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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
DRB
CDK9 in P-TEFb RNAP Ii elongation inhibited rRNA, processing impaired
26
Flavopiridol
CDK9 in P-TEFb RNAP Ii elongation inhibited rRNA, processing impaired
27
Triptolide
XPB in TFIIH RNAP I and RNAP II initiation inhibited
28
Triptolide
XPB in TFIIH RNAP I and RNAP II initiation inhibited
29
Phase I
Funtionalization Oxidation, Reduction, Hydrolysis CYP 450, FMO
30
Phase II
Conjugation Glucuronidation, Sulfation UGT, ST
31
Purpose of Phase I
Convert parent compound into a more polar compound by adding or uncovering functional groups
32
Functional groups provide sites for what?
Phase II reaction
33
Primary Phase I enzymes
CYP450, FMO (Flavin monooxygenase), MAO (monoamine oxidase), esterases, amidases, hydrolases, reductases, dehydrogenases, oxidases
34
CYP3A4*1 is most common with which race?
caucasian
35
Every organ has the same composition of enzymes
False. They are all different
36
CYP1A2
-has major role in drug metabolism of several clin. important drugs -more active in men than in eoman -Smoking increases CYP1A2 activity
37
CYP1A2 substrate CYP1A2 inducer
caffeine smoking
38
CYP2B6
- 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
CYP2B6 substrates
bupropion efavirenz methadone
40
CYP2C9
-most expressed CYP2C found in human liver -CYP2C9*2 and CYP2C9*3 are the best studied variants
41
CYP2C9 substrates
NSAIDS phenytoin S-warfarin
42
CYP2C9 Phenotypes
2- Normal metabolizer 1.5-1- intermediate metabolizer 0.5-0- poor metabolizer n/a- indeterminate
43
CYP2C9 Phenotypes Activity score 2- Normal metabolizer
An individual is carrying the normal function alleles
44
CYP2C9 Phenotypes Activity Score 1.5-1 - intermediate metabolizer
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
CYP2C9 Phenotypes Activity Score 0.5-0- Poor metabolizer
An individual carrying one no function allele plus one decreased function allele OR two no function alleles
46
CYP2C9 Phenotypes Activity Score n/a- indeterminate
An individual carrying allele combinations with uncertain and/or unknown function alleles
47
CYP2C19
established as containing "one of the most clinically relevant CYP450 polymorphisms"
48
CYP2C19 substrates
clopidogrel PPIs SSRIs voriconazole
49
Loss-of-Function
CYP2C19*2 CYP2C19*3
50
Gain-of-Function
CYP2C19*17
51
CYP2D6
-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
CYP2D6 substrates
antidepressants codeine dextromethorphan ondansetron tamoxifen
53
CYP2D6 Phenotypic Variability
Ultrarapid metabolizer >2.25 Normal metabolizer - between 1.25-2.25 intermediate metabolizer - between 1.25 and 0 Poor metabolizer - 0
54
CYP2D6 inhibitors
bupropion fluoxetine paroxetine quinidine terbinafine
55
Whose CYP2D6 activity is automatically adjusted to 0?
Patients on strong CYP2D6 inhibitors
56
How to calculate patients on weak or moderate CYP2D6 inhibitors?
Patient's activity score is multiplied by 0.5 and that the number used to match score with predicted phenotype
57
CYP3A5
-substrate overlap w/ CYP3A4 -barely expressed in whites -majority expressed in blacks
58
CYP3A substrate
tacrolimus
59
CYP3A4*22
Most common drug metabolizing enzyme
60
Conjugation w/ endogenous substrase...
to increase aqueous solubility to lead to excretion
61
Major Phase II reactions
Glucuronidation Sulfation Acetylation Methylation Amino acid conjugation Glutathione conjugation
62
Primary Phase II enzymes
UGT NAT Sulfotransferase TPMT GST
63
UGT1A1 substrate
bilirubin, irinotecan, atazanavir
64
Crigler-Najjar syndrome (CN) UGT1A1 Genetic Variability
-hyperbilirubinemia -jaundice and organ malfunctions
65
Gilbert's Syndrome (more common) UGT1A1 Genetic Variability
-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
What happens to Clearance, plasma [ ], and drug efficacy if there is a loss-of-function?
clearance: decreases plasma [ ]: will increase active: increase; prodrug: decrease
67
What happens to Clearance, plasma [ ], and drug efficacy if there is a gain-of-function?
clearance: increase plasma [ ]: decrease active: decrease; prodrug: increase

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