U4 DRG BIOTRANSFORMATION Flashcards

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
Q

T/F Drugs that are more polar are easier to eliminate

A

T

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23
Q

Maybe metabolized by gastric fluid

A

Penicillin

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23
Q

Must be given 2 hours before meals if given through the
oral route

A

Penicillin

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23
Q

Drugs Metabolized by Gastric Acid

A

Penicillin

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23
Q

Drugs Metabolized by Gastric and digestive enzymes

A

Insulin

24
Q

Drugs Metabolized by Intestinal wall enzymes

A

Epinephrine

24
Q

Most important organ for drug metabolism

A

Liver

25
Q

contains high concentration of PHASE I enzymes

A

Smooth endoplasmic reticulum (SER)

26
Q

Activity of enzymes require ____ and ____

A

NADPH and molecular form of oxygen

27
Q

Ester that is metabolized by plasma choline esterase

A

Succinylcholine

28
Q

In most individuals, the process occurs rapidly

A

Hydrolysis of Esters

29
Q

Genetic Factor

Succinylcholine

A

Hydrolysis of Esters

30
Q

Genetic Factor

Isoniazid (INH)

A

Acetylation of Amines

31
Q

Genetic Factor

hydralazine and procainamide

A

Acetylation of Amines

32
Q

T/F Slow acetylators cause individuals deficient in acetylating capacity and it produces prolonged or toxic responses to normal doses of the drug

A

T

33
Q

Genetic Factor

dextrometorphan, metoprolol, and some tricyclic antidepressants

A

Oxidation

34
Q

Genetic Factor

Metabolized by P450 isoenzymes which are genetically predetermined

A

Oxidation

35
Q

Diest and environmental factors

inhibits the effect of the drug

A

Charcoal

36
Q

Diest and environmental factors

increases the amount of drug in the body

A

Grapefruit juice

37
Q

Age and sex

T/F Drug metabolites do not differ in young and old

A

F; does differ

38
Q

Age and sex

T/F Males metabolize drugs faster than females

A

T

39
Q

Age and sex

T/F Children and elderly metabolize drugs slower

A

True

40
Q

Disease affecting drug metabolism

A

Hyperthyroidism

41
Q

T/F Thyroid hormone
increase the metabolism

A

T

42
Q

Other Drugs

Increase rate of synthesis of the enzyme

A

Enzyme Induction

43
Q

Other Drugs

Reduce the rate of degradation of the enzyme

A

Enzyme Induction

44
Q

Other Drugs

May also induce metabolism of other drugs and reduce its effects

A

Enzyme Induction

45
Q

Other drugs

Inhibit CP450

A

Enzyme Inhibition

46
Q

Other drugs

Increase effect of the drug

A

Enzyme inhibition

47
Q

Other drugs

Metabolism of the drug is diminished

A

Enzyme inhibition

48
Q

Enzyme Induction / Enzyme Inhibition

Phenobarbital

A

Enzyme Induction

49
Q

Enzyme Induction / Enzyme Inhibition

Carbamazepine

A

Enzyme Induction

50
Q

Enzyme Induction / Enzyme Inhibition

Phenytoin

A

Enzyme Induction

51
Q

Enzyme Induction / Enzyme Inhibition

Rifampicin

A

Enzyme Induction

52
Q

In enzyme induction

Some drugs + Drug = increase/decrease effect

A

decreased effect

53
Q

In enzyme inhibition

Some drugs + Drug = increase/decrease effect

A

increased effect

54
Q

Enzyme Induction / Enzyme Inhibition

Cimetidine

A

Enzyme inhibition

55
Q

Enzyme Induction / Enzyme Inhibition

Amiodarone

A

Enzyme inhibition

56
Q

Enzyme Induction / Enzyme Inhibition

Ketoconazole

A

Enzyme inhibition

57
Q

Enzyme Induction / Enzyme Inhibition

Ritonavir

A

Enzyme inhibition

58
Q

Enzyme Induction / Enzyme Inhibition

Firanocoumarin

A

Enzyme inhibition

59
Q

Type of Drug Mechanism

Cholestyramine inhibits the effect of digoxin when combined with it

A

Altered Absorption

60
Q

Type of Drug Mechanism

Affects drug action through enzyme induction or inhibition

A

Altered Metabolism

61
Q

Type of Drug Mechanism

Plasma proteins can diminish the amount of drug that reaches its receptors

A

Altered Plasma Binding Protein

62
Q

Type of Drug Mechanism

Probenecid inhibits the secretion of weak acids

A

Altered Excretion

63
Q

Type of Drug Mechanism

Penicillin inhibits the excretion of probenecid

A

Altered Excretion