propranolol

Brand: Inderal, Inderal LA

⚠ BBW Prototype Drug
Drug Class: beta-blocker
Drug Family: antihypertensive
Subclass: non-selective beta-blocker (lipophilic)
Organ Systems: cardiovascularcns

Mechanism of Action

First non-selective beta-blocker; blocks beta-1 (cardiac) and beta-2 (bronchial, vascular, metabolic) receptors; highly lipophilic with CNS penetration.

beta-1 receptorbeta-2 receptor

Indications

  • hypertension
  • angina
  • post-MI
  • essential tremor
  • migraine prophylaxis
  • hyperthyroidism (thyroid storm)
  • portal hypertension (varices)
  • pheochromocytoma (after alpha-blocker)
  • performance anxiety
  • HOCM

Contraindications

  • asthma/COPD
  • Raynaud's
  • uncontrolled HF
  • cardiogenic shock
  • AV block
  • pheochromocytoma without prior alpha-blocker

Adverse Effects

Common

  • bradycardia
  • fatigue
  • cold extremities
  • vivid dreams
  • depression

Serious

  • bronchospasm
  • masking hypoglycemia
  • Raynaud's exacerbation
  • rebound effects on withdrawal

Pharmacokinetics (ADME)

Absorption 30-40% oral (high first-pass, variable)
Distribution highly lipophilic; CNS penetration
Metabolism extensive hepatic CYP1A2, CYP2D6
Excretion renal (<1% unchanged)
Half-life 3-6 hours
Onset 30-60 min
Peak 1-4 hours
Duration 8-12 hours
Protein Binding 93%
Vd 4-5 L/kg

Drug Interactions

Drug / Agent Mechanism Severity
insulin/oral hypoglycemics masks tachycardia of hypoglycemia; may prolong hypoglycemia moderate
verapamil IV severe bradycardia/asystole major
CYP1A2/2D6 inhibitors increased propranolol levels moderate

Nursing Considerations

  1. Warn diabetic patients that tachycardia (hypoglycemia warning) may be masked
  2. Never give IV propranolol with IV verapamil (asystole risk)
  3. Highly lipophilic — crosses BBB causing CNS effects (depression, vivid dreams)
  4. Multiple indications beyond hypertension — verify indication before administering
  5. Taper over weeks to avoid rebound

Clinical Pearls

  • First beta-blocker (1964); foundational class prototype
  • Non-selective: contraindicated in asthma (beta-2 bronchoconstriction)
  • Unique indication: thyroid storm adjunct (blocks peripheral T4→T3 conversion and tachycardia)
  • Performance anxiety: acute pre-event dosing used off-label

Safety Profile

Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required