Bisoprolol
ZEBETA
Pronunciation: bis-OE-proe-loel
“Bison Zebra beta (blocks)”
LOL hat → beta blocker
What it isHighly beta-1 selective blocker; heart failure with reduced EF and hypertension.
Why this oneOne of only three beta blockers with heart-failure mortality data, and the most cardioselective of them.
What limits itBradycardia, and it must be titrated slowly in heart failure. Never stop abruptly.
Pearls
- Heart-failure use is off-label in the US despite mortality benefit
- Scored tablets ease slow heart-failure titration
Bisoprolol prescription history
Animated chart of estimated U.S. prescriptions per year, Beta blockers (1967–2026). Bisoprolol enters in 1992 (estimated).
FDA-approved for
- hypertension (1992)
Principal riskBradycardia
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityBradycardia, hypotension and bronchospasm; overdose may cause conduction block or cardiogenic shock.
FDA label
Read the full label on DailyMed ↗
NO BOXED WARNINGS
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Hypertension | adult | 5 mg QD (2.5 mg QD may be appropriate in some, e.g. bronchospastic disease) | 5-10 mg QD (individualized) | 20 mg QD |
Renal CrCl <40 mL/min: initial 2.5 mg QD, cautious titration; not dialyzable — no replacement dose needed on dialysis
Hepatic Hepatitis or cirrhosis: initial 2.5 mg QD, cautious titration
Instructions
- Avoid abrupt cessation — taper over ~1 week under observation
- Geriatric: no age-based adjustment unless significant renal/hepatic dysfunction
Available strengths
- tab 2.5, 5, 10 mg
Contraindications
- Cardiogenic shock
- Overt cardiac failure
- Second- or third-degree AV block
- Marked sinus bradycardia
Cautions
- May precipitate or worsen cardiac failure
- Abrupt cessation can exacerbate angina, MI, or ventricular arrhythmia — taper ~1 week
- Bronchospastic disease: beta-blockers generally not recommended; if needed use lowest dose (start 2.5 mg) with beta2-agonist available
- Can aggravate peripheral vascular disease symptoms
- May mask hypoglycemia (tachycardia) in diabetes
- May mask hyperthyroidism; abrupt withdrawal can precipitate thyroid storm
- Anesthesia/major surgery: impaired reflex adrenergic response
- Caution in renal or hepatic impairment
Adverse reactions
- Bradycardia (dose-related)
- Diarrhea (dose-related)
- Asthenia (dose-related)
- Fatigue (dose-related)
- Sinusitis (dose-related)
- Headache
- Dizziness
- URI, rhinitis, pharyngitis
- Peripheral edema
Pregnancy No adequate human studies; fetotoxic/maternotoxic in animals at high multiples of MRHD; use only if benefit justifies fetal risk
Lactation Not known if excreted in human milk (<2% of dose in rat milk); caution in nursing women
Cost
Generic entry2000
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Self-check
- How should bisoprolol be titrated in heart failure?
Slowly. - Can bisoprolol be stopped abruptly?
Never.