Bisoprolol
Unchecked
Beta Blocker, Cardioselective (β1)
Bisoprolol
Zebeta
Bisoprolol is a highly β1-selective beta blocker and one of the four guideline-recommended agents for heart failure with reduced ejection fraction (alongside metoprolol succinate, carvedilol, and bucindolol). Its elimination is approximately 50% hepatic and 50% renal, which makes it forgiving in patients with either hepatic or renal impairment.
Heart rate, blood pressure; in HFrEF, watch for fluid retention during titration.
Do not stop abruptly. Start very low (1.25 mg) in HFrEF and titrate every 1–2 weeks.
Metoprolol, Nebivolol, Propranolol
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Pharmacokinetics
Absorption
~90% oral bioavailability; low first-pass extraction.Distribution
Plasma protein binding ~30%.Metabolism
~50% hepatic; the rest excreted unchanged.Elimination
Renal (50% unchanged); balanced with hepatic clearance.Interactions
No interactions reported yet.
Monitoring
Patient counseling
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See also
References
Summary
Classes
Beta Blocker, Cardioselective (β1)
Common uses
Hypertension0, Heart failure0, Angina0
Pharmacy
Starting dose
2.5–5 mg daily (HTN); 1.25 mg daily (HFrEF, slow titration)
Preparations
5, 10 mg tabs
US FDA Max
20 mg/d
Pharmacology
Routes
Oral
Onset
1–2 h
Duration
24 h
Half-life
9–12 h
Bioavailability
~90% (low first-pass)
Pregnancy
Category C
Legal status
Rx-only in US
Purported mechanism
Highly β1-selective adrenergic antagonist. Greater selectivity than metoprolol or atenolol.