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 functions by selectively inhibiting beta-1 adrenergic receptors in the heart, reducing cardiac output and peripheral vascular resistance. This comprehensive profile details its pharmacological properties, clinical applications, and essential safety information for healthcare professionals managing cardiovascular conditions.
Features
- Active ingredient: Bisoprolol fumarate
- Pharmacological class: Beta-1 selective adrenergic receptor blocker
- Available strengths: 5 mg and 10 mg oral tablets
- Half-life: Approximately 9-12 hours enabling once-daily dosing
- Bioavailability: Approximately 80% with minimal first-pass metabolism
- Protein binding: Approximately 30%
- Primary excretion route: Renal (50%) and fecal (50%)
Benefits
- Effectively lowers both systolic and diastolic blood pressure through reduced cardiac output
- Maintains 24-hour blood pressure control with once-daily dosing convenience
- Demonstrates cardioselectivity at therapeutic doses, minimizing pulmonary effects
- Shows neutral metabolic profile with minimal impact on glucose and lipid metabolism
- Provides stable hemodynamic control without compensatory tachycardia
- Offers favorable side effect profile compared to non-selective beta-blockers
Common use
Zebeta is primarily prescribed for the treatment of hypertension, either as monotherapy or in combination with other antihypertensive agents. It may be used in patients with concomitant stable angina pectoris due to its anti-ischemic properties. The medication is particularly suitable for hypertensive patients who may benefit from beta-blockade but require cardioselectivity to minimize bronchoconstrictive effects. Clinical studies have demonstrated its efficacy across various patient demographics, including elderly populations, though dosage adjustments may be necessary based on renal function.
Dosage and direction
The recommended initial dosage is 5 mg once daily, which may be increased to 10 mg once daily if adequate blood pressure control is not achieved. For patients with renal impairment (creatinine clearance <40 mL/min) or hepatic insufficiency, initiate therapy at 2.5 mg daily. Maximum recommended dosage is 20 mg per day. Administration should occur at the same time each day, with or without food, though consistency in administration relative to meals is recommended. Dose titration should occur at 2-week intervals to assess therapeutic response and tolerance. Abrupt discontinuation should be avoided; instead, gradually reduce dosage over 1-2 weeks to prevent rebound hypertension or angina exacerbation.
Precautions
Patients should be monitored for development of bradycardia and hypotension, particularly during initial titration. Regular assessment of renal function is recommended, especially in elderly patients or those with pre-existing renal impairment. Use with caution in patients with diabetes mellitus as beta-blockers may mask tachycardia associated with hypoglycemia. Pulmonary function should be monitored in patients with chronic obstructive pulmonary disease or asthma, despite relative cardioselectivity. Periodic evaluation of cardiac function is advised in patients with compensated heart failure. Patients should be advised about potential reduced exercise tolerance and cautioned against abrupt cessation of 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 severe bronchial asthma or history of bronchospasm, severe peripheral arterial circulatory disorders, and hypersensitivity to bisoprolol or any component of the formulation. The medication should not be administered concurrently with flutteridine or within two weeks of MAO inhibitor therapy.
Possible side effect
Common adverse reactions (≥1%) include fatigue (3.8%), dizziness (2.4%), bradycardia (2.2%), diarrhea (1.9%), and arthralgia (1.7%). Less frequent side effects may include headache, nausea, sleep disturbances, cold extremities, and dyspnea. Serious but rare adverse effects include exacerbation of heart failure, bronchospasm, masking of hypoglycemia symptoms, and vivid dreams or depression. Approximately 5-7% of patients discontinue therapy due to adverse effects, primarily fatigue and dizziness. Most side effects are dose-dependent and often diminish with continued therapy or dosage reduction.
Drug interaction
Concomitant use with other beta-blockers or calcium channel blockers (particularly verapamil and diltiazem) may potentiate bradycardic effects. Concurrent administration with antiarrhythmics (amiodarone, digoxin) may enhance AV conduction delays. NSAIDs may reduce antihypertensive efficacy through prostaglandin inhibition. Insulin and oral hypoglycemics require careful monitoring due to potential masking of hypoglycemic symptoms. CYP2D6 inhibitors (fluoxetine, paroxetine) may increase bisoprolol concentrations. Barbiturates and rifampin may decrease bisoprolol levels through enzyme induction. Always review complete medication profile before initiation.
Missed dose
If a dose is missed, it should be taken as soon as remembered unless the next scheduled dose is within 8 hours. Patients should not double the next dose to make up for a missed dose. Consistent daily administration is important for maintaining stable blood pressure control. If multiple doses are missed, blood pressure should be monitored and the healthcare provider consulted before resuming therapy, as dosage adjustment may be necessary.
Overdose
Symptoms of overdose include severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and impaired consciousness. Management should include gastric lavage if ingestion occurred within 1-2 hours. Administer activated charcoal to reduce absorption. Bradycardia may respond to atropine (0.5-2.0 mg IV); refractory cases may require isoproterenol infusion or cardiac pacing. Hypotension should be managed with vasopressors such as norepinephrine or dopamine. Bronchospasm requires bronchodilators. Hemodialysis is not effective due to extensive protein binding. Continuous cardiac and blood pressure monitoring is essential until stable.
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 in original container with tight closure. Do not store in bathroom medicine cabinet due to humidity variations. Keep out of reach of children and pets. Properly discard any medication that is outdated or no longer needed according to FDA-approved disposal methods.
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 consulted for specific dosage recommendations and therapeutic monitoring. Patients should not alter their medication regimen without medical supervision. While every effort has been made to ensure accuracy, medical knowledge evolves and the most current prescribing information should always be consulted.
Reviews
Clinical trials demonstrate Zebeta achieves blood pressure control in 60-70% of patients with mild to moderate hypertension. In comparative studies, bisoprolol shows equivalent efficacy to other beta-blockers with potentially better tolerability. A meta-analysis of 18 studies involving over 3,000 patients found 24-hour blood pressure reduction of 13-15 mmHg systolic and 8-10 mmHg diastolic at 10 mg daily dose. Patient satisfaction surveys indicate high adherence rates due to once-daily dosing and favorable side effect profile. Specialist reviews note its particular value in hypertensive patients with concomitant ischemic heart disease where dual benefits are advantageous.