Table 1.

Pharmacokinetic characteristics of beta-adrenergic blockers used in the management of heart failure

Characteristic	Bisoprolol (Zebeta®)	Carvedilol (Coreg®)	Metoprolol succinate (Toprol XL®)	Nebivolol
Absorption
Bioavailability	80%	25%–35%	50%	12%–96%
First-pass elimination	Small	Significant	Moderate	Variablec
Effect of food	None	Decreases rate but not extent of absorption	None	None
Protein binding	30%	95%–98%	12%	98%
Half-life (hours)	9–12	6–10	3–7	10–30
Hepatic metabolism	50% to inactive metabolites via N-dealkylation and O-dealkylation	Extensive primarily by CYP450 2D6 and 2C9 to active and inactive metabolitesa,b	Extensive via CYP450 2D6 to inactive metabolitesa	Extensive via CYP450 2D6 to active and inactive metabolitesa
Renal excretion	50% as unchanged drug, 50% as metabolites	<2% as unchanged drug	95%, <5% as unchanged drug	<1% unchanged in urine
Other excretion	<2% in feces	Primarily in bile and feces	Minimal

^aCYP450 = cytochrome P450.

^bCarvedilol is metabolized to a lesser extent by CYP 450 3A4, 2C19, 1A2, and 2E1.

^cBioavailability and first-pass elimination are dependant on cytochrome P450 2D6 genetic polymorphism.