Antivirals Flashcards
(144 cards)
1
Q
zanamivir mechanism
A
inhibits influenza neuraminidase –> prevents release of progeny virus
2
Q
oseltamivir mechanism
A
inhibits influenza neuraminidase –> prevents release of progeny virus
3
Q
clinical use zanamivir
A
influenza A and B
4
Q
clinical use oseltamivir
A
influenza A and B
5
Q
ribavirin mechanism
A
inhibits synthesis of guanine nucleotides by competitively inhibiting inosine monophosphate dehydrogenase
6
Q
clinical use ribavirin
A
RSV, chronic hepatitis C
7
Q
side effects ribavirin
A
- hemolytic anemia
2. severe teratogen
8
Q
acyclovir, famciclovir, and valacyclovir mechanism
A
monophosphorylated by HSV/VZV thymidine kinase (not in uninfected cells –> few adverse effects)
guanosine analog
triphosphate formed by cellular enzymes
preferentially inhibits viral DNA polymerase by chain termination
9
Q
clinical use acyclovir, famciclovir, and valacyclovir
A
HSV and VZV (weak activity against EBV)
no effect on latent forms
10
Q
is acyclovir, famciclovir, valacyclovir useful for CMV?
A
NO!!
11
Q
which -cyclovir has better oral bioavailability
A
valacyclovir
12
Q
treatment of herpes zoster
A
famciclovir
13
Q
side effects acyclovir, famciclovir, and valacyclovir
A
obstructive crystalline nephropathy and acute renal failure
14
Q
how to prevent renal failure from acyclovir, famciclovir, and valacyclovir
A
hydration!
15
Q
mechanism of resistance to acyclovir, famciclovir, and valacyclovir
A
mutated viral thymidine kinase
16
Q
ganciclovir mechanism
A
5’-monophosphate formed by a CMV viral kinase
guanosine analog
triphosphate formed by cellular kinases
perferentially inhibits viral DNA polymerase
17
Q
clinical use ganciclovir
A
CMV (esp. in immunocompromized)
18
Q
what ganciclovir has better oral bioavailability
A
valganciclovir
19
Q
treatment CMV retinitis
A
ganciclovir
20
Q
side effects ganciclovir
A
- leukopenia
- neutropenia
- thrombocytopenia
- renal toxicity
21
Q
mechanism of resistance to ganciclovir
A
mutated CMV DNA polymerase
lack of viral kinase
22
Q
mechanism foscarnet
A
viral DNA polymerase inhibitor –> binds pyrophophate-binding site
does not require activation by viral kinase
23
Q
clinical use foscarnet
A
CMV retinitis in immunocompromised pts when ganciclovir fails
acyclovir-resistant HSV
24
Q
what to do when ganciclovir fails for CMV retinitis??
A
foscarnet!!
25
side effect foscarnet
nephrotoxicity
26
mechanism of resistance to foscarnet
mutated DNA polymerase
27
cidofovir mechanism
preferentially inhibits viral DNA polymerase
| does not require phosphorylation by viral kinase
28
clinical use cidofovir
CMV retinitis in immunocompromised pts
acyclovir-resistant HSV
long half-life
29
side effects cidofovir
nephrotoxicity
30
how do you reduce the nephrotoxicity associated with cidofovir?
coadminister with probenecid and IV saline
31
what is atazanavir?
protease inhibitor
32
what is darunavir?
protease inhibitor
33
what is fosamprenavir?
protease inhibitor
34
what is indinavir?
protease inhibitor
35
what is lopinavir?
protease inhibitor
36
what is ritonavir?
protease inhibitor
37
what is saquinavir?
protease inhibitor
38
what is abacavir?
NRTI
39
what is didanosine?
NRTI
40
what is emtricitabine?
NRTI
41
what is lamivudine?
NRTI
42
what is stavudine?
NRTI
43
what is tonofovir?
NRTI
44
what is zidovudine?
NRTI
45
what is efavirenz?
NNRTI
46
what is nevirapine?
NNRTI
47
what is delaviridine?
NNRTI
48
what is raltegravir?
integrase inhibitor
49
what is enfuvirtide?
fusion inhibitor
50
what is maraviroc?
fusion inhibitor
51
protease inhibitor mechanism
prevent maturation of new viruses (asembly of virions depends on HIV-1 protease [pol gene], which cleaves polypeptide products into functional parts)
52
which protease inhibitor boosts other drug concentrations by inhibiting cytochrome P-450
ritonavir
53
side effects of protease inhibitors (3)
1. hyperglycemia
2. lipodystrophy (fat redistribution)
3. nephropathy
54
which protease inhibitor causes hematuria?
indinavir
55
which HIV drugs cause fat redistribution?
protease inhibitors
56
which HIV drugs cause hyperglycemia?
protease inhibitors
57
mechanism NRTIs
competitively inhibit nucleotide binding to reverse transcriptase and terminate DNA chain (lack a 3' OH group)
58
which NRTI is a nucleotide?
tenofovir (see the T?)
59
which NRTI is used for prophylaxis and for prevention of mother-to-child transmission?
zidovudine
60
side effects NRTIs
1. bone marrow suppression
2. peripheral neuropathy
3. lactic acidosis (nucleoside)
4. rash (non-nucleosides)
61
which NRTI causes anemia
zidovudine
62
which NRTI causes pancreatitis
didanosine
63
which HIV drugs cause bone marrow suppression?
NRTIs
64
mechanism NNRTIs
bind reverse transcriptase (at site different from NRTIs)
| do not require phosphorylation to be active
65
side effects NNRTIs
1. rash
| 2. hepatotoxicity
66
which NNRTI causes CNS symptoms?
efavirenz
67
which NNRTIs are contraindicated in pregnancy?
efavirenz
| delaviridine
68
mechanism integrase inhibitors
inhibits HIV genome integration into host chromosome by reversibly inhibiting HIV integrase
69
side effect integrase inhibitors
hypercholesterolemia
70
which HIV drug causes hypercholesterolemia
integrase inhibitors (raltegravir)
71
mechanism enfuvirtide
binds gp41, inhibiting viral entry
72
mechanism maraviroc
binds CCR-5 on surface of T cells/monocytes --> inhibits interaction with gp120
73
mechanism interferons
these are glycoproteins normally synthesized by virus-infected cells --> antiviral and antitumoral properties
74
clinical use IFN-alpha
(everything else)
1. hepatitis B and C
2. Kaposi sarcoma
3. hairy cell leukemia
4. condyloma acuminatum
5. renal cell carcinoma
6. malignant melanoma
75
clinical use IFN-beta
multiple sclerosis
76
clinical use IFN-gamma
chronic granulomatous disease
77
side effects interferons
1. neutropenia
| 2. myopathy
78
what happens if you use sulfonamides in pregnancy?
kernicterus
79
what happens if you use aminoglycosides in pregnancy?
ototoxicity
80
what happens if you use fluoroquinolones in pregnancy?
cartilage damage
81
what happens if you use clarithromycin in pregnancy?
embryotoxic
82
what happens if you use tetracyclines in pregnancy?
discolored teeth, inhibition of bone growth
83
what happens if you use ribavirin (antiviral) in pregnancy?
teratogenic
84
what happens if you use griseofulvin (antifungal) in pregnancy?
teratogenic
85
what happens if you use chloramphenicol in pregnancy?
gray baby syndrome
86
cidofovir mechanism
preferentially inhibits viral DNA polymerase
| does not require phosphorylation by viral kinase
87
clinical use cidofovir
CMV retinitis in immunocompromised pts
acyclovir-resistant HSV
long half-life
88
side effects cidofovir
nephrotoxicity
89
how do you reduce the nephrotoxicity associated with cidofovir?
coadminister with probenecid and IV saline
90
what is atazanavir?
protease inhibitor
91
what is darunavir?
protease inhibitor
92
what is fosamprenavir?
protease inhibitor
93
what is indinavir?
protease inhibitor
94
what is lopinavir?
protease inhibitor
95
what is ritonavir?
protease inhibitor
96
what is saquinavir?
protease inhibitor
97
what is abacavir?
NRTI
98
what is didanosine?
NRTI
99
what is emtricitabine?
NRTI
100
what is lamivudine?
NRTI
101
what is stavudine?
NRTI
102
what is tonofovir?
NRTI
103
what is zidovudine?
NRTI
104
what is efavirenz?
NNRTI
105
what is nevirapine?
NNRTI
106
what is delaviridine?
NNRTI
107
what is raltegravir?
integrase inhibitor
108
what is enfuvirtide?
fusion inhibitor
109
what is maraviroc?
fusion inhibitor
110
protease inhibitor mechanism
prevent maturation of new viruses (asembly of virions depends on HIV-1 protease [pol gene], which cleaves polypeptide products into functional parts)
111
which protease inhibitor boosts other drug concentrations by inhibiting cytochrome P-450
ritonavir
112
side effects of protease inhibitors (3)
1. hyperglycemia
2. lipodystrophy (fat redistribution)
3. nephropathy
113
which protease inhibitor causes hematuria?
indinavir
114
which HIV drugs cause fat redistribution?
protease inhibitors
115
which HIV drugs cause hyperglycemia?
protease inhibitors
116
mechanism NRTIs
competitively inhibit nucleotide binding to reverse transcriptase and terminate DNA chain (lack a 3' OH group)
117
which NRTI is a nucleotide?
tenofovir (see the T?)
118
which NRTI is used for prophylaxis and for prevention of mother-to-child transmission?
zidovudine
119
side effects NRTIs
1. bone marrow suppression
2. peripheral neuropathy
3. lactic acidosis (nucleoside)
4. rash (non-nucleosides)
120
which NRTI causes anemia
zidovudine
121
which NRTI causes pancreatitis
didanosine
122
which HIV drugs cause bone marrow suppression?
NRTIs
123
mechanism NNRTIs
bind reverse transcriptase (at site different from NRTIs)
| do not require phosphorylation to be active
124
side effects NNRTIs
1. rash
| 2. hepatotoxicity
125
which NNRTI causes CNS symptoms?
efavirenz
126
which NNRTIs are contraindicated in pregnancy?
efavirenz
| delaviridine
127
mechanism integrase inhibitors
inhibits HIV genome integration into host chromosome by reversibly inhibiting HIV integrase
128
side effect integrase inhibitors
hypercholesterolemia
129
which HIV drug causes hypercholesterolemia
integrase inhibitors (raltegravir)
130
mechanism enfuvirtide
binds gp41, inhibiting viral entry
131
mechanism maraviroc
binds CCR-5 on surface of T cells/monocytes --> inhibits interaction with gp120
132
mechanism interferons
these are glycoproteins normally synthesized by virus-infected cells --> antiviral and antitumoral properties
133
clinical use IFN-alpha
(everything else)
1. hepatitis B and C
2. Kaposi sarcoma
3. hairy cell leukemia
4. condyloma acuminatum
5. renal cell carcinoma
6. malignant melanoma
134
clinical use IFN-beta
multiple sclerosis
135
clinical use IFN-gamma
chronic granulomatous disease
136
side effects interferons
1. neutropenia
| 2. myopathy
137
what happens if you use sulfonamides in pregnancy?
kernicterus
138
what happens if you use aminoglycosides in pregnancy?
ototoxicity
139
what happens if you use fluoroquinolones in pregnancy?
cartilage damage
140
what happens if you use clarithromycin in pregnancy?
embryotoxic
141
what happens if you use tetracyclines in pregnancy?
discolored teeth, inhibition of bone growth
142
what happens if you use ribavirin (antiviral) in pregnancy?
teratogenic
143
what happens if you use griseofulvin (antifungal) in pregnancy?
teratogenic
144
what happens if you use chloramphenicol in pregnancy?
gray baby syndrome
