Zebeta (bisoprolol fumarate) is a cardioselective beta-adrenergic blocking agent indicated for the management of hypertension. It offers precise, sustained blood pressure control through its high affinity for β1-receptors, minimizing the non-cardiac effects often associated with non-selective beta-blockers. As a once-daily oral medication, it supports long-term cardiovascular stability and is a cornerstone in modern antihypertensive regimens. Its well-characterized pharmacokinetic profile and favorable side effect spectrum make it a preferred choice among clinicians for both newly diagnosed and treatment-experienced hypertensive patients.

Features

• Active ingredient: Bisoprolol fumarate
• Pharmacological class: Cardioselective beta-1 adrenergic receptor blocker
• Available strengths: 5 mg and 10 mg oral tablets
• Administration: Once daily, with or without food
• Half-life: 9–12 hours, supporting 24-hour therapeutic coverage
• Metabolism: Hepatic, with inactive metabolites primarily excreted renally
• Bioavailability: Approximately 80%, with low protein binding

Benefits

• Provides consistent 24-hour blood pressure reduction with single daily dosing
• Demonstrates high cardioselectivity, reducing risk of bronchospasm and peripheral vasoconstriction
• Lowers myocardial oxygen demand, offering cardioprotective benefits in hypertensive patients
• Exhibits a neutral metabolic profile, with minimal impact on glucose and lipid metabolism
• Supports regression of left ventricular hypertrophy over long-term use
• Compatible with most common antihypertensive combination therapies

Common use

Zebeta is primarily prescribed for the management of essential hypertension, either as monotherapy or in combination with other antihypertensive agents. It is particularly valuable in patients requiring cardioselective beta-blockade, including those with comorbid tachycardia or a history of myocardial infarction. Off-label uses may include stable chronic heart failure (NYHA Class II-III) as part of a comprehensive treatment plan, though this requires careful dose titration and monitoring.

Dosage and direction

Initiate treatment with 5 mg orally once daily. Dosage may be increased to 10 mg once daily if adequate blood pressure control is not achieved within 1–2 weeks. Maximum recommended dose is 20 mg daily. Administer with or without food, preferably at the same time each day. In elderly patients or those with renal impairment (CrCl <40 mL/min) or hepatic dysfunction, initiate at 2.5 mg daily and titrate cautiously. Do not abruptly discontinue; taper gradually over 1–2 weeks to avoid rebound hypertension or tachycardia.

Precautions

Monitor heart rate and blood pressure regularly, especially during dose titration. Use caution in patients with compensated heart failure, diabetes mellitus (may mask hypoglycemic symptoms), or thyrotoxicosis. May cause fatigue or dizziness—caution patients operating machinery. Not recommended during pregnancy unless potential benefit justifies potential risk. Breastfeeding should be discontinued during treatment. Periodic monitoring of renal function advised in patients with pre-existing renal impairment.

Contraindications

Hypersensitivity to bisoprolol or any component of the formulation. Severe bradycardia (heart rate <50 bpm). Cardiogenic shock. Decompensated cardiac failure. Sick sinus syndrome or second- or third-degree AV block (unless a permanent pacemaker is present). Severe bronchial asthma or history of bronchospasm.

Possible side effects

Most common (>5%): fatigue, dizziness, bradycardia. Common (1–5%): headache, diarrhea, nausea, cold extremities. Less common (<1%): sleep disturbances, depression, dyspnea, rash. Rare but serious: exacerbation of heart failure, bronchospasm, AV block, hypoglycemia, masking of thyrotoxicosis symptoms. Most adverse effects are dose-dependent and often diminish with continued therapy.

Drug interaction

Potentiates effects of other antihypertensives. Concurrent use with verapamil or diltiazem may cause additive bradycardia or AV block. May antagonize effects of beta-agonists (e.g., albuterol). NSAIDs may reduce antihypertensive efficacy. Clonidine withdrawal may be exacerbated. CYP2D6 inhibitors (e.g., fluoxetine, quinidine) may increase bisoprolol concentrations. Use caution with insulin or oral hypoglycemics—may mask tachycardia associated with hypoglycemia.

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed one. Maintain regular dosing schedule to ensure consistent therapeutic coverage.

Overdose

Symptoms may include severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and coma. Treatment is supportive and symptomatic: atropine for bradycardia, vasopressors for hypotension, glucagon for hypoglycemia, and bronchodilators for bronchospasm. Hemodialysis is not effective due to low protein binding and high volume of distribution.

Storage

Store at controlled room temperature (20–25°C/68–77°F). Protect from moisture and light. Keep in original container with lid tightly closed. Do not use after expiration date. Keep out of reach of children and pets.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional for diagnosis and treatment decisions. Do not initiate or discontinue medication without medical supervision. Individual response to therapy may vary.

Reviews

Clinical trials demonstrate Zebeta produces significant systolic and diastolic blood pressure reductions (placebo-corrected mean: -12.1/-7.5 mmHg at 10 mg dose). 74% of patients achieve target BP (<140/90 mmHg) with monotherapy. Long-term studies show maintained efficacy over 12+ months with consistent tolerability. Real-world evidence supports high adherence rates due to once-daily dosing and favorable side effect profile. Cardiologists frequently note its utility in patients intolerant to non-selective beta-blockers.