propranolol INDERAL

Class: Beta Blocker/​Class II Antiarrhythmic
FDA Indications: Hypertension, Essential Tremor, Obstructive Hypertrophic Cardiomyopathy, Pheochromocytoma, Post-MI Mortality Reduction, Stable Angina, Supraventricular Tachycardia, Tachyarrhythmias
Off-Label Use: Akathisia, Performance Anxiety, Supraventricular Tachycardia, Thyroid Storm, Thyrotoxicosis, Lithium-induced Tremor, Variceal Hemorrhage (prophylaxis), Tetralogy Of Fallot Hypercyanotic Spells, Aggression, Panic Disorder, Social Anxiety
Prescribing
Forms: 10, 20, 40, 60, 80mg tablet; 60, 80, 120, 160mg Extended-Release Capsule (Inderal LA)
Dose Range: 20-320 mg/day
Starting: Akathisia: 10 mg bid-tid; Performance anxiety: 40 mg 60-90 min prior to anxiety-provoking event; Lithium-induced tremor: 30-80 mg/day in divided doses

NAMI drug fact sheet

Precautions
Contraindications: Uncompensated CHF (unless the failure is d/t tachyarrhythmias being treated with propranolol), cardiogenic shock; severe sinus bradycardia, sick sinus syndrome, or heart block greater than 1° (except in patients with a functioning artificial pacemaker); bronchial asthma
Side Effects: dizziness, confusion, insomnia, sexual dysfunction, cold extremities, nightmares
Pharmacodynamics
1° MOA: Nonselective β-adrenergic blocker; competitively blocks response to β1- and β2-adrenergic stimulation which results in ↓ heart rate, myocardial contractility, blood pressure, & myocardial O2 demand
2° MOA: Presynaptic 5HT1A
Target: β1, β2
Pharmacokinetics
t½: 4 (3-6)° TMAX: 1-4°
Substrate of: 1A2, 2D6; 2C19, 3A4
Inhibits: 1A2 (weak); Induces:
Active Metabolites: 4-hydroxypropranolol (t½ 5.2-7.5°)
DDIs
Misc
  • - t½: IR 3-6°; Extended-release 8-10°
  • - lipophilic—readily enters the blood-brain barrier
  • - it's thought to be most likely that propranolol aids in breaking the cycle of anxiety in which misappraisal of somatic sensations of sympathetic origin (i.e. palpitations, ↑'d ventilation) fuel the occurrence of panic
  • - there's also evidence to suggest that after a fear memory is recollected, and followed specifically by a prediction error, propranolol selectively blocks protein synthesis, thereby prohibiting 'reconsolidation' of the fear memory
Special Populations

Category C—Apparently not a teratogen, but fetal and neonatal toxicity may occur. Some β-blockers may cause IUGR & ↓'d placental weight (treatment beginning early in the 2nd trimester results in the greatest weight reductions, whereas treatment restricted to the 3rd trimester primarily affects only placental weight)

RID 1%; the American Academy of Pediatrics classified propranolol as compatible with breastfeeding, though the American Academy of Pediatrics classified propranolol as compatible with breastfeeding, though nursing infants exposed to propranolol in breast milk should be closely observed for symptoms of β-blockade

Propranolol is one of the known orally-administered drugs that exhibits ↓ in first-pass metabolism with aging ∴ start low & taper cautiously

Studies have reported a delayed absorption rate and a reduced half-life of propranolol in patients with renal failure of varying severity. Use with caution.

Propranolol is extensively metabolized by the liver. Use with caution.

logo

Developed & Designed by Kevin M. Nasky, D.O. • Built with Bootstrap, PHP & MySQL • Hosted by SiteGround
Last updated January 22 2018 19:18:05. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.