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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.
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 ...
This is known as the first pass effect. As a consequence, certain drugs can only be taken via certain routes. For example, nitroglycerin cannot be swallowed because the liver would deactivate the medication, but it can be taken under the tongue or transdermally (through the skin) and thus is absorbed in a way that bypasses the portal venous system.
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 ...
Effect of digestive juices and the first pass metabolism of drugs. Condition of the patient. In acute situations, in emergency medicine and intensive care medicine, drugs are most often given intravenously. This is the most reliable route, as in acutely ill patients the absorption of substances from the tissues and from the digestive tract can ...
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 greater potency of vaginal estradiol relative to oral estradiol is due to the lack of the first pass associated with oral estradiol and due to low local metabolism of estradiol in the vagina. [10] Because of the high estradiol levels achieved, LH and FSH are more strongly suppressed with vaginal estradiol than with other routes. [72]
In the first step of this cycle, the SAM-dependent methylases (EC 2.1.1) that use SAM as a substrate produce S-adenosyl homocysteine as a product. [4] S -Adenosyl homocysteine is a strong negative regulator of nearly all SAM-dependent methylases despite their biological diversity.