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Chemical Compound Review

Dilevalol     2-hydroxy-5-[(1S)-1-hydroxy- 2-[[(2R)-4...

Synonyms: Unicarde, Dilevalon, Levadil, Unicard, Dilevalolum, ...
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Disease relevance of Dilevalol

  • Dilevalol in severe hypertension. A multicenter trial of bolus intravenous dosing [1].
  • Dilevalol reduced GFR [baseline inulin clearance: 73.3 +/- 38 ml/min/1.73 m2; after dilevalol: 63.3 +/- 28 ml/min/1.73 m2 (P less than 0.05)] and the decrease of proteinuria correlated positively with the reduction of GFR [2].
  • The administration of methylscopolamine, 0.01 mg/kg both i.v. and i.m., to postinfarction animals pretreated with dilevalol, 3.0 mg/kg i.v. q 8 hr for 24 hr, reduced significantly mortality in response to subsequent posterolateral ischemia (mortality: 4 of 10 [40%] dilevalol plus methylscopolamine vs. 14 of 14 [100%] vehicle, P less than .05) [3].
  • The antiarrhythmic and antifibrillatory actions of dilevalol, the R,R-isomer of labetalol, were evaluated in conscious dogs 4 to 6 days after anterior myocardial infarction [3].
  • Coronary occlusion and saline or dilevalol did not modify the myocardial beta receptor density regional distribution [4].

Psychiatry related information on Dilevalol


High impact information on Dilevalol


Chemical compound and disease context of Dilevalol


Biological context of Dilevalol

  • Reduction in blood pressure during dilevalol administration is associated with peripheral vasodilatation, and heart rate remains essentially unchanged [13].
  • At an average daily dose of dilevalol, 444 mg, heart rate at rest decreased significantly (p less than 0.01) during treatment and increased during post-treatment placebo [14].
  • After both acute and subchronic treatment (mean daily dose 1,042 mg), dilevalol significantly reduced mean arterial pressure (MAP, p less than 0.0001), by significantly reducing systemic vascular resistance index (SVRI, p less than 0.001), and by not significantly altering cardiac index (CI) [15].
  • However, a significant reduction versus placebo values was observed for cardiac output at 25% VO2 max, from 13.7 +/- 5.9 during placebo, to 9.4 +/- 2.5 during propranolol, and to 9.6 +/- 2.3 during dilevalol (both p less than 0.01 vs placebo) [16].
  • A significant correlation was observed between the ICG R15 and the area under the plasma concentration-time curve (AUC) of dilevalol, while there was no significant correlation between the CLCR and any pharmacokinetic parameter of the agent [11].

Anatomical context of Dilevalol


Associations of Dilevalol with other chemical compounds


Gene context of Dilevalol

  • Dilevalol 800 mg demonstrated significant partial beta 2-adrenoceptor agonist activity by increasing finger tremor [25].
  • 9. In conclusion, dilevalol 200, 400 and 800 mg demonstrated beta 1-adrenoceptor antagonist activity with no evidence of alpha 1-adrenoceptor antagonist activity [25].
  • Renal function effects of dilevalol, a nonselective beta-adrenergic blocking drug with beta-2 agonist activity [26].
  • Labetalol itself is an alpha 1-antagonist but dilevalol, which has negligible affinity for alpha-receptors, exerts its vasodilator effect via beta 2-agonism [27].
  • The dose ratios for PS20 (means +/- s.d.) were: dilevalol 200 mg 1.1 +/- 0.1, labetalol 400 mg 2.2 +/- 0 [25].

Analytical, diagnostic and therapeutic context of Dilevalol


  1. Dilevalol in severe hypertension. A multicenter trial of bolus intravenous dosing. Wallin, J.D., Cook, M.E., Fletcher, E., Holtzman, J.L., Winer, N., Gavras, H., Grim, C.E., Ramanathan, K.B., Vidt, D.G., Johnson, B.F. Arch. Intern. Med. (1989) [Pubmed]
  2. Renal hemodynamics and reduction of proteinuria by a vasodilating beta blocker versus an ACE inhibitor. Erley, C.M., Harrer, U., Krämer, B.K., Risler, T. Kidney Int. (1992) [Pubmed]
  3. Antifibrillatory efficacy of concomitant beta adrenergic receptor blockade with dilevalol, the R,R-isomer of labetalol, and muscarinic receptor blockade with methylscopolamine. Lynch, J.J., Nelson, S.D., MacEwen, S.A., Driscoll, E.M., Lucchesi, B.R. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  4. The effect of dilevalol on cardiac autonomic neural discharge, plasma catecholamines, and myocardial beta receptor density associated with coronary occlusion. Lathers, C.M., Spivey, W.H., Levin, R.M., Tumer, N. Journal of clinical pharmacology. (1990) [Pubmed]
  5. Impact of dilevalol on haemodynamic changes during emotional stress. Rüddel, H., Langewitz, W., Bähr, M., Düsterwald, M., Schächinger, H. Eur. J. Clin. Pharmacol. (1991) [Pubmed]
  6. Pharmacokinetics and pharmacodynamics of dilevalol. Tenero, D.M., Bottorff, M.B., Given, B.D., Kramer, W.G., Affrime, M.B., Patrick, J.E., Lalonde, R.L. Clin. Pharmacol. Ther. (1989) [Pubmed]
  7. Comparison of intravenous dilevalol with placebo in moderate hypertension. Winer, N., Blasucci, D.J., Medakovic, M. Clin. Pharmacol. Ther. (1989) [Pubmed]
  8. Arterial dilation and reduced wave reflection. Benefit of dilevalol in hypertension. Kelly, R., Daley, J., Avolio, A., O'Rourke, M. Hypertension (1989) [Pubmed]
  9. Progress in antihypertensive therapy with a multiple-action drug. Prichard, B.N., Tomlinson, B. Drugs (1988) [Pubmed]
  10. Dilevalol compared with propranolol and placebo for systemic hypertension. Schoenberger, J.A., Frishman, W.H., Wallin, J.D., Gorwit, J., Davidov, M.E., Michelson, E.L., Bedsole, G.D., Cubbon, J., Poland, M.P. Am. J. Cardiol. (1989) [Pubmed]
  11. Clinical pharmacology of dilevalol (i.v.). Influence of hepatic and renal functions on the disposition of dilevalol and atenolol in hypertensive subjects. Kotegawa, T., Fujimura, A., Ebihara, A. Journal of clinical pharmacology. (1990) [Pubmed]
  12. Double-blind study of dilevalol and captopril, both in combination with hydrochlorothiazide, in patients with moderate to severe hypertension. McGrath, B.P., Matthews, P.G., Louis, W., Howes, L., Whitworth, J.A., Kincaid-Smith, P.S., Fraser, I., Scheinkestel, C., MacDonald, G., Rallings, M. J. Cardiovasc. Pharmacol. (1990) [Pubmed]
  13. Dilevalol. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in hypertension. Chrisp, P., Goa, K.L. Drugs (1990) [Pubmed]
  14. Hemodynamic effects of dilevalol in patients with systemic hypertension and left ventricular dysfunction. Kinhal, V., Kulkarni, A., Pozderac, R., Cubbon, J. Am. J. Cardiol. (1989) [Pubmed]
  15. Mechanism of antihypertensive action of dilevalol compared with that of "cardioselective" beta-blocking agents. Strom, J.A., Vidt, D.G., Bugni, W., Atkins, J., Fouad-Tarazi, F., Cubbon, J., Poland, M.P. Am. J. Cardiol. (1989) [Pubmed]
  16. Role of the Frank-Starling mechanism in maintaining cardiac output during increasing levels of treadmill exercise in beta-blocked normal men. Bevilacqua, M., Savonitto, S., Bosisio, E., Chebat, E., Bertora, P.L., Sardina, M., Norbiato, G. Am. J. Cardiol. (1989) [Pubmed]
  17. Secretion of dilevalol in breast milk. Radwanski, E., Nagabhushan, N., Affrime, M.B., Perentesis, G., Symchowicz, S., Patrick, J.E. Journal of clinical pharmacology. (1988) [Pubmed]
  18. Preclinical pharmacologic properties of dilevalol, an antihypertensive agent possessing selective beta 2 agonist-mediated vasodilation and beta antagonism. Sybertz, E.J., Watkins, R.W. Am. J. Cardiol. (1989) [Pubmed]
  19. Dilevalol: a selective beta-2 adrenergic agonist vasodilator with beta adrenergic blocking activity. Wallin, J.D., Frishman, W.H. Journal of clinical pharmacology. (1989) [Pubmed]
  20. Changes in lymphocyte beta-adrenoceptor density after dilevalol oral treatment. Sbirrazzuoli, V., Drici, M., Garraffo, R., Candito, M., Gibelin, P., Morand, P., Lapalus, P. Drugs under experimental and clinical research. (1989) [Pubmed]
  21. Haemodynamic effects of new beta-blockers with vasodilatory properties in essential hypertension. Tsukiyama, H., Otsuka, K., Horii, M. Drugs (1988) [Pubmed]
  22. Antihypertensive therapy and insulin sensitivity: do we have to redefine the role of beta-blocking agents? Jacob, S., Rett, K., Henriksen, E.J. Am. J. Hypertens. (1998) [Pubmed]
  23. Influence of beta 2 agonism and beta 1 and beta 2 antagonism on adverse effects and plasma lipoproteins: results of a multicenter comparison of dilevalol and metoprolol. Materson, B.J., Vlachakis, N.D., Glasser, S.P., Lucas, C., Ramanathan, K.B., Ahmad, S., Morledge, J.H., Saunders, E., Lutz, L.J., Schnaper, H.W. Am. J. Cardiol. (1989) [Pubmed]
  24. Effects of dilevalol (R,R-labetalol) compared with nifedipine on heart rate, blood pressure and muscle blood flow at rest and on exercise in hypertensive patients. Walley, T., Tsao, Y., Scott, A., Mackay, E., Vandenburg, M., Breckenridge, A. British journal of clinical pharmacology. (1993) [Pubmed]
  25. The dose dependency of the alpha-adrenoceptor antagonist and beta-adrenoceptor partial agonist activity of dilevalol and labetalol in man. Tham, T.C., McKaigue, J.P., Guy, S., Shanks, R.G., Riddell, J.G. British journal of clinical pharmacology. (1993) [Pubmed]
  26. Renal function effects of dilevalol, a nonselective beta-adrenergic blocking drug with beta-2 agonist activity. Cook, M.E., Wallin, J.D., Clifton, G.G., Poland, M. Clin. Pharmacol. Ther. (1988) [Pubmed]
  27. Clinical pharmacokinetics and kinetic-dynamic relationships of dilevalol and labetalol. Donnelly, R., Macphee, G.J. Clinical pharmacokinetics. (1991) [Pubmed]
  28. High-performance liquid chromatographic assay for dilevalol in human plasma and urine using a PRP-1 column and fluorimetric detection. Alton, K.B., Petruzzi, R.F., Patrick, J.E. J. Chromatogr. (1988) [Pubmed]
  29. Pharmacokinetics and bioavailability of dilevalol in normotensive volunteers. Kramer, W.G., Nagabhushan, N., Affrime, M.B., Perentesis, G.P., Symchowicz, S., Patrick, J.E. Journal of clinical pharmacology. (1988) [Pubmed]
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