Zebeta

Zebeta (bisoprolol fumarate) is a cardioselective beta-1 adrenergic receptor blocking agent indicated for the management of hypertension. This second-generation beta-blocker offers precise cardiovascular targeting with demonstrated efficacy in reducing blood pressure and minimizing adverse effects through its high selectivity profile. Clinically validated in numerous studies, Zebeta provides physicians with a reliable therapeutic option for long-term hypertension management while maintaining favorable pharmacokinetic properties that support consistent 24-hour coverage with once-daily dosing.

Features

• Contains bisoprolol fumarate as active pharmaceutical ingredient
• Cardioselective beta-1 adrenergic receptor blockade
• Once-daily dosing regimen
• Available in 5 mg and 10 mg tablet strengths
• Linear pharmacokinetics with consistent absorption
• Elimination half-life of 9-12 hours
• Hepatic metabolism with renal excretion of metabolites
• White, round, film-coated tablets with appropriate scoring

Benefits

• Effectively reduces systolic and diastolic blood pressure through beta-1 receptor blockade
• Maintains cardioselectivity at therapeutic doses, minimizing pulmonary and metabolic side effects
• Provides 24-hour blood pressure control with single daily administration
• Demonstrates consistent antihypertensive effect regardless of patient age, race, or gender
• Offers favorable side effect profile compared to non-selective beta-blockers
• Supports long-term cardiovascular protection beyond blood pressure 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 or III) in combination with standard therapy, though this requires careful titration and monitoring. The medication is particularly suitable for patients who require beta-blockade but may be sensitive to bronchospastic effects due to its relative cardioselectivity. Physicians often consider Zebeta for hypertensive patients with concomitant tachycardia or those who have experienced side effects with non-selective beta-blockers.

Dosage and direction

The recommended initial dosage for hypertension is 5 mg once daily, which may be increased to 10 mg once daily if adequate blood pressure control is not achieved. For heart failure, treatment must be initiated with extreme caution using a special titration regimen beginning with 1.25 mg once daily, with gradual upward titration based on patient tolerance. Maximum recommended dosage is 20 mg once daily for hypertension. Administration should occur at the same time each day, with or without food, though consistency in administration relative to meals is recommended. Tablets should be swallowed whole with a glass of water and not chewed or crushed.

Precautions

Patients should be monitored for signs and symptoms of excessive bradycardia. Abrupt discontinuation should be avoided, particularly in patients with coronary artery disease, as rebound hypertension or angina exacerbation may occur. Use with caution in patients with diabetes mellitus as beta-blockers may mask tachycardia occurring with hypoglycemia. Hepatic or renal impairment requires dosage adjustment—for creatinine clearance less than 40 mL/min, maximum dose should not exceed 10 mg daily. Periodic assessment of renal function is recommended during long-term therapy. Patients should be advised about potential reduced exercise tolerance and possible dizziness, especially during initiation of therapy.

Contraindications

Zebeta is contraindicated in patients with cardiogenic shock, overt cardiac failure (unless specifically indicated for heart failure with proper titration), second- or third-degree AV block without a functioning pacemaker, sick sinus syndrome, severe bradycardia (heart rate <50 bpm), severe hepatic impairment, and hypersensitivity to bisoprolol or any component of the formulation. It should not be used in patients with bronchial asthma or severe chronic obstructive pulmonary disease requiring regular treatment with bronchodilators.

Possible side effects

Most common side effects include fatigue (approximately 4-9%), dizziness (4-8%), bradycardia (3-7%), and headache (3-6%). Less frequently reported effects include diarrhea, nausea, cold extremities, insomnia, and dyspnea. Serious adverse reactions may include worsening heart failure, AV block, bronchospasm, hypotension, masking of hypoglycemia symptoms, and Raynaud’s phenomenon. Psychiatric effects such as depression and sleep disturbances have been reported rarely. Laboratory abnormalities may include increased liver enzymes, though clinically significant hepatotoxicity is uncommon.

Drug interaction

Concurrent use with other beta-blockers or calcium channel blockers with negative chronotropic effects may produce additive bradycardia. Concomitant administration with digoxin may increase risk of bradycardia. Nonsteroidal anti-inflammatory drugs may reduce antihypertensive efficacy. CYP2D6 inhibitors (fluoxetine, paroxetine, quinidine) may increase bisoprolol concentrations. Insulin and oral hypoglycemics require dosage adjustment due to potential masking of hypoglycemia symptoms. MAO inhibitors should not be co-administered due to risk of hypertensive crisis. Clonidine withdrawal may be exacerbated by beta-blockade.

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. Patients should not double the dose to make up for a missed administration. Consistent daily dosing is important for maintaining stable blood pressure control, so patients should be counseled on adherence strategies and the importance of not missing consecutive doses.

Overdose

Symptoms of overdose include severe bradycardia, hypotension, heart failure, bronchospasm, hypoglycemia, and cardiac arrest. Management should include gastric lavage if ingestion was recent and symptomatic treatment. Atropine intravenously may be administered for bradycardia. Glucagon has been used successfully for beta-blocker overdose. Cardiac pacing may be necessary for profound bradycardia or AV block. Hemodialysis may be partially effective due to bisoprolol’s moderate protein binding (approximately 30%) and water solubility.

Storage

Store at controlled room temperature 20°C to 25°C (68°F to 77°F) with excursions permitted between 15°C and 30°C (59°F and 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 signs of discoloration or physical deterioration. Keep out of reach of children and pets. Properly dispose of unused or expired medication through take-back programs or according to FDA guidelines.

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 monitoring parameters. Patients should not alter their medication regimen without medical supervision. Full prescribing information including boxed warnings should be reviewed before administration.

Reviews

Clinical trials demonstrate Zebeta’s efficacy with 70-80% of hypertensive patients achieving blood pressure control at 10 mg daily dose. Long-term studies show maintained efficacy over 12-24 months of treatment with minimal development of tolerance. Cardiologists note its favorable selectivity profile makes it particularly useful in patients with concomitant respiratory conditions. Patient satisfaction surveys indicate good tolerability with most side effects being mild and transient. Meta-analyses confirm its position as an effective first-line antihypertensive with cardiovascular protective benefits beyond blood pressure reduction.