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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 | — | ✓ | ✓ | ✓ | Low | 26 | Hepatic | Bile, renal | |
| atenolol | Tenormin | ✓ | Low | 6–16 | Renal (primarily), fecal |
||||
| betaxolol | — | ✓ | Low | 50 | Hepatic | Renal | ✓ | ||
| bisoprolol | — | ✓ | Low to Medium | ~30 | Hepatic | Renal, fecal | |||
| carvedilol* | Coreg | High | 98 | Hepatic (CYP2C9, CYP2D6) | Fecal (primarily), renal |
✓ | |||
| Coreg CR | |||||||||
| labetalol* | Trandate | ✓ | Medium | ~50 | Hepatic (glucuron– idation) |
Renal, fecal | ✓ | ||
| meto– prolol |
Kapspargo Sprinkle | ✓ | Medium | 12 | Hepatic (CYP2D6) | Renal | |||
| Lopressor | |||||||||
| Toprol-XL | |||||||||
| nadolol | Corgard | Low | 30 | Renal | |||||
| nebivolol | Bystolic | ✓ | Low | 98 | Hepatic | Renal, fecal | ✓ | ||
| pindolol | — | ✓ | Medium | 40 | Hepatic | Renal | |||
| propran– olol |
Inderal | ✓ | High | 90 | Hepatic (CYP2D6, CYP1A2) | Renal | |||
| Inderal LA | |||||||||
| 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. 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. 6/2020) |
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