Bisopro 2.5 mg

Description

Indications

Bisopro 2.5 mg Tablet is prescribed for the treatment of:

• Hypertension (High Blood Pressure)
• Angina (Chest Pain)
• Moderate to Severe Heart Failure

Bisopro is not recommended for the emergency treatment of hypertensive crises.

Always use this medication under the supervision of a registered healthcare professional.

Pharmacology

Bisoprolol Fumarate is a highly selective beta-1 blocker, making it one of the most effective medications for targeting beta-1 adrenergic receptors in the heart. This selective action leads to a reduction in heart rate and cardiac output, which helps lower arterial hypertension (high blood pressure). Unlike other beta-blockers, Bisoprolol does not interfere with lipid metabolism, including the HDL-cholesterol (the good cholesterol), making it safer for long-term use.

Pharmacokinetics

• Absorption: Bisoprolol is almost completely absorbed (>90%) from the gastrointestinal tract. The medication has a low first-pass effect (<10%), resulting in a bioavailability of approximately 88%. Food intake does not impact absorption.

• Distribution: The drug is widely distributed throughout the body, with a medium distribution volume of 3.51 L/kg.

• Metabolism: Bisoprolol is primarily metabolized in the liver through oxidative pathways, with the main metabolites being inactive and excreted through the kidneys. The drug is mainly metabolized by the CYP3A4 enzyme, with CYP2D6 playing a minor role.

• Elimination: Bisoprolol’s elimination is balanced between renal excretion (50%) and hepatic metabolism (50%). The total clearance rate is approximately 15 L/h, with a half-life of 10-12 hours.

Dosage & Administration

• Adults: For the treatment of mild to moderate hypertension, the typical starting dose is 5 mg once daily, either alone or in combination with a diuretic. If needed, the dose can be increased to 10 mg, and if necessary, up to 20 mg once daily, with a 2-week interval between dose increases. Doses above 20 mg generally provide minimal additional benefit.

• Children: The safety and effectiveness of Bisopro 2.5 mg Tablet in children have not been established.

• Renal or Hepatic Impairment: In patients with liver issues (e.g., cirrhosis or hepatitis) or kidney problems (creatinine clearance <40 mL/min), the initial dose should be 5 mg daily. Careful monitoring is required to avoid accumulation. No dialysis is necessary as Bisoprolol is not significantly dialyzed.

• Elderly: No dose adjustment is typically required unless there are significant kidney or liver impairments.

Always follow the advice of your registered healthcare provider.

Drug Interactions

• Other Beta-Blockers: Avoid using Bisopro in combination with other beta-blockers.

• Catecholamine-Depleting Agents: Drugs like reserpine or guanethidine may cause excessive reduction of sympathetic activity when combined with Bisopro.

• Centrally Active Antihypertensive Agents: Careful monitoring is needed when using Bisopro with clonidine, as sudden withdrawal of clonidine may cause rebound hypertension. Discontinue Bisopro before stopping clonidine.

• Antiarrhythmic Agents: Bisopro should be used with caution when combined with myocardial depressants, like verapamil or diltiazem, which may result in severe hypotension, bradycardia, and cardiac failure.

Contraindications

Bisopro 2.5 mg Tablet should not be used in:

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

Side Effects

While side effects may vary, some common reactions to Bisopro include:

• Fatigue and dizziness
• Headache
• Gastrointestinal disturbances, such as nausea, vomiting, constipation, diarrhea, or abdominal pain
• Cold or numb extremities
• Muscle weakness or cramps
• Bradycardia (slow heart rate) and bronchospasm (narrowing of airways), especially in people with asthma or COPD.

Pregnancy & Lactation

• Pregnancy: Studies in rats showed no teratogenic effects up to 150 mg/kg/day, but Bisopro was fetotoxic at higher doses. It is not recommended for use during pregnancy unless the benefits outweigh the risks.

• Lactation: Bisoprolol is minimally excreted in milk in animal studies. As it is unclear whether it passes into human milk, mothers should consider stopping breastfeeding if Bisopro is essential for their treatment.

Precautions & Warnings

• Renal or Hepatic Dysfunction: Bisopro 2.5 mg Tablet should be used cautiously in patients with liver or kidney issues. Regular monitoring is recommended.

• Severe Allergic Reactions: Individuals with a history of severe allergic reactions may not respond to normal doses of epinephrine during anaphylaxis.

Therapeutic Class

• Anti-Adrenergic Agent (Beta Blockers)
• Beta-Adrenoceptor Blocking Drugs

Storage Conditions

• Bisopro 2.5 mg Tablet should be stored in a dry place, away from light and heat.
• Keep the medication out of reach of children.

Common Questions about Bisopro 2.5 mg Tablet

What is Bisopro 2.5 mg Tablet? Bisopro 2.5 mg Tablet is a beta-blocker that helps reduce blood pressure, heart rate, and the workload on the heart, preventing chest pain and improving heart function.

How should I take Bisopro 2.5 mg Tablet? Take Bisopro 2.5 mg Tablet once daily with or without food, ideally at the same time each day.

What are the side effects of Bisopro 2.5 mg Tablet? Some potential side effects include dizziness, fatigue, headache, slow heart rate, difficulty breathing, and cold extremities.

Is it safe to take Bisopro 2.5 mg Tablet? Yes, but consult your doctor first, especially if you have asthma, diabetes, or heart/liver/kidney conditions.

How should I store Bisopro 2.5 mg Tablet? Store in a cool, dry place, and keep away from children.

Quick Tips

• Bisopro 2.5 mg Tablet may cause dizziness; rise slowly from a sitting or lying position.
• If you are diabetic, Bisopro can mask symptoms of low blood sugar. Monitor your blood sugar regularly.
• Do not stop Bisopro suddenly as this may cause a sudden rise in blood pressure, increasing the risk of heart attack or stroke.

Always follow the instructions of your healthcare provider for proper use.