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
Drugs Metabolized by Gastric and digestive enzymes
Insulin
Drugs Metabolized by Intestinal wall enzymes
Epinephrine
Most important organ for drug metabolism
Liver
contains high concentration of PHASE I enzymes
Smooth endoplasmic reticulum (SER)
Activity of enzymes require ____ and ____
NADPH and molecular form of oxygen
Ester that is metabolized by plasma choline esterase
Succinylcholine
In most individuals, the process occurs rapidly
Hydrolysis of Esters
Genetic Factor
Succinylcholine
Hydrolysis of Esters
Genetic Factor
Isoniazid (INH)
Acetylation of Amines
Genetic Factor
hydralazine and procainamide
Acetylation of Amines
T/F Slow acetylators cause individuals deficient in acetylating capacity and it produces prolonged or toxic responses to normal doses of the drug
T
Genetic Factor
dextrometorphan, metoprolol, and some tricyclic antidepressants
Oxidation
Genetic Factor
Metabolized by P450 isoenzymes which are genetically predetermined
Oxidation
Diest and environmental factors
inhibits the effect of the drug
Charcoal
Diest and environmental factors
increases the amount of drug in the body
Grapefruit juice
Age and sex
T/F Drug metabolites do not differ in young and old
F; does differ
Age and sex
T/F Males metabolize drugs faster than females
T
Age and sex
T/F Children and elderly metabolize drugs slower
True
Disease affecting drug metabolism
Hyperthyroidism
T/F Thyroid hormone
increase the metabolism
T
Other Drugs
Increase rate of synthesis of the enzyme
Enzyme Induction
Other Drugs
Reduce the rate of degradation of the enzyme
Enzyme Induction
Other Drugs
May also induce metabolism of other drugs and reduce its effects
Enzyme Induction
Other drugs
Inhibit CP450
Enzyme Inhibition
Other drugs
Increase effect of the drug
Enzyme inhibition
Other drugs
Metabolism of the drug is diminished
Enzyme inhibition
Enzyme Induction / Enzyme Inhibition
Phenobarbital
Enzyme Induction
Enzyme Induction / Enzyme Inhibition
Carbamazepine
Enzyme Induction
Enzyme Induction / Enzyme Inhibition
Phenytoin
Enzyme Induction
Enzyme Induction / Enzyme Inhibition
Rifampicin
Enzyme Induction
In enzyme induction
Some drugs + Drug = increase/decrease effect
decreased effect
In enzyme inhibition
Some drugs + Drug = increase/decrease effect
increased effect
Enzyme Induction / Enzyme Inhibition
Cimetidine
Enzyme inhibition
Enzyme Induction / Enzyme Inhibition
Amiodarone
Enzyme inhibition
Enzyme Induction / Enzyme Inhibition
Ketoconazole
Enzyme inhibition
Enzyme Induction / Enzyme Inhibition
Ritonavir
Enzyme inhibition
Enzyme Induction / Enzyme Inhibition
Firanocoumarin
Enzyme inhibition
Type of Drug Mechanism
Cholestyramine inhibits the effect of digoxin when combined with it
Altered Absorption
Type of Drug Mechanism
Affects drug action through enzyme induction or inhibition
Altered Metabolism
Type of Drug Mechanism
Plasma proteins can diminish the amount of drug that reaches its receptors
Altered Plasma Binding Protein
Type of Drug Mechanism
Probenecid inhibits the secretion of weak acids
Altered Excretion
Type of Drug Mechanism
Penicillin inhibits the excretion of probenecid
Altered Excretion