Possible Interaction: Epinephrine and Carvedilol

“ Carvedilol , a nonselective β-adrenergic receptor antagonist, suppressed the facilitating effects of Epi on the Atrogin-1 mRNA induction by LPS, and abolished the effects of Epi on the MHC protein loss in the presence of LPS.”

“The nonselective -adrenergic and 1-adrenergic blocking properties of carvedilol lead to peipheral vasodilation, decreased cardiac epinephrine levels, nd increased parasympathetic none.”

“ Chronic carvedilol treatment of patients with non-terminal heart failure reduced the inotropic sensitivity of atrial trabeculae to noradrenaline and adrenaline 5.6-fold and 91.2-fold, respectively, compared to beta1-blocker-treated patients, consistent with persistent preferential blockade of beta2-adrenoceptors.”

“In terminal heart failure carvedilol treatment reduced 1.8-fold and 25.1-fold the sensitivity of right ventricular trabeculae to noradrenaline and adrenaline , respectively, but metoprolol treatment did not reduce the sensitivity to the catecholamines.”

“RESULTS Ca vedilol wa s a 13-fold more potent competitive antagonist of the effects of adr enaline at beta2-adrenoceptors (-logKB=10.13+/-0.08) than of noradrenaline at beta1-adrenoceptors (-logKB=9.02+/-0.07) in human right atrium.”

“ Carvedilol can, more effectively than atenolol, inhibit these effects of epinephrine.”

“These effects of epinephrine were completely inhibited by carvedilol.”

“Pretreatment of carvedilol orally at a dose of 1 mg/kg body weight for 2 weeks significantly prevented initial reduction in serum electrolyte levels induced by adrenaline.”

“Because carvedilol is both a nonselective β- and α1-selective adrenergic receptor-blocking agent, we hypothesized that pre-treatment with carvedilol would convert the actions of epinephrine to that of a selective a2-agonist.”

“ Carvedilol pretreatment followed by epinephrine treatment reduced early postresuscitation ventricular ectopy (116 ± 147 vs 834 ± 380, P < .01) and minimized increases in arterial blood lactate at 5 minutes after resuscitation (10.9 ± 2.1 mmol/L vs 17.4 ± 3.5 mmol/L, P < .01).”

“The … of carvedilol decreased, depending on the stimulus used, in the following rank order of potency (in parentheses the respective mean inhibitory concentrations of carvedilol … are given in w mol/l): PMA (19 and 34) > thrombin (55 and 77) > Ca 2+ -ionophore A23187 (58 and 81) > epinephrine (86 … 118).”