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<blockquote data-quote="madman" data-source="post: 240746" data-attributes="member: 13851"><p><strong>Fig. 1.<u> Drug Metabolism and Transport</u>. Orally administered drugs may initially undergo metabolism in the intestine via gastrointestinal/bacterial enzymes and potentially Phase 1 metabolism in enterocytes, followed by transportation into portal vessels and the liver. Afterward, drugs may undergo Phase 1 and/or Phase 2 enzymatic alterations to form metabolites that may be excreted into the bile. If converted into polar conjugates, metabolites may be released into the circulation, and then excreted by the kidney [19]. </strong></p><p><strong></strong></p><p><strong><u>Phase 1 drug metabolism</u>: Oxidation, reduction, and/or hydrolysis via cytochrome P450 enzymes. </strong></p><p><strong></strong></p><p><strong><u>Phase 2 drug metabolism</u>: Conjugation via glucuronidation, acetylation, glutathione conjugation, sulfate conjugation, methylation. </strong></p><p><strong></strong></p><p><strong><u>Phase 3 drug metabolism</u>: Distribution and elimination of drugs mediated by transporters. </strong></p><p><strong></strong></p><p><strong>Cytochrome P450 (CYP450) proteins generally reside within cellular membranes (i.e., endoplasmic reticulum or mitochondrial membrane) and function to metabolize drugs via Phase 1 drug metabolism. The most common CYP450 isoenzyme for drug metabolism is CYP450 3A4. </strong></p><p><strong></strong></p><p><strong>Organic Anion-Transporting Polypeptides (OATP), Multidrug-Resistant-Associated Protein (MRP), P-glycoproteins (P-gp), and Breast Cancer Resistance Protein (BCRP) facilitate drug movement in and out of intestinal and hepatic cells.</strong></p><p><strong>[ATTACH=full]27600[/ATTACH]</strong></p></blockquote><p></p>
[QUOTE="madman, post: 240746, member: 13851"] [B]Fig. 1.[U] Drug Metabolism and Transport[/U]. Orally administered drugs may initially undergo metabolism in the intestine via gastrointestinal/bacterial enzymes and potentially Phase 1 metabolism in enterocytes, followed by transportation into portal vessels and the liver. Afterward, drugs may undergo Phase 1 and/or Phase 2 enzymatic alterations to form metabolites that may be excreted into the bile. If converted into polar conjugates, metabolites may be released into the circulation, and then excreted by the kidney [19]. [U]Phase 1 drug metabolism[/U]: Oxidation, reduction, and/or hydrolysis via cytochrome P450 enzymes. [U]Phase 2 drug metabolism[/U]: Conjugation via glucuronidation, acetylation, glutathione conjugation, sulfate conjugation, methylation. [U]Phase 3 drug metabolism[/U]: Distribution and elimination of drugs mediated by transporters. Cytochrome P450 (CYP450) proteins generally reside within cellular membranes (i.e., endoplasmic reticulum or mitochondrial membrane) and function to metabolize drugs via Phase 1 drug metabolism. The most common CYP450 isoenzyme for drug metabolism is CYP450 3A4. Organic Anion-Transporting Polypeptides (OATP), Multidrug-Resistant-Associated Protein (MRP), P-glycoproteins (P-gp), and Breast Cancer Resistance Protein (BCRP) facilitate drug movement in and out of intestinal and hepatic cells. [ATTACH type="full"]27600[/ATTACH][/B] [/QUOTE]
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