U4 DRG BIOTRANSFORMATION Flashcards

(70 cards)

1
Q

Mechanism by which the body terminates the action of
some drugs

A

Drug Metabolism

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2
Q

T/F Drug Metabolism serves to activate prodrugs in some cases.

A

T

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3
Q

3 possible pathways of drug metabolism

A
  1. Active > Inactive (readily excreted by the kidneys)
  2. Active > Active metabolites
  3. Inactive (prodrug) > Active (prodrug)
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4
Q

Types of Metabolic Reactions

Used for non-synthetic reactions

A

Phase I

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5
Q

Types of Metabolic Reactions

Convert the parent drug to a more polar conjugate (water soluble) or more reactive product

A

Phase I

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6
Q

Types of Metabolic Reactions

Done through introducing/inserting/unmasking a polar functional group

A

Phase I

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7
Q

Types of Metabolic Reactions (Phase)

Oxidation

A

Phase I

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8
Q

Types of Metabolic Reactions (Phase)

Reduction

A

Phase I

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9
Q

Types of Metabolic Reactions (Phase)

Deamination

A

Phase I

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10
Q

Types of Metabolic Reactions (Phase)

Hydrolysis

A

Phase I

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11
Q

Types of Metabolic Reactions

Used for synthetic reactions

A

Phase II

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12
Q

Types of Metabolic Reactions

Endogenous substrate is conjugated to the parent drug

A

Phase II

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13
Q

Types of Metabolic Reactions (Phase)

Glucoronidation-glucoronic acid

A

Phase II

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14
Q

Types of Metabolic Reactions (Phase)

Acetylation-acetyl CoA

A

Phase II

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15
Q

Types of Metabolic Reactions (Phase)

Sulfation

A

Phase II

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16
Q

Types of Metabolic Reactions (Phase)

Methylation

A

Phase II

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17
Q

Types of Metabolic Reactions (Phase)

Glycineconjugation-glycine

A

Phase II

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18
Q

Types of Metabolic Reactions (Phase)

Methylation

A

Phase II

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19
Q

Types of Metabolic Reactions (Phase)

Glycine conjugation-glycine

A

Phase II

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20
Q

Types of Metabolic Reactions (Phase)

Glutathione conjugation

A

Phase II

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21
Q

Types of Metabolic Reactions (Phase)

H2O conjugation

A

Phase II

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22
Q

Phase ___ > Phase ___ is the most common pathway

A

Phase I > Phase II

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23
Q

Pathway that most drug uses

A

Phase 1 > Phase II

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23
Q

Pathway that other drug uses

A

Phase II > Phase I

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23
T/F Drugs that are more polar are easier to eliminate
T
23
Maybe metabolized by gastric fluid
Penicillin
23
Must be given 2 hours before meals if given through the oral route
Penicillin
23
Drugs Metabolized by Gastric Acid
Penicillin
23
Drugs Metabolized by Gastric and digestive enzymes
Insulin
24
Drugs Metabolized by Intestinal wall enzymes
Epinephrine
24
Most important organ for drug metabolism
Liver
25
contains high concentration of PHASE I enzymes
Smooth endoplasmic reticulum (SER)
26
Activity of enzymes require ____ and ____
NADPH and molecular form of oxygen
27
Ester that is metabolized by plasma choline esterase
Succinylcholine
28
In most individuals, the process occurs rapidly
Hydrolysis of Esters
29
Genetic Factor Succinylcholine
Hydrolysis of Esters
30
Genetic Factor Isoniazid (INH)
Acetylation of Amines
31
Genetic Factor hydralazine and procainamide
Acetylation of Amines
32
T/F Slow acetylators cause individuals deficient in acetylating capacity and it produces prolonged or toxic responses to normal doses of the drug
T
33
Genetic Factor dextrometorphan, metoprolol, and some tricyclic antidepressants
Oxidation
34
Genetic Factor Metabolized by P450 isoenzymes which are genetically predetermined
Oxidation
35
Diest and environmental factors inhibits the effect of the drug
Charcoal
36
Diest and environmental factors increases the amount of drug in the body
Grapefruit juice
37
Age and sex T/F Drug metabolites do not differ in young and old
F; does differ
38
Age and sex T/F Males metabolize drugs faster than females
T
39
Age and sex T/F Children and elderly metabolize drugs slower
True
40
Disease affecting drug metabolism
Hyperthyroidism
41
T/F Thyroid hormone increase the metabolism
T
42
Other Drugs Increase rate of synthesis of the enzyme
Enzyme Induction
43
Other Drugs Reduce the rate of degradation of the enzyme
Enzyme Induction
44
Other Drugs May also induce metabolism of other drugs and reduce its effects
Enzyme Induction
45
Other drugs Inhibit CP450
Enzyme Inhibition
46
Other drugs Increase effect of the drug
Enzyme inhibition
47
Other drugs Metabolism of the drug is diminished
Enzyme inhibition
48
Enzyme Induction / Enzyme Inhibition Phenobarbital
Enzyme Induction
49
Enzyme Induction / Enzyme Inhibition Carbamazepine
Enzyme Induction
50
Enzyme Induction / Enzyme Inhibition Phenytoin
Enzyme Induction
51
Enzyme Induction / Enzyme Inhibition Rifampicin
Enzyme Induction
52
In enzyme induction Some drugs + Drug = increase/decrease effect
decreased effect
53
In enzyme inhibition Some drugs + Drug = increase/decrease effect
increased effect
54
Enzyme Induction / Enzyme Inhibition Cimetidine
Enzyme inhibition
55
Enzyme Induction / Enzyme Inhibition Amiodarone
Enzyme inhibition
56
Enzyme Induction / Enzyme Inhibition Ketoconazole
Enzyme inhibition
57
Enzyme Induction / Enzyme Inhibition Ritonavir
Enzyme inhibition
58
Enzyme Induction / Enzyme Inhibition Firanocoumarin
Enzyme inhibition
59
Type of Drug Mechanism Cholestyramine inhibits the effect of digoxin when combined with it
Altered Absorption
60
Type of Drug Mechanism Affects drug action through enzyme induction or inhibition
Altered Metabolism
61
Type of Drug Mechanism Plasma proteins can diminish the amount of drug that reaches its receptors
Altered Plasma Binding Protein
62
Type of Drug Mechanism Probenecid inhibits the secretion of weak acids
Altered Excretion
63
Type of Drug Mechanism Penicillin inhibits the excretion of probenecid
Altered Excretion