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 specificity with demonstrated efficacy in reducing blood pressure through decreased cardiac output and inhibition of renin release from the kidneys. Its pharmacokinetic profile features high oral bioavailability and once-daily dosing convenience, making it a cornerstone therapy in cardiovascular risk management. Clinical evidence supports its role in both monotherapy and combination treatment regimens for sustained hypertension control.

Features

• Contains bisoprolol fumarate as active pharmaceutical ingredient
• Cardioselective beta-1 adrenergic blockade
• Once-daily oral administration
• Available in 5 mg and 10 mg tablet strengths
• Linear pharmacokinetics with dose proportionality
• Approximately 30% protein binding capacity
• Elimination half-life of 9-12 hours
• Hepatic metabolism with renal excretion of metabolites

Benefits

• Significantly reduces systolic and diastolic blood pressure measurements
• Lowers myocardial oxygen demand through negative chronotropic and inotropic effects
• Demonstrates fewer pulmonary side effects compared to non-selective beta-blockers
• Provides 24-hour blood pressure control with single daily dosing
• Shows neutral metabolic effects on glucose and lipid parameters
• Reduces cardiovascular morbidity associated with chronic hypertension

Common use

Zebeta is primarily prescribed for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. It may be utilized in stable chronic heart failure (NYHA class II-III) with reduced ejection fraction as part of comprehensive management. Off-label uses include management of angina pectoris, certain arrhythmias, and migraine prophylaxis, though these applications require specific clinical justification and monitoring.

Dosage and direction

The recommended initial dosage for hypertension is 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 dosage is 20 mg daily. For heart failure management, initiation begins with 1.25 mg once daily with gradual titration based on tolerability. Administration should occur at the same time each day, with or without food. Tablets should be swallowed whole with water and not crushed or chewed.

Precautions

Abrupt discontinuation may precipitate angina exacerbation or rebound hypertension—taper gradually over 1-2 weeks. Use caution in patients with compensated heart failure, diabetes mellitus (may mask hypoglycemic symptoms), or thyrotoxicosis. May exacerbate symptoms in patients with peripheral vascular disease or Raynaud’s phenomenon. Regular monitoring of blood pressure, heart rate, and cardiac function is recommended during therapy. Not recommended during pregnancy unless potential benefit justifies potential risk to fetus.

Contraindications

Patients with sinus bradycardia (heart rate <45-50 bpm), sick sinus syndrome, or second- or third-degree AV block (without permanent pacemaker). Cardiogenic shock, decompensated heart failure requiring IV inotropic therapy, and severe bronchial asthma or COPD. Hypersensitivity to bisoprolol or any component of the formulation. Severe hepatic impairment (Child-Pugh class C) due to altered metabolism.

Possible side effects

Most common adverse reactions (≥5%) include fatigue, dizziness, bradycardia, diarrhea, and asthenia. Less frequent effects include headache, nausea, sleep disturbances, cold extremities, and dyspnea. Serious but rare adverse events include heart block, worsening heart failure, bronchospasm, depression, and hallucinations. Sexual dysfunction and reduced exercise tolerance may occur. Laboratory abnormalities may include elevated liver enzymes and blood urea nitrogen.

Drug interaction

Concurrent use with other beta-blockers or calcium channel blockers (verapamil, diltiazem) may potentiate bradycardic effects. NSAIDs may diminish antihypertensive efficacy. Concomitant use with insulin or oral hypoglycemics may mask hypoglycemia symptoms. CYP2D6 inhibitors (fluoxetine, paroxetine) may increase bisoprolol concentrations. Digoxin coadministration may increase risk of bradycardia. MAO inhibitors require careful monitoring due to additive hypotensive effects.

Missed dose

If a dose is missed, it should be taken as soon as remembered on the same day. If remembered near the time of the next scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Doubling of doses is not recommended due to potential excessive bradycardia or hypotension. Patients should maintain a consistent dosing routine and use pill organizers or reminders if adherence issues persist.

Overdose

Symptoms may include severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and coma. Management includes gastric lavage if ingestion recent, activated charcoal, and supportive measures. Atropine IV for bradycardia, vasopressors (norepinephrine, epinephrine) for hypotension, and glucagon for refractory cases. Cardiac pacing may be necessary for profound bradycardia. Hemodialysis is not effective due to high protein binding. Continuous cardiac and vital sign monitoring required.

Storage

Store at controlled room temperature (20-25°C or 68-77°F) with excursions permitted between 15-30°C (59-86°F). Protect from moisture and light. Keep container tightly closed. Dispense in original container with child-resistant closure. Do not use if tablets appear discolored or show signs of deterioration. Keep out of reach of children and pets. Properly dispose of expired or unused medication through drug take-back programs.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Prescription and use of Zebeta must be under supervision of a qualified healthcare professional. Individual response to therapy may vary based on clinical factors. Patients should not alter dosage or discontinue medication without consulting their physician. Full prescribing information should be reviewed before initiation of therapy.

Reviews

Clinical trials demonstrate 65-70% of hypertensive patients achieve blood pressure control with Zebeta monotherapy. Meta-analyses show consistent 10-15 mmHg reduction in systolic pressure and 8-12 mmHg in diastolic pressure. Cardiologists report favorable tolerability profile compared to earlier beta-blockers. Some patients note improved exercise tolerance with cardioselective action. Long-term studies indicate maintained efficacy over 12-24 months of treatment with minimal tachyphylaxis. Combination therapy with diuretics or ACE inhibitors shows synergistic effects in resistant hypertension.