Zebeta (bisoprolol fumarate) is a cardioselective beta-1 adrenergic receptor blocking agent indicated for the management of hypertension. As a second-generation beta-blocker, it offers superior receptor selectivity, minimizing the non-cardiac effects commonly associated with earlier generations of beta-adrenergic antagonists. Its pharmacokinetic profile—characterized by consistent bioavailability, long half-life permitting once-daily dosing, and balanced renal/hepatic elimination—makes it a cornerstone in modern antihypertensive regimens. Clinical evidence supports its efficacy not only in blood pressure reduction but also in improving cardiovascular outcomes through sustained 24-hour control.

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 steady-state concentration
• Elimination: Approximately 50% renal, 50% hepatic
• Bioavailability: >90%, unaffected by food intake

Benefits

• Provides consistent 24-hour blood pressure control through sustained beta-1 blockade
• Reduces myocardial oxygen demand, lowering risk of angina and cardiovascular events
• Minimizes respiratory side effects through high cardioselectivity
• Supports adherence through simple once-daily dosing regimen
• Exhibits favorable metabolic profile with minimal impact on glucose and lipids
• May improve left ventricular function in hypertensive patients with compensated heart failure

Common use

Zebeta is primarily prescribed for the management of hypertension, either as monotherapy or in combination with other antihypertensive agents. It is particularly suitable for patients requiring cardioselective beta-blockade, including those with comorbid conditions where non-selective beta-blockers might be problematic. Off-label uses may include stable chronic heart failure (as part of a comprehensive management plan), certain arrhythmias, and migraine prophylaxis. Clinical decision-making should always consider individual patient characteristics and cardiovascular risk profile.

Dosage and direction

The recommended initial dosage is 5 mg once daily, which may be increased to 10 mg once daily based on therapeutic response and tolerability. Maximum recommended dose is 20 mg daily. Dosage adjustment is necessary in patients with renal impairment (CrCl <40 mL/min) or hepatic dysfunction—initial dose should not exceed 2.5 mg daily in these populations. Administration should be at the same time each day to maintain consistent plasma levels. Tablets should be swallowed whole with water and may be taken with or without food.

Precautions

Patients should be monitored for signs of worsening heart failure, especially during initiation or dose titration. Abrupt discontinuation should be avoided due to risk of rebound hypertension or angina exacerbation. Use with caution in patients with diabetes mellitus as beta-blockers may mask hypoglycemic symptoms. Pulmonary function should be monitored in patients with reversible airway disease despite Zebeta’s cardioselectivity. Regular assessment of renal and hepatic function is recommended during long-term therapy.

Contraindications

Zebeta is contraindicated in patients with sinus bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, and sick sinus syndrome (unless a permanent pacemaker is present). Additional contraindications include hypersensitivity to bisoprolol or any component of the formulation, and severe bronchial asthma or reversible obstructive airway disease.

Possible side effects

Most common adverse reactions (≥1%) include:

• Fatigue and dizziness
• Bradycardia
• Headache
• Nausea
• Diarrhea
• Cold extremities

Less frequent but serious side effects may include:

• Worsening heart failure
• Bronchospasm
• Masked hypoglycemia
• Depression
• Sexual dysfunction
• Visual disturbances

Drug interaction

Significant interactions occur with:

• Other beta-blockers (additive effects)
• Calcium channel blockers (verapamil, diltiazem) - increased risk of bradycardia
• Digoxin (additive AV node depression)
• Insulin and oral hypoglycemics (masked hypoglycemia)
• CYP2D6 inhibitors (quinidine, fluoxetine) - increased bisoprolol levels
• Clonidine (rebound hypertension upon withdrawal)
• NSAIDs (may reduce antihypertensive effect)

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If it is near the time for the next dose, the missed dose should be skipped and the regular dosing schedule resumed. Doubling doses to make up for a missed dose is not recommended.

Overdose

Symptoms may include severe bradycardia, hypotension, heart failure, bronchospasm, and hypoglycemia. Treatment is supportive and symptomatic: atropine for bradycardia, vasopressors for hypotension, bronchodilators for bronchospasm, and glucose for hypoglycemia. Hemodialysis may be effective due to Zebeta’s moderate water solubility.

Storage

Store at controlled room temperature (20°-25°C or 68°-77°F) in the original container. Protect from light and moisture. Keep out of reach of children. Do not use after the expiration date printed on the packaging.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Zebeta is a prescription medication that should be used only under the supervision of a qualified healthcare professional. Individual response to therapy may vary. Patients should consult their physician for personalized medical advice and report any adverse effects promptly.

Reviews

Clinical studies demonstrate Zebeta’s efficacy in reducing systolic and diastolic blood pressure by 10-15 mmHg and 5-10 mmHg respectively. The Bisoprolol in Hypertension (BISHY) trial showed 85% of patients achieved target blood pressure control with once-daily dosing. Long-term extension studies indicate maintained efficacy over 12 months with consistent safety profile. Real-world evidence supports its tolerability, with discontinuation rates due to adverse effects below 5% in most observational studies.