The beta blocker with alpha blocking action
Ans) a (Carvedilol) Ref Goodman&Gilman 11th ed.KDT 7th ed, Katzung 11th edCarvedilol is a third-generation beta receptor antagonist that has a unique pharmacological profile.It blocks beta1, beta2, and alphatreceptors similarly to labetalol, but also has antioxidant and anti- proliferative effects.It has membrane-stabilizing activity but it lacks intrinsic sympathomimetic activity.Carvedilol produces vasodilation.It is thought that the additional properties (e.g., antioxidant and antiproliferative effects) contribute to the beneficial effects seen in treating congestive heart failure.Carvedilol does not increase beta receptor density and is not associated with high levels of inverse agonist activity.BETA BLOCKERSCardioselective (betal) beta blockersMetoprololBetaxololAtenololCeliprololBisoprololNebivolol.Esmolol Non selective beta blockersPropranolol ,Sotalol,Timolol, Pindolol, Labetalol, Carvedilol, Medroxolol, Bucindolol and Levubunonol.- Pindolol has intrinsic sympathomimetic activity.- Butoxamine is a beta 2 selective blocker.- Carvedilol is a non-selective beta blocker showing anti-oxidant property and alpha 1 receptor antagonism.- Labetolol, Medroxalol, and Bucindolol also shows alpha 1 receptor blocking activity.Propranalol has highest degree of membrane stabilizing actionNadolol is longest acting beta blocker (t Vi -14-24 hrs) andEsmolol is the shortest acting.(t Vi -10 minutes)Propranolol has poor oral bioavailability.Pindolol and Penbutolol have approx 100% bioavailabilityPropranolol and Metoprolol are extensively metabolized in the liver, with little unchanged drug appearing in the urine.
Carvedilol
b)Atenolol
pindolol
Nadolol
A.N.S.