Bisopro 5 mg
Description
Indications:
Bisopro 5 mg Tablet is commonly prescribed for the treatment of:
- Hypertension (High Blood Pressure)
- Angina (Chest Pain)
- Moderate to Severe Heart Failure
Note: Bisopro 5 mg Tablet is not suitable for the emergency treatment of hypertensive crises.
Important Notice: Always use Bisopro 5 mg Tablet under the guidance of a registered medical professional.
Pharmacology:
Bisopro 5 mg Tablet contains Bisoprolol Fumarate, a highly selective Beta-1 (ß1) blocker. Bisoprolol is known for its superior affinity to ß1 adrenergic receptors when compared to other available beta-blockers. By selectively blocking these receptors in the heart and blood vessels, Bisoprolol reduces heart rate and cardiac output, resulting in lowered blood pressure.
Unlike other beta-blockers, Bisoprolol does not interfere with lipid metabolism and does not cause any changes in cholesterol levels, including the cardioprotective HDL cholesterol, when used long-term.
Pharmacokinetics:
- Absorption & Bioavailability: Bisoprolol is absorbed almost entirely from the gastrointestinal tract, with more than 90% absorption. It has a low first-pass effect, resulting in a bioavailability of 88%, and food intake does not affect absorption.
- Distribution: The drug is widely distributed throughout the body, with a medium distribution volume of 3.51 L/kg.
- Metabolism: Bisoprolol is metabolized in the liver by oxidative pathways, with metabolites being excreted in the urine. Its primary metabolic pathway involves CYP3A4, with only a minor contribution from CYP2D6.
- Elimination: Approximately 50% of Bisoprolol is eliminated through the kidneys in its unchanged form, while the remainder is processed by the liver. The drug has an elimination half-life of 10 to 12 hours, allowing for once-daily dosing.
Dosage & Administration:
- Adults: The starting dose for managing mild to moderate hypertension is typically 5 mg once daily, either alone or with a diuretic. Depending on the patient’s response, the dosage can be increased to 10 mg and, if necessary, up to 20 mg daily. The dose should be adjusted with a minimum 2-week interval between adjustments.
- Children: Safety and effectiveness in children have not been established.
- Renal or Hepatic Impairment: In patients with liver or kidney issues (creatinine clearance <40 mL/min), the initial dose should be 5 mg. Dose titration should be done cautiously to avoid accumulation. There is no need to adjust the dosage in patients on dialysis as Bisoprolol is not dialyzable.
- Elderly: Dosage adjustment is usually unnecessary unless there is significant renal or hepatic dysfunction.
Important Notice: Always consult a registered medical professional before taking any medication.
Drug Interactions:
- Other Beta-Blockers: Bisopro should not be used with other beta-blockers.
- Catecholamine-Depleting Drugs: Caution should be exercised when used alongside drugs like reserpine or guanethidine, as these may intensify the effects of Bisopro, potentially leading to excessive reduction of sympathetic activity.
- Centrally Active Antihypertensive Agents: If combined with clonidine, bisopro should be discontinued several days before stopping clonidine to avoid rebound hypertension.
- Antiarrhythmic Agents & Calcium Channel Blockers: Caution is necessary when used with myocardial depressants or calcium antagonists (e.g., verapamil, diltiazem), as the combination can result in serious effects like bradycardia, hypotension, or cardiac failure.
Contraindications:
Bisopro 5 mg Tablet should not be used 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:
Side effects can vary from person to person. Some common side effects include:
- Fatigue
- Dizziness
- Headache
- Gastrointestinal disturbances (nausea, vomiting, diarrhea, constipation, abdominal pain)
- Cold or numb extremities
- Muscle weakness or cramps
- Slow heart rate (bradycardia)
- Breathing difficulties (especially in asthma or COPD patients due to bronchospasm)
Pregnancy & Lactation:
- Pregnancy: Bisopro 5 mg Tablet should only be used during pregnancy if the potential benefits outweigh the risks to the fetus. Animal studies have shown that high doses can cause fetotoxicity and maternal toxicity.
- Lactation: Bisopro is detected in rat milk in small quantities. It is unknown if Bisopro passes into human breast milk. If it is essential for the mother to take Bisopro, breastfeeding should be discontinued.
Precautions & Warnings:
- Use caution when adjusting the dose in patients with renal or hepatic impairment.
- Patients with a history of severe anaphylactic reactions may experience heightened sensitivity to allergens and may not respond to usual doses of epinephrine.
Storage:
Store Bisopro 5 mg Tablet in a cool, dry place, away from light and heat. Keep out of the reach of children.
Frequently Asked Questions (FAQs):
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What is Bisopro 5 mg Tablet? Bisopro 5 mg Tablet is a selective beta-blocker that helps lower blood pressure, reduce heart workload, and alleviate chest pain.
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What is Bisopro 5 mg Tablet used for? It is used to manage hypertension (high blood pressure), angina (chest pain), and moderate to severe heart failure.
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How should I take Bisopro 5 mg Tablet? Take one tablet once daily, either with or without food, at the same time each day.
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What are the side effects of Bisopro 5 mg Tablet? Common side effects include dizziness, fatigue, headache, slow heart rate, breathing difficulties, and cold extremities.
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Is Bisopro 5 mg Tablet safe to take? Bisopro 5 mg Tablet is generally safe, but consult a doctor before use if you have conditions like asthma, diabetes, heart issues, or liver/kidney problems.
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Should Bisopro 5 mg Tablet be taken before or after food? It is recommended to take the tablet after food as prescribed by your healthcare provider.
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What are the storage instructions for Bisopro 5 mg Tablet? Store the tablet in its original packaging in a dry, cool place, out of the reach of children.
Quick Tips:
- Bisopro 5 mg Tablet may cause dizziness. If this happens, rise slowly from a sitting or lying position.
- For diabetic patients, Bisopro can mask symptoms of low blood sugar, so regular blood sugar monitoring is essential.
- Never stop taking Bisopro 5 mg Tablet suddenly without consulting your doctor, as it may cause a rapid increase in blood pressure.
Note: Always follow the advice of a registered medical professional when using Bisopro 5 mg Tablet.
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