Bisoprolol | Pharmacology Mentor

Generic Name

Bisoprolol

Brand Names

for propranolol* in some countries—ensure you’re prescribing the correct generic.

Mechanism

Selective β1‑receptor blockade → ↓ sympathetic tone on cardiac myocytes and conducting tissue.
Resulting effects:
Decrease heart rate and contractility (negative chronotropic & inotropic).
Reduce myocardial oxygen demand and improve diastolic filling.
Lower renin release → ↓ systemic vasoconstriction (indirect antihypertensive effect).
Clinical impact: Particularly useful in patients where β2‑mediated bronchodilation or vasodilation is undesirable.

Pharmacokinetics

Absorption: Oral; ~40–60 % oral bioavailability; peak plasma concentration 1–4 h post‑dose.
Distribution: Widely distributed; protein‑binding ~70 %.
Metabolism: Hepatic: primarily cytochrome P‑450 2D6 (CYP2D6) with significant inter‑individual variability.
Excretion: Renal (~20 %) and fecal; terminal half‑life 7–12 h.
Drug interactions:
CYP2D6 inhibitors (e.g., fluoxetine) ↑ bisoprolol levels.
Concomitant antihypertensives → additive hypotension.
Digoxin & other β‑blockers → additive bradycardia/heart block.

Indications

Hypertension – first‑line or add‑on therapy.
Chronic heart failure (NYHA II–IV) – improves survival in combination with ACEi/ARB.
Stable angina pectoris – reduces cardiac workload.
Post‑myocardial infarction – part of β‑blocker regimen to diminish arrhythmia risk.
Headache prophylaxis – secondary use in treating migraine.
Oral antihypertensive/heart‑failure regimens in patients intolerant to non‑selective β‑blockers.

Contraindications

Contraindications
• Cardiac conduction abnormalities: complete heart block, second‑degree AV block (without pacemaker).
• Bradycardia (<50 bpm when at rest).
• Sick sinus syndrome.
• Severe asthma/COPD (if β2‑mediated bronchodilation needed).
• Uncontrolled hypovolemia or shock.

Warnings
• Heart failure & ischemia: Start low‑dose, titrate slowly to avoid precipitating decompensation.
• Kidney disease: Renal clearance is limited; adjust dose in CKD.
• Diabetes: Mask hypoglycemia symptoms; monitor blood glucose.
• Pregnancy/Lactation: Category C; use only if benefits outweigh risks.

Dosing

Condition	Initial Dose	Titration	Max Dose	Formulation
Hypertension	10 mg PO once daily	↑10 mg q2‑wk until target	40 mg/day	Tablet 10–40 mg
Chronic HF	5 mg PO once daily	↑5 mg q2‑wk up to 20 mg	20 mg/day	Tablet
Angina	5–10 mg PO once daily	↑5 mg q2‑wk as tolerated	40 mg/day	Tablet

• Administer with a full meal to reduce GI upset.
• Avoid abrupt discontinuation; taper over 1–2 weeks to prevent rebound hypertension or tachycardia.

Adverse Effects

Common (≥5 %)
• Fatigue, dizziness, mild hypotension.
• Bradycardia, syncope (especially at initiation).
• Gastrointestinal upset (nausea, diarrhea).
• Peripheral edema (rare).

Serious (≤1 %)
• Severe bradycardia or heart block.
• Exacerbation of heart failure.
• Asthma attack/febrile bronchospasm.
• Severe dizziness leading to falls.

Rare
• Skin rash, photosensitivity.
• Hypoglycemia masking (in diabetics).

Global Safety Note – Monitor ECG and vital signs, particularly within the first 2–4 weeks.

Monitoring

Baseline: Blood pressure, HR, ECG (QTc), serum creatinine, electrolytes.
During therapy:
BP & HR every 1–2 weeks during dose titration.
Monthly weight & edema assessment in HF patients.
Renal panels every 3 months—or sooner if CKD.
Long‑term: Annual ECG or Holter for symptomatic patients; glucose testing in diabetics.

Clinical Pearls

“Big‑B” rule: Bisoprolol is the *brand name for propranolol* in some countries—ensure you’re prescribing the correct generic.
CYP2D6 phenotypes matter: Poor metabolizers may experience higher plasma levels; consider lower starting doses.
Heart‑failure titration: The “oligosaccharide” algorithm—increase dose every 2 weeks, re‑evaluate EF and symptoms at 6 weeks.
Hypertensive crisis? Stop bisoprolol; treat underlying volume overload first.
Diabetics? Bisoprolol can blunt hypoglycemia signs—add glucose meter alarms.
Pregnancy‑risk: Use only if the alternative (ACEi) is contraindicated; review safety data before prescribing.
Non‑selective check: If a patient presents with asthma or COPD, verify that bisoprolol is truly cardioselective and not a mis‑coppied β1 antagonist.
Drug‑drug synergy: Combine with ACEi/ARB + diuretic for optimal HF outcomes (the “Gold 4” combo).

*Reference‑friendly* – Use drug monographs, UpToDate, and FDA labels for updates.