Brand Name
Lopressor
Broad Category
Antihypertensive / Antiarrythmic / Antianginal
Class
Selective Beta-1 adrenergic receptor antagonist
MOA
selectively and competitively antagonizes Beta-1 receptors resulting in decreased contractility and HR
- dose-dependent selectivity
Uses
Rapid HR and Contractility Control
Decreased CO thus decreases BP
Treatment for MI
Chronic heart failure (reduce mortality and improve survival)
Dosing
1-5 mg IV q2-5 mins up to 15 mg
Concentration
1 mg/mL
CV effects
Decreased HR
Decreased Contractility
Decreased CO
- which decreases BP
decreased myocardial oxygen demand
increased coronary perfussion d/t prolonged diastole
General SE
fatigue
depression
decreased exercise tolerance
Metabolic effects
Masks hypoglycemia
Contraindications (absolute)
Cardiogenic shock
pre-existing bradycardia
advanced heart block
uncompensated heart failure
Precautions
Reactive Airway disease (COPD or Asthma)
CYP2D6 poor metabolizers
Other Concerns
Withdrawal syndrome without titration due to upregulation
BP may tank with anesthetics
Metabolism
Extensive Hepatic
- CYP2D6
Excretion
Renal (metabolites)
< 10% excreted unchanged
Elimination Half-life
3-4 hours
Vd considerations
Large Vd
- highly lipophilic
- extensive tissue distribution
Clearance considerations
Flow dependent (prolonged by hepatic disease or low flow states)
Protein binding
Low