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 a favorable pharmacokinetic profile, making it a cornerstone in modern antihypertensive regimens. Its once-daily dosing and well-tolerated nature position it as a first-line option for clinicians seeking effective blood pressure control while minimizing adverse effects. This agent demonstrates particular utility in patients requiring precise modulation of sympathetic nervous system activity without compromising pulmonary or metabolic parameters.

Features

• Contains bisoprolol fumarate as active pharmaceutical ingredient
• Selective beta-1 adrenergic receptor antagonism
• Once-daily oral administration
• Linear pharmacokinetics with dose proportionality
• High oral bioavailability (~90%)
• Balanced renal and hepatic elimination pathways
• Available in 5 mg and 10 mg tablet strengths
• White, round, film-coated tablets with functional score

Benefits

• Precise Blood Pressure Control: Demonstrates consistent 24-hour antihypertensive efficacy through sustained beta-1 receptor blockade
• Cardioprotective Effects: Reduces myocardial oxygen demand and attenuates inappropriate sympathetic activation
• Metabolic Neutrality: Minimal impact on glucose metabolism and lipid profiles compared to non-selective beta-blockers
• Renal Function Preservation: Maintains renal blood flow and glomerular filtration rate through selective action
• Improved Tolerability: Lower incidence of bronchospasm and peripheral vasoconstriction versus non-selective agents
• Flexible Dosing: Functional score allows precise dose titration according to individual patient response

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 suitable for patients with concomitant conditions where selective beta-blockade is advantageous, including stable angina pectoris, post-myocardial infarction management, and certain arrhythmias. The medication finds special utility in hypertensive patients with compensated heart failure where beta-blockade is indicated, though initiation requires careful titration under specialist supervision.

Dosage and direction

Initiate treatment with 5 mg orally once daily, preferably in the morning. Dosage may be increased to 10 mg once daily after 1-2 weeks based on therapeutic response. Maximum recommended dose is 20 mg daily. In elderly patients or those with renal impairment (creatinine clearance <40 mL/min) or hepatic dysfunction, initiate with 2.5 mg daily. Tablets should be swallowed whole with water and may be taken with or without food. Dose titration should occur at minimum 2-week intervals with careful blood pressure monitoring.

Precautions

Exercise caution in patients with compensated heart failure, diabetes mellitus, thyrotoxicosis, or peripheral vascular disease. Monitor pulmonary function in patients with chronic obstructive pulmonary disease or asthma. Regular assessment of heart rate, blood pressure, and clinical status is recommended during therapy initiation and titration. Abrupt discontinuation may precipitate rebound hypertension or angina exacerbation; taper gradually over 1-2 weeks. Use with caution during major surgery due to potential interactions with anesthetic agents.

Contraindications

Hypersensitivity to bisoprolol or any component of the formulation. Severe bradycardia (heart rate <50 bpm). Cardiogenic shock. Decompensated cardiac failure requiring intravenous inotropic support. Second- or third-degree atrioventricular block without permanent pacemaker. Severe bronchial asthma or reactive airway disease. Severe hepatic impairment (Child-Pugh class C). Concurrent use with floctafenine or sultopride.

Possible side effect

Common (≥1/100 to <1/10): Fatigue, dizziness, headache, bradycardia, cold extremities Uncommon (≥1/1,000 to <1/100): Sleep disturbances, depression, dyspnea, gastrointestinal disturbances Rare (≥1/10,000 to <1/1,000): Bronchospasm, heart failure exacerbation, AV conduction disturbances Very rare (<1/10,000): Hallucinations, Peyronie’s disease, thrombocytopenia Most adverse reactions are dose-dependent and diminish with continued therapy or dose reduction

Drug interaction

Potentiates hypotensive effects: Other antihypertensives, nitrates, antipsychotics Risk of bradycardia: Digitalis glycosides, amiodarone, ivabradine Metabolic interactions: Insulin and oral hypoglycemics (masked hypoglycemia symptoms) Enzyme inhibitors: CYP2D6 inhibitors (quinidine, fluoxetine) may increase bisoprolol concentrations Enzyme inducers: Rifampicin may decrease bisoprolol efficacy Anesthetic agents: Enhanced cardiodepressant effects during general anesthesia

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next scheduled dose. Do not double the dose to make up for a missed administration. If multiple doses are missed, contact healthcare provider for guidance on resumption of therapy, as dose retitration may be necessary.

Overdose

Symptoms include severe bradycardia, hypotension, heart failure, bronchospasm, and hypoglycemia. Management involves gastric lavage if recent ingestion, followed by activated charcoal. Administer atropine 0.5-2.0 mg IV for bradycardia. Glucagon 1-10 mg IV may reverse cardiovascular effects. Cardiac pacing and inotropic support may be required for refractory cases. Hemodialysis is not effective due to high protein binding.

Storage

Store at controlled room temperature (20-25°C/68-77°F). Protect from moisture and light. Keep container tightly closed. Do not use after expiration date printed on packaging. Keep out of reach of children and pets. Do not transfer tablets to other containers as this may affect stability.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional before starting or changing any medication regimen. Dosage and administration should be determined by a physician based on individual patient characteristics. Not all possible uses, interactions, or adverse effects are listed here.

Reviews

Clinical studies demonstrate Zebeta’s efficacy in reducing systolic and diastolic blood pressure by 10-15 mmHg and 5-10 mmHg respectively at maintenance doses. The TOMH study showed superior quality of life parameters compared to other antihypertensives. Long-term extension studies indicate maintained efficacy over 2+ years of treatment with consistent safety profile. Real-world evidence supports its position as a well-tolerated option in diverse patient populations, particularly those requiring cardioselective beta-blockade.