U4 DRG BIOTRANSFORMATION Flashcards
Mechanism by which the body terminates the action of
some drugs
Drug Metabolism
T/F Drug Metabolism serves to activate prodrugs in some cases.
T
3 possible pathways of drug metabolism
- Active > Inactive (readily excreted by the kidneys)
- Active > Active metabolites
- Inactive (prodrug) > Active (prodrug)
Types of Metabolic Reactions
Used for non-synthetic reactions
Phase I
Types of Metabolic Reactions
Convert the parent drug to a more polar conjugate (water soluble) or more reactive product
Phase I
Types of Metabolic Reactions
Done through introducing/inserting/unmasking a polar functional group
Phase I
Types of Metabolic Reactions (Phase)
Oxidation
Phase I
Types of Metabolic Reactions (Phase)
Reduction
Phase I
Types of Metabolic Reactions (Phase)
Deamination
Phase I
Types of Metabolic Reactions (Phase)
Hydrolysis
Phase I
Types of Metabolic Reactions
Used for synthetic reactions
Phase II
Types of Metabolic Reactions
Endogenous substrate is conjugated to the parent drug
Phase II
Types of Metabolic Reactions (Phase)
Glucoronidation-glucoronic acid
Phase II
Types of Metabolic Reactions (Phase)
Acetylation-acetyl CoA
Phase II
Types of Metabolic Reactions (Phase)
Sulfation
Phase II
Types of Metabolic Reactions (Phase)
Methylation
Phase II
Types of Metabolic Reactions (Phase)
Glycineconjugation-glycine
Phase II
Types of Metabolic Reactions (Phase)
Methylation
Phase II
Types of Metabolic Reactions (Phase)
Glycine conjugation-glycine
Phase II
Types of Metabolic Reactions (Phase)
Glutathione conjugation
Phase II
Types of Metabolic Reactions (Phase)
H2O conjugation
Phase II
Phase ___ > Phase ___ is the most common pathway
Phase I > Phase II
Pathway that most drug uses
Phase 1 > Phase II
Pathway that other drug uses
Phase II > Phase I
T/F Drugs that are more polar are easier to eliminate
T
Maybe metabolized by gastric fluid
Penicillin
Must be given 2 hours before meals if given through the
oral route
Penicillin
Drugs Metabolized by Gastric Acid
Penicillin