Zebeta: Advanced Beta-Blocker Therapy for Hypertension Control
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Synonyms
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Zebeta (bisoprolol fumarate) is a cardioselective beta-adrenergic blocking agent indicated for the management of hypertension. It offers precise cardiovascular control through its high affinity for β1-receptors, minimizing non-cardiac effects commonly associated with non-selective beta-blockers. This medication represents a cornerstone in modern antihypertensive therapy, providing reliable 24-hour blood pressure reduction with once-daily dosing. Clinical evidence supports its efficacy in both monotherapy and combination treatment regimens for sustained cardiovascular protection.
Features
- Contains bisoprolol fumarate as active pharmaceutical ingredient
- Selective β1-adrenergic receptor blockade
- Once-daily dosing regimen
- Available in 5mg and 10mg tablet strengths
- Extended duration of action (24-hour coverage)
- Linear pharmacokinetics across therapeutic range
- Minimal protein binding (approximately 30%)
- Hepatic metabolism with renal elimination of metabolites
Benefits
- Effective blood pressure control: Provides consistent 24-hour antihypertensive effect through sustained β1-receptor blockade
- Cardioselective action: Higher affinity for cardiac β1-receptors reduces incidence of bronchospasm and peripheral vascular complications
- Metabolic neutrality: Demonstrates minimal impact on glucose metabolism and lipid profiles compared to non-selective beta-blockers
- Convenient dosing: Once-daily administration improves patient adherence and maintains therapeutic coverage
- Cardioprotective effects: Reduces myocardial oxygen demand and provides anti-arrhythmic properties
- Well-tolerated profile: Lower incidence of fatigue and cold extremities compared to older beta-blockers
Common use
Zebeta is primarily prescribed for the management of hypertension, either as monotherapy or in combination with other antihypertensive agents. It may be utilized in patients with stable chronic heart failure (NYHA class II-III) as part of comprehensive management, though this represents an off-label use in some regions. The medication is particularly valuable in hypertensive patients who may benefit from cardioselective beta-blockade, including those with concomitant tachycardia or certain arrhythmias. Clinical practice often employs Zebeta in stepped-care approaches when thiazide diuretics or ACE inhibitors require supplementation for adequate blood pressure control.
Dosage and direction
Initial dosing: 5mg orally once daily, preferably in the morning Titration: May increase to 10mg once daily after 1-2 weeks based on therapeutic response Maximum dose: 20mg once daily (though 10mg is typically sufficient for most patients) Renal impairment: For creatinine clearance <40 mL/min, initiate with 2.5mg daily and titrate cautiously Hepatic impairment: Use similar precautions as with renal impairment due to balanced hepatic/renal elimination Administration: Should be taken with or without food, but consistency in administration relative to meals is recommended Monitoring: Blood pressure should be assessed 2-4 weeks after initiation or dose adjustment
Precautions
Abrupt withdrawal: Avoid sudden discontinuation; taper gradually over 1-2 weeks to prevent rebound hypertension or angina exacerbation Diabetes mellitus: May mask tachycardia associated with hypoglycemia; monitor blood glucose regularly Thyrotoxicosis: Can conceal clinical signs of hyperthyroidism such as tachycardia Peripheral vascular disease: Use with caution in patients with Raynaud’s phenomenon or peripheral arterial disease Anesthesia: Inform anesthesiologist about beta-blocker therapy before surgical procedures Pheochromocytoma: Should only be administered after alpha-blockade has been established Psoriasis: May exacerbate symptoms in predisposed individuals Ocular effects: Rare reports of keratoconjunctivitis sicca; consider ophthalmologic evaluation if visual changes occur
Contraindications
- Sinus bradycardia (heart rate <50 bpm)
- Second- or third-degree AV block without functioning pacemaker
- Cardiogenic shock
- Overt cardiac failure (unless specifically indicated and carefully monitored)
- Hypersensitivity to bisoprolol or any component of the formulation
- Severe bronchial asthma or chronic obstructive pulmonary disease requiring regular bronchodilator therapy
- Sick sinus syndrome
- Hypotension (systolic BP <90 mmHg)
Possible side effects
Common (≥1%):
- Fatigue and tiredness (approximately 6%)
- Dizziness (4%)
- Bradycardia (3%)
- Cold extremities (2%)
- Headache (2%)
Less common (0.1-1%):
- Sleep disturbances including insomnia or vivid dreams
- Gastrointestinal complaints (nausea, diarrhea)
- Dyspnea on exertion
- Erectile dysfunction
- Depression
Rare (<0.1%):
- AV conduction disturbances
- Bronchospasm in susceptible individuals
- Hallucinations
- Alopecia
- Hepatitis
- Thrombocytopenia
Drug interaction
Potentiating interactions:
- Other antihypertensives: Enhanced hypotensive effect with diuretics, ACE inhibitors, calcium channel blockers
- Antiarrhythmics: Increased risk of bradycardia with digoxin, amiodarone, diltiazem, verapamil
- CNS depressants: Additive effects with alcohol, barbiturates, opioids
- Insulin/oral hypoglycemics: Masked hypoglycemic symptoms and potentially altered glucose metabolism
Metabolic interactions:
- CYP2D6 inhibitors: Fluoxetine, paroxetine, quinidine may increase bisoprolol concentrations
- Rifampin: May decrease bisoprolol levels through CYP induction
Pharmacodynamic interactions:
- Sympathomimetics: Reduced efficacy of beta-agonists like albuterol
- MAO inhibitors: Risk of hypertensive crisis requires at least 14-day washout period
- Clonidine: Exaggerated rebound hypertension if discontinued concurrently
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 scheduled dose, the missed dose should be skipped and the regular dosing schedule resumed. Patients should never take a double dose to make up for a missed one. Consistent daily administration is important for maintaining stable blood pressure control, so use of pill organizers or reminder systems is recommended for patients with adherence challenges.
Overdose
Symptoms: Severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and impaired consciousness. Cardiovascular manifestations typically dominate the clinical picture.
Management:
- Gastric lavage if presentation is early after ingestion
- Atropine 0.5-2.0 mg IV for bradycardia
- Glucagon 1-10 mg IV for myocardial support
- Beta-adrenergic agonists (e.g., isoproterenol, dobutamine) for refractory cases
- Cardiac pacing for profound bradycardia or heart block
- IV fluids and vasopressors for hypotension unresponsive to above measures
- Continuous cardiac monitoring for at least 24 hours due to prolonged effects
Storage
Store at controlled room temperature (20-25°C or 68-77°F) in the original container. Protect from light and excessive moisture. Keep tightly closed and out of reach of children. Do not use if tablets show signs of discoloration or physical deterioration. Proper disposal of unused medication should follow local regulations, typically through drug take-back programs rather than flushing or household trash.
Disclaimer
This information is provided for educational purposes only and does not constitute medical advice. Treatment decisions should be made by qualified healthcare professionals based on individual patient characteristics. The prescribing physician should be consulted for specific recommendations regarding diagnosis, treatment, and monitoring. Full prescribing information including boxed warnings should be reviewed before initiating therapy.
Reviews
Clinical studies demonstrate Zebeta’s efficacy in reducing systolic and diastolic blood pressure by 10-15 mmHg and 8-12 mmHg respectively from baseline. In the Treatment of Mild Hypertension Study, bisoprolol showed superior 24-hour blood pressure control compared to other antihypertensives. Long-term extension studies indicate maintained efficacy over 2+ years of treatment with persistence rates exceeding 70%. Patient-reported outcomes generally reflect good tolerability, though individual responses vary. Real-world evidence supports its position as a well-tolerated option within the beta-blocker class, particularly for patients requiring cardioselective therapy.