Table 2.

β-blockers studied for the treatment of HF

Name	β-blocking property	α1-blocking property	Elimination routea	References
Carvedilol	Nonselective	Yes	Oral bioavailability: About 25–35%	[4, 12–15]
			Both CYP2D6 and CYP2C9 are major metabolizing enzymes
			CYP2D6 is responsible for 30–50% of metabolism of carvedilol
			CYP2C9 is responsible for 5–20% of metabolism of carvedilol
Metoprolol	β1-selective	No	Oral bioavailability:	[4, 12, 16, 17]
			Immediate release form: About 50%
			Controlled release form: About 25–30%
			CYP2D6 is a major hepatic enzyme responsible for 60–70% of metoprolol metabolism.
Bisoprolol	β1-selective	No	Oral bioavailability: 80–90%	[4, 12, 18]
			Approximately 50% of oral dose is recovered as parent drug in urine
Bucindolol	Nonselective	Yes but weak	Oral bioavailability: About 30%	[4, 12, 19]
			Extensively metabolized by liver enzymes

^aElimination of parent drug

CYP, cytochrome P450