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Pharmacogenetics > Exam 1- lectures 5,6,&7 > Flashcards

Exam 1- lectures 5,6,&7 Flashcards

1
Q

PM

A

poor metabolizers

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2
Q

EM

A

extensive metabolizers

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3
Q

What phase of metabolism are CYP enzymes?

A

Phase I

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4
Q

what phase of metabolism are NAT, UGT & GST?

A

Phase II

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5
Q

CYP450 oxidizes drugs by adding:

A

an -OH group

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6
Q

CYP4 is mainly used for

A

lipid metabolism

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7
Q

CUP1A2

A

caffeine, melatonin, theophylline

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8
Q

CYP2A6

A

Coumarin, Nicotine

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9
Q

CYP2B6

A

buproprion, efavirenz, S-mephenytoin

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10
Q

CYP2C8

A

paclitaxel, pioglittazone

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11
Q

CYP2C19

A

omeprazole, S-mephenytoin

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12
Q

CYP2D6

A

dextromethorphan, debrisoquine, metoprolol

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13
Q

CYP3A

A

midazoleam, cortisol

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14
Q

CYP3A4

A
  • largest form expressed in the liver
  • metabolizes 45-60%
  • NO grapefruit juice
  • 18 variants
  • erythromycin, nifedipine, cyclosporin, midazolam
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15
Q

CYP2C9

A
  • 20% of liver P450
  • warfarin, phenytoin, losartan, fluvastain, NSAIDs
  • 2 major variants
  • mainly caucasians
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16
Q

CYP2C9*2

A

cys 144 instead of Arg 144; fairly small effects

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17
Q

CYP2C9*3

A

leu 359 instead of Ile 359; pronounced reduction in catalytic activity; PM

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18
Q

CYP2C19

A
  • S-mephenytoin
  • 9 variants
  • many drugs are metabolized by other P450
  • Caucasians lowest
  • chinese highest
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19
Q

CYP2D6

A
  • PM autosomal recessive- so need to be homo
  • 4 groups of metabolizers
  • debrisoquine- dextromethorphan, codeine, oxycodone, TCAs, SSRIs, beta blockers
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20
Q

phase I enzymes convert drug to what form?

A

may be active or inactive

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21
Q

phase II enzymes convert drug to what form?

A

usually inactive

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22
Q

phase II drugs

A

improve drugs water solubility & prepare it for elimination

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23
Q

glucuronyl transferase (UGT) MOA

A
  • takes UDP-glucuronic acid & transfers the sugar group to drug
  • conjugates bilirubin
  • imp. for NSAIDs & tylenol & inrinotecan
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24
Q

crigler-najjar disease

A

deficiency of UGTA1 & leads to jaundice

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25
Q

gilbert’s syndrome

A

associated with UGT1A1 deficiency

- compromised bilirubin elimination

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26
Q

UGT1A6 deficiency

A

can lead to acetominophen sensitivity

27
Q

glutathione-S-Transferase (GST)

A
  • conjugates drugs through formation of thioester linkage
  • highly expressed in liver
  • 4 classes: A,M,P,T
28
Q

N-Acetyl Transferase (NAT)

A
  • acetylators
29
Q

where is NAT1 found?

A

in most tissues

30
Q

where is NAT2 found?

A

in liver & gut

significant polymorphisms

31
Q

wild type NAT

A

probably rapid acetylatos

32
Q

isoniazid-phenytoin interaction

A

slow acetylators show higher [] of isoniazid which inhibits hydroxylationof phenytoin, increasing its []->toxicity

33
Q

PM effects

A
  • < first pass metabolism
  • > oral bioavailability
  • < metabolic clearance
  • > half life
  • > drug effects & toxicity
  • < metabolits
  • possible inhibition of metabolism of other drugs
34
Q

ultra-rapid metabolizer effetcs

A
  • > first pass metabolism
  • < oral bioavailibility
  • > metabolic clearance
  • < half life
  • < therapeutic effects
  • > metabolites
35
Q

GPCRs

A

beta adrenergic receptor, serotonin receptor, mu-opiod receptor (beta-blockers, antipsycotics/antidepressants, opioid analgesics)

36
Q

Transporters & ion channels

A

sodium channel, K channel, serotonin transporter (antiarrhythmics, antipsycotics/antidepressents)

37
Q

nuclear hormone receptors

A

estrogen receptor, androgen receptor, glucocorticoid receptor (hormone therapy, glucocorticoids)

38
Q

enzymes

A

angiotensin converting enzyme (ACE),(ACEI)

39
Q

beta-agonist

A

reactive airway disease

40
Q

beta-blockers

A

cardiovascular disease

41
Q

beta 1

A

heart

42
Q

beta 2

A

lungs

43
Q

enhanced receptor down regulation in response to beta2 agonist

A

less efficacy

44
Q

resistant to receptor down regulation

A

better efficacy

45
Q

reduced affinity for some beta2 agonist

A

less binding, less efficacy

46
Q

activatio of 5-LOX receptor produces:

A

leukotrienes

47
Q

decreased expression of ALOX5

A

less responsive to leukotriene inhibitors-> disease not mediated by leukotrienes

48
Q

increased expression of ALOX5

A

more responsive to leukotriene inhibitors->leukotrienes play a major role in disease

49
Q

what is clozapine used to treat and where does it act?

A

acts on 5-HT2A receptors to treat schizophrenia

50
Q

mutation in 5-HT2A receptor

A

his->Tyr

51
Q

side effects of clozapine

A

agranulocytosis, seizures, mycarditis

52
Q

CYP2D6 role in opioids

A

codeine->morphine (active)

53
Q

UGT role in opioids

A

morphine->metabolites

54
Q

QT prolongation risk factors

A

female, concomitant meds, long QT syndrome (LQTS)- mutations in various ion channels

55
Q

LQT1

A

potassium ion

most common

56
Q

LQT2

A

potassium ion
second most common
drug induced

57
Q

LQT3

A

sodium ion

58
Q

LQT5 &6

A

potassium ion

rare

59
Q

LQT1&2 treatment

A

K supplementation & K channel openers

60
Q

LQT3 treatment

A

Na channel openers

61
Q

abacavir genotype

A 
HLA-B*5701 (MCH class I)
can be fatal
62
Q

carbamazepine genotype

A

HLA-B*1502
stevens-johnson syndrome
can be fatal

63
Q

allopurinol genotype

A

HLA-B*5801

Pharmacogenetics (8 decks)

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