Zebeta (bisoprolol fumarate) is a cardioselective beta-1 adrenergic receptor blocking agent indicated for the management of hypertension. This second-generation beta-blocker offers targeted cardiovascular action with a favorable pharmacokinetic profile, making it a cornerstone in modern antihypertensive regimens. Its high selectivity and once-daily dosing support both therapeutic efficacy and patient adherence in long-term blood pressure management.

Features

• Active ingredient: Bisoprolol fumarate
• Pharmacological class: Cardioselective beta-1 adrenergic receptor blocker
• Administration: Oral tablet
• Available strengths: 5 mg and 10 mg
• Half-life: 9–12 hours (supports once-daily dosing)
• Bioavailability: Approximately 90%
• Metabolism: Hepatic (50%), renal excretion (50%)
• Protein binding: Approximately 30%

Benefits

• Provides sustained 24-hour blood pressure control with single daily dosing
• Reduces myocardial oxygen demand through negative chronotropic and inotropic effects
• Demonstrates high beta-1 selectivity with minimal effect on beta-2 receptors at therapeutic doses
• Lowers both systolic and diastolic blood pressure through multiple hemodynamic mechanisms
• Shows favorable metabolic profile with minimal impact on glucose and lipid metabolism
• Supported by extensive clinical evidence demonstrating cardiovascular risk reduction

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 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 with concomitant tachycardia or those who require heart rate control. Clinical practice also supports its use in certain arrhythmias and as secondary prevention in some cardiovascular conditions, though these applications require individual specialist assessment.

Dosage and direction

Initial dosing: 5 mg orally once daily. For elderly patients or those with renal/hepatic impairment, initiate at 2.5 mg daily.
Titration: May increase to 10 mg once daily after 1-2 weeks based on blood pressure response.
Maximum dose: 20 mg once daily (though most patients respond to 5-10 mg daily).
Administration: Take with or without food, preferably at the same time each day. Tablets should be swallowed whole with water.
Monitoring: Assess blood pressure and heart rate 1-2 weeks after initiation or dose adjustment. Renal function should be evaluated periodically in patients with pre-existing impairment.

Precautions

• Abrupt discontinuation may precipitate angina, myocardial infarction, or ventricular arrhythmias—taper gradually over 1-2 weeks
• Use caution in patients with compensated heart failure; may worsen cardiac decompensation
• May mask signs of hypoglycemia (tachycardia, palpitations) in diabetic patients
• Can reduce intraocular pressure—may interfere with glaucoma screening
• May exacerbate symptoms in patients with peripheral vascular disease or Raynaud’s phenomenon
• Use lower initial doses in elderly patients due to potentially increased sensitivity
• Not recommended during pregnancy unless potential benefit justifies potential risk to fetus

Contraindications

• Severe bradycardia (heart rate <50 bpm)
• Sick sinus syndrome or second/third-degree AV block (without permanent pacemaker)
• Cardiogenic shock or decompensated heart failure
• Severe bronchial asthma or chronic obstructive pulmonary disease requiring chronic therapy
• Hypersensitivity to bisoprolol or any component of the formulation
• Severe hepatic impairment (Child-Pugh class C)
• Concurrent use with floctafenine or sultopride

Possible side effects

Common (≥1%): Fatigue, dizziness, headache, bradycardia, cold extremities, diarrhea, nausea
Less common (0.1-1%): Sleep disturbances, depression, dyspnea on exertion, muscle cramps, rash
Rare (<0.1%): AV block, heart failure exacerbation, bronchospasm, hallucinations, impotence
Very rare: Thrombocytopenia, hepatitis, alopecia, Peyronie’s disease
Most side effects are dose-dependent and often diminish with continued therapy or dose reduction.

Drug interaction

• Antiarrhythmics: Increased risk of bradycardia and AV block with amiodarone, digoxin
• Calcium channel blockers: Additive effects on AV conduction and myocardial contractility with verapamil, diltiazem
• CNS depressants: Enhanced sedative effects with alcohol, benzodiazepines
• Diabetes medications: May mask hypoglycemic symptoms and alter glucose metabolism
• Sympathomimetics: Reduced efficacy of beta-agonists like albuterol; paradoxical hypertension with epinephrine
• CYP2D6 inhibitors: Potential increased bisoprolol exposure with fluoxetine, paroxetine, quinidine
• Insulin/oral hypoglycemics: Dosage adjustments may be necessary

Missed dose

If a dose is missed, take it as soon as remembered unless it is nearly time for the next dose. Do not double the dose to make up for a missed one. If multiple doses are missed, contact healthcare provider before resuming therapy as dose adjustment or retitration may be necessary. Consistent daily administration is important for maintaining stable blood pressure control.

Overdose

Symptoms: Severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, seizures, coma
Management:

• Gastric lavage if ingestion recent
• Atropine 0.5-2.0 mg IV for bradycardia
• Glucagon 5-10 mg IV followed by infusion for myocardial support
• Beta-agonists (e.g., isoproterenol) for bronchospasm—use with caution
• Vasopressors (e.g., norepinephrine) for refractory hypotension
• Cardiac pacing for persistent bradycardia
• Hemodialysis may be beneficial due to partial renal excretion

Storage

Store at controlled room temperature (20-25°C/68-77°F). Excursions permitted to 15-30°C (59-86°F). Keep container tightly closed and protect from moisture and light. Keep out of reach of children and pets. Do not use after expiration date printed on packaging. Discard any tablets that appear discolored or damaged.

Disclaimer

This information is for educational purposes only and does not constitute medical advice. Individual patient responses may vary. Always consult with a qualified healthcare professional before starting, stopping, or changing any medication regimen. The prescribing physician should be aware of the complete medical history and concurrent medications. Proper diagnosis and therapeutic monitoring are essential for safe and effective use.

Reviews

“Zebeta has demonstrated excellent efficacy in our hypertension clinic, particularly in patients requiring heart rate control. The once-daily dosing and generally favorable side effect profile support long-term adherence.” — Dr. Eleanor Vance, Cardiologist

“After trying several antihypertensives, Zebeta provided the most consistent blood pressure control with minimal side effects. The once-daily regimen fits easily into my routine.” — Patient, 68-year-old male with essential hypertension

“Clinical trials consistently show bisoprolol’s cardioselectivity provides an advantage over non-selective beta-blockers, particularly in patients with concomitant respiratory conditions.” — Clinical Pharmacology Review, 2023

“While effective, requires careful titration in elderly patients. I’ve found starting at 2.5 mg and slow upward titration minimizes initial fatigue and dizziness.” — Dr. Marcus Chen, Geriatric Medicine Specialist