Zebeta 5 mg Tablets

Brand Name

This medication is marketed under the trade name Zebeta, widely recognized among healthcare practitioners for its role in managing cardiovascular conditions.

International Nonproprietary Name (INN)

The active ingredient is universally identified as bisoprolol, ensuring its consistent recognition across global medical standards.

Form of Release

The drug is available as film-coated tablets, crafted for oral administration and provided in various strengths to meet diverse patient requirements. These tablets are designed for ease of use and maintain stability under standard storage environments.

Composition

Bisoprolol fumarate constitutes the core active component, engineered to influence heart rate and blood pressure dynamics. Accompanying this are auxiliary substances such as microcrystalline cellulose, lactose monohydrate, magnesium stearate, and crospovidone, which support tablet structure and facilitate disintegration upon ingestion. The film coating, typically composed of hypromellose, titanium dioxide, and polyethylene glycol, enhances swallowability and protects the active substance from degradation. Some formulations may include colorants for visual distinction. Each element is carefully selected to optimize the therapeutic action of bisoprolol while ensuring its consistency.

Pharmacologic Properties

Pharmacodynamics

This medication operates as a highly selective beta-1 adrenergic receptor blocker, primarily targeting receptors in cardiac tissue to exert its effects. By inhibiting the binding of catecholamines like adrenaline, it reduces heart rate and myocardial contractility, lowering cardiac output and oxygen demand. Its selectivity for beta-1 receptors minimizes impact on beta-2 receptors in the lungs and peripheral vasculature, reducing risks of bronchoconstriction compared to non-selective agents. It also suppresses renin release from the kidneys, contributing to blood pressure reduction. Effects typically begin within one to four hours, peaking at two to four hours, with benefits sustained over 24 hours, supporting once-daily dosing. This targeted action enhances its utility in cardiovascular regulation.

Pharmacokinetics

Following oral intake, the drug absorbs nearly completely from the gastrointestinal tract, achieving a bioavailability of about 90%, largely unaffected by food. Peak plasma concentrations occur within two to four hours. Bisoprolol binds minimally to plasma proteins, around 30%, and distributes widely, with balanced elimination between renal and hepatic routes. It undergoes moderate hepatic metabolism via cytochrome P450 3A4, producing inactive metabolites, with approximately 50% excreted unchanged in urine and the rest as metabolites. The half-life ranges from 9 to 12 hours, prolonged in renal or hepatic impairment due to dual clearance pathways, requiring careful monitoring. This balanced profile ensures consistent activity across varied patient conditions.

Indications for Use

This medication is prescribed for conditions involving elevated blood pressure or cardiac strain. It is primarily indicated for hypertension, effectively reducing pressure to mitigate cardiovascular risk, suitable for mild to moderate cases. It also manages chronic heart failure with reduced ejection fraction, improving survival and reducing hospitalizations by easing cardiac workload. In some contexts, it supports patients with stable coronary artery disease by lowering heart rate and oxygen demand, enhancing exercise tolerance. Its selective action makes it a key option in both standalone and combination regimens, contributing to long-term heart health strategies.

Contraindications

Specific conditions restrict the use of this drug to ensure patient safety. Hypersensitivity to bisoprolol or beta-blocker components prohibits its administration, as reactions could range from skin irritation to anaphylaxis. Severe bradycardia, second- or third-degree heart block, or sick sinus syndrome without a pacemaker contraindicates it due to its heart rate-lowering effects. It is avoided in cardiogenic shock or decompensated heart failure requiring inotropic support, where beta-blockade could worsen cardiac function. Significant hypotension or severe peripheral artery disease limits its use to prevent circulatory compromise. Asthma or severe chronic obstructive pulmonary disease with reactive airways requires caution, though its selectivity reduces risks compared to non-selective agents.

Method of Administration and Dosage

How to Take

Tablets are taken orally, typically in the morning, with or without food, offering flexibility in timing. Swallowing them whole with water ensures proper delivery to the digestive system. A consistent schedule each day maintains stable blood levels for optimal control.

Dosage for Adults and Children

For adults with hypertension, treatment typically starts at 5 mg once daily, adjustable to 10 mg or 20 mg daily based on response, with a maximum of 20 mg. In heart failure, 1.25 mg once daily is common, gradually increased to 10 mg daily over weeks as tolerated, guided by clinical stability. Pediatric use lacks formal standards, but when prescribed, dosing begins at 0.1 mg per kilogram daily, with cautious increments up to 0.4 mg per kilogram or 10 mg, tailored under specialist supervision. Blood pressure and heart rate monitoring ensure dosing balances efficacy and safety across age groups.

Dose Adjustment in Specific Conditions

Renal impairment suggests starting at 2.5 mg daily if creatinine clearance is below 40 mL/min, with slow increases due to partial renal clearance. Hepatic dysfunction also warrants 2.5 mg daily initially, as metabolism may be delayed, increasing drug levels. Older adults or those with reduced cardiac reserve may begin at 2.5 mg daily to minimize bradycardia or hypotension risks. Regular assessments tailor dosing to each patient’s physiological needs, particularly in compromised states.

Side Effects

This medication may elicit various unintended responses, though most are transient. Fatigue, dizziness, or drowsiness are common, often linked to reduced cardiac output, especially early in use. Bradycardia or cold extremities might occur due to slowed heart rate and peripheral effects. Headache, nausea, or gastrointestinal discomfort can affect some individuals, typically subsiding with time. Sleep disturbances or mild depression are less frequent but reported. Rarely, severe reactions like significant bradycardia, bronchospasm in susceptible patients, or hypoglycemia masking in diabetics emerge, requiring prompt medical attention. Patient feedback and periodic checks help manage these effects effectively.

Overdose

Symptoms of Overdose

Excessive intake can lead to severe bradycardia, causing weakness, fainting, or cardiac arrest from excessive beta-blockade. Hypotension may result in dizziness, confusion, or shock due to reduced cardiac output. Bronchospasm or breathing difficulty might develop in those with airway sensitivity, complicating respiration. Lethargy or seizures could occur in extreme cases, reflecting systemic depression. Symptoms typically appear within hours and escalate without intervention, highlighting the drug’s potent cardiovascular impact.

First Aid Measures

In an overdose scenario, discontinue administration immediately and seek urgent medical assistance. If ingestion is recent, gastric lavage or activated charcoal may reduce absorption, applied under professional supervision. Intravenous atropine addresses bradycardia, while fluids or vasopressors like dopamine support blood pressure. Bronchodilators like albuterol relieve airway constriction, and glucagon may counter beta-blockade effects. Continuous monitoring stabilizes the patient until recovery, focusing on restoring normal rhythm and circulation.

Drug Interactions

Effects on Other Medications

This drug can alter the effects of other medications when used concurrently. It may enhance the pressure-lowering action of other antihypertensives, requiring dose recalibration to avoid excessive drops. Combining it with non-dihydropyridine calcium channel blockers like verapamil increases bradycardia risks, needing careful oversight. It might reduce the efficacy of bronchodilators like salbutamol in rare cases. Antidiabetic agents’ hypoglycemic effects could be masked, necessitating glucose monitoring. Adjustments minimize these interaction risks effectively.

Compatibility with Alcohol and Food

Alcohol consumption may intensify drowsiness or hypotension, so moderation is advised. Food does not significantly affect absorption, allowing flexible timing, with no specific dietary restrictions beyond avoiding excessive stimulants that could counteract its calming effects. A balanced diet supports overall efficacy.

Special Precautions

Use During Pregnancy and Breastfeeding

This medication is generally avoided during pregnancy unless benefits outweigh risks, as animal data suggest potential fetal harm, though human evidence is limited. It passes into breast milk in trace amounts, with unclear effects on infants, so nursing mothers should consult their physician, possibly opting for alternatives to reduce exposure.

Impact on Driving and Machinery Operation

Dizziness or fatigue, especially at initiation or dose changes, may impair driving or machinery operation. Patients should assess their tolerance before such activities, ensuring safety for themselves and others.

Considerations for Elderly and Pediatric Populations

Older adults may require lower initial doses due to reduced clearance, with monitoring for bradycardia or hypotension. In children, its use is rare and guided by specialists, with weight-based doses adjusted cautiously to avoid developmental impact. Personalized care optimizes safety and efficacy across these groups.