Probis 2.5

Indications

Probis tablets are prescribed for the following conditions:

• Hypertension
• Angina
• Moderate to severe heart failure

Note: Probis is not intended for the emergency treatment of hypertensive crises.
Always use medications as advised by a registered physician.

Pharmacology of Probis (Bisoprolol Hemifumarate)

Bisoprolol Hemifumarate is the most selective β1-adrenergic blocker currently available. It exhibits a high affinity for β1-receptors in the heart and vascular smooth muscle, effectively reducing heart rate and cardiac output, which leads to decreased arterial hypertension. Unlike non-β1 selective blockers, Bisoprolol does not adversely affect cholesterol levels, including HDL-cholesterol, even during long-term therapy.

Key Properties:

• Absorption & Bioavailability: Over 90% absorption from the gastrointestinal tract, with an absolute bioavailability of 88%. Food intake does not interfere with absorption.
• Distribution: Widely distributed with a medium distribution volume of 3.5 L/kg.
• Metabolism: Metabolized via oxidative pathways, with metabolites excreted renally and lacking pharmacological activity. Primarily metabolized by CYP3A4.
• Elimination: Balanced between renal (50%) and hepatic (50%) pathways, with a half-life of 10–12 hours, allowing for a single daily dose.

Dosage & Administration

Adults: For mild to moderate hypertension, the initial dose is 5 mg once daily, with potential increases to 10 mg or 20 mg based on patient response. Dose adjustments should occur at 2-week intervals.

Children: Safety and efficacy have not been established for pediatric use.

Renal or Hepatic Impairment: Start with 5 mg daily. Exercise caution with dose titration due to potential accumulation.

Elderly: Dose adjustments are typically unnecessary unless significant renal or hepatic dysfunction is present.

Always follow the advice of a registered physician.

Drug Interactions

• Other β-blocking Agents: Avoid concurrent use.
• Catecholamine-Depleting Drugs: Use with caution to prevent excessive sympathetic activity suppression.
• Centrally Active Antihypertensives: May worsen rebound hypertension during withdrawal. Adjust β-blocker timing accordingly.
• Antiarrhythmic Agents: Use cautiously with calcium channel blockers (e.g., verapamil, diltiazem) or other myocardial depressants.
• Calcium Channel Blockers: Combined use can cause severe hypotension, bradycardia, or cardiac failure in patients with impaired ventricular function.

Contraindications

Probis should not be used in patients with:

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

Possible Side Effects

Individuals may experience side effects such as:

• Fatigue, dizziness, or headaches
• Gastrointestinal disturbances (e.g., nausea, vomiting, diarrhea)
• Cold or numb extremities
• Muscle cramps or weakness
• Respiratory difficulties in asthma or COPD patients

Note: Not everyone will experience these side effects.

Use During Pregnancy & Lactation

• Pregnancy: Use only if the potential benefit outweighs the risk to the fetus, as animal studies indicate potential fetal risks.
• Lactation: Trace amounts may pass into breast milk. If essential, discontinue breastfeeding.

Precautions & Warnings

• Use cautiously in patients with impaired renal or hepatic function.
• Patients with severe allergic reactions may show reduced responsiveness to epinephrine while taking beta-blockers.

Storage Instructions

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