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Pillars > Exam 1 > Flashcards

Exam 1 Flashcards

1
Q

Antifolates (methotrexate)

A

inhibit both purine and pyrimidine synthesis

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2
Q

Pyrimidine antimetabolite (5-Fluourouracil)

A

pyrimidine synthesis blocker and cell division

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3
Q

6-Mercaptopurine (6-MP)
–Purine antimetabolite–

A

purine synthesis blocker

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4
Q

6-Thioguanine (6-TG)
–Purine antimetabolite–

A

purine synthesis blocker

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5
Q

Hydroxyurea (HU)
–Purine antimetabolite–

A

inhibits purine and pyrimidine

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6
Q

Cytosine Arabinoside (AraC)
-Chain Elongation inhibitor-

A

Dan synthesis termination

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7
Q

Gemcitabine
-Chain Elongation inhibitor-

A

DNA synthesis termination and topoisomerase 1 trapping

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8
Q

Acyclovir (Ac)
–Antiviral–

A

Termination of DNA synthesis

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9
Q

Ganciclovir
–Antiviral–

A

Termination of DNA synthesis

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10
Q

Foscarnet
–Antiviral–

A

Similar to Ganciclovir

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11
Q

Aphidicolin (APH)
-DNA polymerase inhibitors-

A

Eukaryotic DNA polymerase inhibitor

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12
Q

Foscarnet (FOS)
-DNA polymerase inhibitors-

A

Eukaryotic DNA polymerase inhibitor

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13
Q

DNA alkylating agents (Methylmethanesulfonate, Nitrogen mustards)
–DNA damaging drugs–

A

inhibit DNA synthesis

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14
Q

Cisplatin, carboplatin, oxaplatin
–DNA damaging drugs–

A

inhibit DNA synthesis

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15
Q

Camptothecin, Aphidicolin
-DNA Topoisomerase inhibitor-

A

Topoisomerase I inhibitor

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16
Q

Etoposide, doxorubicin, anthracyclines
-DNA Topoisomerase inhibitor-

A

Topoisomerase I inhibitor

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17
Q

Macrolides–>Erythromycin

A

inhibit formation of 50S ribosome blocking tanspeptidation or translocation

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18
Q

Azalides–>
azithromycin
clarithyromycin

A

inhibit formation of 50S ribosome blocking tanspeptidation or translocation

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19
Q

Macrolides and Azalides can…

A

They can interfere with CYP450 enzymes leading to an increase of other drugs, e.g. dilantin, warfarin, cyclosporine

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20
Q

Lincosamide–>Clindamycin

A

similar to macrolides

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21
Q

Streptogramins –> combination drug:
quinupristin and dalfopristin

A

Q-inhibit peptide chain elongation
D-interfered with peptide transferase

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22
Q

Oxazolidinone–>linezolid

A

Binds ribosomal subunit and inhibits formation of initiation complex

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23
Q

Actinomycin D

A

DNA intercalation
RNA polymerase elongation inhibited

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24
Q

alpha-amanitin

A

RNAPII»RNAPIII
RNA synthesis inhibited

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25
Q

DRB

A

CDK9 in P-TEFb
RNAP Ii elongation inhibited rRNA, processing impaired

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26
Q

Flavopiridol

A

CDK9 in P-TEFb
RNAP Ii elongation inhibited rRNA, processing impaired

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27
Q

Triptolide

A

XPB in TFIIH
RNAP I and RNAP II initiation inhibited

28
Q

Triptolide

A

XPB in TFIIH
RNAP I and RNAP II initiation inhibited

29
Q

Phase I

A

Funtionalization
Oxidation, Reduction, Hydrolysis
CYP 450, FMO

30
Q

Phase II

A

Conjugation
Glucuronidation, Sulfation
UGT, ST

31
Q

Purpose of Phase I

A

Convert parent compound into a more polar compound by adding or uncovering functional groups

32
Q

Functional groups provide sites for what?

A

Phase II reaction

33
Q

Primary Phase I enzymes

A

CYP450, FMO (Flavin monooxygenase), MAO (monoamine oxidase), esterases, amidases, hydrolases, reductases, dehydrogenases, oxidases

34
Q

CYP3A4*1 is most common with which race?

A

caucasian

35
Q

Every organ has the same composition of enzymes

A

False. They are all different

36
Q

CYP1A2

A

-has major role in drug metabolism of several clin. important drugs
-more active in men than in eoman
-Smoking increases CYP1A2 activity

37
Q

CYP1A2 substrate
CYP1A2 inducer

A

caffeine
smoking

38
Q

CYP2B6

A
  • represents ~2-5% of hepatic CYP content
  • expressed in the brain which is important in the metabolism of CNS-acting drugs and neurological side-effects of drugs
39
Q

CYP2B6 substrates

A

bupropion
efavirenz
methadone

40
Q

CYP2C9

A

-most expressed CYP2C found in human liver
-CYP2C92 and CYP2C93 are the best studied variants

41
Q

CYP2C9 substrates

A

NSAIDS
phenytoin
S-warfarin

42
Q

CYP2C9 Phenotypes

A

2- Normal metabolizer
1.5-1- intermediate metabolizer
0.5-0- poor metabolizer
n/a- indeterminate

43
Q

CYP2C9 Phenotypes Activity score 2- Normal metabolizer

A

An individual is carrying the normal function alleles

44
Q

CYP2C9 Phenotypes Activity Score 1.5-1 - intermediate metabolizer

A

An individual carrying one normal function allele plus one decreased function allele; OR one normal function allele plus one noe function allele; OR 2 decreased function alleles

45
Q

CYP2C9 Phenotypes Activity Score 0.5-0- Poor metabolizer

A

An individual carrying one no function allele plus one decreased function allele OR two no function alleles

46
Q

CYP2C9 Phenotypes Activity Score n/a- indeterminate

A

An individual carrying allele combinations with uncertain and/or unknown function alleles

47
Q

CYP2C19

A

established as containing “one of the most clinically relevant CYP450 polymorphisms”

48
Q

CYP2C19 substrates

A

clopidogrel
PPIs
SSRIs
voriconazole

49
Q

Loss-of-Function

A

CYP2C192
CYP2C193

50
Q

Gain-of-Function

A

CYP2C19*17

51
Q

CYP2D6

A

-responsible for metabolism of ~15-20% of all clinically used drugs
-greatest impact of genetic polymorphisms among all major metabolizing CYPs
-non-inducible by any drug

52
Q

CYP2D6 substrates

A

antidepressants
codeine
dextromethorphan
ondansetron
tamoxifen

53
Q

CYP2D6 Phenotypic Variability

A

Ultrarapid metabolizer >2.25
Normal metabolizer - between 1.25-2.25
intermediate metabolizer - between 1.25 and 0
Poor metabolizer - 0

54
Q

CYP2D6 inhibitors

A

bupropion
fluoxetine
paroxetine
quinidine
terbinafine

55
Q

Whose CYP2D6 activity is automatically adjusted to 0?

A

Patients on strong CYP2D6 inhibitors

56
Q

How to calculate patients on weak or moderate CYP2D6 inhibitors?

A

Patient’s activity score is multiplied by 0.5 and that the number used to match score with predicted phenotype

57
Q

CYP3A5

A

-substrate overlap w/ CYP3A4
-barely expressed in whites
-majority expressed in blacks

58
Q

CYP3A substrate

A

tacrolimus

59
Q

CYP3A4*22

A

Most common drug metabolizing enzyme

60
Q

Conjugation w/ endogenous substrase…

A

to increase aqueous solubility to lead to excretion

61
Q

Major Phase II reactions

A

Glucuronidation
Sulfation
Acetylation
Methylation
Amino acid conjugation
Glutathione conjugation

62
Q

Primary Phase II enzymes

A

UGT
NAT
Sulfotransferase
TPMT
GST

63
Q

UGT1A1 substrate

A

bilirubin, irinotecan, atazanavir

64
Q

Crigler-Najjar syndrome (CN)
UGT1A1 Genetic Variability

A

-hyperbilirubinemia
-jaundice and organ malfunctions

65
Q

Gilbert’s Syndrome (more common)
UGT1A1 Genetic Variability

A

-caused by promoter or coding region of UGT1A1
-UGT1A1 activity is ~70% normal
-Affects 2-17% of different populations
-increase bilirubin concentration in the body

66
Q

What happens to Clearance, plasma [ ], and drug efficacy if there is a loss-of-function?

A

clearance: decreases
plasma [ ]: will increase
active: increase; prodrug: decrease

67
Q

What happens to Clearance, plasma [ ], and drug efficacy if there is a gain-of-function?

A

clearance: increase
plasma [ ]: decrease
active: decrease; prodrug: increase

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