Table 2.

Detailed metabolic profile of beta-blockers.

Beta-blocker name	Metabolites	Enzymes	References
Acebutolol	Diacetolol	CYP2D6	[49]
Alprenolol	4-Hydroxy-alprenolol	CYP2D6	[50, 68]
Atenolol	Not metabolized		[51]
Betaxolol	α-Hydroxy betaxolol	CYP1A2, CYP2D6	[52, 53]
Bisoprolol	Demethyl carboxylic acid	CYP3A4, CYP2D6	[54]
	Deethyl carboxylic acid		[54]
	Deethyl derivative		[54]
Carvedilol	8-Hydroxy carvedilol	CYP1A2, CYP3A4, CYP1A1	[55]
	4'-Hydroxy carvedilol	CYP2D6, CYP2E1, CYP2C9	[55]
	5'-Hydroxy carvedilol	CYP2D6, CYP2E1, CYP2C9	[55]
	O-Desmethyl carvedilol	CYP2C9, CYP2D6, CYP1A2, CYP2E1	[55]
	1-Hydroxy carvedilol	Prostaglandin G/H synthase 1	[55]
	4'-Hydroxyphenyl carvedilol		[55]
Esmolol	Methanol	Esterases	[56]
Labetalol	7 Glucuronides metabolites	UDP-Glucuronosyltransferase	[57, 58]
	3-Amino-1-phenyl butane	GI mucosa	[57, 58]
	3-Amino-1-(4-hydroxyphenyl) butane	GI mucosa	[57, 58]
	Benzyl acetone	GI mucosa	[57, 58]
Metoprolol	α-Hydroxy metoprolol	CYP2D6	[59]
Nadolol	Not metabolized		[60]
Nebivolol	Hydroxy alicyclic metabolites	CYP2D6	[61]
	Hydroxy aromatic metabolites	CYP2D6	[61]
	1st generation glucuronides	UDP-Glucuronosyltransferase	[61]
	N-dealkylation	CYP2D6	[61]
	2nd generation glucuronides (after the hydroxylation)	UDP-Glucuronosyltransferase	[61]
Oxprenolol	Glucuronides of unchanged oxprenolol	UDP-Glucuronosyltransferase	[62, 63]
	Hydroxylation to the aromatic ring of unchanged oxprenolol	CYP2D6	[62, 63]
	Glucuronides of hydroxylated oxprenolol	UDP-Glucuronosyltransferase	[62, 63]
	N-dealkylation, producing the hydroxy carboxylic acid	CYP2D6	[62, 63]
	Carbinol	CYP2D6	[62, 63]
	Monoallyl ether of catechol	CYP2D6	[62, 63]
Penbutolol	Glucuronide metabolite	UDP-Glucuronosyltransferase	[64, 66]
	4-Hydroxy metabolite		[64, 66]
Pindolol	Hydroxylated metabolites		[67]
	Glucuronides of hydroxylated metabolites	UDP-Glucuronosyltransferase	[67]
	Sulfate metabolites	Sulfotransferases	[67]
Propanolol	N-Desisopropyl propranolol	CYP1A2	[68]
	4'-Hydroxy propanolol	CYP2D6	[68]