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PHA337 > Metabolism > Flashcards

Metabolism Flashcards

1
Q

Most common CYP enzyme to metabolite drugs which is responsible for 50% of drug metabolism is:

A. CYP2D6
B. CYP2E1
C. CYP3A4
D. CYP2C9

A

C. CYP3A4

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2
Q

Which of the following is Phase 1 reaction in metabolism?

A. Reduction
B. Sulfonation
C. Glucuronidation
D. Acytilation

A

A. Reduction

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3
Q

CYP450 has how many families?

A. 4
B. 18
C. 43
D. 450

A

B. 18

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4
Q

Chronic alcohol intake increases the activity of which CYP enzyme?

A. CYP2E1
B. CYP4A3
C. CYP2C1
D. CYP2C9

A

A. CYP2E1

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5
Q

Metabolism lead to toxicity by which process?

A. Metabolic enzymes are itself toxic materials
B. Supplying more toxic materials
C. Saturation of detoxifying pathways
D. Converting drug to toxic chemical

A

C. Saturation of detoxifying pathways

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6
Q

Which type of drug will have more chance to be metabolized in liver?

A. Large molecule and hydrophilic drug
B. Small molecule, lipophilic drug and unbound
C. Small molecule protein bound drug
D. Protein bound drug

A

B. Small molecule, lipophilic drug and unbound.

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7
Q

Which enzyme increases the risk of cancer by enhancing the activation of carcinogens?

A. CYP3A4
B. CYP2C19
C. CYP2D12
D. CYPE21

A

D. CYPE21

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8
Q

A medication or compound that, after administration, is metabolized into a pharmacologically active drug is defined as:

A. Antigen
B. Excipient
C. Prodrug
D. Antibody

A

C. Prodrug

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9
Q

In enzyme CYP3A4, the letter A represents:

A. Family
B. Cytochrome
C. Subfamily
D. Enzyme number

A

C. Subfamily

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10
Q

In metabolism process, oxidation by addition of functional groups such as -OH, -SH, -COOH, -NH2 to drug happens in:

A. Phase 1
B. Phase 2
C. Phase 3
D. Phase 4

A

A. Phase 1

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11
Q

Which of the following is not a site of metabolism?

A. Kidney
B. Lung
C. Bone
D. Skin

A

C. Bone

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12
Q

Which is a common reaction in phase 2 metabolism process?

A. Glucuronidation
B. Reduction
C. Oxidation
D. Hydrolysis

A

A. Glucuronidation

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13
Q

Which enzyme is mostly responsible for elimination of the top 200 prescribed drugs in US and Europe?

A. CYP2C9
B. CYP3A4
C. CYP2D6
D. CYP2E1

A

B. CYP3A4

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14
Q

Major organ of drug metabolism for endogenous chemicals.

A

Liver

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15
Q

Conjugation phase.

A

Phase 2

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16
Q

Types of Phase 1 Metabolism Reactions

A

Oxidation
Reduction
Hydrolysis

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17
Q

Most common reaction for phase 1.

A

Oxidation

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18
Q

Types of Phase 2 Metabolism Reactions

A 
Glucuronic acid conjugation
Sulfonation
Amino acid conjugation
Glutathione conjugation
Acetylation
Methylation
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19
Q

Drug metabolism (Biotransformation reaction) is divided into:

A 
Phase 1 (oxidation)
Phase 2 (conjugation)
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20
Q

3 main of 74 CYP gene families that involve in drug metabolism.

A

CYP 1
CYP 2
CYP 3

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21
Q

What are main enzymes of phase 2?

A

GSTs: Glutathione-S-transferase
UGTs: UDP glucuronosyltransferase

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22
Q

Which one is the Family No, Subfamily, and Enzyme No for CYP3A4?

A

Family No.: 3
Subfamily: A
Enzyme No.: 4

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23
Q

Which isoforms activate many carcinogens? Select all that apply.

A. CYP2D6
B. CYP2E1
C. CYP2A6
D. CYP3A4
E. CYP2B1
A

B. CYP2E1
C. CYP2A6
E. CYP2B1

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24
Q

Which one metabolized a 25% of drugs, particular basic drugs?

A. CYP2D6
B. CYP3A4
C. CYP2E1
D. CYP2B1

A

A. CYP2D6

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25
Q

Is a medication or compound that , after administration, is metabolized into a pharmacologically active drug.

A

Prodrug

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26
Q

Is the most abundant and metabolizes 50% of drugs

A

CYP3A4

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27
Q

Metabolize many acidic drugs: (2)

A. CYP2E1
B. CYP2C9
C. CYP2C19
D. CYP2B4

A

B. CYP2C9

C. CYP2C19

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28
Q

How many subfamilies do CYP450 have?

A. 45
B. 18
C. 43
D. 3

A

D. 43

29
Q

Are synthetic reaction & involve conjugation (attachment of a substituent group) which results in inactive products

Substrates for conjugation reactions contains (OH-), (NH2-), (-COOH).

A

Phase 2

30
Q

Occur mainly in liver.

Catabolic reaction (oxidation/reduction, hydrolysis).

A

Phase 1

31
Q

Other sites of drug metabolism.

A

Kidney
Skin
Lungs

32
Q

Orally administered drugs often absorbed in the GI tract then transport to liver via portal vein

A

First-pass effect

33
Q

When a drug undergoes metabolism it always produces an active metabolite similar to the drug, but with a shorter half life.

A. True
B. False

A

False

34
Q

Which of the following is NOT a major enzyme important to metabolism of drugs?

A. CYP3A4
B. CYP2D6
C. CYP2C9
D. CYP2C29

A

D. CYP2C29

35
Q

Conjugation reactions always increase hydrophilicity of substrates.

A. True
B. False

A

B. False

Conjugation reaction can generally either increase or decrease hydrophilicity of substrates if not specified clearly.

36
Q

If a drug is more non polar it will be eliminated by kidneys.

A. True
B. False

A

B. False

More polar is more eliminated by the kidneys.

37
Q

CYP450 enzymes can catalyze oxidations of many but they cannot catalyze reductions.

A. True
B. False

A

False.

It can catalyze reductions.

38
Q

Which of the following undergoes Phase II metabolism?

A. Methylation
B. Acetylation
C. Sulfation
D. All of the above

A

D. All of the above

39
Q

The most common pathways in metabolism are:

A. Drug—> Phase 1—> Elimination
B. Drug—>Phase 1–>Phase 2–>Elimination
C. Drug—>Phase 2–>Elimination
D. Drug—>Phase 2—> Phase 1—>Elimination

A

A. Drug—>Phase 1–>Elimination

B. Drug->Phase 1–>Phase 2–>Elimination

40
Q

Drugs that are more hydrophilic are generally eliminated by the _____, where drugs that are more lipophilic are generally eliminated by the _________.

A 
Kidneys (Urine)
Bile acids (Stool)
41
Q

Phase 2 metabolism results in an increase in lipophilic by oxidation, reduction, and hydrolysis reactions.

A. True
B. False

A

B. False

Phase 1 is the one metabolism results in a decrease in lipophilicity by oxidation, reduction, and hydrolysis reactions.

42
Q

Non-polar species are eliminated by what process?

A. Renal elimination
B. Biliary elimination

A

B. Biliary elimination

43
Q

What are CYP’s classification based on? Select all that apply

A. Family
B. Subfamily
C. Isozyme
D. Organ Location

A

A. Family
B. Subfamily
C. Isozyme

44
Q

Polar metabolites generally undergo renal elimination (urine) and non-polar metabolites generally undergo biliary elimination (stool).

A. True
B. False

A

A. True

45
Q

Phase 1 Methylation and phase 2 Acylation reactions both decrease water solubility.

A. True
B. False

A

B. False

Methylation is also phase 2.

46
Q

What are types of oxidation reactions in phase 1 metabolism?

A. Hydroxylation
B. Oxidation
C. Methyltransferases
D. Dealkylation
E. All of the above
A

A. Hydroxylation
B. Oxidation
D. Dealkylation

47
Q

What action should a pharmacist take in adjusting the dosage of a medication that undergoes extensive first pass metabolism in a patient who has decreased hepatic blood flow due to heart failure?

A. Increase the dose
B. Decrease the dose
C. Do not make any changes
D. None of the above

A

B. Decrease the dose

Because a reduction in first-pass effect can result in increase of effective oral drug.

48
Q

Which of the following is the most common reaction in drug metabolism?

A. Oxidation
B. Acetylation
C. Reduction
D. Sulfation

A

A. Oxidation

49
Q

A drug must always go through phase 1 metabolism first, and then phase 2 metabolism before it is eliminated.

A. True
B. False

A

B. False

50
Q

The liver and kidney organs are consider as both pre-systemic and systemic metabolic sites.

A. True
B. False

A

False

Only the liver is both while the kidneys are categorized as systemic metabolism

51
Q

What phase are sulfonation reactions present in?

A. Phase 1
B. Phase 2
C. Phase A
D. Phase B
E. All of the above
A

B. Phase 2

52
Q

Patients with chronic alcohol use have elevated _______ enzyme.

A. CYP2E1
B. CYP2A6
C. CYP2B1
D. CYP3A4

A

A. CYP2E1

53
Q

Main CYP450 metabolizing enzyme in the gut wall is:

A. CYP3A4
B. CYP2D6
C. CYP2C9
D. CYP2D6

A

A. CYP3A4

54
Q

Hepatic artery accounts for ___ % of the liver blood flow whereas the hepatic portal vein accounts for__%

A. 50% and 50%
B. 75% and 25%
C. 25% and 75%
D. Non of at above

A

C. 25% and 75%

55
Q

Hepatic elimination consists of:

A

Hepatic metabolism

Biliary excretion

56
Q

What are the genetic factors? (2)

A
  1. Pharmacogenetics/Pharmacogenomics

2. Genetic polymorphism

57
Q

Drug related factors? (2)

A
  1. Dose

2. Route of administration

58
Q

Physiological factors? (5)

A
  1. Age
  2. Gender
  3. Pregnancy
  4. Disease
  5. Diet
59
Q

Which are Factors Affecting Drug metabolism? Select all that apply

A. Genetic factor 
B. Drug related factors
C. Drug-plasma protein biding
D. Environmental factors
E. All of the above
A

E. All of the above

60
Q

Factors Affecting Drug Meytabolism: (6)

A
  1. Genetic factors
  2. Physiologic factors
  3. Drug related factors
  4. Enzyme induction/inhibition(drug-drug interactions)
  5. Environmental (external) factors (smoking, alcohol)
  6. Drug-plasma protein biding
61
Q

Polycyclic aromatic hydrocarbon induces which enzymes: Select all that apply.

A. CYP1A1
B. CYP1A2
C. CYP2E1
D. CYP2C9

A

A. CYP1A1
B. CYP1A2
C. CYP2E1

62
Q

Smoking increases the risk of cancer by enhancing which enzyme?

A

CYP2E1

63
Q

Smoking increases metabolism of which type of drugs? 2 examples

A
  1. Propranolol

2. Tricyclics Antidepressants

64
Q

Alcohol

A
  1. Chronic alcohol intake increases the activity of CYP2E1 through enzyme induction.
  2. Metabolism of drugs that are substrate of CYP2E1 is therefore increased in cases of chronic use.
  3. Acute use of alcohol inhibits metabolism of many drugs
65
Q

_________ may not be available as substrates for liver enzymes, resulting in reduced drug metabolism.

A

Bound drugs

66
Q

Increase in drug metabolism:

A. Reduce plasma concentration
B. Reduce oral bioavailability
C. Increase oral bioavailability
D. Increase plasma concentration

A

A. Reduce plasma concentration

B. Reduce oral bioavailability

67
Q

Enzyme inhibition

A
  1. Reduce the enzyme activity

2. Example: Cimetidine and Erythromycin

68
Q

Increase in drug metabolism means:

A
  1. reduce of plasma concentration

2. reduce oral bioavailability

69
Q

Enzyme induction:

A
  1. Many drugs can induce the enzymes to the metabolize themselves and/or other drugs leading to change in their pharmacological and toxicological effects.
  2. The drug may be metabolized more rapidly to metabolites that are more potent, more toxic, or less active than the parent drugs.
  3. Example: Rifampin and Phenobarbital

PHA337 (5 decks)

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