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First-pass metabolism may occur in the liver (for propranolol, lidocaine, clomethiazole, and nitroglycerin) or in the gut (for benzylpenicillin and insulin). [4] The four primary systems that affect the first pass effect of a drug are the enzymes of the gastrointestinal lumen, [5] gastrointestinal wall enzymes, [6] [7] [8] bacterial enzymes [5] and hepatic enzymes.
Furthermore, after absorption from the gastrointestinal tract, such drugs must pass to the liver, where they may be extensively altered; this is known as the first pass effect of drug metabolism. Due to the digestive activity of the stomach and intestines, the oral route is unsuitable for certain substances, such as salvinorin A .
The hepatic vein subsequently drains into the inferior vena cava. The hepatic artery provides 30 to 40% of the oxygen to the liver, while only accounting for 25% of the total liver blood flow. The rest comes from the partially deoxygenated blood from the portal vein. The liver consumes about 20% of the total body oxygen when at rest.
Enterohepatic circulation of drugs. Enterohepatic circulation is the circulation of biliary acids, bilirubin, drugs or other substances from the liver to the bile, followed by entry into the small intestine, absorption by the enterocyte and transport back to the liver.
In particular, the oral route is subject to a high first-pass effect, which results in high levels of testosterone in the liver and consequent hepatic androgenic effects, as well as low potency due to first-pass metabolism in the intestines and liver into metabolites like dihydrotestosterone and androgen conjugates. [2]
In addition, the rectal route bypasses around two-thirds of the first-pass metabolism as the rectum's venous drainage is two-thirds systemic (middle and inferior rectal vein) and one-third hepatic portal system (superior rectal vein). This means the drug will reach the circulatory system with significantly less alteration and in greater ...
A portal triad (also known as portal canal, portal field [citation needed], portal area [citation needed], or portal tract [citation needed]) is a distinctive arrangement within lobules. It consists of the following five structures: [6] proper hepatic artery, an arteriole branch of the hepatic artery that supplies oxygen
Although FMO5 was the first distinct FMO, it is not clear what function it serves since it does not oxygenate the typical FMO substrates involved in first-pass metabolism. Analyses of FMO genes across several species have shown extensive silent DNA mutations, which indicate that the current FMO gene family exists because of selective pressure ...