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PK/PD > p450 reactions > Flashcards

p450 reactions Flashcards

1
Q

AUC and steady state concentrations are dependent only on what

A

the enzymes involved

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2
Q

phases of liver metabolism

A
  • phase 0 - uptake to hepatocyte
  • phase 1 - oxidation, reduction, hydrolysis
  • phase 2 - glucuronidation, methylate, acetylate
  • phase 3 - excrete into blood
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3
Q

pharmacodynamics definition

A

what drugs do to the body

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4
Q

metabolism phase 1 reactions

A

oxidation
reduction
hydrolysis

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5
Q

metabolism phase 2 reactions

A

glucuronide conjugation
methylation
acetylation

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6
Q

metabolic processes affected my gene mutations

A

metabolism
transport
PD

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7
Q

5 functions of P450’s

A
  • metabolize drugs
  • synthesize steroid hormones/bile acid
  • synthesize prostaglandin, thromboxane, leukotriene
  • metabolize fat-soluble vitamins
  • synthesize vitamin D3
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8
Q

where are P450s

A
  • ER of cells
  • mainly in liver
  • gut, lung, skin, kidney
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9
Q

most common P450s

A 
1A2
2C9/2C19
2D6
2E1
3A4
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10
Q

solute carrier transporters typically go which direction

A

extracellular to intra (influx transport)

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11
Q

ATP binding cassette transporters go which direction

A

efflux

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12
Q

example of ATP binding cassette transporter

A

P-glycoprotein

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13
Q

P-glycoprotein drug importance when deficient

A
  • tumor drug resistance

- reduction DOAC effect

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14
Q

power source of P-gp

A

ATP

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15
Q

reversible inhibition

A

temporary association with CYP

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16
Q

irreversible inhibition

A

suicide substrate that covalently binds to enzyme

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17
Q

types of reversible inhibition

A

competitive
noncompetitive
uncompetitive

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18
Q

noncompetitive inhibition

A

binds to a non-active site, making enzyme not function

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19
Q

uncompetitive inhibition

A

binds to enzyme-substrate complex

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20
Q

degree of inhibition depends on

A

affinity to enzyme

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21
Q

strong inhibitor classification

A

> 5 fold increase in plasma AUC or >80% reduction in clearance

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22
Q

moderate inhibitor classification

A

> 2 fold increase in plasma AUC or 50-80% reduction in clearance

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23
Q

weak inhibitor classification

A

> 1.25 and <2 fold increase in plasma AUC or 20-50% reduction in clearance

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24
Q

when does inhibition occur

A
  • within 24 hours
  • can be concentration-dependent
  • clinical effect may take a couple days
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25
Q

inducers function

A

-form more CYP enzymes or transporters via transcription

26
Q

rifampin induces

A 
2C9
2C19
3A4
P-gp
OATP
27
Q

ritonavir induces

A

3A4
P-gp
OATP

28
Q

how long to see induction effects

A

3-5 days

29
Q

things that cause autoinduction

A

carbamazepine
smoke
alcohol

30
Q

strong inducer classification

A

> 80 decrease in AUC

31
Q

moderate inducer classification

A

50-80% decrease in AUC

32
Q

weak inducer classification

A

20-50% decrease in AUC

33
Q

examples of prodrugs

A

cyclophosphamide
codeine
hydrocodone

34
Q

1A2 substrates

A 
caffeine
clozapine
duloxetine
naproxen
theophylline
cyclobenzaprine
35
Q

1A2 inhibitors

A

cimetidine
ciprofloxacin
fluvoxamine
amiodarone

36
Q

1A2 inducers

A

charbroil
tobacco
rifampin

37
Q

2C9 substrates

A 
NSAIDS
fluoxetine
losartan
glipizide
phenytoin
warfarin
38
Q

2C9 inhibitors

A 
amiodarone
fluconazole (Strong)
isoniazide
metronidazole
paroxetine
Sulfamethoxazole
voriconazole
39
Q

2C9 inducers

A

barbiturates
rifampin
SJW

40
Q

2C19 substrates

A 
amitriptyline
cyclophosphamide
clopidogrel
diazepam
lansoprazole
omeprazole
phenytoin
41
Q

2C19 inhibitors

A 
cimetidine
ketoconazole
fluoxetine
fluvoxamine
lansoprazole
omeprazole
42
Q

2C19 inducers

A

efavirenz
rifampin
ritonavir
SJW

43
Q

2D6 substrates

A 
SGA's
codein
duloxetine
metoprolol
paroxetine
tramadol
tamoxifen
44
Q

2D6 inhibitors

A 
bupropion (S)
cimetidine
duloxetine
fluoxetine (S)
paroxetine (S)
quinidine (S)
ritonavir (S)
methadone
45
Q

2D6 inducers

A

none, its resistant

46
Q

2E1 substrates

A

APAP

acute alcohol

47
Q

2E1 inhibitors

A

disulfiram

48
Q

2E1 inducers

A

chronical alcohol

49
Q

3A4 substrates

A 
macrolides
benzos
immune modulators
HIV protease inhibs
CCB
statins
DOACs
methadone
50
Q

3A4 inhibitors

A 
amiodarone
nefazodone (S)
CCBs
grapefruit
ketoconazole (S)
clarithromycin (S)
erythromycin
cimetidine
51
Q

3A4 inducers

A 
carbamazepine
phenobarbital
phenytoin
rifabutin
rifampin
SJW
52
Q

P-gp substrates

A 
apixaban
rivaroxaban
dabigatran
digoxin
losartan
53
Q

P-gp inhibitors

A

amiodarone
diltiazem
carvedilol
verapamil

54
Q

P-gp inducer

A

amiodarone

55
Q

fluoxetine primarily inhibits

A

2C19

2D6

56
Q

fluvoxamine inhibits

A

1A2
2C19
2D6
3A4

57
Q

paroxetine primarily inhibits

A

2D6

3A4

58
Q

citalopram inhibits

A

barely any, very little DDI

59
Q

2 herbal interactions to know about

A

SJW induce 3A4

Dill may inhibit 3A4

60
Q

high risk drug interactions

A
  • narrow therapeutic window drugs
  • no alternate elimination pathways
  • no alternatives
  • dose adjustments not known
61
Q

top 4 drug interactions to be aware of

A
  • sildenafil + isosorbide mononitrate (nitrate)
  • potassium and spironolactone
  • warfarin and basically anything
  • tyrosine kinase inhibs + 3A4 inhib/QT drugs/P-gp inhib/PPIs
62
Q

rate of DDIs increase with

A
  • # of prescribed meds
  • # of OTC meds
  • increased age age

PK/PD (3 decks)

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