Myocardial infarction: Treatment of hemodynamically stable acute myocardial infarction (MI) to reduce cardiovascular mortality (injection to be used in combination with metoprolol oral maintenance therapy). Note: Beta-blockers are not recommended as first-line therapy (ACC/AHA ). Hypertension: Management of hypertension. Heart failure with reduced ejection fraction (HFrEF) (ER oral formulation): Treatment of stable, symptomatic (NYHA class II or III) heart failure of ischemic, hypertensive, or cardiomyopathic origin to reduce the rate of mortality plus hospitalization in patients already receiving ACE inhibitors, diuretics, and/or digoxin. Use: Labeled IndicationsĪngina: Long-term treatment of angina pectoris. Poor CYP2D6 metabolizers (~8% Caucasians ~2% other populations) have several-fold higher metoprolol plasma concentrations. ~10% to 12% to albumin Use in Specific Populations Special Populations: Hepatic Function ImpairmentĮlimination half-life may be considerably prolonged, depending on severity. Neonates: 5 to 10 hours (Morselli 1989) Adults: 3 to 4 hours (7 to 9 hours in poor CYP2D6 metabolizers or hepatic impairment) Protein Binding Oral: Immediate release: Variable (dose-related 50% reduction in maximum heart rate after single doses of 20, 50, and 100 mg occurred at 3.3, 5, and 6.4 hours, respectively), Extended release: ~24 hours Half-Life Elimination Oral: Immediate release tablets: Within 1 hour Peak effect: Oral: 1 to 2 hours (Regardh 1980) IV: 20 minutes (when infused over 10 minutes) Duration of Action Urine (95%, <5% to 10% as unchanged drug increased to 30% to 40% in poor CYP2D6 metabolizers) Onset of Action V d: 3.2 to 5.6 L/kg crosses the blood brain barrier CSF concentrations are 78% of plasma concentrations MetabolismĮxtensively hepatic via CYP2D6 significant first-pass effect (~50%) Excretion Selective inhibitor of beta 1-adrenergic receptors competitively blocks beta 1-receptors, with little or no effect on beta 2-receptors at oral doses <100 mg (in adults) does not exhibit any membrane stabilizing or intrinsic sympathomimetic activity Pharmacokinetics/Pharmacodynamics Absorption Generic: 25 mg, 50 mg, 100 mg, 200 mg Pharmacology Mechanism of Action Tablet Extended Release 24 Hour, Oral, as succinate: Solution Cartridge, Intravenous, as tartrate: Kapspargo Sprinkle: 25 mg, 50 mg, 100 mg, 200 mg Excipient information presented when available (limited, particularly for generics) consult specific product labeling.

Half life of metoprolol