Antiviral and Antifungal Flashcards
(111 cards)
1
Q
HIV receptor?
A
CD4+
2
Q
HIV co-receptor?
A
CCR5
CXCR4
3
Q
What part of HIV binds to CD4+ receptor?
A
Env gp 120
4
Q
What part of HIV fuses with host membrane?
A
gp 41
5
Q
This anti-HIV drug TARGET that splices polyproteins
A
protease
6
Q
This anti-HIV drug TARGET which acts on host DNA to form proviral DNA
A
reverse transcriptase
RNA-dependent DNA polymerase
7
Q
This entry/fusion inhibitor (anti-HIV) binds to CCR5
A
maraviroc
gp120 cannot bind to CCR5 –> blocks entry
8
Q
This entry/fusion inhibitor (anti-HIV) binds to gp41
A
enfuviritide
blocks fusion of membranes. uses gp41 not gp120 because of gp120’s mutation frequency
9
Q
This entry/fusion inhibitor requires tropism test (HIV tropism = what cell the HIV infects) and Tx-experienced adults.
(Not for CXCR4 tropic or dual/mixed R5X4)
A
maraviroc
Binds to CCR5 not CXCR4
10
Q
This entry/fusion inhibitor acts on T-cell
A
Maraviroc (CCR5)
11
Q
This entry/fusion inhibitor acts on HIV
A
enfuviritide (gp41)
12
Q
Anti-HIV drug TARGET that inserts viral cDNA into host genome.
A
integrase
13
Q
RTI subgroup that:
1) are prodrugs: chain terminators
2) are myelosuppressive
A
NRTIs
14
Q
RTI subgroup that are NOT prodrugs and do not cause myelosuppression
A
NNRTIs
15
Q
Which nucleoside reverse transcriptase inhibitor acts on nucleoTide not nucleoSide
A
tenofovir
16
Q
Non-competitive inhibition of RT by NNRTI is achieved by:
A
binding to HIV-1 RT away from catalytic site
17
Q
These anti-HIV drugs cause lactic acidosis and hepatic steatosis
A
NRTIs
18
Q
NRTI that causes most BM depression
A
zidovudine, ZDV
aka azidothymidine or AZT
19
Q
NRTI that causes peripheral neuropathy and pacreatitis
A
stavudine
didanosine
zalcitabine
20
Q
NRTI that causes headache/nausea/fatigue
A
lamivudine
LEAST TOXIC NRTI
21
Q
NRTI that causes hyperpigmentation
A
emtricitabine
Newer, more active form of lamivudine
22
Q
NRTI that causes rash/HSR (5% patients develop allergy)
A
abacavir
23
Q
NRTI that causes nephropathy
A
tenofovir
24
Q
Which group of anti-HIV drugs require phosphorylation? (thymidine kinsase)
A
NRTIs
25
NNRTIs are metabolized by
CYP450 (CYP3A4 inducer)
26
HIV drug that causes insomnia and nightmares:
efavirenz
27
HIV drug that causes insomnia and depression
rilpivirine
28
NNRTI's that causes rash
nevirapine
delavirine
etravirine
29
Integrase inhibitor:
raltegravir
inhibiting HIV integrase prevents the insertion of HIV DNA into human genome
30
HIV drug that causes toxic epidermal necrolysis
raltegravir
31
-navir drugs =
protease inhibitors
| think NAVIR/never TEASE
32
These HIV drugs block cleavage of polyproteins
protease inhibitors
33
Inhibition of HIV-1 protease results in the production of these particles:
non-infectious virions
34
Least potent protease inhibitor, also least toxic and lowest bioavail
saquinavir
35
Most potent protease inhibitor.
ritonavir
36
Protease inhibitor always formulated in combination with ritonavir
lopinavir
37
Ritonavir inhibits CYP34A metabolism of this protease inhibitor
lopinavir
38
Protease inhibitors that cause sulfa allergy
darunavir
tipranavir
fosamprenavir
DTF
39
Protease inhibitor that has replaced amprenavir
fosamprenavir
40
Protease that causes most drug interactions by acting on CYP450 groups
ritonavir
induce 1A2
inhibit 2D6, 3A4
41
Fixed combo of elvitegravir, cobicistat, tenofovir, emtricitabine:
Stribild
Elvitegravir is ONLY used in this combination.
42
Fixed combination of tenofovir + emtricabone
Truvada
43
Drug group that causes DM Type 2 like syndrome: hyperglycemia, lipodystrophy
Protease inhibitors
44
Fusion inhibitor for HSV-1?
docosanol
45
When to use docosanol?
during PRODROME, before visible lesions
46
DNA Polymerase inhibitor used in HSV and VZV
acyclovir
newer drugs: famciclovir, valaciclovir
47
Prodrug of acyclovir (+valine)
valaciclovir
better bioavailabilty than acyclovir
48
Prodrug of penciclovir
famciclovir
[valaciclovir --> acyclovir
famciclovir --> penciclovir]
49
Ophthalmic herpetic drugs
vidarabine
trifluridine
idoxuridine
50
Drug therapy for herpes labialis
oral acyclobir, famciclovir, valaciclovir
then
decosanol (oral), acyclovir (topical)
51
Drug therapy for disseminated herpes simplex
IV acyclovir
52
Drug therapy for herpes simplex genitalis
Oral therapy not topical
53
Drug therapy for chicken pox
acyclovir, valaciclovir
54
DNA polymerase inhibitors used for CMV infection (CMV retinitis)
ganciclovir
valganciclovir
cidofovir
55
What drug is a prodrug of ganciclovir?
valganciclovir
| better BA
56
DNA polymerase inhibitors REQUIRE vrial kinase phosphorylation except for:
cidofovir - nucleoside DNA PI
foscarnet - non-nucleoside DNA PI
cidofovir requires cellular kinases.
foscarnet does not require phosphorylation.
57
Foscarnet is an analog of
pyrophosphate
NON-NUCLEOSIDE analog DNA polymerase inhibitor --> THEREFORE not an antimetabolite --> does NOT cause BMS!!
58
MoA: inhibit pyrophosphate exchange during DNA replication
foscarnet
59
DNA polymeriase inhibitor used as 2nd line of defense against infections which are resistant to ganciclovir or acyclovir
foscarnet
60
Mechanism of resistance against acyclovir
lack of thymidine kinase
61
Mechanism of resistance against ganciclovir
lack of viral kinase
| mutated CMV DNA polymerase
62
Drug therapy for Influenza A only
amantidine
| rimantidine
63
MoA of anti-influenza A only drugs:
Blocks M2 protein (proton channel) --> blocks influx of protons --> THEREBY blocking uncoating (uncoating occurs AFTER viral ENTRY)
64
Derivative of amantadine with fewer CNS effects and extensive hepatic metabolism
rimantidine
65
Anti-viral used as weak therapy in Parkinson's
amantidine
66
Drug therapy for Influenza A or B
zanamivir
| oseltamivir
67
MoA of anti-influenza A/B:
Inhibits neuraminidase (NA) --> inhibits RELEASE and spread
68
Release inhibitor (influenza A/B) delivered directly via diskhaler
zanamivir
69
Release inhibitor (Influenza A/B) delivered orally
oseltamivir
70
Oseltamivir is activated by what enzymes?
hepatic esterases
71
DNA polymerase inhibitors for Hep B
```
lamivudine (least toxic NRTI for HIV)
entecavir
telbivudin
adefovir
tenofovir (NtRTI for HIV)
```
72
HIV NRTI/NtRTI also used in Hep B?
lamivudine
| tenofovir
73
Hep C drug
ribavirin
74
Quadrivalent HPV vaccine (6, 11, 16, 18)
gardasil
75
Bivalent HPV vaccine (16 and 18)
cervarix
76
This drug is a guanosine analog (antimetabolite) that inhibits IMP dehydrogenase which inhibits GUANINE nucleotide synthesis.
ribavirin
77
Drug therapy for HPV -- antimitotic
podofilox
78
Drug therapy for HPV -- immunomodulation
imiquimod
induces cytokines/chemokines for antiviral effects.
79
Anti-fungals which bind to ERGOSTEROL as their MoA
polyene macrolides (amphotericin B, nystatin)
80
Polyene macrolide for systemic, serious infections
amphotericin B
81
Polyene macrolide used for topical
nystatin
82
Immediate toxic effects of amphotericin B can be countered by using:
paracetamol (fever/chills/headache)
83
Most significant toxicity caused by ampho B
nephrotoxicity
also hematotoxic (anemia) and causes phlebitis
84
Newer preparation of amphotericin B that reduces toxicity
lipid formulation --> promotes slower release of drug
85
Drug therapy for mucocutaneous candidiasis
nystatin
86
Anti-fungal MoA: inhibit ergosterol SYNTHESIS by inhibiting CYP450 enzyme that converts lanosterol to ergosterol (also substrate of human CYP)
Azoles
87
Only imidazole with oral and topical preparation
ketoconazole
88
Azole subgroup with HIGHER selectivity for fungal CYP450
triazole
89
Ketoconazole decreases absorption of these drugs
antacids
H2 blockers
PPIs
anticholinergics
90
Most popular purely topical imidazole
clotrimazole
91
Triazole used for tinea unguium and as an alternative to amphotericin B for aspergillosis
itraconazole
92
Triazole used in cryptococcus meningitis, candidiasis BUT NO activity against aspergillus
fluconazole
93
DOC for invasive aspergillosis
voriconazole
94
Azole with BROADEST spectrum; only azole active against mucormycosis and zygomycosis
posaconazole
95
Azole that can cause changes in vision like blurring or color changes
voriconazole
96
Drug therapy for dermatophytosis AND fungicidal?
allylamine (terbinafine)
fungistatic drug for dermatophytosis = griseofulvin
97
MoA: binds to fungal TUBULIN (antimitotic)
griseofulvin
fungistatic --> does not treat infected structures but protects new structures
98
Antifungal drug that is converted to 5-FU and inhibits fungal thymidylate synthetase
flucytosine
99
MoA of allylamines
inhibits squalene epoxidase --> which inhibits ergosterol synthesis
squalene is toxic to fungus as well
100
Combination therapy in cryptococcal meningitis
Amphotericin B + flucytosine
| also treated with fluconazole
101
Combination therapy in chromoblastomycosis
itraconazole + flucytosine
102
Inhibits SQUALENE epoxidase causing accumulation of squalene
terbinafine
103
Drug used in invasive aspergillosis and approved as empiric therapy during FEBRILE NEUTROPENIA (presumed fungal infections)
caspofungin
104
Echinocandins MoA
inhibit glucan synthase complex resulting in a disruption of fungal cell wall --> cell death
105
Treatment of tinea capitis (mode of delivery)
oral
106
Treatment of tinea barbae
topical - mild
| oral - severe
107
Treatment of tinea corporis
topical - small
| oral - extensive
108
Treatment of tinea manuum
oral or topical
109
Treatment of tinea cruris
oral and topical combination
110
Treatment of tinea pedis
topical
| oral - thickening of soles
111
Treatment of unguium
oral (itraconazole, terbinafine, griseofulvin)
