Concepts
Non-clinical sciences/Pharmacology principles · Pharmacokinetics

Bioavailability & first-pass

What it means

Bioavailability (F) = fraction of an administered dose reaching the systemic circulation unchanged. IV F = 1.0 by definition. Reduced by incomplete gut absorption, intestinal efflux and first-pass metabolism (gut wall + liver). High first-pass drugs (GTN, propranolol, morphine, lidocaine) need a much larger oral than parenteral dose, or a non-oral route.

Worked example

GTN is given sublingually/transdermally because near-complete hepatic first-pass metabolism destroys an oral dose.

In the exam

A drug is given sublingually rather than swallowed because the liver would otherwise metabolise almost all of an oral dose before it reaches the circulation.

What settles it

First-pass metabolism reduces ORAL bioavailability specifically; it is bypassed by IV/SL/transdermal/PR routes.

Classically confused with

Volume of distribution

Source: StatPearls — Pharmacokinetics