Carvedilol Pathway


Carvedilol is a racemic mixture in which nonselective beta-adrenoreceptor blocking activity is present in the S(-) enantiomer and alpha-adrenergic blocking activity is present in both R(+) and S(-) enantiomers at equal potency. Carvedilol’s beta-adrenergic receptor blocking ability decreases the heart rate, myocardial contractility, and myocardial oxygen demand. Carvedilol also decreases systemic vascular resistance via its alpha adrenergic receptor blocking properties. Carvedilol and its metabolite BM-910228 (a less potent beta blocker, but more potent antioxidant) have been shown to restore the inotropic responsiveness to Ca2+ in OH- free radical-treated myocardium. Carvedilol and its metabolites also prevent OH- radical-induced decrease in sarcoplasmic reticulum Ca2+-ATPase activity. Therefore, carvedilol and its metabolites may be beneficial in chronic heart failure by preventing free radical damage.

Pathway legend Zoom in

Pathway Image

Pathway legend Zoom in

References

  1. Borchard, U. (1998). Pharmacological properties of beta-adrenoceptor blocking drugs. Journal of Clinical and Basic Cardiology, 1(1), 5-9.
  2. Carvedilol. (2009). [Electronic version]. e-CPS. Retrieved July 25, 2009.
  3. DiPiro, J.T., Talbert, R.L., Yee, G.C., Matzke, G.R., Wells, B.G, & Posey, M.L. (2005). Pharmacotherapy: A pathologic approach. (6 th ed) pp.207-208. New York: McGraw-Hill Medical Publishing Division.