HEMANGIOL

Propranolol is a racemic mixture of 2 enantiomers where the S(-)-enantiomer has approximately 100 times the binding affinity for beta adrenergic receptors.

Propranolol is used to treat a number of conditions but most commonly is used for hypertension. 8, 9, 10 Propranolol was granted FDA approval on 13 November 1967.

Propranolol is indicated to treat hypertension. 10, 9 Propranolol is also indicated to treat angina pectoris due to coronary atherosclerosis, atrial fibrillation, myocardial infarction, migraine, essential tremor, hypertrophic subaortic stenosis, pheochromocytoma, and proliferating infantile hemangioma. 9,

Propranolol is a beta-adrenergic receptor antagonist used to treat hypertension. 9, 10 Propranolol has a long duration of action as it is given once or twice daily depending on the indication. 8, 9, 10 When patients abruptly stop taking propranolol, they may experience exacerbations of angina and myocardial infarctions.

Patients taking doses of 40 mg, 80 mg, 160 mg, and 320 mg daily experienced C max values of 18±15ng/mL, 52±51ng/mL, 121±98ng/mL, and 245±110ng/mL respectively.

Propranolol has a

T max of approximately 2 hours, though this can range from 1-4 hours in fasting patients.

Taking propranolol with food does not increase T max but does increase bioavailability.

The volume of distribution of propranolol is approximately 4 L/kg 8, 9 or 320 L.

Propranolol undergoes side chain oxidation to α-naphthoxylactic acid, ring oxidation to 4'-hydroxypropranolol, or glucuronidation to propranolol glucuronide.

It can also be N-desisopropylated to become N-desisopropyl propranolol. 1 17% of a dose undergoes glucuronidation and 42% undergoes ring oxidation.

Hover over products below to view reaction partners Propranolol N-desisopropylpropranolol 4'-hydroxypropanolol Propranolol Glucuronide α-Naphthoxylactic Acid.

91% of an oral dose of propranolol is recovered as 12 metabolites in the urine.

The elimination half-life of propranolol is approximately 8 hours.

The plasma half-life of propranolol is 3-6 hours. 8, 9.

The clearance of propranolol is 2.7±0.03 L/h/kg in infants 90 days.

Propranolol clearance increases linearly with hepatic blood flow.

Propranolol has a clearance in hypertensive adults of 810 mL/min.

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Symptoms of overdose include hypotension, hypoglycemic seizure, restlessness, euphoria, insomnia.

Patients with asthma may develop bronchospasm.

In case of overdose, monitor vital signs, mental status, and blood glucose.

Treat hypotension with intravenous fluids, bradycardia with atropine, and isoproterenol and aminophylline for bronchospasm.

If patients do not respond to intravenous fluids, follow up with glucagon 50-150 µg/kg Intravenous, then 1-5 mg/hour, followed by catecholamines. 8, 9, 10 Dialysis will not be useful as propranolol is highly protein bound. 8, 9, 10.