II. Indications
III. Mechanism
- See Beta Adrenergic ReceptorAntagonist
- Selective Beta Antagonist that primarily inhibits B1 activity by blocking B1 Receptors
- Reduces Myocardial Contractility, Blood Pressure, myocardial oxygen demand
- Also Antiarrhythmic and slows ventricular response in Atrial Fibrillation
- Contrast with non-selective Beta Blockers (e.g. Propranolol)
- Non-selective Beta Blockers also act at B2 Receptors (bronchoconstriction) and B3 Receptors (block lipolysis)
IV. Adverse Effects
- See Beta Blocker
V. Drug Interactions
- See Beta Blocker
VI. Dosing: Adults
- Start: 25-50 mg orally daily
- Despite daily dosing, duration of activity is not a a full 24 hours
- Consider dividing dosing into twice daily (e.g. 50 mg twice daily)
- Target: 50-100 mg orally daily (may divide dose twice daily)
- Maximum dose: 100 mg (50 mg if GFR <35 ml/min, 25 mg if GFR <15 ml/min)
VII. Efficacy
- Not as effective as other Beta Blockers in cardiovascular disease prevention (especially with Hypertension present)
- Consider Metoprolol, Bisoprolol, Carvedilol or Nadolol instead
- Carlberg (2004) Lancet 364:1684-9 [PubMed]
VIII. Safety
- Pregnancy Category D
- Avoid in Lactation
- Risk of Hypoglycemia in newborns
IX. Metabolism
- Bioavailability 50%
- Not lipophilic
- Renal excretion
X. Resources
XI. References
- (2019) Presc Lett, Resource #350503, Comparison of Oral Beta Blockers
- (2020) Med Lett Drugs Ther 62(1598): 73-80
- Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 66-7
- Hamilton (2020) Tarascon Pocket Pharmacopoeia
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