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Beta Blocker Propertieis

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Beta blocker properties

Beta-1 Half life,


Drug Alpha blockade ISA MSA Lipophilicity Usual dose* Elimination
selectivity hours ¶

Acebutolol No Yes Yes Yes Low 100 to 400 mg 3 to 4 Hepatic (primary)


twice per day
Renal (secondary)

Atenolol No Yes No No Low 50 to 200 mg once 6 to 9 Renal


daily

Betaxolol No Yes No Yes Low 10 to 20 mg once 14 to 22 Hepatic (primary)


daily
Renal (secondary)

Bisoprolol No Yes No No Moderate 2.5 to 20 mg once 9 to 12 Renal and hepatic


daily

Carteolol No No Yes No Low 2.5 to 5 mg once 6 Renal


daily

Carvedilol Yes No No Yes High 3.125 to 25 mg 7 to 10 Biliary (primary)


twice per day
Hepatic
(secondary)

Esmolol No Yes No No Low IV only 250 to 500 9 minutes Blood esterases


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

Labetalol Yes No Yes (Beta 2 ) Low Moderate IV 20 mg Δ 3 to 4 Hepatic

Orally 100-400 mg
two or three times
per day

Metoprolol tartrate No Yes No Low Moderate IV 1.25 to 5 mg Δ 3 to 4 Hepatic via


(7 to 9 hours in CYP2D6
Orally 25 to 100
poor metabolizers) (polymorphic)
mg two times per
day

Metoprolol No Yes No Low Moderate Orally 50 to 400 Apparent half-life Hepatic via
succinate mg once daily prolonged by CYP2D6
(extended release) continuous (polymorphic)
osmotic release
over ~20 hours

Nadolol No No No No Low 40 to 160 mg once 20 to 24 Renal


daily

Nebivolol No Yes No No High 5 to 40 mg once 10 to 12 Hepatic


daily (19 to 32 poor
metabolizers)

Oxprenolol ◊ No No Yes Yes Moderate 40 to 80 mg three 1.5 Hepatic


times per day

Penbutolol No No Yes No High 10 to 40 mg once 5 Hepatic


daily

Pindolol No No Yes Low Moderate 5 to 30 mg twice 3 to 4 Hepatic (primary)


per day
Renal (secondary)

Propranolol No No No Yes High IV 1 to 5 mg Δ 3 to 4 Hepatic

Orally 10 to 80 mg
two to four times
daily

Sotalol § No No No No Low 80 to 160 mg twice 12 Renal


per day

Timolol No No No No Moderate 10 to 30 mg twice 4 to 5 Hepatic (primary)


per day
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:​


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

Graphic 82571 Version 10.0

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