Bisoren 2.5 mg

Description

Bisoren Tablet

Indications Bisoren is prescribed for the management of the following conditions:

• Hypertension
• Angina
• Moderate to severe heart failure

It is not intended for the emergency treatment of hypertensive crises.

Pharmacology Bisoprolol Fumarate is a highly selective β1-blocker with the highest affinity for β1 receptors among available beta-blockers. It functions by selectively inhibiting β1 adrenergic receptors in the heart and vascular smooth muscle, leading to a reduction in heart rate and cardiac output, which helps lower blood pressure. Unlike non-selective β-blockers, Bisoprolol does not adversely affect lipid metabolism or cardioprotective HDL-cholesterol levels during long-term therapy.

Pharmacokinetics:

• Absorption & Bioavailability: Bisoprolol is efficiently absorbed (>90%) from the gastrointestinal tract, with a minimal first-pass effect (<10%), resulting in an absolute bioavailability of 88%. Food intake does not impact its absorption.
• Distribution: Bisoprolol is extensively distributed in the body, with an average distribution volume of 3.5 L/kg.
• Metabolism: The drug is metabolized through oxidative pathways without conjugation. Its metabolites are highly polar and eliminated through the kidneys. The primary metabolic enzyme involved is CYP3A4 (~95%), with minor involvement from CYP2D6.
• Elimination: Bisoprolol is excreted equally through renal elimination (50%) and hepatic metabolism (50%), with an approximate total clearance of 15 L/h. The elimination half-life is between 10-12 hours.

Dosage & Administration

• Adults: The dosage is individualized based on patient response. The standard starting dose is 5 mg once daily, which may be increased to 10 mg and, if necessary, up to 20 mg daily. Dose titration should occur at intervals of approximately two weeks. Higher doses beyond 20 mg per day provide minimal additional benefit.
• Children: Safety and efficacy in pediatric patients have not been established.
• Patients with Renal or Hepatic Impairment: For individuals with hepatic impairment (e.g., cirrhosis, hepatitis) or renal dysfunction (creatinine clearance <40 mL/min), the initial dose should be 5 mg daily, with caution exercised in dose adjustments to prevent accumulation.
• Geriatric Patients: No routine dosage adjustments are necessary for elderly patients unless significant renal or hepatic impairment is present.

Drug Interactions

• Other β-Blockers: Concomitant use of Bisoren with other β-blockers is not recommended.
• Catecholamine-Depleting Drugs: Patients using agents like reserpine or guanethidine should be monitored closely due to the risk of excessive sympathetic activity reduction.
• Centrally Acting Antihypertensive Agents: If combined with clonidine, Bisoren should be withdrawn several days before discontinuing clonidine to prevent rebound hypertension.
• Antiarrhythmic Agents: Caution is needed when using Bisoren with myocardial depressants or conduction inhibitors like verapamil, diltiazem, or disopyramide.
• Calcium Channel Blockers: Co-administration with calcium channel blockers possessing negative inotropic effects may lead to conduction abnormalities, severe hypotension, bradycardia, or cardiac failure.

Contraindications Bisoren is contraindicated in patients with:

• Cardiogenic shock
• Overt heart failure
• Second or third-degree atrioventricular (A-V) block
• Right ventricular failure due to pulmonary hypertension
• Sinus bradycardia

Side Effects While individual responses vary, common side effects may include:

• Fatigue, dizziness, headache
• Gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation, abdominal pain)
• Cold or numb extremities (hands and feet)
• Muscle weakness or cramps
• Bradycardia (slow heart rate)
• Breathing difficulties in patients with asthma or COPD

Pregnancy & Lactation

• Pregnancy: Animal studies indicate potential fetal risks at high doses; therefore, Bisoprolol should only be used during pregnancy if the benefits outweigh the risks.
• Lactation: Small amounts of Bisoprolol have been detected in the milk of lactating rats, but human data is unavailable. If necessary, breastfeeding should be discontinued.

Precautions & Warnings

• Dose adjustments may be necessary in patients with impaired renal or hepatic function.
• Patients with a history of severe allergic reactions may have a heightened response to allergens and reduced effectiveness of epinephrine treatment.
• Abrupt discontinuation should be avoided, as it may cause a sudden increase in blood pressure or worsen existing heart conditions.

Therapeutic Class

• Anti-adrenergic agent (Beta-blockers)
• Beta-adrenoceptor blocking drugs
• Beta-blockers

Storage Conditions

• Store in a dry place, protected from light and heat.
• Keep out of reach of children.

Frequently Asked Questions

What is Bisoren 2.5 mg Tablet? Bisoren 2.5 mg Tablet is a beta-blocker that works by inhibiting the effects of adrenaline. It helps lower blood pressure, reduce cardiac workload, and prevent chest pain.

What is Bisoren 2.5 mg Tablet used for? It is prescribed for conditions such as:

• High blood pressure (hypertension)
• Chest pain (angina)
• Heart failure

How should I take Bisoren 2.5 mg Tablet? Take Bisoren orally once daily, with or without food. It is best to take it at the same time each day for optimal effectiveness.

What are the side effects of Bisoren 2.5 mg Tablet? Possible side effects include dizziness, fatigue, headache, slow heart rate, breathing difficulties, and cold hands or feet.

Is Bisoren 2.5 mg Tablet safe to take? Bisoren is generally safe but should be used with caution in patients with conditions such as:

• Asthma
• Diabetes
• Heart disorders
• Liver or kidney disease
• Low blood pressure
• Depression

Should Bisoren 2.5 mg Tablet be taken before or after food? It should be taken after food at the prescribed dosage.

How should Bisoren 2.5 mg Tablet be stored? Store in a cool, dry place in its original packaging, away from children and pets.

Quick Tips

• Bisoren may cause dizziness; rise slowly from sitting or lying positions.
• It can mask symptoms of low blood sugar in diabetic patients, so regular monitoring is advised.
• Do not stop taking Bisoren suddenly, as it may cause a sudden spike in blood pressure, increasing the risk of heart attack or stroke.