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Bisoprolol

Class
Adrenergic receptor blockers
Subclass
Cardioselective β-blockers
Substance name
Bisoprolol fumarate
Brand names
Zebeta®, Ziac®
Common formulations
Film-coated tablet
Dosage and administration
Adults patients
Treatment
Hypertension
•
Start at: 2.5-5 mg PO daily
•
Maintenance: 2.5-10 mg PO daily
•
Maximum: 20 mg per day
Titrate at minimum weekly intervals based on response to therapy and tolerance.
AF • Rate control • Off-label
•
2.5-10 mg PO daily
Atrial flutter • Rate control • Off-label
•
2.5-10 mg PO daily
Congestive HF • Off-label
•
Start at: 1.25 mg PO daily
•
Maintenance: 10 mg PO daily
Initiate in clinically stable, hospitalized patients not on intravenous inotropes.
HCM • Off-label
•
Start at: 1.25 mg PO daily
•
Maintenance: 1.25-20 mg PO daily
Titrate every 2 weeks to the maximum tolerated dose or a target LVOT gradient of < 30 mmHg.
Stable angina • Off-label
•
5-20 mg PO daily
Ventricular arrhythmias • Off-label
•
Start at: 2.5 mg PO daily
•
Maintenance: 2.5-10 mg PO daily
•
Maximum: 10 mg per day
Titrate gradually based on response and tolerance.
Prevention
AF, before CABG surgery • Off-label
•
1.25-20 mg PO daily, started 2-3 days before surgery
Titrate gradually based on BP and HR, and continue prophylaxis postoperatively.
Postoperative cardiac complications • Off-label
•
2.5-10 mg PO daily, started 30 to 2 days before surgery, preferably at least 1 week prior
Titrate gradually to achieve a resting HR of 60-70 bpm and a SBP > 100 mmHg.
Indications for use
Labeled indications
Adults
•
Treatment of hypertension
Off-label indications
Adults
•
Treatment of AF (rate control)
•
Treatment of atrial flutter (rate control)
•
Treatment of congestive HF
•
Treatment of HCM
•
Treatment of stable angina
•
Treatment of ventricular arrhythmias
•
Prevention of AF, before CABG surgery
•
Prevention of postoperative cardiac complications
Safety risks
Contraindications
Hypersensitivity to bisoprolol or its components
Marked sinus bradycardia, second- or third-degree AV block, cardiogenic shock, or overt cardiac failure
Warnings and precautions
AV block, bradycardia
•
Use caution in patients with impaired atrioventricular node function, older adults, or those on concurrent medications that impair atrioventricular nodal conduction (such as, CCBs, digoxin, ivabradine, antiarrhythmic agents).
CNS adverse events
•
Maintain a high level of suspicion, as bisoprolol is associated with an increased risk of CNS effects, including fatigue, insomnia, vivid dreams, memory impairment, and sexual dysfunction. If CNS or sexual side effects occur, reduce the dose or discontinue therapy. Symptoms are generally reversible upon dose adjustment or cessation.
Exacerbation of angina
•
Use caution in patients with vasospastic angina as β-blockers without alpha1-blocking activity can cause unopposed coronary vasoconstriction, worsening symptoms.
Exacerbation of bronchospasm
•
Use extreme caution in patients with bronchospastic disease, as β-blockers are generally contraindicated. However, due to its relative beta1-selectivity, bisoprolol may be considered in patients who cannot tolerate or do not respond to other antihypertensive treatments. Initiate therapy at the lowest dose and titrate cautiously. Keep a beta2-agonist (bronchodilator) readily available to manage potential bronchospasm.
Exacerbation of HF
•
Use caution in patients with compensated HF. Monitor closely for signs of decompensation, and discontinue gradually if HF develops.
Exacerbation of hypersensitivity reactions
•
Use extreme caution in patients with a history of severe anaphylactic reactions, as they may be more reactive to allergen exposure (accidental, diagnostic, or therapeutic). Beta-blockers may reduce responsiveness to standard epinephrine doses in anaphylaxis.
Exacerbation of muscle weakness, double vision
•
Use caution in patients with myasthenia gravis.
Exacerbation of myocardial infarction, ventricular arrhythmia, angina
•
Do not discontinue abruptly in patients with coronary artery disease, chronic β-blocker use, or a history of hypertension. Gradually taper the dose over one week with close monitoring. If withdrawal symptoms or acute coronary insufficiency develop, reinstitute bisoprolol therapy and initiate appropriate medical management.
Exacerbation of peripheral vascular disease, Raynaud disease
•
Use caution in patients with peripheral circulatory disorders, including Raynaud's disease or syndrome and peripheral occlusive vascular disease.
Exacerbation of psoriasis
•
Use caution in patients with psoriasis.
Hypertension
•
Use extreme caution in patients with untreated pheochromocytoma. Ensure adequate α-blockade is achieved before initiating bisoprolol to prevent a paradoxical increase in BP.
Major surgery
•
Maintain a high level of suspicion, as β-blockers should not be routinely withdrawn before major surgery, but their effect on adrenergic response may increase anesthesia and surgical risks.
Mask symptoms of hyperthyroidism
•
Use caution in patients with hyperthyroidism. Avoid abrupt withdrawal of β-blocker therapy to prevent symptom exacerbation or the precipitation of a thyroid storm.
Mask symptoms of hypoglycemia
•
Use caution in patients with diabetes.
Specific populations
Renal impairment
eGFR > 50 mL/min/1.73 m²
•
Use acceptable. No dose adjustment required. Titrate slowly.
eGFR 10-50 mL/min/1.73 m²
•
Reduce starting dose. Start at dose of 2.5-5 mg per day. Titrate slowly.
eGFR < 10 mL/min/1.73 m²
•
Reduce starting dose. Start at dose of 2.5 mg. Maximal dose of 10 mg. Titrate slowly.
Renal replacement therapy
Continuous renal replacement
•
Reduce starting dose. Start at a dose of 2.5 mg. Maximal dose of 10 mg. Titrate slowly.
Intermittent hemodialysis
•
Reduce starting dose. Start at a dose of 2.5 mg. Maximal dose of 10 mg. Titrate slowly. Dose after hemodialysis on dialysis days.
Peritoneal dialysis
•
Reduce starting dose. Start at a dose of 2.5 mg. Maximal dose of 10 mg. Titrate slowly.
Hepatic impairment
Any severity
•
Use with caution. Start at dose of 2.5 mg daily. Titrate slowly.
Pregnancy and breastfeeding
Pregnancy
All trimesters • Australia Category: C
•
Use only if benefits outweigh potential risks. Evidence of fetal harm in animals. Monitor placental blood flow. Monitor fetal growth. Monitor neonates for signs and symptoms of β-blockade.
Breastfeeding
Consider alternative agents that may be safer.
Unknown amount excreted in breastmilk.
Unknown drug levels in breastfed infants.
May potentially cause adverse effects in breastfed infants.
Adverse reactions
Very common > 10%
•
Headache
Common 1-10%
•
Diaphoresis, ↑ liver enzymes, peripheral edema, pharyngitis, angina pectoris, arthralgia, asthenia, chest pain, diarrhea, dizziness, dry mouth, dyspnea, fatigue, hypoesthesia, nausea, nightmares, vomiting, rhinitis
Uncommon < 1%
•
Bradycardia, depression
Unknown frequency
•
AV block, acne vulgaris, angioedema, bronchospasm, ↓ blood glucose, diabetes mellitus, erythroderma, heart failure, hypertension, ↑ blood glucose, ↑ serum triglycerides, orthostatic hypotension, peripheral vasoconstriction, Peyronie's disease, back pain, ↓ libido, erectile dysfunction, hair loss, hallucination, itching, muscle cramps, musculoskeletal pain, myalgia, palpitations, skin flushing, skin rash, syncope, tachycardia, tremor, vasculitis, wheezing
Interactions
Drug(s)
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