Metoprolol
From Pharmacopedia
More actions
Beta Blocker, Cardioselective (β1)
Metoprolol
Lopressor (tartrate), Toprol XL (succinate)
Metoprolol is a cardioselective (β1-preferring) beta blocker that comes in two salt forms: tartrate (short-acting, BID dosing) and succinate (extended-release, once-daily, and the only form approved for heart failure with reduced ejection fraction). Cardioselectivity makes it a reasonable first-line option in patients with mild reactive airway disease, though β2 effects emerge at higher doses.
Heart rate, blood pressure; in HFrEF, watch for fluid retention during titration.
Do not stop abruptly. Tartrate and succinate are NOT interchangeable mg-for-mg — succinate is once-daily and the only form proven in HF trials.
Propranolol, Bisoprolol, Nebivolol
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Pharmacokinetics
Absorption
~50% oral bioavailability.Distribution
Modest plasma protein binding (~12%). Some CNS penetration but less than propranolol.Metabolism
Hepatic via CYP2D6. Poor metabolizers have higher exposure and more pronounced effect.Elimination
Renal excretion of metabolites.Interactions
Pharmacogenomic + mechanism interactions
Pharmacogenomic guideline recommendationsCPIC and Dutch Pharmacogenetics Working Group clinical guidelines
CPIC rec 8094566 [Strong]: Initiate standard dosing CPIC pair-level B (CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers) [PMID 38951961]
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Mechanism description, if it needs work:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
CPIC rec 8094578 [Moderate]: Initiate therapy with lowest recommended starting dose. Carefully titrate dose upward to clinical effect or guideline-recommended dose; monitor more closely for bradycardia. Alternatively, consider selecting another beta-blocker. CPIC pair-level B (CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers) [PMID 38951961]
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Mechanism description, if it needs work:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
CPIC rec 8094574 [Moderate]: Initiate standard dosing CPIC pair-level B (CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers) [PMID 38951961]
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Mechanism description, if it needs work:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
CPIC rec 8094565 [No Recommendation]: No recommendation for metoprolol therapy due to insufficient evidence regarding diminished metoprolol effectiveness clinically CPIC pair-level B (CYP2D6, ADRB1, ADRB2, ADRA2C, GRK4, and GRK5 and Beta-Blockers) [PMID 38951961]
Rate this interaction. Reports are anonymous and help curate the page.
Clinical relevance: does this interaction matter in practice?trivialcritical
Mechanism description, if it needs work:
Is this row worth surfacing?
Your own experience with this combination:
Experience (1 a little, 5 a lot)
Outcome (-100 worst, +100 best)
Patient experience
No patient-experience reports yet.
Monitoring
Patient counseling
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
See also
References
Summary
Classes
Beta Blocker, Cardioselective (β1)
Common uses
Hypertension0, Angina0, Post-MI cardioprotection0, Heart failure (succinate only)0, SVT0
Pharmacy
Starting dose
25–50 mg BID (tartrate); 25–100 mg daily (succinate); 12.5 mg daily in HFrEF
Preparations
Tartrate: 25, 50, 100 mg tabs; 1 mg/mL IV. Succinate ER: 25, 50, 100, 200 mg.
US FDA Max
400 mg/d
Pharmacology
Routes
Oral, IV
Onset
1–2 h (PO); immediate (IV)
Duration
6–12 h (tartrate); 24 h (succinate)
Half-life
3–7 h
Bioavailability
~50%
Pregnancy
Category C
Legal status
Rx-only in US
Purported mechanism
Cardioselective β1-adrenergic antagonist. Selectivity is dose-dependent and partially lost at higher doses.