Bisopro 5 mg

Description

Indications:

Bisopro 5 mg Tablet is prescribed for the treatment of:

• Hypertension (high blood pressure)
• Angina (chest pain)
• Moderate to severe heart failure

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

Note: Follow your healthcare provider’s advice regarding medication usage.

Pharmacology:

Bisoprolol Fumarate is a highly selective β1 blocker. Among all beta-blockers available, it shows the greatest affinity for the β1 receptor, targeting the heart and vascular smooth muscles. By selectively blocking the β1 adrenergic receptors, Bisopro reduces heart rate and cardiac output, leading to a decrease in arterial blood pressure.

Unlike non-selective beta-blockers, Bisoprolol does not negatively affect lipid metabolism or alter cholesterol levels, including protective HDL-cholesterol, even with long-term usage.

The pharmacokinetic properties of Bisoprolol allow for a convenient once-daily dosage. Its low variability in plasma concentration ensures high therapeutic reliability.

Absorption & Bioavailability: Bisoprolol is extensively absorbed (over 90%) from the gastrointestinal tract. The absorption rate is high with minimal first-pass effect (<10%), resulting in a bioavailability of approximately 88%. The absorption is unaffected by food intake.

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

Metabolism: Bisoprolol is metabolized primarily through oxidative pathways without conjugation. The metabolites, being highly polar, are excreted via the kidneys. Most of the metabolites in the blood and urine do not have pharmacological effects. In liver microsome studies, Bisoprolol is mainly metabolized by CYP3A4 (95%), with CYP2D6 playing a minor role.

Elimination: The drug is cleared from the body through both renal excretion (50%) and hepatic metabolism (50%), with the metabolites also being eliminated through the kidneys. Its clearance rate is around 15 L/h, and its half-life is between 10-12 hours.

Dosage & Administration:

Adults: For the treatment of mild to moderate hypertension, the initial dose of Bisopro is typically 5 mg once daily, either alone or with a diuretic. If the response to 5 mg is insufficient, the dose may be increased to 10 mg and then to 20 mg if needed, typically after a 2-week interval. Further increases beyond 20 mg provide minimal additional benefit.

Children: The safety and efficacy of Bisopro in children have not been established.

Patients with Renal or Hepatic Impairment: In patients with liver or kidney dysfunction, the starting dose should be 5 mg daily. Due to the risk of accumulation, dose titration should be done cautiously. Bisoprolol is not dialyzable, so drug replacement is not required for patients undergoing dialysis.

Elderly: Generally, no dose adjustment is needed unless there is significant renal or hepatic impairment.

Interactions:

Other β-Blockers: Bisopro should not be combined with other β-blockers.

Catecholamine-Depleting Drugs: Medications like reserpine or guanethidine may intensify the effects of Bisopro, leading to excessive suppression of sympathetic activity.

Centrally Active Antihypertensive Drugs: Concurrent use with clonidine can cause rebound hypertension upon discontinuation. If both drugs are used together, Bisopro should be withdrawn several days before clonidine is stopped, and the introduction of Bisopro should be delayed after discontinuing clonidine.

Antiarrhythmic Agents: Caution should be exercised when combining Bisopro with certain calcium antagonists (e.g., verapamil, diltiazem) or antiarrhythmic drugs (e.g., disopyramide), as this combination can significantly affect heart conduction.

Calcium Channel Blockers: Bisopro should be used cautiously with calcium channel blockers with negative inotropic effects, as this can lead to prolonged conduction and severe complications such as hypotension, bradycardia, or heart failure.

Contraindications:

Bisopro is contraindicated in patients with:

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

Side Effects:

Common side effects of Bisopro 5 mg Tablet may include:

• Fatigue
• Dizziness
• Headache
• Gastrointestinal issues (nausea, vomiting, diarrhea, constipation, abdominal pain)
• Cold or numb extremities (e.g., hands or feet)
• Muscle weakness or cramps
• Bradycardia (slow heart rate)
• Breathing difficulties due to airway constriction (bronchospasm), particularly in individuals with asthma or chronic obstructive pulmonary disease (COPD)

Note: Not everyone experiences these side effects. Consult your doctor if you have concerns.

Pregnancy & Lactation:

Pregnancy: Bisopro is not teratogenic in animal studies; however, it has shown fetotoxic effects at high doses. There are no sufficient studies in pregnant humans. Bisopro should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Small quantities of Bisopro may pass into breast milk in animals, but it is unknown whether the drug is excreted in human milk. If Bisopro is deemed necessary, mothers should consider discontinuing breastfeeding.

Precautions & Warnings:

• Renal or Hepatic Impairment: Caution should be exercised when adjusting the dose in patients with liver or kidney issues.
• Anaphylactic Reactions: Patients with a history of severe allergic reactions may be more prone to experiencing exaggerated reactions to allergens while taking Bisopro.
• Epinephrine Use: Patients may be less responsive to epinephrine in the case of anaphylaxis.

Storage Instructions:

Store in a cool, dry place away from direct light and heat. Keep out of the reach of children.

Common Questions About Bisopro 5 mg Tablet:

What is Bisopro 5 mg Tablet? Bisopro 5 mg Tablet is a beta-blocker medication used to manage high blood pressure, angina, and heart failure by lowering heart rate and expanding blood vessels.

How should I take Bisopro 5 mg Tablet? Take Bisopro by mouth once daily, with or without food, at the same time each day for best results.

What are the side effects of Bisopro 5 mg Tablet? Common side effects include dizziness, fatigue, headache, slow heart rate, cold extremities, and breathing difficulties. Always report any adverse reactions to your doctor.

Is Bisopro 5 mg Tablet safe to take? Generally safe when prescribed by a doctor. However, consult your healthcare provider if you have any underlying health conditions, such as asthma, diabetes, or heart problems.

Can Bisopro 5 mg Tablet be taken on an empty stomach? It can be taken with or without food, but following your doctor’s prescription is essential.