First pass effect

Illustration showing the hepatic portal vein system

The first pass effect (also known as first-pass metabolism or presystemic metabolism) is a phenomenon of drug metabolism at a specific location in the body which leads to a reduction in the concentration of the active drug before it reaches the site of action or systemic circulation.[1][2] The effect is most associated with orally administered medications, but some drugs still undergo first-pass metabolism even when delivered via an alternate route (e.g., IV, IM, etc.).[3] During this metabolism, drug is lost during the process of absorption which is generally related to the liver and gut wall. The liver is the major site of first pass effect; however, it can also occur in the lungs, vasculature or other metabolically active tissues in the body.

Notable drugs that experience a significant first pass effect are buprenorphine, chlorpromazine, cimetidine, diazepam, ethanol (drinking alcohol), imipramine, insulin, lidocaine, midazolam, morphine, pethidine, propranolol, and tetrahydrocannabinol (THC).

First-pass metabolism is not to be confused with phase I metabolism, which is a separate process.

  1. ^ Rowland, Malcolm (January 1972). "Influence of route of administration on drug availability". Journal of Pharmaceutical Sciences. 61 (1): 70–74. doi:10.1002/jps.2600610111. ISSN 0022-3549. PMID 5019220.
  2. ^ Pond, Susan M.; Tozer, Thomas N. (January 1984). "First-Pass Elimination". Clinical Pharmacokinetics. 9 (1): 1–25. doi:10.2165/00003088-198409010-00001. ISSN 0312-5963. PMID 6362950. S2CID 28006040.
  3. ^ Carlin, Michelle G. (2023-01-01), "Pharmacology and Mechanism of Action of Drugs", in Houck, Max M. (ed.), Encyclopedia of Forensic Sciences, Third Edition (Third Edition), Oxford: Elsevier, pp. 144–154, doi:10.1016/b978-0-12-823677-2.00086-6, ISBN 978-0-12-823678-9, retrieved 2024-01-17

From Wikipedia, the free encyclopedia · View on Wikipedia

Developed by Nelliwinne