BIOTRANSFORMATION, Drug metabolism, detoxification

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BIOTRANSFORMATION, Drug metabolism, detoxification. Phase 2 conjugation. GSH conjugation. acetylation. sulfation. Glucuronidation (80%) Conjugation with amino acids glycosylation. 12%. su. phase I. phase II. nucleophilic metabolites. glucuronides sulfate esters. X. electrophilic - PowerPoint PPT Presentation

Transcript of BIOTRANSFORMATION, Drug metabolism, detoxification

1. diaConjugation of
salicylic acid
16.bin
morphin
steroids
Dubin Johnson syndr.
Ways of conjugation
Sulfation – PAPS - sulfotransferases
Sulfation – PAPS – sulfotransferases
Biotransformation of
Sulfation – PAPS – sulfotransferases
Acetylation – acetyl CoA
Methylation - SAM
Phisiological substrates:
intracellular receptors: CAR, PXR, VDR, FXR, RXR, HNF4
Overlapping substrate, inducer specificity
Bile acid
steroid hormones
Oxidation of aceton
Toxicity 1.
5-10 different drugs/patient
Logarythmic increase of adverse drug effects with the number of drugs
nutrition
alkoholism
Treatment of mothers at delivery
chloramphenicol
morfin
Pathological circumstances