Bislol 2.5 mg

Description

Indications

Bislol tablet is primarily used to manage the following health conditions:

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

Please note that Bislol is not intended for the emergency treatment of hypertensive crises.

Important Reminder: Always use this medication as directed by a registered healthcare professional.

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Pharmacology

Bisoprolol Fumarate is a highly selective ß1-adrenergic blocker. It specifically targets the ß1 receptors in the heart and vascular smooth muscles, which helps reduce heart rate and cardiac output, ultimately lowering blood pressure.

Unlike some other non-selective beta-blockers, Bisoprolol does not affect cholesterol metabolism, including the beneficial HDL-cholesterol levels, even during long-term use. This makes it a favorable option for patients requiring consistent heart rate and blood pressure management.

Absorption and Bioavailability:

• Bisoprolol is well absorbed (over 90%) in the gastrointestinal tract.
• It has a high absorption rate and minimal first-pass effect (<10%), leading to an impressive bioavailability of 88%.
• Food intake does not affect its absorption.

Metabolism:

• Bisoprolol undergoes oxidative metabolism without conjugation. Its primary metabolites are inactive.
• It is primarily metabolized by CYP3A4, with CYP2D6 contributing only minimally to its breakdown.

Elimination:

• Bisoprolol’s elimination is balanced between renal and hepatic processes.
• The clearance rate is approximately 15 L/h, and it has a half-life of 10–12 hours.

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Dosage & Administration

Adults:

• Hypertension: Start with 5 mg once daily. If necessary, increase the dose to 10 mg and up to 20 mg daily.
• The dose should be adjusted after 2 weeks based on the patient’s response. Doses higher than 20 mg have minimal additional benefits.

Children:

• The safety and efficacy of Bisoprolol in children have not been established.

Renal or Hepatic Impairment:

• In patients with renal dysfunction (creatinine clearance below 40 mL/min) or hepatic impairment, start with a dose of 5 mg daily, with caution in dose titration. Bisoprolol is not significantly dialyzable, so no replacement is necessary for dialysis patients.

Geriatric Use:

• No dose adjustment is typically required for elderly patients unless they also have significant renal or hepatic impairment.

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Drug Interactions

• Other Beta-blockers: Do not combine with other beta-blockers.
• Catecholamine-Depleting Drugs: If combined with drugs like reserpine or guanethidine, monitor closely for excessive reduction in sympathetic activity.
• Centrally Active Antihypertensives (e.g., clonidine): If both are used together, discontinue the beta-blocker several days before stopping clonidine to avoid rebound hypertension.
• Antiarrhythmic Drugs and Calcium Channel Blockers: Use with caution as these may intensify myocardial depression and prolong AV conduction, especially in patients with impaired heart function.

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Contraindications

Bislol should not be used in patients with the following conditions:

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

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Side Effects

Common side effects may include:

• Fatigue
• Dizziness
• Headache
• Gastrointestinal issues (nausea, vomiting, diarrhea, constipation, abdominal pain)
• Cold extremities (hands and feet)
• Muscle weakness/cramps
• Bradycardia (slower heart rate)
• Bronchospasm (in patients with asthma or COPD)

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Pregnancy and Lactation

Pregnancy:

• Bisoprolol has shown no teratogenic effects in animal studies but was fetotoxic (caused late resorptions) at high doses. It is not recommended during pregnancy unless the potential benefit outweighs the potential risks to the fetus.

Lactation:

• Small amounts of Bisoprolol have been detected in the milk of lactating rats. It is unknown whether the drug passes into human milk. It is advised to discontinue breastfeeding if Bisoprolol is considered essential for treatment.

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Precautions and Warnings

• Use caution when prescribing Bisolol to patients with renal or hepatic impairment.
• Patients with a history of severe allergic reactions may experience heightened sensitivity to allergens and reduced effectiveness of epinephrine in emergencies.
• Beta-blockers like Bisolol can mask signs of low blood sugar in diabetic patients, so regular monitoring is advised.

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Therapeutic Class

• Anti-adrenergic agents (Beta-blockers)

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Storage Instructions

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

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Chemical Structure

• Molecular Formula: C18H31NO4

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Common Questions about Bislol 2.5 mg Tablet

What is Bislol 2.5 mg Tablet?

Bislol 2.5 mg Tablet is a beta-blocker that works by blocking the effects of adrenaline. It helps lower blood pressure, reduce heart rate, and prevent chest pain (angina).

How should I take Bislol 2.5 mg Tablet?

Take Bislol 2.5 mg Tablet once daily, with or without food, ideally at the same time each day.

What are the side effects of Bislol 2.5 mg Tablet?

Possible side effects include dizziness, fatigue, headache, cold extremities, and slow heart rate.

Is Bislol 2.5 mg Tablet safe to take?

Bislol is safe for most patients. However, speak with your doctor if you have conditions like asthma, diabetes, heart issues, or liver or kidney problems.

Should I take Bislol 2.5 mg Tablet on an empty stomach or after food?

It is recommended to take the tablet after food as directed.

How should I store Bislol 2.5 mg Tablet?

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

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Quick Tips

• Dizziness: If you feel dizzy, rise slowly from sitting or lying down.
• Blood Sugar: Diabetics should monitor their blood sugar levels regularly, as beta-blockers like Bisolol can mask low blood sugar symptoms.
• Do not stop suddenly: Avoid abruptly stopping Bisolol as it may cause a sudden increase in blood pressure, heightening the risk of heart attack or stroke.

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Important Note: Always follow the advice and guidance of a registered healthcare professional when using Bislol.