Pharm

Propranolol

search

Propranolol, Inderal

  • See Also
  • Background
  1. Propranolol was the first Beta Blocker, developed in the 1960s by James Black
    1. Dr. Black later won the Nobel Prize in 1988 for Beta Blocker development
  • Indications
  1. Primary
    1. Migraine Headache Prophylaxis
    2. Esophageal Varices Prevention of Recurrent Bleeding (not FDA approved)
    3. Essential Tremor
    4. Thyrotoxicosis (Hyperthyroidism) (not FDA approved)
    5. Performance Anxiety (not FDA approved)
    6. Perioperative Pheochromocytoma Management
      1. Must be used with alpha blocker
  2. Other indications for which Selective Beta Blockers Preferred instead of Propranolol
    1. Hypertension
    2. Atrial Fibrillation Rate Control
  • Mechanism
  1. Non-Selective Beta Blocker
  2. Beta 1 Adrenergic Receptor Antagonist
    1. Decreases Heart Rate, Cardiac Output, and Sympathetic System output (decreased renin release)
    2. Prolongs AV conduction and refractory period
  3. Beta 2 Adrenergic Receptor Antagonist
    1. Risk of bronchoconstriction
  • Precautions
  1. Patients may have very different responses to various formulations (regular, LA, XL)
  • Dosing
  • Primary Indications
  1. Migraine Headache Prophylaxis
    1. Regular: Start 40 mg orally twice daily
    2. XR/LA: 80 mg orally daily
    3. Maximum: 240 mg/day)
  2. Pheochromocytoma Surgery
    1. Must be used concurrently with alpha blocker
    2. Start three days before surgery: 60 mg orally two to three times daily
  3. Essential Tremor
    1. Start 40 mg orally twice daily
    2. Target 120 to 320 mg/day
  4. Thyrotoxicosis (not FDA approved)
    1. Start 60 to 80 mg orally every 4 hours OR
    2. Start 0.5 to 1 mg IV over 10 minutes every 3 hours
  5. Esophageal Varices Prevention of Recurrent Bleeding (not FDA approved)
    1. Start 20 to 40 mg orally twice daily
    2. Titrate up to 180 mg twice daily as needed, targeting Heart Rate drop of 25% from baseline
  6. Performance Anxiety (not FDA approved)
    1. Take 20-40 mg orally as needed 45 minutes before performance
  • Dosing
  • Other Indications
  1. Rarely Used for Hypertension, Angina or SVT management
    1. Propranolol has been replaced by newer, selective Beta Blockers for these indications
    2. As the first Beta Blocker developed, Propranolol has historical indications for Hypertension, CAD and a fib RVR
  2. Hypertension
    1. Propranolol (regular release)
      1. Start 20 to 40 mg orally twice daily
      2. Target 160 to 480 mg/day
      3. Maximum 640 mg/day
    2. Propranolol LA (long acting)
      1. Start 60 to 80 mg orally at bedtime
      2. Target 120 to 160 mg daily
      3. Maximum 640 mg/day
  3. Angina
    1. Propranolol (regular release)
      1. Start 10 to 20 mg orally three to four times daily
      2. Target 160 to 240 mg/day
      3. Maximum 320 mg/day
    2. Propranolol LA (long acting)
      1. Start 80 mg orally at bedtime
      2. Target 160 to 240 mg/day
      3. Maximum 320 mg/day
  4. Atrial Fibrillation Rate Control
    1. Start 10 to 30 mg orally three to four times daily
  5. Intravenous Dosing in life threatening Arrhythmia (very rare use)
    1. Avoid in Hypertensive Emergency
    2. Load: 1-3 mg IV over 2-5 minutes
    3. May repeat once in 2 minutes (to a total maximum up to 0.1 mg/kg)
    4. Sustained response for 6-8 hours (do not give additional doses for 4 hours)
  • Adverse Effects
  1. See Beta Blocker
  2. Transient Hypertension
    1. Beta 2 Adrenergic ReceptorAntagonists transiently constrict large arteries
  3. Rebound Hypertension
    1. Sudden discontinuation of Propranolol
  4. CNS Adverse Effects
    1. CNS penetration
  5. Congestive Heart Failure Exacerbation
    1. May worsen acute, decompensated CHF
  • Safety
  1. Pregnancy Category C
  2. Consider safe in Lactation
  • Pharmacokinetics
  1. Protein bound 90%
  2. Hepatic metabolism and renal excretion
  • Drug Interactions
  1. Cimetidine
    1. Increases Propanolol serum levels
  2. Alcohol
    1. Acute Alcohol Intoxication increases Propranolol levels
    2. Chronic Alcohol use decreases Propranolol levels
  3. Digoxin
    1. Fatal Third degree AV Block has occurred
  • References
  1. Olson (2020) Clinical Pharmacology, Medmaster Miami, p. 78-9
  2. Hamilton (2020) Tarascon Pocket Pharmacopoeia