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Exam 2 - Keshvara

Total questions: 56

Worksheet time: 4hrs 6mins

Name
Class
Date
1.

What are xenobiotics?

a)

"foreign" or exogenous substances

b)

modified in the body to become more polar forms

2.

What is biotransformation/drug metabolism?

a)

"foreign" or exogenous substances

b)

modified in the body to become more polar forms

3.

Polar xenobiotics

a)

need to be modified

b)

do not need to be modified

4.

Non-polar xenobiotics

a)

need to be modified

b)

do not need to be modified

5.

Select some examples of xenobiotics

a)

alcohol

b)

insulin

c)

pesicides

d)

drugs (except endogenous)

e)

food additives

6.

What major organ is involved in biotransformation

a)

liver

b)

stomach

c)

intestines

d)

spleen

7.

What happens during pre-systemic (first pass) metabolism

a)

drugs will get metabolized

b)

decreases bioavailability of oral drugs

c)

drugs get into circulation

8.

What happens during post-systemic metabolism

a)

drugs will get metabolized

b)

decreases bioavailability of oral drugs

c)

drugs get into circulation

9.

Why does dosage affect bioavailability

a)

due to liver enzymes

b)

due to stomach enzymes

c)

due to urea cycle

d)

due to intestinal enzymes

10.

Main organs of first pass effect

a)

liver

b)

GI tract

c)

blood

d)

spleen

11.

How does Phase I reactions increase polarity

a)

oxidation

b)

reduction

c)

hydrolysis

d)

covalent conjugation

12.

How does Phase II reactions increase polarity

a)

oxidation

b)

reduction

c)

hydrolysis

d)

covalent conjugation

13.

What happens to a drug after a Phase I reaction

a)

involves changes in functional groups

b)

increases polarity

c)

modification phase

d)

drugs not necessarily inactivated (prodrugs activated)

e)

pharmacological activity is almost always lost

14.

What happens after a drug goes through a Phase II reaction

a)

covalent conjugation of drugs with large polar groups

b)

significant increase in polarity

c)

pharmacological activity is almost always lost

d)

drug not necessarily inactivated

15.

If a drug undergoes both Phase I and Phase II metabolism, which Phase generally comes first?

a)

Phase 2

b)

Phase 1

16.

Why is Phase I often referred to as a functionalization phase?

a)

it does small modifications

b)

it does large modifications

17.

What happens during a phase I oxidation reaction

a)

+O2; catalyzed by CYP450

b)

+ e- (causing H+ to follow); catalyzed by CYPs & other reductases

c)

+H2O; catalyzed by esterases & amidases

18.

What happens during a phase I reduction reaction

a)

+O2; catalyzed by CYP450

b)

+ e- (causing H+ to follow); catalyzed by CYPs & other reductases

c)

+H2O; catalyzed by esterases & amidases

19.

What happens during a phase I hydrolysis reaction

a)

+O2; catalyzed by CYP450

b)

+ e- (causing H+ to follow); catalyzed by CYPs & other reductases

c)

+H2O; catalyzed by esterases & amidases

20.

Which enzyme group is responsible for most of the oxidation reactions?

a)

P450

b)

CYP enzymes

c)

hydrolase (esterases and amidase)

d)

reductases

21.

What type of reaction is this

a)

Phase I Oxidative Hydroxylation

b)

Phase I Reduction

c)

Phase I Hydrolysis

d)

Phase I Oxidative O-dealkylation

22.

What type of reaction is this

a)

Phase I Oxidative N-Dealkylation

b)

Phase I Deamination

c)

Phase I Hydrolysis

d)

Phase I Oxidative O-dealkylation

23.

What type of reaction is this

a)

Phase I Oxidative N-Dealkylation

b)

Phase I Deamination

c)

Phase I Hydrolysis

d)

Phase I Oxidative O-dealkylation

24.

What is Codeine and how is it converted to Morphine

a)

prodrug

b)

active metabolite

c)

O-dealkylation

d)

hydroxylation

25.

What type of reaction is this

a)

Phase I Oxidative N-Dealkylation

b)

Phase I Oxidative Deamination

c)

Phase I Hydrolysis

d)

Phase I Oxidative O-dealkylation

26.

What happens when you remove an amine from a drug

a)

inactivates the drug

b)

activates the drug

27.

What is this

a)

Catechol

b)

Benzene

c)

Phenyl

28.

What is MAO

a)

Monoamine Oxidase

b)

Many Amine + Oxygen

c)

Monoamide Oxidase

29.

What were among the first group of antidepressants on the market

a)

MAO inhibitors

b)

atypical

c)

SSRI

d)

SNRI

e)

tricyclic

30.

How is MAO different from Phase I enzymes that carry out deamination

a)

CYP P450

b)

O2

c)

CYP 3A4

31.

What is hydrolysis

a)

addition of H2O

b)

removal of H2O

c)

addition of O2

d)

removal of O2

32.

What are the two major types of hydrolysis

a)

N-Dealkylation hydrolysis

b)

O-Dealkylation hydrolysis

c)

P-Dealkylation hydrolysis

d)

S-Dealkylation hydrolysis

33.

What two groups of enzymes are involved with hydrolysis

a)

esterases

b)

amidases

c)

etherases

d)

aminases

34.

Why are many prodrugs are esters

a)

better absorbed orally

b)

harder to absorb orally

35.

What is more stable

a)

ester

b)

amide

36.

What is a reduction rxn

a)

opposite of oxidation

b)

addition of e-

c)

not as common

d)

carried out by P450 & other enzymes

37.

What do CYP enzymes contain in the center

a)

heme group

b)

O2 group

c)

CC double bond

38.

What does the heme group in the center of a CYP enzyme do

a)

help coordinate O2

b)

help coordinate substrates

c)

thru reductive steps, substrate gets oxidized

39.

CYPs are present in all living things, what role do they carry out

a)

steroid synthesis

b)

FA synthesis

c)

hormone synthesis

40.

Which CYP is involved in Biotransformation

a)

CYP3A4

b)

CYP2D6

c)

CYP2C9

d)

CYP2C19

e)

CYP P450

41.

Why are CYPs considered flexible

a)

one CYP can metabolize hundreds of xenobiotics

b)

a drug may undergo metabolism catalyzed by multiple CYPs

c)

many drug-drug interactions occur at CYP level

d)

a CYP can bend

42.

Why is CYP3A4 important

a)

responsible for metabolizing almost half the drugs on the market

b)

responsible for metabolizing cancer saving drugs

c)

responsible for allowing drugs that prevent illness to go through

43.

What major drug classes are metabolized by CYP3A4

a)

benzodiazepine

b)

Ca2+ channel blockers

c)

HIV protease inhibitors

d)

macrolides

e)

statins

44.

What are CYP3A4 inhibitors

a)

antifungal azoles

b)

CCBs

c)

HIV prot inhibs

d)

macrolides

e)

grapefruit juice

45.

What are CYP3A4 inducers

a)

carbamazepine

b)

phenobarbital

c)

phenyltoin

d)

rifampin

e)

St. John's Wort

46.

How does grapefruit juice inhibit CYP3A4

a)

raises serum alprazolam concentration

b)

lowers serum alprazolam concentration

47.

How does St. John's Wort induce CYP3A4

a)

raises serum alprazolam concentration

b)

lowers serum alprazolam concentration

48.

Which CYP can chargrilled meat, cruciferous vegetables, and smoking induce

a)

CYP1A2

b)

CYP2E1

c)

CYP2D6

d)

CYP2C9

e)

CYP2C19

49.

Which CYP can chronic alcohol use induce

a)

CYP1A2

b)

CYP2E1

c)

CYP2D6

d)

CYP2C9

e)

CYP2C19

50.

Which CYP can be dramatically different in certain individuals (due to genes) and could cause significant drug-drug interactions that may not be seen in those with normal enzyme levels

a)

CYP1A2

b)

CYP2E1

c)

CYP2D6

d)

CYP2C9

e)

CYP2C19

51.

What are the Phase II reactions

a)

glucuronidation

b)

glutathion conjugation

c)

glycine conjugation

d)

sulfation

e)

acetylation

52.

Glucuronidation

a)

uses UDP-glucuronosyl transferases

b)

conjugates with glucuronic acid grp

c)

req free -OH

d)

conjugates with glutathione

53.

Glutathione Conjugation

a)

uses glutathione-S-transferases

b)

conjugates with a glutathione

c)

makes a tripeptide

d)

adds a sulfate

54.

Sulfation

a)

adds a sulfate

b)

is carried out by sulfotransferases

c)

adds an acetyl group

55.

Acetylation

a)

uses N-acetyl transferases

b)

adds an acetyl group on nitrogen

c)

uses acetyl CoA as the cofactor

d)

does not increase water solubility

56.

Which phase II reaction does not increase water solubility

a)

glucuronidation

b)

glutathione conjugation

c)

glycine conjugation

d)

sulfation

e)

acetylation

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