drugs Flashcards

1
Q

fluoroquinolone target

A

termination of bacterial DNA replication

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2
Q

fluoroquinolone MOA

A

inhibits gyrase and topo IV so it inhibits both gram pos/neg bacteria

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3
Q

topoisomerase poisons target

A

Eukaryote DNA

replication

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4
Q

topoisomerase poisons MOA

A

Trap topo:DNA
complex -> cause single
and double-strand DNA breaks
topo trap

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5
Q

topoisomerase uses

A

cancer therapy

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6
Q

Alkylating agents target

A

Modification of DNA

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7
Q

Alkylating agents MOA

A

Interstrand cross-link to DNA

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8
Q

Crosslinking agents target

A

Modification of DNA

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9
Q

Crosslinking agents MOA

A

Intrastrand cross-link DNA

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10
Q

Rifampicin target

A

prokaryotic RNAP

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11
Q

Rifampicin MOA

A

binds to beta subunit>prevent movement of sigma factor>RNAP cannot interact w/promoter>prevent transcription at early stage

prevent interaction with beta sigma fam

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12
Q

alpha-amantitin target

A

eukaryotic RNAP 2

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13
Q

alpha-amantitin MOA

A

inhibit RNAP>inhibit elongation phase of transcription

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14
Q

Rifampicin uses

A

tuberculosis

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15
Q

Rifampicin resistance

A

2 ways:

1) bacteria acquires mutations at particular positions around the binding site
2) expressing Arr: ADP-ribosylates Rifampicin

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16
Q

RNAi therapy target

A

deleterious genes (mRNA)

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17
Q

RNAi therapy MOA

A

forms RISC, binds miRNA and mediates formation of duplex btwn guide strand and mRNA, prevents translation by stim degradation of polyA tail

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18
Q

RNAi therapy uses

A

treatment of hereditary transthyretin-mediated amyloidosis

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19
Q

Tetracycline MOA

A

delivery of activated tRNA to A site by elongation factor EF-Tu inhibited

cycling=delivery

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20
Q

streptomycin MOA

A

inhibits GTP-powered proofreading by EF-Tu

“streps” away ability to read

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21
Q

chloramphenicol MOA

A

blocks A-site and peptidyl transfer

“ram” into A site

22
Q

erythromycin MOA

A

bind just outside the P-site, inhibit translocation

erythro=red
blush at “P” site

23
Q

puromycin MOA

A

binds to A site (mimics 3’ end of aa-tRNA)> prevents subsequent peptidyl transfer> triggers premature termination

“pur”= mimicking cat

24
Q

SW02

A

allosteric agonist of Hsp70,
enhancing its ability to inhibit protein aggregation

“SWeet you’re gonna help me”

25
Q

Gusperimus

A

Hsp70 inhibitor approved as an immunosuppressant in Europe and Japan

“Gusto”= large, covers both countries

26
Q

Tanespimycin

A

Hsp90 inhibitors, developed as anti-cancer drugs

“Tanes”=tails, nine(90) tales

27
Q

bortezomib MOA

A

inhibit proteasome

a(bort) proteasome

28
Q

bortezomib use

A

treatment of relapsed multiple myeloma

29
Q

Tafamidis MOA

A

binding to Transthyretin (TTR)’s tetramer> stabilized, potentially inhibit aggregation, arrest disease progression

prevents fam from breaking up

30
Q

Tafamidis use

A

Transthyretin (TTR) aggregation treatment

31
Q

Ivacaftor MOA

A

treats missense mutations, binding to misfolded CFTR, forces it into native state

“caft”= crafty

32
Q

Ivacaftor use

A

Cystic Fibrosis

33
Q

tunicamycin

A

blocks N-linked glycosylation, inhibits 1st sugar being added

tuna sugar

34
Q

bactitracin MOA

A

inhibits phosphorylation of Dol-PP to Dol-P

bacteria in your Dole whip

35
Q

b-lactams MOA

A

inhibit transpeptidase (breask cross linking peptidoglycan chains)

milk melting cell wall

36
Q

DGAT-1 inhibitors MOA

A

inhibits DAG
2 fncs: last step in esterification of TAGs
serves as precursor for phospholipid synthesis

37
Q

DGAT-1 inhibitors use

A

obesity/metabolic syndrome

38
Q

statins MOA

A

targets HMG-CoA reductase

HMG-CoA>Mevalonate»squalene»cholesterol/isoprenoids eg dolichol

39
Q

CYP19A1 (aromatase) inhibitors MOA

A

blocks conversion of testosterone (androgens) >aromatase>estrogen
eg letrozole
“-zole” usually CYP inhibitor

40
Q

CYP19A1 (aromatase) inhibitors use

A

hormone-receptor-positive breast cancer

41
Q

tetrodotoxin MOA

A

fugu toxin, inhibits voltage gated NA channels

42
Q

Ca channel blockers MOA

A

inhibit VDCCs in heart muscle>decr influx of Ca2+ into cardiac/smooth muscle> decr cardiac contractibility and causes vasodilation> lowers bp

eg amlodipine

“am low in Ca”>hurts heart

43
Q

Ca channel blockers use

A

hypertension

44
Q

diazepam/zolpidem MOA

A

enhance GABA receptor activity, allosterically

45
Q

nAChR inhibitors/antagonists

A

Non-depolarizing neuromuscular junction agents bind to the nAChR and competitively inhibit ACh binding
eg d-turbocurarine, atracurium
“cur” Ach

46
Q

P-gp (P-glycoprotein) inhibitor

A

P-gp pumps xenobiotic compounds out of cytoplasm, ATP dep
eg quinidine
P=Potter and quidditch

47
Q

cardiac glycosides

A

incr intensity of heart muscle contraction
eg digoxin
digging (digo) makes dogs heart race

48
Q

mAbs (monoclonal antibodies)

A

EGFR-targeting

egcetuximab, erlotinib

49
Q

cetuximab MOA

A

inhibit EGF binding

50
Q

erlotinib MOA

A

inhibit autophosphorylation and downstream signaling

51
Q

bevacizumab/ranibizumab MOA

A

bind to VEGF, prevent recognition by VEGFR

52
Q

GPCR targeted by

A

loratadine, ranitidine, perphenazine