Drug metabolism and transport

Question 1

codeine

Answer 1

morphine

Question 2

primary site of metabolism

Answer 2

liver

Question 3

CYP

Answer 3

microsomal enzyme

Question 4

CYP 450

Answer 4

oxidation and phase 1

Question 5

Glucuronidation

Answer 5

Phase II

Question 6

what is the difference between omeprazole and nexium?

Answer 6

nexium is quicker and lower dose is needed

Question 7

inactive drug

Answer 7

pro-drug

Question 8

what happens when you digest alcohol and acetominophen?

Answer 8

alcohol induces the activity of the CYP that converts acetimnophen to the toxic metabolite

Question 9

rifampin

Answer 9

CYP450 inducer

Question 10

anticonvulsants

Answer 10

CYP450 inducer

Question 11

clearance occurs in the

Answer 11

kidney

Question 12

what happens to those that are poor metabolizers of the drug

Answer 12

drug accumulates

Question 13

pre-systemic extraction by GI enzymes

Answer 13

first pass effect

Question 14

what happens when there is an extraction by GI enzymes?

Answer 14

lower bioavailability

Question 15

increase active enzymes through transcription/translation- slow process

Answer 15

induction

Question 16

decreases active enzymes- immediate

Answer 16

inhibition

Question 17

An active drug has ______ effect when metabolizing enzymes are induced–> it is eliminated _________

Answer 17

An active drug has less effect when metabolizing enzymes are induced–> it is eliminated more quickly

Question 18

a prodrug has _______ effect when metabolizing enzymes are induced–> active metabolite is _________

Answer 18

a prodrug has greater effect when metabolizing enzymes are induced–> active metabolite is made at a greater quantity

Question 19

CYP450 enzymes in GI tract and liver metabolize the majority of drugs

Answer 19

Phase I

Question 20

UGT enzymes preform Glucoronidation, adding polar end group for enhanced renal elimination

Answer 20

Phase II

Question 21

membrane transporters regulate drug movement across membranes _______________

Answer 21

without altering structure

Question 22

P-glycoprotein pumps out a variety of foreign substances but what happens to oral absorption?

Answer 22

it decreases

Question 23

acetaminophen has 2 pathways: detox by ______ or ________

Answer 23

detox by adding polar group and bioactivation

Question 24

the intermediate in bioactivation pathway for acetaminophen is

Answer 24

toxic

Question 25

what will increase chances of toxicity by taking acetaminophen?

Answer 25

1. higher dose and CYP450 inducers

2. low glutathione stores in alcoholics and extreme dieters