Bisoprolol

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.

Experience

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Problems

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Titration strategies

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Effects

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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

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Monitoring

Heart rate, blood pressure; in HFrEF, watch for fluid retention during titration.

Patient counseling

Do not stop abruptly. Start very low (1.25 mg) in HFrEF and titrate every 1–2 weeks.

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See also

Metoprolol, Nebivolol, Propranolol

References

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

Common uses

Classification(s)

Classes

Beta Blocker, Cardioselective (β1)

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.