Bisopro 2.5 mg
Description
Indications:
Bisopro 2.5 mg Tablet is primarily prescribed for the following conditions:
- Hypertension (high blood pressure)
- Angina (chest pain)
- Moderate to severe heart failure
Please note, Bisopro is not suitable for the emergency treatment of hypertensive crises.
Always take this medicine according to the advice of your registered physician.
Pharmacology:
Bisopro 2.5 mg Tablet contains Bisoprolol Fumarate, which is one of the most selective β1-blockers available. It has a high affinity for the β1-receptor, more so than any other beta-blocker on the market. Bisoprolol selectively blocks the β1-adrenergic receptors in the heart and smooth muscle of the blood vessels, which leads to a reduction in heart rate and cardiac output. This helps lower arterial blood pressure.
While many beta-blockers can affect lipid metabolism, Bisoprolol does not alter cholesterol levels, including HDL-cholesterol, which has protective effects on the heart, even during long-term therapy.
The pharmacokinetic properties of Bisopro allow for once-daily dosing, ensuring a consistent therapeutic effect and low variability in plasma concentrations across individuals.
- Absorption: Bisoprolol is almost fully absorbed (>90%) from the digestive tract. It has a bioavailability of 88% due to a small first-pass effect (<10%).
- Distribution: Bisoprolol is widely distributed throughout the body, with a medium distribution volume of 3.51 L/kg.
- Metabolism: Bisoprolol is metabolized mainly through oxidative pathways, and its metabolites are excreted via the kidneys. Its primary metabolite has no significant pharmacological effect. Bisoprolol is metabolized by the enzyme CYP3A4 (95%) with a minor role for CYP2D6.
- Elimination: The drug’s clearance is approximately 15 L/h, with 50% being excreted unchanged via the kidneys and the other 50% through liver metabolism. Bisoprolol has an elimination half-life of 10-12 hours.
Dosage and Administration:
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Adults: For the management of mild to moderate hypertension, the usual starting dose is 5 mg once daily, either as a monotherapy or combined with a diuretic. If the response is inadequate, the dose can be increased to 10 mg, and later to 20 mg once daily. Any dose increase should be made with a 2-week interval. Doses above 20 mg/day offer minimal additional benefit.
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Children: Safety and efficacy for pediatric patients have not been established.
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Patients with Renal or Hepatic Impairment: For patients with liver conditions (e.g., cirrhosis) or severe kidney dysfunction (creatinine clearance below 40 mL/min), the initial dose should be 5 mg daily. Dose adjustment should be done with caution to prevent drug accumulation. Bisoprolol is not significantly dialyzable, so no replacement is required in dialysis patients.
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Elderly: Generally, no dose adjustment is necessary unless there is concurrent renal or hepatic impairment.
Always follow the advice of your registered physician when taking this medicine.
Interactions:
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Other β-Blockers: Bisopro should not be taken with other beta-blockers.
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Catecholamine-Depleting Drugs: Medications like reserpine or guanethidine may cause an excessive reduction in sympathetic activity when used with Bisopro.
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Centrally Active Antihypertensive Agents: If Bisopro is used with clonidine, the beta-blocker should be stopped several days before discontinuing clonidine to avoid exacerbating rebound hypertension.
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Antiarrhythmic Agents: Bisopro should be used with caution when combined with drugs that depress myocardial activity or inhibit A-V conduction, such as certain calcium channel blockers (e.g., verapamil, diltiazem) or antiarrhythmic medications like disopyramide.
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Calcium Channel Blockers: Combining beta-blockers with calcium channel blockers can lead to prolonged S-A and A-V conduction, particularly in patients with impaired heart function, potentially causing severe hypotension, bradycardia, or heart failure.
Contraindications:
Bisopro should not be used in the following conditions:
- Cardiogenic shock
- Severe heart failure
- Second or third degree A-V block
- Right ventricular failure secondary to pulmonary hypertension
- Sinus bradycardia
Side Effects:
While Bisopro is generally well tolerated, potential side effects include:
- Fatigue
- Dizziness
- Headaches
- Gastrointestinal issues (e.g., nausea, vomiting, diarrhea, constipation, abdominal discomfort)
- Cold or numb extremities (hands and feet)
- Muscle weakness or cramps
- Slow heart rate (bradycardia)
- Breathing difficulties due to airway narrowing (bronchospasm), especially in patients with asthma or chronic obstructive pulmonary disease (COPD)
Pregnancy and Lactation:
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Pregnancy: Bisoprolol fumarate has not shown teratogenic effects in animal studies but can cause fetotoxicity and maternotoxicity at higher doses. There are no human studies available. The use of Bisopro during pregnancy should be considered only if the potential benefits justify the potential risks to the fetus.
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Lactation: Small amounts of Bisopro may be excreted in the milk of lactating rats, though it’s unknown whether it is excreted in human breast milk. If use during breastfeeding is necessary, the mother should consider stopping nursing.
Precautions and Warnings:
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Renal or Hepatic Impairment: Caution should be exercised when adjusting the dosage in patients with kidney or liver problems.
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Anaphylactic Reactions: Patients with a history of severe allergic reactions may have a heightened response to allergens when taking beta-blockers, and may not respond as effectively to usual doses of epinephrine.
Therapeutic Class:
- Anti-adrenergic agents (Beta-blockers)
Storage Instructions:
- Store in a dry place, away from light and heat.
- Keep out of reach of children.
Chemical Composition:
- Molecular Formula: C18H31NO4
- Chemical Structure: Bisoprolol Fumarate Structure
Common Questions about Bisopro 2.5 mg Tablet:
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What is Bisopro 2.5 mg Tablet?
- Bisopro 2.5 mg Tablet is a beta-blocker medication used to manage high blood pressure (hypertension), chest pain (angina), and heart failure.
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How should I take Bisopro 2.5 mg Tablet?
- Take Bisopro 2.5 mg Tablet by mouth once daily, with or without food, ideally at the same time each day.
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What are the side effects?
- Possible side effects include dizziness, fatigue, headache, slow heart rate, difficulty breathing, and cold hands and feet.
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Is Bisopro 2.5 mg Tablet safe?
- Generally, it is safe for most people. However, consult your doctor before taking it if you have asthma, diabetes, heart conditions, liver or kidney issues, low blood pressure, or depression.
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Can I take it on an empty stomach?
- It’s recommended to take Bisopro 2.5 mg Tablet after food as per your doctor’s instructions.
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How should I store it?
- Keep Bisopro 2.5 mg Tablet in a cool, dry place and ensure it is out of reach of children.
Quick Tips:
- Bisopro 2.5 mg Tablet may cause dizziness. Stand up slowly if you feel dizzy after sitting or lying down.
- If you have diabetes, Bisopro 2.5 mg Tablet can mask the symptoms of low blood sugar, so monitor your blood sugar regularly.
- Do not stop taking Bisopro 2.5 mg Tablet suddenly, as this may cause a rapid rise in blood pressure and increase the risk of heart attack or stroke.
Always take the medicine as per the advice of your registered physician.
Additional information
Weight | 0.15 g |
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