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AU14 Drug Mechanisms > Exam 5; Mechanisms > Flashcards

Exam 5; Mechanisms Flashcards

1
Q

penicillin G

A

anti-bacterials - natural penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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2
Q

penicillin V

A

anti-bacterials - natural penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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3
Q

nafcillin

A

anti-bacterials - b-lactamase resistant penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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4
Q

oxacillin

A

anti-bacterials - b-lactamase resistant penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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5
Q

cloxacillin

A

anti-bacterials - b-lactamase resistant penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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6
Q

dicloxacillin

A

anti-bacterials - b-lactamase resistant penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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7
Q

methicillin

A

anti-bacterials - b-lactamase resistant penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase
(no longer in use, too toxic)

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8
Q

amoxicillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase
amino penicillin

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9
Q

ampicillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase
amino penicillin

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10
Q

ticarcillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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11
Q

piperacillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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12
Q

mezlocillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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13
Q

carbenicillin

A

anti-bacterials - broad/extended spectrum penicillins
cell wall inhibitors
b-lactam ring –> inhibit transpeptidase

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14
Q

sulbactam

A

non-antibiotic b-lactam ring containing agents
inhibit penicillinase (a b-lactamase)
(used in combo: broad spectrum + penicillinase inhibitor)

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15
Q

clavulanic acid

A

non-antibiotic b-lactam ring containing agents
inhibit penicillinase (a b-lactamase)
(used in combo: broad spectrum + penicillinase inhibitor)

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16
Q

cephalexin

A

anti-bacterial - cephalosporin (1st gen)

b-lactam ring –> inhibit transpeptiation

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17
Q

cefazolin

A

anti-bacterial - cephalosporin (1st gen)

b-lactam ring –> inhibit transpeptiation

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18
Q

cefaclor

A

anti-bacterial - cephalosporin (2nd gen)

b-lactam ring –> inhibit transpeptiation

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19
Q

cefuroxime

A

anti-bacterial - cephalosporin (2nd gen)

b-lactam ring –> inhibit transpeptiation

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20
Q

cefoxitin

A

anti-bacterial - cephalosporin (2nd gen)

b-lactam ring –> inhibit transpeptiation

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21
Q

cefotetan

A

anti-bacterial - cephalosporin (2nd gen)

b-lactam ring –> inhibit transpeptiation

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22
Q

ceftazidime

A

anti-bacterial - cephalosporin (3rd gen)

b-lactam ring –> inhibit transpeptiation

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23
Q

ceftriaxone

A

anti-bacterial - cephalosporin (3rd gen)

b-lactam ring –> inhibit transpeptiation

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24
Q

cefaperazone

A

anti-bacterial - cephalosporin (3rd gen)

b-lactam ring –> inhibit transpeptiation

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25
Q

cefepime

A

anti-bacterial - cephalosporin (4th gen)

b-lactam ring –> inhibit transpeptiation

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26
Q

ceftaroline

A

anti-bacterial - cephalosporin (5th gen)

b-lactam ring –> inhibit transpeptiation

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27
Q

imipenem

A

anti-bacterial - carbapenems

smaller, penicillinase-resistant b-lactams

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28
Q

meropenem

A

anti-bacterial - carbapenems

smaller, penicillinase-resistant b-lactams

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29
Q

aztreonam

A

anti-bacterial - monobactam

synthetic b-lactam ring –> inhibit transpeptidation

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30
Q

vancomycin

A

anti-bacterial - non b-lactam cell wall inhibitor

binds dialanine residues on subunits of cell wall –> prevents cross-linking

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31
Q

televancin

A

anti-bacterial - non b-lactam cell wall inhibitor

binds dialanine residues and disrupts cell membranes

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32
Q

dalbavancin

A

anti-bacterial - non b-lactam cell wall inhibitor

binds dialanine residues and disrupts cell membranes

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33
Q

bacitracin

A

anti-bacterial - non b-lactam cell wall inhibitor

inhibits recycling of bactoprenol carrier

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34
Q

fosfomycin

A

anti-bacterial - non b-lactam cell wall inhibitor

inhibits synthesis of N-acetylmuramic acid

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35
Q

cycloserine

A

anti-bacterial - non b-lactam cell wall inhibitor

inhibits enzyme for incorporation of alanine into n-acetyl muramic acid

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36
Q

erythromycin

A

anti-bacterial - protein synthesis inhibitor
macrolide
reversibly binds 50S subunit
inhibit translocation of tRNA –> cannot bind P site of ribosome

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37
Q

clarithromycin

A

anti-bacterial - protein synthesis inhibitor
macrolide
reversibly binds 50S subunit
inhibit translocation of tRNA –> cannot bind P site of ribosome

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38
Q

azithromycin

A

anti-bacterial - protein synthesis inhibitor
macrolide
reversibly binds 50S subunit
inhibit translocation of tRNA –> cannot bind P site of ribosome

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39
Q

telithromycin

A

anti-bacterial - protein synthesis inhibitor
macrolide
reversibly binds 50S subunit
inhibit translocation of tRNA –> cannot bind P site of ribosome

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40
Q

streptomycin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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41
Q

gentamycin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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42
Q

tobramycin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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43
Q

neomycin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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44
Q

amikacin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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45
Q

kanamycin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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46
Q

netilmicin

A

anti-bacterial - protein synthesis inhibitor
aminoglycoside
reversibly bind 30S subunit
inhibit tRNA binding along mRNA (including initiation site) –> irreversible mRNA reading

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47
Q

tetracycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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48
Q

doxycycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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49
Q

minocycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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50
Q

tigecycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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51
Q

demeclocycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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52
Q

oxytetracycline

A

anti-bacterial - protein synthesis inhibitor
tetracycline
reversibly bind 30S subunit
inhibits binding of tRNA to “A” site

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53
Q

chloramphenicol

A

anti-bacterial - protein synthesis inhibitor

inhibits peptidyl transferase

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54
Q

clindamycin

A

anti-bacterial - protein synthesis inhibitor
lincosamide
inhibits translocation in ribosome

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55
Q

lincomycin

A

anti-bacterial - protein synthesis inhibitor
lincosamide
inhibits translocation in ribosome

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56
Q

quinupristin + dalfopristin

A

anti-bacterial - protein synthesis inhibitor
streptogramins
Q - inhibits A and P sites
D - inhibits P site

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57
Q

linezolid

A

anti-bacterial - protein synthesis inhibitor
oxazolidinones (linezolid <– tedizolid)
inhibits binding of f-methionyl tRNA to P site
prevents initiation of synthesis process

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58
Q

tedizolid

A

anti-bacterial - protein synthesis inhibitor
oxazolidinones (linezolid <– tedizolid)
inhibits binding of f-methionyl tRNA to P site
prevents initiation of synthesis process

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59
Q

fidaxomycin

A

anti-bacterial - not cell wall or protein synthesis inhibitor
inhibits C. diff RNA polymerase

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60
Q

daptomycin

A

anti-bacterial - not cell wall or protein synthesis inhibitor
bacterial cell wall “membrane disruptor”
forms pores in cell wall

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61
Q

ciprofloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

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62
Q

ofloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

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63
Q

gatifloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

64
Q

moxifloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

65
Q

levofloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

66
Q

gemifloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

67
Q

norfloxacin

A

anti-bacterial - other
fluoroquinolines (nucleic acid inhibitor)
inhibit topoisomerase II and IV

68
Q

sulfisoxazole

A

anti-bacterial - other
sulfonamides (nucleic acid inhibitor)
reversibly inhibit dihydropterate synthase

69
Q

sulfacetamide

A

anti-bacterial - other
sulfonamides (nucleic acid inhibitor)
reversibly inhibit dihydropterate synthase

70
Q

sulfadiazine

A

anti-bacterial - other
sulfonamides (nucleic acid inhibitor)
reversibly inhibit dihydropterate synthase

71
Q

trimethoprim

A

anti-bacterial - other
(nucleic acid inhibitor)
inhibits dihydrofolate reductase
in combo with sulfmethoxazole

72
Q

metronidazole

A

anti-bacterial - other
anaerobic DNA inhibitor (nucleic acid inhibitor)
converted to active molecule, a free radical, by obligate anaerobe bacteria

73
Q

nitrofurantoin

A

anti-bacterial - other
anaerobic DNA inhibitor (nucleic acid inhibitor)
reduced by bacteria to highly reactive molecule

74
Q

polymixin B

A

anti-bacterial - other, topical

binds negatively charged sites on LPS on Gm - –> inc membrane permeability

75
Q

gramicidin

A

anti-bacterial - other, topical
forms pores in bacterial membrane
mixture of three diff peptide antibiotics

76
Q

neomycin

A

anti-bacterial - other, topical

aminoglycoside

77
Q

retapamulin

A

anti-bacterial - other, topical

inhibits peptidyl transferase

78
Q

mupirocin

A

anti-bacterial - other, topical

binds bacterial isoleucyl tRNA synthesis

79
Q

isoniazid

A

anti-bacterial - anti-mycobacterial
prodrug, activated by mycobacterium
produces multiple inhibitors of myco enzymes –> inhibits cell wall synthesis

80
Q

rifampin

A

anti-bacterial - anti-mycobacterial

inhibits DNA-dependent RNA synthase

81
Q

pyrazinamide

A

anti-bacterial - anti-mycobacterial
prodrug, converted in macrophage where TB lives
inhibits fatty acid synthesis by TB

82
Q

ethambutol

A

anti-bacterial - anti-mycobacterial

inhibits arabinosyl transferase enzyme (necessary for cell wall synthesis)

83
Q

bedaquiline

A

anti-bacterial - anti-mycobacterial

inhibits mycobacterial ATP synthetase

84
Q

dapsone

A

anti-bacterial - anti-mycobacterial

inhibits dihydropteroate synthase

85
Q

nystatin

A

anti-fungal - polyene, topical

bind ergosterol in fungal CM –> fungicidal

86
Q

amphotericin B

A

anti-fungal - polyene, topical & DOC for systemic

bind ergosterol in fungal CM –> fungicidal

87
Q

natamycin

A

anti-fungal - polyene, topical

bind ergosterol in fungal CM –> fungicidal

88
Q

tolnaftate

A

anti-fungal - topical for ringworm

89
Q

ciclopirox

A

anti-fungal - topical for ringworm

90
Q

terbinafine

A

anti-fungal - topical for ringworm, systemic for skin, systemic
inhibits squalene epoxidase –> inhibits ergosterol synthesis (squalene accumulates)

91
Q

miconazole

A

anti-fungal - topical for ringworm and candida

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

92
Q

griseofulvin

A

anti-fungal - systemic for skin infection
taken up by mammalian cell –> conc in keratin
bind fungal MT –> inhibit mitosis

93
Q

ketoconazole

A

anti-fungal - systemic

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

94
Q

fluconazole

A

anti-fungal - systemic, a triazole

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

95
Q

itraconazole

A

anti-fungal - systemic, a triazole

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

96
Q

posaconazole

A

anti-fungal - systemic, a triazole

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

97
Q

voriconazole

A

anti-fungal - systemic, a triazole

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) –> inhibit ergosterol synthesis; fungistatic

98
Q

flucytosine → 5-fluorouracil

A

anti-fungal - systemic
converted to 5-fluorouracial in fungus
inhibits thymadylate synthase

99
Q

caspofungin

A

anti-fungal - echinocandin for systemic
inhibit enzyme for fungal CW synthesis
fungicidal

100
Q

micafungin

A

anti-fungal - echinocandin for systemic
inhibit enzyme for fungal CW synthesis
fungicidal

101
Q

anidulafungin

A

anti-fungal - echinocandin for systemic
inhibit enzyme for fungal CW synthesis
fungicidal

102
Q

“conazole”

A

anti-fungal - for ringworm and candida & systemic

inhibit fungal cytochrome P450 (and lanosterol 14-x demethylase) → inhibit ergosterol synthesis; fungistatic

103
Q

acyclovir

A

DNA anti-viral for herpes simplex/zoster
prodrug - phosphorylated by viral kinase
inhibits viral DNA polymerase

104
Q

valacyclovir

A

DNA anti-viral for herpes simplex/zoster
prodrug –> acyclovir
inhibits viral DNA polymerase

105
Q

famciclovir

A

DNA anti-viral for herpes simplex/zoster
prodrug –> acyclovir analog
inhibits viral DNA polymerase

106
Q

ganciclovir

A

DNA anti-viral for CMV
prodrug - activated by viral kinase
inhibits viral DNA polymerase

107
Q

valganciclovir

A

DNA anti-viral for CMV
prodrug - activated by viral kinase –> ganciclovir
inhibits viral DNA polymerase

108
Q

cidofovir

A

DNA anti-viral for CMV
prodrug - activated by host kinase
inhibits viral DNA polymerase

109
Q

foscarnet

A

DNA anti-viral for CMV
not prodrug
directly inhibits viral DNA polymerase

110
Q

adefovir

A

DNA anti-viral for hepatitis B

inhibit Hep B reverse transcriptase

111
Q

telbivudine

A

DNA anti-viral for hepatitis B

inhibit Hep B reverse transcriptase

112
Q

tenofovir

A

DNA anti-viral for hepatitis B

inhibit Hep B reverse transcriptase

113
Q

entecavir

A

DNA anti-viral for hepatitis B

inhibit Hep B reverse transcriptase

114
Q

ribavirin

A

RNA anti-viral for RSV

inhibits RNA-dependent DNA polymerase

115
Q

palivizumab

A

RNA anti-viral for RSV

blocks antigenic site of RSV (blocks fusion of virus with target cell)

116
Q

amantadine

A

RNA anti-viral for Influenza A

blocks H+ channel formation in endosome

117
Q

rimantadine

A

RNA anti-viral for Influenza A

blocks H+ channel formation in endosome

118
Q

zanamivir

A

RNA anti-viral for Influenza A + B

inhibits neuraminidase

119
Q

oseltamivir

A

RNA anti-viral for Influenza A + B

inhibits neuraminidase

120
Q

“cyclovir”

A

DNA anti-viral for herpes or CMV

inhibit viral DNA polymerase

121
Q

“ciclovir”

A

DNA anti-viral for herpes or CMV

inhibit viral DNA polymerase

122
Q

lamivudine

A

DNA anti-viral for hepatitis B

inhibit Hep B reverse transcriptase

123
Q

recombinant interferon alpha

A

RNA anti-viral for hepatitis (esp C)

inhibits mRNA processing by ribosome

124
Q

boceprevir

A

RNA anti-viral for hepatitis (esp C)

inhibits HCV protease

125
Q

telaprevir

A

RNA anti-viral for hepatitis (esp C)

inhibits HCV protease

126
Q

simeprevir

A

RNA anti-viral for hepatitis (esp C)

inhibits HCV protease

127
Q

sofosbuvir

A

RNA anti-viral for hepatitis (esp C)
prodrug
inhibits HCV RNA-dep RNA polymerase
+ ledipasvir = Harvoni

128
Q

ledipasvir

A

RNA anti-viral for hepatitis
+ sofosbuvir = Harvoni
binds and inhibits protein for HCV replication

129
Q

Harvoni

A

RNA anti-viral for hepatitis
ledipasvir + sofosbuvir = Harvoni
binds and inhibits protein for HCV replication

130
Q

didanosine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

131
Q

abacavir

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

132
Q

zidovudine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

133
Q

lamivudine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

134
Q

emtricitabine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

135
Q

stavudine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

136
Q

telbivudine

A

RNA anti-viral for HIV - NRTIs
phosphorylated in cell
competitive inhibitors of nucleosides
inhibit reverse transcriptase and inhibit normal nucleosides

137
Q

tenofovir

A

RNA anti-viral for HIV - NRTIs
already phosphorylated
competitive inhibitors of nucleotides
inhibit reverse transcriptase

138
Q

nevirapine

A

RNA anti-viral for HIV - NNRTI (1st)
non-competitive
inhibits reverse transcriptase

139
Q

delavirdine

A

RNA anti-viral for HIV - NNRTI (1st)
non-competitive
inhibits reverse transcriptase

140
Q

efavirenz

A

RNA anti-viral for HIV - NNRTI (1st)
non-competitive
inhibits reverse transcriptase

141
Q

etravirine

A

RNA anti-viral for HIV - NNRTI (2nd)
non-competitive
inhibits reverse transcriptase

142
Q

rilpivirine

A

RNA anti-viral for HIV - NNRTI (2nd)
non-competitive
inhibits reverse transcriptase

143
Q

saquinavir

A

RNA anti-viral for HIV - protease inhibitor

used in combo with ritonavir

144
Q

ritonavir

A

RNA anti-viral for HIV - protease inhibitor

used in combo with LADS

145
Q

indinavir

A

RNA anti-viral for HIV - protease inhibitor

146
Q

nelfinavir

A

RNA anti-viral for HIV - protease inhibitor

147
Q

atazanavir

A

RNA anti-viral for HIV - protease inhibitor

used in combo with ritonavir

148
Q

darunavir

A

RNA anti-viral for HIV - protease inhibitor

used in combo with ritonavir

149
Q

lopinavir

A

RNA anti-viral for HIV - protease inhibitor

used in combo with ritonavir

150
Q

tipranavir

A

RNA anti-viral for HIV - protease inhibitor

151
Q

fosamprenavir

A

RNA anti-viral for HIV - protease inhibitor

152
Q

enfuvirtide

A

RNA anti-viral for HIV - fusion inhibitor

blocks site on virus that binds target

153
Q

maraviroc

A

RNA anti-viral for HIV - fusion inhibitor

blocks site on host macropahge that binds virus

154
Q

reltegravir

A

RNA anti-viral for HIV - integrase inhibitor

inhibits HIV-1 integrase enzyme

155
Q

dolutegravir

A

RNA anti-viral for HIV - integrase inhibitor

inhibits HIV-1 integrase enzyme

156
Q

elvitegravir

A

RNA anti-viral for HIV - integrase inhibitor

inhibits HIV-1 integrase enzyme

157
Q

“previr”

A

RNA anti-viral for hepatitis virus

inhibit HCV protease

AU14 Drug Mechanisms (7 decks)

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