Exam 1- Lectures 3 & 4

Question 1

1 cause of monogenic hypercholesterolemia

Answer 1

familial hypercholesterolemia (FH)

Question 2

FH is

Answer 2

autosomeal co-dominant

Question 3

FH class 1

Answer 3

no LDL receptors made

Question 4

treatment for FH

Answer 4

HMG-CoA reductase inhibitors (statins)

Question 5

what class can you not treat with HMG-CoA reductase inhibitors (statins) and why?

Answer 5

class 1- bc it requires at least some working receptors.

Question 6

what kind of enzyme is NAT2?

Answer 6

phase II enzyme

Question 7

NAT2 is

Answer 7

autosomal dominant

Question 8

all NAT2 mutations are

Answer 8

SNPs

Question 9

what is the function of NAT2?

Answer 9

detoxification/inactivation of xenobiotics by acetylation

Question 10

slow acetylations due to NAT2 mutation increase risk of what cancers?

Answer 10

lung, liver, colon, bladder, non-hodgkin’s lymphoma

Question 11

slow acetylators:

Answer 11

increases toxicities

Question 12

fast acetylators

Answer 12

decreases therapeutic effects

Question 13

drug toxicity

Answer 13

drug induced anemia (G6PD enzyme)

Question 14

drug efficacy

Answer 14

colorectal cancer (K-ras & EGFR)

Question 15

what drugs can cause drug induced anemia due to GDPD

Answer 15

primaquine, salicylates, sulfonamides, nitrofurans, vitamin K derivatives

Question 16

G6PD is

Answer 16

x-linked recessive

Question 17

EFGR pathway

Answer 17

causes tumor proliferation if activated

Question 18

what mutation can occur in tumor cells that makes it not respond to the receptor and be always activated ?

Answer 18

k- ras

Question 19

a patient would not respond to anti-EGFR therapy if

Answer 19

the tumor has a k-ras mutation

Question 20

pharmacokinetics is

Answer 20

what the body does to the drug

ADME

Question 21

absorption

Answer 21

route of dose
first pass metabolism
active transport systems

Question 22

distribution

Answer 22

protein binding

tissue barriers

Question 23

metabolism

Answer 23

chemical structure changes in drug
phase I/phase II
P450

Question 24

Elimination

Answer 24

kidneys/liver
milk
skin, hair

Question 25

methods in identifying drug response phenotype

Answer 25

drug metabolism
drug receptors
drug transporters
biomarkers- efficacy & toxicity
disease susceptibility

Question 26

major pharmacogenomic considerations

Answer 26

intestinal wall/drug uptake
liver, first pass metabolism
food/water composition

Question 27

decreased first-pass metabolism often leads to

Answer 27

increased drug bioavailability

Question 28

alpha1-acid glycoprotein

Answer 28

mainly binding of basic drugs

ORM2- most important; major source of variability in the binding of basic drugs

Question 29

C3435T mutation

Answer 29

causes reduced levels of P-gp & higher plasma [] of drugs transported through P-gp

Question 30

P-gp is a biomarker for

Answer 30

drug resistance & prognosis in cancer patients

Question 31

P-gp is a target for

Answer 31

novel anticancer agents

Question 32

multiple drug resistance protein (MRP) transport what?

Answer 32

acids

Question 33

organic acid transporter (OAT) transports

Answer 33

organic acids

Question 34

Organic anion transporting polypeptide (OATP) transports

Answer 34

lipophilic agents

Question 35

organic cation transporter (OCT) transports

Answer 35

efflux of cations

Question 36

test 1=

Answer 36

required

Question 37

test 2=

Answer 37

recommended

Question 38

test 3=

Answer 38

info only