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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
Is a medication or compound that , after administration, is metabolized into a pharmacologically active drug.
Prodrug
26
Is the most abundant and metabolizes 50% of drugs
CYP3A4
27
Metabolize many acidic drugs: (2) A. CYP2E1 B. CYP2C9 C. CYP2C19 D. CYP2B4
B. CYP2C9 | C. CYP2C19
28
How many subfamilies do CYP450 have? A. 45 B. 18 C. 43 D. 3
D. 43
29
Are synthetic reaction & involve conjugation (attachment of a substituent group) which results in inactive products Substrates for conjugation reactions contains (OH-), (NH2-), (-COOH).
Phase 2
30
Occur mainly in liver. Catabolic reaction (oxidation/reduction, hydrolysis).
Phase 1
31
Other sites of drug metabolism.
Kidney Skin Lungs
32
Orally administered drugs often absorbed in the GI tract then transport to liver via portal vein
First-pass effect
33
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
False
34
Which of the following is NOT a major enzyme important to metabolism of drugs? A. CYP3A4 B. CYP2D6 C. CYP2C9 D. CYP2C29
D. CYP2C29
35
Conjugation reactions always increase hydrophilicity of substrates. A. True B. False
B. False Conjugation reaction can generally either increase or decrease hydrophilicity of substrates if not specified clearly.
36
If a drug is more non polar it will be eliminated by kidneys. A. True B. False
B. False | More polar is more eliminated by the kidneys.
37
CYP450 enzymes can catalyze oxidations of many but they cannot catalyze reductions. A. True B. False
False. | It can catalyze reductions.
38
Which of the following undergoes Phase II metabolism? A. Methylation B. Acetylation C. Sulfation D. All of the above
D. All of the above
39
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. Drug—>Phase 1–>Elimination | B. Drug->Phase 1–>Phase 2–>Elimination
40
Drugs that are more hydrophilic are generally eliminated by the _____, where drugs that are more lipophilic are generally eliminated by the _________.
``` Kidneys (Urine) Bile acids (Stool) ```
41
Phase 2 metabolism results in an increase in lipophilic by oxidation, reduction, and hydrolysis reactions. A. True B. False
B. False | Phase 1 is the one metabolism results in a decrease in lipophilicity by oxidation, reduction, and hydrolysis reactions.
42
Non-polar species are eliminated by what process? A. Renal elimination B. Biliary elimination
B. Biliary elimination
43
What are CYP’s classification based on? Select all that apply A. Family B. Subfamily C. Isozyme D. Organ Location
A. Family B. Subfamily C. Isozyme
44
Polar metabolites generally undergo renal elimination (urine) and non-polar metabolites generally undergo biliary elimination (stool). A. True B. False
A. True
45
Phase 1 Methylation and phase 2 Acylation reactions both decrease water solubility. A. True B. False
B. False | Methylation is also phase 2.
46
What are types of oxidation reactions in phase 1 metabolism? ``` A. Hydroxylation B. Oxidation C. Methyltransferases D. Dealkylation E. All of the above ```
A. Hydroxylation B. Oxidation D. Dealkylation
47
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
B. Decrease the dose | Because a reduction in first-pass effect can result in increase of effective oral drug.
48
Which of the following is the most common reaction in drug metabolism? A. Oxidation B. Acetylation C. Reduction D. Sulfation
A. Oxidation
49
A drug must always go through phase 1 metabolism first, and then phase 2 metabolism before it is eliminated. A. True B. False
B. False
50
The liver and kidney organs are consider as both pre-systemic and systemic metabolic sites. A. True B. False
False | Only the liver is both while the kidneys are categorized as systemic metabolism
51
What phase are sulfonation reactions present in? ``` A. Phase 1 B. Phase 2 C. Phase A D. Phase B E. All of the above ```
B. Phase 2
52
Patients with chronic alcohol use have elevated _______ enzyme. A. CYP2E1 B. CYP2A6 C. CYP2B1 D. CYP3A4
A. CYP2E1
53
Main CYP450 metabolizing enzyme in the gut wall is: A. CYP3A4 B. CYP2D6 C. CYP2C9 D. CYP2D6
A. CYP3A4
54
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
C. 25% and 75%
55
Hepatic elimination consists of:
Hepatic metabolism | Biliary excretion
56
What are the genetic factors? (2)
1. Pharmacogenetics/Pharmacogenomics | 2. Genetic polymorphism
57
Drug related factors? (2)
1. Dose | 2. Route of administration
58
Physiological factors? (5)
1. Age 2. Gender 3. Pregnancy 4. Disease 5. Diet
59
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 ```
E. All of the above
60
Factors Affecting Drug Meytabolism: (6)
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
Polycyclic aromatic hydrocarbon induces which enzymes: Select all that apply. A. CYP1A1 B. CYP1A2 C. CYP2E1 D. CYP2C9
A. CYP1A1 B. CYP1A2 C. CYP2E1
62
Smoking increases the risk of cancer by enhancing which enzyme?
CYP2E1
63
Smoking increases metabolism of which type of drugs? 2 examples
1. Propranolol | 2. Tricyclics Antidepressants
64
Alcohol
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
_________ may not be available as substrates for liver enzymes, resulting in reduced drug metabolism.
Bound drugs
66
Increase in drug metabolism: A. Reduce plasma concentration B. Reduce oral bioavailability C. Increase oral bioavailability D. Increase plasma concentration
A. Reduce plasma concentration | B. Reduce oral bioavailability
67
Enzyme inhibition
1. Reduce the enzyme activity | 2. Example: Cimetidine and Erythromycin
68
Increase in drug metabolism means:
1. reduce of plasma concentration | 2. reduce oral bioavailability
69
Enzyme induction:
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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