Antivirals/HIV meds Flashcards
1
Q
This antiviral class prevents late protein synthesis and processing…
A
proteasae inhibitors (HIV)
2
Q
These drugs prevent viral packaging, assembly and release from the cell
A
neuraminidase inhibitors (flu)
Prisoners who can’t leave their cell say: “Nerd, im in a daze!”
3
Q
acyclovir, valacyclovir, and docosanol are active against __________
A
HSV/VZV
4
Q
ganciclovir, valganciclovir, foscarnet, and cidofovir are active against both ________ and _________.
A
CMV and Herpes
5
Q
ribavarin is the only drug active against what disease?
A
RSV
6
Q
These three drugs work against influenza
A
oseltamivir, zanamivir, and baloxavir
Sell Tami, and Zane in Biloxi
7
Q
these three drugs are active against HBV
A
tenofovir, entecavir and lamivudine
“TEL hep b to fuck off!”
8
Q
These two drugs are active against HCV
A
sofosbuvir/ledipasvir
sofosbuvir/velpatasvir
9
Q
What is the DOC for VZV?
A
acyclovir/valacyclovir
10
Q
what is the mechanism by which acyclovir/valacyclovir achieves antiviral status?
A
inhibits DNA synthesis by competing with dGTP.
11
Q
what type of analogue is acyclovir?
A
guanosine analogue
12
Q
how does acyclovir receive its first phosphorylation within the cell?
A
using viral thymidine kinase
13
Q
how is resistance to acyclovir achieved?
A
mutation of thiamine kinase preventing first phosphorylation
14
Q
what makes valacyclovir attractive in place of acyclovir?
A
because it is a prodrug which is converted to acyclovir, it has a higher bioavailability
15
Q
what are the adverse effects of acyclovir?
A
nephrotoxicity w/ high IV dose
16
Q
is acyclovir safe for pregnant patients?
A
yes
17
Q
This drug inhibits viral fusion to host cell membrane preventing the virus from entering the cell, and is active against HSV
A
docosanol
18
Q
what is docosanol used for?
A
herpes simplex
19
Q
what are common side effects for docosanol?
A
skin irritation, headache
20
Q
these two drugs are guanosine analogues that are activated by viral kinases within the cell which inhibits DNA polymerase
A
ganciclovir/valganciclovir
21
Q
what are the routes of admin for ganciclovir?
A
ocular implant, oral, IV
22
Q
what are the routes of admin for valganciclovir?
A
PO only
23
Q
_______ treats…
PO tx/prophylaxis of CMV/herpes in immuncompromised patients
Oral, IV, ocular implant for CMV retinitis
IV for life threatening CMV
A
ganciclovir
24
Q
what are the adverse effects of ganciclovir?
A
myelosuppression
CNS: HA, confusion, seizures
25
what is the mechanism by which foscarnet achieves antiviral status?
directly inhibits DNA and RNA polymerase and reverse transcriptase
26
does foscarnet require phosphorylation to be activated?
no
27
what is the DOC for CMV encephalitis?
foscarnet + ganciclovir
28
what is the DOC for ganciclovir resistant CMV retinitis?
foscarnet
29
what is the DOC for acyclovir/ganciclovir resistant HSV?
foscarnet
30
describe the toxicity of foscarnet...
renal toxicity based on creatinine clearance.
hydration reduces toxicity significantly
31
who should be cautioned to use foscarnet?
renal insufficient patients
32
what is the mechanism of action fo cidofovir?
cytosine analogue that inhibits viral DNA polymerase
Cidofovir = cytosine
33
does cidofovir require viral enzymes for phosphorylation?
no, activity can therefore be maintained agasint kinase deficient CMV or HSV
34
This drug is given for:
IV for CMV retinitis in ganciclovir resistant CMV
IV/topical for acyclovir resistant HSV
cidofovir
35
describe the adverse effects of cidofovir
dose dependent nephrotoxicity avoidable by hydration
same SE as acyclovir!
36
what is the mechanism of action for oseltamivir and zanamivir?
both are neuraminidase inhibitors, which block the release of the virus from infected cells
37
what is the therapeutic use of oseltamivir and zanamivir?
used against influenza A and B
38
which anti-flu has been approved for bird flu?
oseltamavir
39
what is the route of admin for zanamavir?
nasal or oral inhaler approved for pts > 7 yo
40
This drug may worsen respiratory fxn in COPD, worsen bronchospasm in asthma.
Not recommended for those w/ airway disease.
zanamivir (inhaler, nasal spray)
41
oseltamivir has what adverse effects?
NV, better if taken w/ food
42
This antiviral prevents viral gene transcription by inhibiting endonuclease activity
baloxavir/marboxil
43
what is baloxavir marboxil approved for,
approved for influenza A and B
44
what are the adverse effects of baloxavir marboxil?
diarrhea, nausea and headache
45
This drug is a guanosine analogue that is phosphorylated by host enzymes to inhibit RNA polymerase, and is active against RSV
ribavirin
46
what is the primary use of ribavirin?
as an aerosol against RSV and in HCV PO combined w/ interferon
47
When this drug is given PO dose dependent hemolytic anemia can occur
ribavirin
48
When delivered as an aerosol, respiratory depression, cardiac arrest, hypotension can occur?
ribavirin
49
what are the adverse effects when ribavirin is given IV?
psychiatric sxs
50
describe the severity of ribavirin's teratogenic effects...
must not conceive a child for at least 6 months after exposure to the drug.
occupational exposure is problematic as a result
51
This drug is an adenosine analogue that inhibits HBV DNA polymerase
tenofovir
52
This HBV drug is a guanosine analogue that inhibits HBV DNA polymerase
entecavir
53
what is the DOC for HBV?
tenofovir
54
what is a rare adverse effect of entecavir?
hepatic encephalopathy
55
what is the mechanism of action of lamivudine?
cytosine analogue that inhibits HBV DNA polymerase
56
what is a rare side effect for lamivudine?
pancreatitis
57
after more than 5 years of treatment with lamivudine, what can be expected?
resistance
58
This drug is uridine analogue that inhibits viral NS5B RNA polymerase, causes termination of DNA
sofobuvir
59
This drug inhibits HCV NS5A protein to prevent phosphorylation and replication
ledipasvir/velpatasvir
60
what is the DOC for HCV?
sofosbuvir/ledipasvir
or
sofosbuvir/velpatasvir
61
what 2 NRTIs are DOC for HAART therapy in HIV?
emtricitabine and tenofovir
62
What is a second acceptable NRTI duo to consider for the triple cocktail of HIV therapy?
lamivudine and abacavir
63
what 5 drugs are considered nucleoside reverse transcriptase inhibitors?
zidovudine, emtricitabine, tenofovir, lamivudine, abacavir
64
This class of drugs are nucleoside analogue requiring 3x phosphorylation to be incorporated into viral DNA to inhibit viral reverse transcriptase
NRTIs
65
Which NRTIs are safe to use in pregnancy?
zidovudine, lamivudine
66
which NRTI has good CNS penetration and can be useful for AIDS dementia?
zidovudine
67
what is zidovudine commonly combined with?
lamivudine (prevent resistance)
68
The major side effects of ______ include:
Initial: CNS- HA, NV, insomnia, myalgia
later: lactic acidosis, hepatotoxicity, myelosuppression
zidovudine
69
This drug has the following precautions:
caution when using other drugs that cause myelosuppression like ganciclovir or ribavirin.
zidovudine
consider adding epogen or neupogen
70
These two drugs treat HIV via inhibition of reverse transcriptaase?
tenofovir and emtricitabine
71
what are two drugs of first choice when treating HIV?
tenofovir and emtricitabine in combo
72
what is the mechanism of action for lamivudine in HIV and HBV
HIV inhibits reverse transcriptase, HBV inhibits polymerase
73
describe the toxicity of lamivudine
very low toxicity
74
is lamivudine safe in preganncy?
yes
75
what drugs are frequently combined with abacavir?
lamivudine or zidovudine
76
This drug has the following serious toxicities.
serious hypersensitivity, SJS.
screen for HLA-B-5701
abacavir
"lose your BACK w/ abacavir. HLA B testing needed"
77
what can happen if you discontinue abacavir therapy due to hypersensitivity and then restart the drug?
fatal consequences
78
what are the two major, serious side effects of all NRTIs?
lactic acidosis and hepatotoxicity
79
what is the mechanism of action for the NNRTIs?
bind directly to inhibit viral reverse transcriptase
80
what are the 2 NNRTIs?
efavirenz and rilpivirine
81
which of the NNRTIs is DOC for initial therapy?
efavirenz
82
what should you combine efavirenz with?
nucleoside analogues
83
what are two major cautions of efavirenz use?
CYP3A4 inducer which reduces effectiveness of OC
and
teratogenic
84
which NNRTI do you use in pregnant patients?
rilpivirine
85
This drug is not recommended for HIV pts w/ hepatitis because it can increase liver enzymes...
rilpivirine
86
what is the common suffix of protease inhibitors and what is the one exception?
avir suffix, abacavir is the exception as an NRTI
87
These drugs bind to proteases to inhibit function. prevents maturation of viral particles
protease inhibitors
88
protease inhibitors must be combined with what class of HIV antiretroviral in order to prevent mutations/resistance?
NRTIs
89
what metabolizes protease inhibitors?
CYP3A4
90
due to the metabolism by CYP3A4, protease inhibitors are often combined with what drug to decrease PI metabolism?
combined with ritonavir which is a potent inhibitor of 3A4
91
what drugs will decrease PI levels?
3A4 inducers like rifampin, rifabutin, st. john's wort
92
what are the common adverse effects of protease inhibitors?
altered body fat distribution, insulin resistance, increased cholesterol, spontaneous bleeding w hemophilia
93
ritonavir is used for what purpose?
inhibits CYP3A4 to increase bioavailability of protease inhibitors
94
what drugs should not be combined with ritonavir?
saquinavir, metronidazole, cephalosporins, or isoniazid
95
what shouldn't ritonavir be given with saquinavir?
QT
96
why shouldn't ritonavir be combined with metronidazole or cephalosporins?
disulfiram like reaction
97
which protease inhibitor is DOC?
darunavir
98
Which two PIs contain sulfa and should be avoided in sulfa allergy?
darunavir, tipranavir
99
which protease inhibitor is drug of second choice?
atazenavir
100
what advantage does atazenavir have with respect to the adverse effects of other protease inhibitors?
less effect on body fat distribution
101
This PI causes nephrolithiasis and hyperbilirubinemia mitigated by hydration
indinavir
102
why can't you combine saquinavir with ritonavir?
QT prolongation
103
what is unique about tipranavir?
it is a non-peptide PI
104
This drug should be considered for treatment experienced HIV patients who have PI resistant strains
tipranavir
105
what combination of tipranavir should be avoided for patients with head trauma?
tipranovir and ritonavir increases risk of intracranial hemorrhage
106
This drug can cause liver toxicity, especially in HBV, HCV coinfection
tipranavir
107
This drug binds to gp41 of the viral envelope, preventing fusion to the target cell
enfuvirtide
108
The only parenteral antiretroviral
enfuvirtide
109
what infection has an increased risk when taking enfuvirtide?
bacterial pneumonia
110
This drug prevents viral fusion by binding to CCR5 receptor in CD4 T-Cells
maraviroc
111
This drug can only be used for CCR5-trophic HIV for whom no other treatment has been effective
maraviroc
112
What must be performed prior to administration of maraviroc?
testing to ensure CCR5-trophic infection. will not work on CXCR4 or mixed tropism
113
This drug is an integrase inhibitor that blocks the integrase enzyme needed for viral replication
dolutegravir
"dolute the integrase!"
114
when should you consider dolutegravir?
tx resistant patients where other drugs aren't working
