Bisoren 5 mg

Description

Bisoren 5 mg Tablet

Indications:
Bisoren 5 mg Tablet is indicated for the treatment of:

• Hypertension (High blood pressure)
• Angina (Chest pain)
• Moderate to severe heart failure

Please note: Bisoren is not suitable for the emergency treatment of hypertensive crises.

Always take Bisoren as per the advice of a registered healthcare provider.

Pharmacology

Bisoren 5 mg Tablet contains Bisoprolol Fumarate, which is a highly selective β1-adrenergic receptor blocker. It has a higher affinity for the β1 receptor than any other beta-blocker currently available. Bisoprolol selectively blocks the β1 receptors in the heart and vascular smooth muscle, resulting in a reduction in heart rate and cardiac output, thus lowering blood pressure.

Unlike non-selective β-blockers, Bisoprolol does not affect lipid metabolism significantly, including no changes in HDL-cholesterol (the cardioprotective cholesterol) during long-term therapy.

Pharmacokinetics

• Absorption & Bioavailability: Bisoprolol is more than 90% absorbed from the gastrointestinal tract. It has a bioavailability of 88%, with a minimal first-pass effect (less than 10%). Food intake does not significantly impact its absorption.

• Distribution: Bisoprolol is widely distributed in the body, with an average distribution volume of 3.51 L/kg.

• Metabolism: Bisoprolol is primarily metabolized in the liver through oxidative processes, and its metabolites are eliminated through the kidneys. The drug is primarily metabolized by the CYP3A4 enzyme, with minor involvement of CYP2D6.

• Elimination: The drug is eliminated equally through the kidneys (50%) and liver (50%). Bisoprolol has a half-life of 10-12 hours, allowing for once-daily administration.

Dosage and Administration

• Adults:
  For the treatment of mild to moderate hypertension, the recommended starting dose is 5 mg once daily. This can be taken alone or combined with a diuretic. If the response to the initial dose is insufficient, the dose can be increased to 10 mg and then to 20 mg once daily, with a 2-week interval between dose adjustments.

• Children:
  Safety and effectiveness in children have not been established.

• Patients with Renal or Hepatic Impairment:
  The initial dose for patients with liver or kidney dysfunction (creatinine clearance below 40 mL/min) should be 5 mg. Care should be taken during dose titration to avoid accumulation. Bisoprolol is not significantly dialyzable, so no dosage adjustment is needed for patients on dialysis.

• Geriatrics:
  Generally, dose adjustments are not necessary unless the patient has significant renal or hepatic impairment.

Drug Interactions

• Other Beta-blockers:
  Bisoren should not be used concurrently with other beta-blockers.

• Catecholamine-Depleting Drugs:
  If taking catecholamine-depleting drugs (e.g., reserpine, guanethidine), patients should be monitored closely as Bisoren may excessively reduce sympathetic activity.

• Centrally Acting Antihypertensive Agents:
  Bisoprolol may worsen rebound hypertension following the discontinuation of clonidine. If both are used together, Bisoren should be withdrawn before stopping clonidine.

• Antiarrhythmic Agents and Calcium Channel Blockers:
  Exercise caution when using Bisoren alongside antiarrhythmic agents or calcium channel blockers, especially those that affect myocardial function (e.g., verapamil, diltiazem), as they can worsen bradycardia or hypotension.

Contraindications

Bisoren should not be used in patients with:

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

Side Effects

Some known side effects include:

• Fatigue, dizziness, and headaches
• Gastrointestinal disturbances: nausea, vomiting, diarrhea, constipation, abdominal pain
• Cold or numb extremities
• Muscle cramps or weakness
• Bradycardia (slow heart rate)
• Bronchospasm (narrowing of airways in asthma or COPD patients)

Pregnancy and Lactation

• Pregnancy:
  Bisoprolol should only be used during pregnancy if the potential benefit outweighs the risks to the fetus. There are no conclusive studies in pregnant women.

• Lactation:
  Small amounts of Bisoprolol are excreted in rat milk. It is unknown if the drug is present in human breast milk. If treatment with Bisoprolol is necessary, breastfeeding should be discontinued.

Precautions & Warnings

• Renal or Hepatic Impairment:
  Caution is required when adjusting doses in patients with kidney or liver conditions.

• Anaphylactic Reactions:
  Patients with a history of severe allergic reactions may be more sensitive to allergens while on Bisoprolol and might not respond to standard doses of epinephrine.

Therapeutic Class

• Beta-blockers (Beta-adrenergic blockers)

Storage Conditions

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