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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.
Pharmacologists have linked drugs to glucuronic acid to allow for more effective delivery of a broad range of potential therapeutics. Sometimes toxic substances are also less toxic after glucuronidation. The conjugation of xenobiotic molecules with hydrophilic molecular species such as glucuronic acid is known as phase II metabolism.
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 ...
For example, antibiotics that kill gut bacteria often reduce enterohepatic drug circulation and this requires a temporary increase of the drug's dose until the antibiotic use is discontinued and the gut repopulates with bacteria. This effect of antibiotics on enterohepatic circulation of other drugs is one of several types of drug interactions.
Many drugs that are absorbed through the GI tract are substantially metabolized by the liver before reaching general circulation. This is known as the first pass effect . As a consequence, certain drugs can only be taken via certain routes.
Ethanol does not bind to plasma proteins or other biomolecules. [13] [2] [3] The rate of distribution depends on blood supply, [4] specifically the cross-sectional area of the local capillary bed and the blood flow per gram of tissue. [13] As such, ethanol rapidly affects the brain, liver, and kidneys, which have high blood flow. [2]
Time course of drug plasma concentrations over 96 hours following oral administrations every 24 hours (τ). Absorption half-life 1 h, elimination half-life 12 h. Biological half-life ( elimination half-life , pharmacological half-life ) is the time taken for concentration of a biological substance (such as a medication ) to decrease from its ...
The other elimination pathways are less important in the elimination of drugs, except in very specific cases, such as the respiratory tract for alcohol or anaesthetic gases. The case of mother's milk is of special importance. The liver and kidneys of newly born infants are relatively undeveloped and they are highly sensitive to a drug's toxic ...