Presystemic extraction: mechanisms and consequences

Journal of Clinical Pharmacology
D J Greenblatt

Abstract

Many drugs have incomplete systemic availability after oral dosage. This can be attributed to incomplete absorption from the gastrointestinal tract, or to presystemic extraction, in which a fraction of an orally administered dose is biotransformed before reaching the systemic circulation. Presystemic extraction can occur either via biotransformation by gastrointestinal mucosa or enteric flora, or via metabolism during the "first-pass" through the liver. For drugs with low oral bioavailability due to high presystemic extraction, impaired clearance leads to increased peak plasma levels and greater area under the concentration-time curve, but minimal change in elimination half-life.

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Citations

Dec 1, 1994·Journal of Clinical Pharmacology·L L von MoltkeR I Shader
Nov 8, 2001·Journal of Clinical Pharmacology·K VenkatakrishnanD J Greenblatt
Mar 10, 2000·Clinical Pharmacokinetics·K VenkatakrishnanD J Greenblatt
Mar 19, 2016·Journal of Clinical Pharmacology·David J Greenblatt, Paul N Abourjaily
Oct 3, 1998·Clinical Pharmacology and Therapeutics·D J GreenblattR I Shader
Dec 1, 1996·Journal of Clinical Psychopharmacology·D J GreenblattR I Shader
Jun 1, 1996·Journal of Clinical Psychopharmacology·R I ShaderD J Greenblatt
Feb 23, 2019·The Journal of Pharmacy and Pharmacology·Ala NozariJ A Jeevendra Martyn

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