BETAFIX 5 TAB 5 mg

Description

Indications
Betafix 5 mg Tablet is primarily indicated for the following conditions:

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

Please note that Betafix is not recommended for the emergency treatment of hypertensive crises.

Always follow the advice of a registered healthcare professional when taking this medication.

Pharmacology

Bisoprolol Fumarate, the active ingredient in Betafix, is a highly selective β1 blocker, offering the greatest affinity for the β1 receptors compared to other beta-blockers. By selectively blocking the β1 adrenergic receptors in the heart and vascular smooth muscle, Bisoprolol helps reduce heart rate and cardiac output, resulting in a reduction of arterial hypertension. Unlike non-selective β-blockers, Bisoprolol does not affect lipid metabolism and does not alter cholesterol fractions, including beneficial HDL cholesterol, even with long-term use.

Bisoprolol’s pharmacokinetic properties allow for a once-daily dose, with minimal variability in plasma concentration across different individuals, ensuring reliable therapeutic effects.

• Absorption and Bioavailability: Bisoprolol is almost entirely absorbed (>90%) from the gastrointestinal tract, with a minimal first-pass effect (<10%) resulting in an absolute bioavailability of 88%. Food intake does not impact its absorption.
• Distribution: It is extensively distributed throughout the body, with a medium distribution volume of 3.51 L/kg.
• Metabolism: Bisoprolol is primarily metabolized by oxidative processes via CYP3A4, with CYP2D6 contributing minimally. The metabolites have no significant pharmacological activity.
• Elimination: The drug is eliminated through both renal excretion of unchanged Bisoprolol (~50%) and hepatic metabolism (~50%). The elimination half-life is approximately 10-12 hours.

Dosage & Administration

Adult Dosage:

• For Hypertension: The usual starting dose is 5 mg once daily, either alone or in combination with a diuretic. If necessary, the dose can be increased to 10 mg and then to 20 mg once daily at intervals of 2 weeks.
• For Heart Failure: The dosage should be tailored based on individual patient needs.

Pediatric Use:
Safety and efficacy for children have not been established.

Renal or Hepatic Impairment:
In patients with liver or kidney impairment (creatinine clearance <40 mL/min), the starting dose should be 5 mg once daily. Adjustments should be made cautiously due to the possibility of drug accumulation. Bisoprolol is not significantly dialyzed.

Geriatric Use:
For elderly patients, the dose typically does not require adjustment unless there is coexisting significant renal or hepatic dysfunction.

Always follow your doctor’s prescribed dosage and guidelines.

Drug Interactions

Other Beta-Blockers:
Do not combine Betafix with other β-blocking agents.

Catecholamine-Depleting Drugs:
Patients receiving drugs such as reserpine or guanethidine should be closely monitored, as the additional β-blockade can lead to excessive sympathetic reduction.

Antihypertensive Agents:
Beta-blockers like Betafix may exacerbate rebound hypertension after stopping clonidine. If switching from clonidine, the β-blocker should be introduced several days after clonidine has been discontinued.

Antiarrhythmic and Calcium Channel Blockers:
Use Betafix cautiously in combination with antiarrhythmic drugs (like disopyramide) or calcium channel blockers, especially those that affect heart rhythm (e.g., verapamil and diltiazem). These combinations may result in severe hypotension, bradycardia, and cardiac failure.

Contraindications

Betafix should not be used in patients with:

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

It is also contraindicated in patients who are hypersensitive to Bisoprolol or other β-blockers.

Side Effects

Common side effects of Betafix may include:

• Fatigue
• Dizziness
• Headaches
• Gastrointestinal issues (nausea, vomiting, diarrhea, constipation)
• Cold or numb extremities
• Muscle weakness or cramps
• Slower heart rate (bradycardia)
• Respiratory difficulties (bronchospasm), particularly in individuals with asthma or COPD

Pregnancy & Lactation

Pregnancy:
Bisoprolol has shown no teratogenic effects in rats at high doses but was fetotoxic at certain doses. Due to limited human studies, Betafix should only be used during pregnancy if the benefits outweigh the risks to the fetus.

Lactation:
It is unknown if Bisoprolol passes into human breast milk. If necessary, mothers should discontinue breastfeeding while using Betafix.

Precautions & Warnings

• Renal or Hepatic Impairment: Caution is needed when adjusting the dose in patients with liver or kidney dysfunction.
• Allergic Reactions: Patients with a history of severe anaphylactic reactions may be less responsive to epinephrine when taking beta-blockers like Betafix.
• Asthma or Respiratory Conditions: Use with caution in patients with asthma, as it may trigger bronchospasm.
• Diabetes: Beta-blockers can mask symptoms of hypoglycemia, so diabetic patients should monitor blood sugar levels closely.

Storage Instructions

Store Betafix in a cool, dry place, protected from light and heat. Keep it out of the reach of children.

Chemical Structure

• Molecular Formula: C18H31NO4
• Chemical Structure: Bisoprolol Fumarate

Frequently Asked Questions

What is Betafix 5 mg Tablet?
Betafix 5 mg Tablet is a beta-blocker used to manage conditions like high blood pressure, chest pain, and heart failure. It works by reducing heart rate and relaxing blood vessels.

How should I take Betafix 5 mg Tablet?
Take Betafix once daily with or without food, preferably at the same time each day. Always follow the prescribed dosage.

What are the side effects?
Common side effects include dizziness, fatigue, headache, slow heart rate, and cold extremities. If you experience any severe reactions, contact your doctor immediately.

Is it safe to take Betafix 5 mg Tablet?
Betafix is generally safe for most people when taken as prescribed. However, it may not be suitable for people with asthma, diabetes, or certain heart conditions. Always consult your doctor before use.

How should Betafix be stored?
Keep the tablet in its original packaging, in a cool, dry place, and out of the reach of children.

Always consult with a registered healthcare provider before using this medication to ensure it is suitable for your health needs.