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A comparison of carvedilol and metoprolol antioxidant activities in vitro.
J Cardiovasc Pharmacol. 2000 Aug; 36(2):277-81.JC

Abstract

Carvedilol is a vasodilating beta-blocker and antioxidant approved for treatment of mild to moderate hypertension. angina, and congestive heart failure. Metoprolol is a beta1-selective adrenoceptor antagonist. When carvedilol and metoprolol were recently compared in clinical trials for heart failure, each showed beneficial beta-blocker effects such as improved symptoms, quality of life, exercise tolerance, and ejection fraction, with no between-group differences. When thiobarbituric acid reactive substance (TBARS) levels were measured in serum as an indirect marker of free radical activity, there were also no between-group differences. However, we had noted superior cardioprotection by carvedilol in comparison to metoprolol in ischemia and reperfusion models. We therefore examined antioxidant activity directly in cells and tissues. Here we show that in cultured rat cerebellar neurons, and in brain and heart membranes, carvedilol has far greater antioxidant activity than metoprolol, which is essentially inactive as an antioxidant in these model systems. The antioxidant activity of carvedilol could be explained by a greater degree of lipophilicity, as measured by its ClogP value of 3.841 as contrasted to a ClogP value of 1.346 for metoprolol. Alternatively, the molecular structure of carvedilol favors redox recycling, which the structure of metoprolol does not. Therefore, carvedilol could have additional pharmacologic effects that are favorable for long-term therapy.

Authors+Show Affiliations

Department of Cardiovascular Pharmacology, SmithKline Beecham Pharmaceuticals, King of Prussia, Pennsylvania 19406-0939, USA. Paul_G_Lysko@sbphrd.comNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article

Language

eng

PubMed ID

10942172

Citation

Lysko, P G., et al. "A Comparison of Carvedilol and Metoprolol Antioxidant Activities in Vitro." Journal of Cardiovascular Pharmacology, vol. 36, no. 2, 2000, pp. 277-81.
Lysko PG, Webb CL, Gu JL, et al. A comparison of carvedilol and metoprolol antioxidant activities in vitro. J Cardiovasc Pharmacol. 2000;36(2):277-81.
Lysko, P. G., Webb, C. L., Gu, J. L., Ohlstein, E. H., Ruffolo, R. R., & Yue, T. L. (2000). A comparison of carvedilol and metoprolol antioxidant activities in vitro. Journal of Cardiovascular Pharmacology, 36(2), 277-81.
Lysko PG, et al. A Comparison of Carvedilol and Metoprolol Antioxidant Activities in Vitro. J Cardiovasc Pharmacol. 2000;36(2):277-81. PubMed PMID: 10942172.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - A comparison of carvedilol and metoprolol antioxidant activities in vitro. AU - Lysko,P G, AU - Webb,C L, AU - Gu,J L, AU - Ohlstein,E H, AU - Ruffolo,R R,Jr AU - Yue,T L, PY - 2000/8/15/pubmed PY - 2001/2/28/medline PY - 2000/8/15/entrez SP - 277 EP - 81 JF - Journal of cardiovascular pharmacology JO - J Cardiovasc Pharmacol VL - 36 IS - 2 N2 - Carvedilol is a vasodilating beta-blocker and antioxidant approved for treatment of mild to moderate hypertension. angina, and congestive heart failure. Metoprolol is a beta1-selective adrenoceptor antagonist. When carvedilol and metoprolol were recently compared in clinical trials for heart failure, each showed beneficial beta-blocker effects such as improved symptoms, quality of life, exercise tolerance, and ejection fraction, with no between-group differences. When thiobarbituric acid reactive substance (TBARS) levels were measured in serum as an indirect marker of free radical activity, there were also no between-group differences. However, we had noted superior cardioprotection by carvedilol in comparison to metoprolol in ischemia and reperfusion models. We therefore examined antioxidant activity directly in cells and tissues. Here we show that in cultured rat cerebellar neurons, and in brain and heart membranes, carvedilol has far greater antioxidant activity than metoprolol, which is essentially inactive as an antioxidant in these model systems. The antioxidant activity of carvedilol could be explained by a greater degree of lipophilicity, as measured by its ClogP value of 3.841 as contrasted to a ClogP value of 1.346 for metoprolol. Alternatively, the molecular structure of carvedilol favors redox recycling, which the structure of metoprolol does not. Therefore, carvedilol could have additional pharmacologic effects that are favorable for long-term therapy. SN - 0160-2446 UR - https://www.unboundmedicine.com/medline/citation/10942172/A_comparison_of_carvedilol_and_metoprolol_antioxidant_activities_in_vitro_ L2 - https://doi.org/10.1097/00005344-200008000-00020 DB - PRIME DP - Unbound Medicine ER -