2 Carvedilol and its metabolites may undergo further sulfate conjugation or glucuronidation before elimination. 2 Carvedilol can also be demethylated by CYP2C9, CYP2D6, CYP1A2, or CYP2E1 to form O-desmethylcarvedilol. 4 MetabolismĬarvedilol can be hydroxlated at the 1 position by CYP2D6, CYP1A2, or CYP1A1 to form 1-hydroxypheylcarvedilol at the 4 position by CYP2D6, CYP2E1, CYP2C9, or CYP3A4 to form 4'-hydroxyphenylcarvedilol at the 5 position by CYP2D6, CYP2C9, or CYP3A4 to form 5'-hydroxyphenylcarvedilol and at the 8 position by CYP1A2, CYP3A4, and CYP1A1 to form 8-hydroxycarbazolylcarvedilol. 5, 6 95% of carvedilol is bound to serum albumin. 6 Protein bindingĬarvedilol is 98% protein bound in plasma. 4 Volume of distributionĬarvedilol has a volume of distribution of 1.5-2L/kg 4 or 115L. 4 Carvedilol doses of 12.5mg lead to a C max of 58-69µg/L and an AUC of 208-225µg/L*h. 4 Carvedilol doses of 25mg lead to a C max of 24-151µg/L and an AUC of 272-947µg/L*h. 4 Carvedilol doses of 50mg lead to a C max of 122-262µg/L and an AUC of 717-1600µg/L*h. 4 Taking carvedilol with a meal increases T max without increasing AUC. 4, 5, 6 Carvedilol has a T max of 1 to 2 hours. 1 TargetĬarvedilol has a bioavailability of 25-35%. 1 The antioxidant activity of carvedilol prevents oxidation of low density lipoprotein and its uptake into coronary circulation. 1, 4 At higher doses, calcium channel blocking and antioxidant activity can also be seen.

4 Carvedilol's action on alpha-1 adrenergic receptors relaxes smooth muscle in vasculature, leading to reduced peripheral vascular resistance and an overall reduction in blood pressure. 5, 6 Mechanism of actionĬarvedilol inhibits exercise induce tachycardia through its inhibition of beta adrenoceptors.

5, 6 Patients taking carvedilol should not abruptly stop taking this medication as this may exacerbate coronary artery disease. 5, 6 It has a long duration of action as it is generally taken once daily and has a broad therapeutic index as patients generally take 10-80mg daily. Carvedilol reduces tachycardia through beta adrenergic antagonism and lowers blood pressure through alpha-1 adrenergic antagonism.

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