Beta blocker properties

Drug	Alpha blockade	Beta-1 selectivity	ISA	MSA	Lipophilicity	Usual dose*	Half life, hours^¶	Elimination
Acebutolol	No	Yes	Yes	Yes	Low	100 to 400 mg twice per day	3 to 4	Hepatic (primary) Renal (secondary)
Atenolol	No	Yes	No	No	Low	50 to 200 mg once daily	6 to 9	Renal
Betaxolol	No	Yes	No	Yes	Low	10 to 20 mg once daily	14 to 22	Hepatic (primary) Renal (secondary)
Bisoprolol	No	Yes	No	No	Moderate	2.5 to 20 mg once daily	9 to 12	Renal and hepatic
Carteolol	No	No	Yes	No	Low	2.5 to 5 mg once daily	6	Renal
Carvedilol	Yes	No	No	Yes	High	3.125 to 25 mg twice per day	7 to 10	Biliary (primary) Hepatic (secondary)
Esmolol	No	Yes	No	No	Low	IV only 250 to 500 micrograms/kg over one minute then 25 to 50 micrograms/kg per minute as IV infusion; titrate incrementally up to maximum of 300 microgram/kg per minute^Δ	9 minutes	Blood esterases
Labetalol	Yes	No	Yes (Beta₂)	Low	Moderate	IV 20 mg^Δ Orally 100-400 mg two or three times per day	3 to 4	Hepatic
Metoprolol tartrate	No	Yes	No	Low	Moderate	IV 1.25 to 5 mg^Δ Orally 25 to 100 mg two times per day	3 to 4 (7 to 9 hours in poor metabolizers)	Hepatic via CYP2D6 (polymorphic)
Metoprolol succinate (extended release)	No	Yes	No	Low	Moderate	Orally 50 to 400 mg once daily	Apparent half-life prolonged by continuous osmotic release over ~20 hours	Hepatic via CYP2D6 (polymorphic)
Nadolol	No	No	No	No	Low	40 to 160 mg once daily	20 to 24	Renal
Nebivolol	No	Yes	No	No	High	5 to 40 mg once daily	10 to 12 (19 to 32 poor metabolizers)	Hepatic
Oxprenolol^◊	No	No	Yes	Yes	Moderate	40 to 80 mg three times per day	1.5	Hepatic
Penbutolol	No	No	Yes	No	High	10 to 40 mg once daily	5	Hepatic
Pindolol	No	No	Yes	Low	Moderate	5 to 30 mg twice per day	3 to 4	Hepatic (primary) Renal (secondary)
Propranolol	No	No	No	Yes	High	IV 1 to 5 mg^Δ Orally 10 to 80 mg two to four times daily	3 to 4	Hepatic
Sotalol^§	No	No	No	No	Low	80 to 160 mg twice per day	12	Renal
Timolol	No	No	No	No	Moderate	10 to 30 mg twice per day	4 to 5	Hepatic (primary) Renal (secondary)

ISA: intrinsic sympathomimetic activity; MSA: membrane stabilizing activity; IV: intravenous.
* Range of usual, oral, anti-hypertensive dose, unless "IV" noted.
¶ Duration of hypotensive effect, in general, is longer than may be predicted by serum half-life.
Δ Usual initial IV dose. Subsequent dosing generally needed. See drug monograph for detail.
◊ Not available in US.
§ Sotalol has independent class III antiarrhythmic activity.

Prepared with data from:

Frishman WH, Alwarshetty M. β-Adrenergic blockers in systemic hypertension pharmacokinetic considerations related to current guidelines. Clin Pharmacokinet 2002; 41:505.
Brubacher JR. β-Adrenergic Antagonists. In: Goldfrank's Toxicologic Emergencies, 9th ed, Nelson LS (Ed), McGraw-Hill, New York 2010.

Graphic 82571 Version 11.0

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Beta blocker properties