Propranolol

Products

Propranolol is commercially available in tablet, sustained-release capsule, and solution forms (Inderal, generic, hemangiol). It has been approved in many countries since 1965.

Structure and properties

Propranolol (C16H21NO2, 259.34 g/mol) is present in drugs as propranolol hydrochloride, a white powder that is soluble in water. Propranolol is a racemate. The -enantiomer is predominantly active.

Effects

Propranolol (ATC C07AA05) lowers blood pressure, decreases heart rate, decreases myocardial contractility, and has antianginal, vasoconstrictor, and antiarrhythmic properties. It reduces cardiac work and decreases oxygen consumption. The effects are due to antagonism at adrenergic beta receptors (beta1 and beta2). Propranolol is a non-selective and lipophilic beta-blocker, which is well absorbed and also crosses the blood–brain barrier. It has high first-pass metabolism and active metabolites. The half-life is approximately 3 to 6 hours.

Indications

  • Hypertension
  • Angina pectoris
  • For prophylaxis after a heart attack.
  • Cardiac arrhythmias
  • Anxiety-related acute somatic complaints and tachycardias.
  • Hypertrophic obstructive cardiomyopathy
  • Migraine prophylaxis
  • Essential tremor
  • Pheochromocytoma, in combination with an alpha blocker.
  • Hyperthyroidism and thyrotoxic crisis.
  • Hemangioma see under propranolol hemangioma.

Dosage

According to the professional information. Dosage depends on the indication and the dosage form. The tablets are taken one to four times daily.

Contraindications

  • Hypersensitivity
  • Bronchial asthma, bronchospasm
  • Certain cardiovascular diseases, e.g., a bradycardia, hypotension, AV block.
  • Metabolic acidosis
  • Prolonged fasting, hypoglycemic tendency.

Full precautions can be found in the drug label.

Interactions

Propranolol is a substrate of CYP2D6, CYP1A2, and CYP2C19, and corresponding drug-drug interactions are possible. Propranolol also has potential for pharmacodynamic interactions.

Adverse effects

The most common potential adverse effects include fatigue, sleep disturbances, nightmares, slow pulse, cold extremities, and indigestion.