -0.51, p < 0.01), but not with the alpha-hydroxylation of metoprolol, implying that imipramine N-demethylation is under a coregulatory pharmacogenetic control of CYP2C19, but not of CYP2D6 [28].
  • In contrast, metoprolol, a compound with similar permeability but no affinity for PGP had no effect on PGP expression [29].
  • 4. RU 24969 (7.5 mg kg-1 i.p.)-induced hyperlocomotion was inhibited by the (-)-, but not (+)-isomers of pindolol (4 mg kg-1) and propranolol (20 mg kg-1) but not by metoprolol (10 mg kg-1) or ICI 118,551 (5 mg kg-1), consistent with an involvement of 5-HT1A or 5-HT1B receptors [30].
  • Administration of the adrenergic antagonist metoprolol completely reversed the tachycardia seen in MCHR1(-/-) mice, suggesting an increased sympathetic tone [31].

Analytical, diagnostic and therapeutic context of metoprolol


  1. The effect of weight reduction on left ventricular mass. A randomized controlled trial in young, overweight hypertensive patients. MacMahon, S.W., Wilcken, D.E., Macdonald, G.J. N. Engl. J. Med. (1986) [Pubmed]
  2. A double-blind trial of metoprolol in acute myocardial infarction. Effects on ventricular tachyarrhythmias. Rydén, L., Ariniego, R., Arnman, K., Herlitz, J., Hjalmarson, A., Holmberg, S., Reyes, C., Smedgård, P., Svedberg, K., Vedin, A., Waagstein, F., Waldenström, A., Wilhelmsson, C., Wedel, H., Yamamoto, M. N. Engl. J. Med. (1983) [Pubmed]
  3. A comparison of electrophysiologically guided antiarrhythmic drug therapy with beta-blocker therapy in patients with symptomatic, sustained ventricular tachyarrhythmias. Steinbeck, G., Andresen, D., Bach, P., Haberl, R., Oeff, M., Hoffmann, E., von Leitner, E.R. N. Engl. J. Med. (1992) [Pubmed]
  4. Treatment of migraine with metoprolol. Ljung, O. N. Engl. J. Med. (1980) [Pubmed]
  5. Metoprolol for intermittent explosive disorder. Mattes, J.A. The American journal of psychiatry. (1985) [Pubmed]
  6. The effect of beta-blockers on mental performance on older hypertensive patients. Gengo, F.M., Fagan, S.C., de Padova, A., Miller, J.K., Kinkel, P.R. Arch. Intern. Med. (1988) [Pubmed]
  7. Successful prophylaxis of recurrent transient global amnesia with metoprolol. Berlit, P. Neurology (2000) [Pubmed]
  8. Efficacy of low-dose metoprolol in neuroleptic-induced akathisia. Kim, A., Adler, L., Angrist, B., Rotrosen, J. Journal of clinical psychopharmacology. (1989) [Pubmed]
  9. The relationship between serum concentrations and central nervous system actions of metoprolol. Gengo, F.M., Ermer, J.C., Carey, C., Kalonaros, G.C., McHugh, W.B. J. Neurol. Neurosurg. Psychiatr. (1985) [Pubmed]
  10. Effect of cardioselective and non-selective beta-blockade on the hypoglycaemic response in insulin-dependent diabetics. Lager, I., Blohmé, G., Smith, U. Lancet (1979) [Pubmed]
  11. Action of sotalol on potential reentrant pathways and ventricular tachyarrhythmias in conscious dogs in the late postmyocardial infarction phase. Cobbe, S.M., Hoffman, E., Ritzenhoff, A., Brachmann, J., Kübler, W., Senges, J. Circulation (1983) [Pubmed]
  12. Comparative effects of nitroglycerin, nifedipine and metoprolol on regional left ventricular function in patients with one-vessel coronary disease. Pfisterer, M., Glaus, L., Burkart, F. Circulation (1983) [Pubmed]
  13. Use of beta adrenoceptor blockade during and after acute myocardial infarction. Sleight, P. Annu. Rev. Med. (1986) [Pubmed]
  14. Effect of carvedilol in comparison with metoprolol on myocardial collagen postinfarction. Wei, S., Chow, L.T., Sanderson, J.E. J. Am. Coll. Cardiol. (2000) [Pubmed]
  15. Beneficial effects of metoprolol in idiopathic dilated cardiomyopathy. Metoprolol in Dilated Cardiomyopathy (MDC) Trial Study Group. Waagstein, F., Bristow, M.R., Swedberg, K., Camerini, F., Fowler, M.B., Silver, M.A., Gilbert, E.M., Johnson, M.R., Goss, F.G., Hjalmarson, A. Lancet (1993) [Pubmed]
  16. Long-term beta-blockade in dilated cardiomyopathy. Effects of short- and long-term metoprolol treatment followed by withdrawal and readministration of metoprolol. Waagstein, F., Caidahl, K., Wallentin, I., Bergh, C.H., Hjalmarson, A. Circulation (1989) [Pubmed]
  17. Comparative hemodynamic, left ventricular functional, and antiadrenergic effects of chronic treatment with metoprolol versus carvedilol in the failing heart. Gilbert, E.M., Abraham, W.T., Olsen, S., Hattler, B., White, M., Mealy, P., Larrabee, P., Bristow, M.R. Circulation (1996) [Pubmed]
  18. Effects of regional alpha- and beta-blockade on resting and hyperemic coronary blood flow in conscious, unstressed humans. Hodgson, J.M., Cohen, M.D., Szentpetery, S., Thames, M.D. Circulation (1989) [Pubmed]
  19. Improvement in symptoms and exercise tolerance by metoprolol in patients with dilated cardiomyopathy: a double-blind, randomized, placebo-controlled trial. Engelmeier, R.S., O'Connell, J.B., Walsh, R., Rad, N., Scanlon, P.J., Gunnar, R.M. Circulation (1985) [Pubmed]
  20. Autoradiographic characterization of beta adrenergic receptors in coronary blood vessels and myocytes in normal and ischemic myocardium of the canine heart. Muntz, K.H., Olson, E.G., Lariviere, G.R., D'Souza, S., Mukherjee, A., Willerson, J.T., Buja, L.M. J. Clin. Invest. (1984) [Pubmed]
  21. Reduction in infarct size and enhanced recovery of systolic function after coronary thrombolysis with tissue-type plasminogen activator combined with beta-adrenergic blockade with metoprolol. Van de Werf, F., Vanhaecke, J., Jang, I.K., Flameng, W., Collen, D., De Geest, H. Circulation (1987) [Pubmed]
  22. Beneficial effects of metoprolol treatment in congestive heart failure. Reversal of sympathetic-induced alterations of immunologic function. Maisel, A.S. Circulation (1994) [Pubmed]
  23. Endothelial dysfunction in response to psychosocial stress in monkeys. Strawn, W.B., Bondjers, G., Kaplan, J.R., Manuck, S.B., Schwenke, D.C., Hansson, G.K., Shively, C.A., Clarkson, T.B. Circ. Res. (1991) [Pubmed]
  24. Antihypertensive treatment with metoprolol or hydrochlorothiazide in patients aged 60 to 75 years. Report from a double-blind international multicenter study. Wikstrand, J., Westergren, G., Berglund, G., Bracchetti, D., Van Couter, A., Feldstein, C.A., Ming, K.S., Kuramoto, K., Landahl, S., Meaney, E. JAMA (1986) [Pubmed]
  25. Evidence for beta adrenoceptors in proximal tubules. Isoproterenol-sensitive adenylate cyclase in pars recta of canine nephron. Murayama, N., Ruggles, B.T., Gapstur, S.M., Werness, J.L., Dousa, T.P. J. Clin. Invest. (1985) [Pubmed]
  26. Hypertension, exercise, and beta-adrenergic blockade. Ades, P.A., Gunther, P.G., Meacham, C.P., Handy, M.A., LeWinter, M.M. Ann. Intern. Med. (1988) [Pubmed]
  27. Significant interaction between the nonprescription antihistamine diphenhydramine and the CYP2D6 substrate metoprolol in healthy men with high or low CYP2D6 activity. Hamelin, B.A., Bouayad, A., Méthot, J., Jobin, J., Desgagnés, P., Poirier, P., Allaire, J., Dumesnil, J., Turgeon, J. Clin. Pharmacol. Ther. (2000) [Pubmed]
  28. Steady-state plasma concentrations of imipramine and desipramine in relation to S-mephenytoin 4'-hydroxylation status in Japanese depressive patients. Koyama, E., Tanaka, T., Chiba, K., Kawakatsu, S., Morinobu, S., Totsuka, S., Ishizaki, T. Journal of clinical psychopharmacology. (1996) [Pubmed]
  29. Rapid induction of P-glycoprotein expression by high permeability compounds in colonic cells in vitro: a possible source of transporter mediated drug interactions? Collett, A., Tanianis-Hughes, J., Warhurst, G. Biochem. Pharmacol. (2004) [Pubmed]
  30. Evidence that RU 24969-induced locomotor activity in C57/B1/6 mice is specifically mediated by the 5-HT1B receptor. Cheetham, S.C., Heal, D.J. Br. J. Pharmacol. (1993) [Pubmed]
  31. Mice lacking melanin-concentrating hormone receptor 1 demonstrate increased heart rate associated with altered autonomic activity. Astrand, A., Bohlooly-Y, M., Larsdotter, S., Mahlapuu, M., Andersén, H., Tornell, J., Ohlsson, C., Snaith, M., Morgan, D.G. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2004) [Pubmed]
  32. Drug therapy: metoprolol. Koch-Weser, J. N. Engl. J. Med. (1979) [Pubmed]
  33. Effects of controlled-release metoprolol on total mortality, hospitalizations, and well-being in patients with heart failure: the Metoprolol CR/XL Randomized Intervention Trial in congestive heart failure (MERIT-HF). MERIT-HF Study Group. Hjalmarson, A., Goldstein, S., Fagerberg, B., Wedel, H., Waagstein, F., Kjekshus, J., Wikstrand, J., El Allaf, D., Vítovec, J., Aldershvile, J., Halinen, M., Dietz, R., Neuhaus, K.L., Jánosi, A., Thorgeirsson, G., Dunselman, P.H., Gullestad, L., Kuch, J., Herlitz, J., Rickenbacher, P., Ball, S., Gottlieb, S., Deedwania, P. JAMA (2000) [Pubmed]
  34. Effect on mortality of metoprolol in acute myocardial infarction. A double-blind randomised trial. Hjalmarson, A., Elmfeldt, D., Herlitz, J., Holmberg, S., Málek, I., Nyberg, G., Rydén, L., Swedberg, K., Vedin, A., Waagstein, F., Waldenström, A., Waldenström, J., Wedel, H., Wilhelmsen, L., Wilhelmsson, C. Lancet (1981) [Pubmed]
  35. Noradrenergic activity and silent ischaemia in hypertensive patients with stable angina: effect of metoprolol. Lee, D.D., Kimura, S., DeQuattro, V. Lancet (1989) [Pubmed]
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