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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.
Due to the first pass through the liver, disproportionate and supraphysiological levels of estrogens occur locally in the liver with oral estradiol. [ 117 ] [ 12 ] These levels are approximately 4- to 5-fold higher than in the circulation, based on differences in hepatic estrogenic potency for oral estradiol relative to transdermal estradiol.
By definition, when a medication is administered intravenously, its bioavailability is 100%. [ 2 ] [ 3 ] However, when a medication is administered via routes other than intravenous, its bioavailability is lower due to intestinal epithelium absorption and first-pass metabolism .
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.
Drug metabolism is the metabolic breakdown of drugs by living organisms, usually through specialized enzymatic systems. More generally, xenobiotic metabolism (from the Greek xenos "stranger" and biotic "related to living beings") is the set of metabolic pathways that modify the chemical structure of xenobiotics, which are compounds foreign to an organism's normal biochemistry, such as any drug ...
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
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 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 ...