exam 3 Flashcards

1
Q

cyps account for 70% of metabolism . whtat cyps are involved most inmeyabolism

A

VYP3A4/5, CYP 2D6, 2C19. 2B6

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

what organ plays the most role in metabolism

A

liver

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

0examples of prodrugs:

A

probenecid

codeine: ctyp 2d6 removes methyl group and yields morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

contributer to unexpected metabolism

A

DDI/ food interactions
induces expression
natural variability

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

cyps that have genetic variation:

A

cyp2c9: decreased functional genee varient exists
cyp2c19: defective gene varient in 3-16% of individuals
cyp2d6: highly polymorphic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

phase !! metabolism enzyme examples

A

NAT
COMT
TPMT

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

when should you watch for metabolism variability

A

regulates a majorroute of elimination
yields pharmacologically active metabolites
the drup has a narrow TI

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

role of membrane transporters:

A

move nutrients or metabolites/ toxins across membranes

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

three sides of membrane

A

basolateral membrane: access to organs, often facing blood
intracellular membrane:
apical membrane

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

influx

A

movement of ions into cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

efflux:

A

movement of ions out of cell

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

OASTPs

A

OATP1. mediates hepatic uptake of drugs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

influx transporters examples

A
OATP
PEPT1
ASBT
MCT1
oct2
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

efflux transporters examples

A

BCRP

PGP

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

OATP1 and OATP2 function

A

mediate uptake into gut

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

clearance

A

total elimination of drug from body

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

liver can metabolize/eliminate significant portion of absorbed drug through what effect

A

first pASs effect

18
Q

clearance is determinant on two major parameters

A

blood flow

difference between incoming concentration (arterial blood) and outgooing concentraion (venous blood)

19
Q

ER= fraction of drug removed from body by organ

A

fraction of drug removed from body by organ

20
Q

what does a high extraction ratio mean

A

since ER is the amount of drug removed by the liver, a high ER would mean that majority of the drug is removed by first pass metabolism

21
Q

intrinsic clearance

A

measure of intrinsic hepatic eliminating ability (google definition: ability of the liver to remove drug in the absense of flow limitations or protein binding)

22
Q

factors increases blood flow

A

supine position and exercise
transiently increases after eating
transiently increases after dug exposure

23
Q

factors that decrease bloodflow

A

thermal stress
disease states, CHF, cirrhosis
drug exposure

24
Q

factors that mediate protein binding

A

saturation at high conc
changes in protein conc
displacement of protein binding sites

25
Q

albumin binds to which kind of drugs

A

acidic and neutral drugs

most abundant found protein in humans

26
Q

most important protein for binding of basic drugs

A

AAG

27
Q

ke

A

rate of elimination via renal clearance

28
Q

U

A

amount in urine

29
Q

factors affecting renal clearance

A

GFR
tubular secretion
tubular reabsorption
urinary elimination

30
Q

CLrf

A

renal clearance by filtration

31
Q

if CLr is > than CLrf.

A

tubular secretion must occur

32
Q

if CLrf > CLr

A

reabsorption must occure

33
Q

what size compounds tend to be eliminated by biliary excretrion

A

high MW compounds

34
Q

enteroheparic recyclinng

A

occurs when excreted drug in bile is reabsorbed back into the liver

35
Q

hepatocyte hopping

A

metabolized drug hops between hepatocytes until it reaches efflux transpporter
prevents saturation of biliary excretion

36
Q

ABCC3 responsible for

A

hepatocyte hopping

37
Q

most drug interaction involve which phase enzymes

A

phase 1

38
Q

CYP2E1 inducers

A

ethanol, isoniazid

39
Q

CYP3a4

A

rifampin, phenytoin, st johns wort,

40
Q

DDIs that arent always bad

A

poinavir/ ritonavir AIDS. ritinovir increases oral bioavailability of lopinavir, reducing its daily dose

LDOPA/carbidopa

41
Q

grape fruit juice

A

increaes bioavailability / systemic conc of 3A4 substrates

inhibits OATP