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Metoprolol Succinate

Metoprolol Succinate is a selective beta-1 adrenergic receptor blocker primarily used in the management of cardiovascular conditions. It is the extended-release formulation of metoprolol, offering once-daily dosing for consistent therapeutic effects.


Mechanism of Action:

  • Selectively blocks beta-1 adrenergic receptors in the heart, reducing:
    • Heart rate (negative chronotropy).
    • Myocardial contractility (negative inotropy).
    • Cardiac output and oxygen demand.
  • Reduces sympathetic nervous system stimulation, improving outcomes in cardiovascular conditions.
  • Recommended Usage
Indications:
  • Hypertension: Lowers blood pressure, reducing the risk of cardiovascular events.
  • Angina Pectoris: Improves exercise tolerance and reduces anginal episodes.
  • Heart Failure: Used in stable, symptomatic heart failure with reduced ejection fraction.
  • Myocardial Infarction: Reduces mortality and recurrence risk.
  • Arrhythmias: Effective in treating atrial fibrillation, supraventricular tachycardia, and ventricular arrhythmias.
  • Migraine Prophylaxis (off-label).
Dosage and Administration:

Administer orally, once daily. Individualize dose based on clinical response.

  • Hypertension:
    • Initial dose: 25–100 mg once daily.
    • Maximum dose: 400 mg/day.
  • Angina Pectoris:
    • Initial dose: 100 mg once daily.
    • Maximum dose: 400 mg/day.
  • Heart Failure (NYHA Class II–III):
    • Initial dose: 12.5–25 mg once daily.
    • Gradually titrate every 2 weeks to a target dose of 200 mg once daily, based on tolerance.
  • Post-Myocardial Infarction:
    • 100–200 mg once daily.
  • Arrhythmias:
    • Typical dose: 50–100 mg once daily (adjust as needed).
Precautions:
  • Contraindications:
    • Severe bradycardia, heart block greater than first degree (without a pacemaker).
    • Decompensated heart failure.
  • Caution in:
    • Diabetes: May mask symptoms of hypoglycemia.
    • Asthma/COPD: Higher doses may affect beta-2 receptors and worsen bronchospasm.
  • Pregnancy and Lactation:
    • Category C: Use only if benefits outweigh risks.
    • Excreted in breast milk; caution advised during breastfeeding.
  • Drug Interactions:
    • Additive bradycardia or hypotension with other antihypertensives (e.g., calcium channel blockers, digoxin).
    • CYP2D6 inhibitors (e.g., fluoxetine, paroxetine) can increase metoprolol levels.
Key Benefits:
  • Beta-1 Selectivity: Reduces cardiovascular effects with minimal impact on bronchial beta-2 receptors, making it safer in respiratory conditions compared to non-selective beta-blockers.
  • Once-Daily Dosing: Extended-release formulation ensures consistent blood levels and improved patient compliance.
  • Proven Cardiovascular Protection: Reduces mortality in heart failure and post-myocardial infarction patients.
  • Symptom Relief: Effective in reducing anginal attacks, arrhythmias, and blood pressure.
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