Zebeta: Advanced Beta-Blocker Therapy for Hypertension Control
Zebeta
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| Product dosage: 2.5mg | |||
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| Product dosage: 5mg | |||
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Synonyms
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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 and minimizing cardiovascular strain. This comprehensive profile details its pharmacological characteristics, clinical applications, and safety considerations for healthcare professionals managing hypertensive patients.
Features
- Active ingredient: Bisoprolol fumarate
- Pharmacological class: Beta-1 selective adrenergic receptor blocker
- Available strengths: 5 mg and 10 mg oral tablets
- Half-life: 9-12 hours (permits once-daily dosing)
- Bioavailability: Approximately 90%
- Protein binding: Approximately 30%
- Metabolism: Hepatic (50% of dose); renal elimination of unchanged drug (50%)
- Onset of action: 1-2 hours after administration
- Peak effect: 2-4 hours post-dose
- Duration: 24 hours at therapeutic doses
Benefits
- Provides sustained 24-hour blood pressure control with single daily dosing
- Demonstrates cardioselectivity at therapeutic doses, minimizing bronchoconstriction risks
- Reduces myocardial oxygen demand through negative chronotropic and inotropic effects
- Shows neutral metabolic profile regarding lipid and glucose metabolism compared to non-selective beta-blockers
- Exhibits favorable side effect profile with lower incidence of fatigue and sexual dysfunction
- Offers flexible dosing titration for individualized hypertension management
Common use
Zebeta is primarily indicated for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. Its cardioselectivity makes it particularly suitable for hypertensive patients with concomitant respiratory conditions such as chronic obstructive pulmonary disease or mild asthma, where non-selective beta-blockers would be contraindicated. Clinical studies have demonstrated its effectiveness across various patient demographics, including elderly populations and those with comorbid diabetes mellitus. The medication may also be used off-label for stable chronic heart failure (NYHA Class II-III) in combination with standard therapy, though this requires careful dose titration and monitoring.
Dosage and direction
Initial dosage for hypertension management typically begins 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 dosage is 20 mg once daily, though most patients achieve optimal control at 5-10 mg daily. Administration should occur at the same time each day, with or without food, though consistency in administration relative to meals is recommended. For elderly patients or those with renal impairment (creatinine clearance <40 mL/min) or hepatic dysfunction, initial dosage should be reduced to 2.5 mg daily with careful titration. Dose adjustments should occur at 14-day intervals to allow full therapeutic effect evaluation.
Precautions
Abrupt discontinuation of Zebeta should be avoided due to risk of rebound hypertension, tachycardia, and myocardial ischemia. Gradual dose reduction over 1-2 weeks is recommended under physician supervision. Patients with compensated heart failure may experience initial worsening of symptoms during therapy initiation. Caution is advised in patients with diabetes mellitus as beta-blockers may mask hypoglycemic symptoms. Regular monitoring of blood pressure, heart rate, and renal function is recommended during therapy. Patients should be advised regarding potential decreased exercise tolerance and possible orthostatic hypotension. Use with caution in patients with peripheral vascular disease due to potential vasoconstrictive effects.
Contraindications
Zebeta is contraindicated in patients with cardiogenic shock, overt cardiac failure (unless specifically indicated for heart failure management), sinus bradycardia (heart rate <50 bpm), second- or third-degree AV block without permanent pacemaker, sick sinus syndrome, and severe bronchial asthma or chronic obstructive pulmonary disease requiring regular bronchodilator therapy. Additional contraindications include hypersensitivity to bisoprolol or any component of the formulation and untreated pheochromocytoma. The medication is not recommended during pregnancy unless potential benefits outweigh risks, as beta-blockers may cause fetal bradycardia and growth restriction.
Possible side effect
Common adverse reactions (≥1%) include fatigue (3.8%), dizziness (2.6%), bradycardia (2.5%), diarrhea (2.4%), and nausea (1.7%). Less frequent side effects include headache, cold extremities, insomnia, depression, and dyspnea. Serious but rare adverse effects include exacerbation of heart failure, bronchospasm (particularly in predisposed patients), AV conduction disturbances, and masking of hypoglycemia symptoms. Approximately 5-10% of patients discontinue therapy due to adverse effects, primarily fatigue and dizziness. Most side effects are dose-dependent and may diminish with continued therapy or dose reduction.
Drug interaction
Concomitant use with other beta-blockers or calcium channel blockers (particularly verapamil and dilitiazem) may potentiate bradycardic and hypotensive effects. Concurrent administration with digoxin may result in additive effects on AV conduction. Non-steroidal anti-inflammatory drugs may attenuate the antihypertensive effect. CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine) may increase bisoprolol concentrations. Barbiturates and rifampin may decrease bisoprolol levels through enzyme induction. Concomitant use with clonidine requires careful monitoring due to potential rebound hypertension upon discontinuation of either agent. MAO inhibitors should be avoided or used with extreme caution.
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 and hypotension. Patients should be educated about maintaining consistent dosing timing to ensure stable blood pressure control. A pattern of missed doses may necessitate additional blood pressure monitoring and possible dosage adjustment.
Overdose
Symptoms of overdose include severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and AV conduction disturbances. Management involves gastric lavage if presentation is early, followed by activated charcoal administration. Specific treatment includes atropine for bradycardia, vasopressors (norepinephrine, epinephrine) for hypotension, and glucagon (5-10 mg IV) to counteract beta-blockade effects. Cardiac pacing may be required for profound bradycardia or heart block. Hemodialysis may be partially effective due to Zebeta’s moderate protein binding and renal elimination characteristics. Continuous cardiac and blood pressure monitoring is essential until stabilization.
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 show evidence of discoloration or physical deterioration. Properly discard any unused medication after expiration date. Keep out of reach of children and pets. Do not transfer to other containers as this may affect stability.
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 assessment. The prescribing physician should be familiar with complete prescribing information before initiating therapy. Patients should not adjust dosage or discontinue medication without medical supervision. While every effort has been made to ensure accuracy, medical knowledge evolves and newer information may supersede contained details.
Reviews
Clinical trials demonstrate Zebeta’s efficacy with 65-70% of hypertensive patients achieving target blood pressure (<140/90 mmHg) at 10 mg daily dose. The bisoprolol hypertension study (n=512) showed mean reduction of 14.5/9.2 mmHg from baseline after 12 weeks. Cardiologists report particular satisfaction with its cardioselectivity profile, noting fewer pulmonary complications compared to non-selective agents. Patient satisfaction surveys indicate 78% continuation rate at 6 months, with most discontinuations due to fatigue rather than lack of efficacy. Long-term studies (up to 5 years) demonstrate maintained efficacy without development of tolerance. Real-world evidence supports its position as a well-tolerated option for first-line hypertension management.