Propranolol

Pharmacokinetics

Propranolol is one of an increasing number of drugs, with a name ending in the now-famliar string LOL.

Propranolo is rapidly and completely absorbed, with peak plasma levels achieved about 1–3 hours after ingestion. Coadministration with food appears to enhance bioavailability.

Despite complete absorption, propranolol has a variable bioavailability due to extensive first-pass metabolism. Hepatic impairment therefore increases its bioavailability. The main metabolite 4-hydroxypropranolol, with a longer half-life (5.2–7.5 hours) than the parent compound (3–4 hours), is also pharmacologically active.

Propranolol is a highly lipophilic drug achieving high concentrations in the brain. The duration of action of a single oral dose is longer than the half-life and may be up to 12 hours, if the single dose is high enough (e.g., 80 mg). Effective plasma concentrations are between 10 and 100 mg/l. Toxic levels are associated with plasma concentrations above 2000 mg/l.

Propranolol was discovered in 1964. It is on the World Health Organization's List of Essential Medicines, the most effective and safe medicines needed in a health system.

Propranolol is available as a generic medication.

The wholesale cost in the developing world is between 0.24 and 2.16 USD per month as of 2014. In the United States it costs about 15 USD per month at a typical dose.