Hypertension: Beta-Blocker Pharmacokinetics

HYPERTENSION: BETA-BLOCKER PHARMACOKINETICS
Generic Brand Cardio-
selec
tivity
ISA MSA Lipid
Solu-
bility
Protein
Bound
(%)
Metab-
olism
Elimination Vaso-
dila-
tory
acebutolol Sectral Low 26 Hepatic Bile, renal  
atenolol Tenormin     Low 6–16   Renal
(primarily), fecal
 
betaxolol     Low 50 Hepatic Renal
bisoprolol Ziac     Low to Medium ~30 Hepatic Renal, fecal  
Zebeta
carvedilol* Coreg       High 98 Hepatic (CYP2C9, CYP2D6) Fecal
(primarily), renal
Coreg CR
labetalol* Trandate     Medium ~50 Hepatic (glucuron-
idation)
Renal, fecal
meto-
prolol
Lopressor     Medium 12 Hepatic (CYP2D6) Renal  
Toprol-XL
nadolol Corgard       Low 30 Hepatic Renal  
nebivolol Bystolic     Low 98 Hepatic Renal, fecal
penbutolol Levatol     Medium 80–98 Hepatic (conju-
gation, oxidation)
Renal  
pindolol   Medium 40 Hepatic Renal  
propran-
olol
Inderal     High 90 Hepatic (CYP2D6, CYP1A2) Renal  
InnoPran
 XL
timolol       Medium <10 Hepatic Renal  
NOTES

Cardioselective products are less likely to cause bronchospasm, peripheral vasoconstriction, or hypoglycemia than non-cardioselective ones.

ISA: Intrinsic sympathomimetic activity may partially reduce the cardiac depressant and bronchoconstricting effects of β-blockade.

MSA: Membrane stabilizing activity may contribute to the clinical management of cardiac arrhythmias.

*These have both α- and β-blocking activity.

†Combination drug with more than one active drug ingredient.

Lipid solubility determines how readily the drug passes through the blood brain barrier and possibly the placenta. Those drugs that have high lipid solubility pass through more readily than those agents with low lipid solubility. The incidence of CNS side effects may be higher in products with higher lipid solubility.

(Rev. 8/2014)

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