Antiretroviral Medications Flashcards
(167 cards)
1
Q
ART that will exacerbate Hep B if discontinued? [3]
A
TAF, TDF, lamivudine, emtricitabine.
2
Q
What is 3TC/FTC?
A
Lamivudine, emtricitabine.
3
Q
FTC side effect?
A
Skin hyperpigmentation
4
Q
What CD4 and viral load can abacavir be started at?
A
CD4 >200, viral load <100,000
5
Q
What HLA needs to be tested prior to abacavir use?
A
B*5701
6
Q
Abacavir has what side effect?
A
MI in cohort studies
7
Q
ABC?
A
Abacavir
8
Q
Name the NRTIs [6]
A
Lamivudine, emtricitabine, abacavir, TAF, TDF, zidovudine
9
Q
Name the 3 NNRTIs
A
Efavirenz, rilpivirine, doravirine
10
Q
EFV
A
Efavirenz
11
Q
RPV
A
rilpivirine
12
Q
DOR
A
doravirine
13
Q
Efavirenz side effects?
A
Vivid dreams, dizziness, somnolence, insomnia, hallucinations, [50% with CNS toxicity] depression, SI, rash
14
Q
How should rilpivirine be taken?
A
With food [400 cal], needs acid [PPI contraindicated, H2 needs to be 12 hours before or 4 hours after], Needs >200 CD4 and viral load <100,000
15
Q
Rilpivirine side effects?
A
QT prolongation, neuropsychiatric.
16
Q
Name the 4 INSTIs [integrase strand transfer inhibitors]
A
Raltegravir, Dolutegravir, bictegravir [preferred]. Elvitegravir [alt].
17
Q
RAL
A
Raltegravir
18
Q
DTG
A
Dolutegravir
19
Q
BIC
A
Bictegravir
20
Q
Raltegravir side effects
A
CPK elevation, weakness, rhabdo
21
Q
Dolutegravir claim to fame?
A
Higher barrier to resistance than RAL or ETG. If there is preexisting INSTI resistance BID dosing
22
Q
DTG dosing considerations?
A
Calcium, iron, zinc, antacids reduce DTGs efficacy and caution is needed regarding timing.
23
Q
DTG pregnancy considerations?
A
Neural tube defects. Ensure adequate birth control.
24
Q
BIC claim to fame?
A
Does not need boosting, high barrier to resistance with activity to most INSTI-resistant variants
25
ETG
Elvitegravir
26
Which INSTI needs boosting and with what?
ETG [Elvitegravir] with cobicistat
27
Name the 3 protease inhibitors
Ritonavir, darunavir [DRV] [preferred], atazanavir [ATV] [alt]
28
DRV
darunavir
29
ATV
atazanavir
30
Darunavir side effects
Sulfa drug, rash in 10%, erythema multiforme, SJS, TEN
31
Atazanavir side effects
Kidney and gall stones, PR prolongation, indirect hyperbilirubinemia.
32
Atazanavir dosing considerations
Needs acid, do not use with PPI, boosting is preferred. MUST be boosted with TAF
33
MVC
Maraviroc
34
Maraviroc contraindications?
Avoid in dual/mixed CXCR4-tropic HIV-1 infection.
35
T20?
Enfuvirtide
36
What is Enfuvirtide?
Fusion inhibitor, BID injection.
37
Didanosine SE [DDI] (Not frequently used)
Pancreatitis, peripheral neuropathy, lactic acidosis [life threatening]
38
Stavudine SE [d4T] (Not frequently used)
Lipodystrophy, peripheral neuropathy, lactic acidosis, pancreatitis
39
Zidovudine SE [AZT] (Not frequently used)
Anemia, neutropenia, myopathy, lipodystrophy
40
Etravirine [ETR] SE (Not frequently used)
Rash - this can be a life threatening hypersensitivity reacation
41
Nevirapine [NPV] SE (Not frequently used)
Hepatotoxicity
42
Fosamprenavir [FPV] SE (Not frequently used)
SJS
43
Indinavir [IDV] SE (Not frequently used)
Renal stones
44
Lopinavir [LPV] SE (Not frequently used)
Diarrhea
45
Nelfinavir [NFV] SE (Not frequently used)
ONLY UNBOOSTED PI. Hepatoxicity in moderate to severe liver disease
46
Saquinavir [SQV] SE (Not frequently used)
Arrhythmia
47
Tipranavir [TPV] SE (Not frequently used)
ICH, hepatotoxicity
48
Maraviroc [MVC] SE (Not frequently used)
Hepatotoxicity preceded by severe rash or system allergic reaction.
49
Four empiric regiments for HAART recommended.
```
INSTI + 2 NRTIs
BIC/TAF/FTC
DTG/ABC/3TC
DTG + TAF/FTC
RAL + TAF/FTC
```
50
What is virologic failure?
Inability to achieve or maintain HIV RNA <200
51
Most common type of HIV resistance mutation?
NNRTI mutations
52
Class side effect of NRTI? [4]
Lactic acidosis, hepatitis steatosis, lipoatrophy
53
Class SE of NNRTI? [1]
Rash [TEN, SJS]
54
Class SE of INSTI? [1]
Rarely depression or SI
55
Class SE of PI? [4]
Dyslipidemia, hyperglycemia, insulin resistance, lipodystrophy
56
MOA of NRTI?
Structural analogs of normal nucleosides or nucleotides that terminate HIV DNA synthesis by targeting reverse transcriptase
57
MOA Of NNRTI?
Binds noncompetitively to reverse transcriptase and blocks polymerization of the viral DNA
58
MOA of INSTI?
Binds to HIV integrase and blocks the insertion of HIV pro viral DNA into host cells thus inhibiting HIV-catalyzed strand transfer
59
MOA of PI?
Binds to HIV protease preventing the packaging of virions
60
In general what are the drug classes in an initial regimen for HIV treatment?
2 NRTI + INSTI
61
Name the 4 most common starting regimens for treatment of HIV
1. TAF/FTC/BIC [NRTI/NRTI/INSTI]
2. ABC/3TC/DTG [NRTI/NRTI/INSTI]
3. TAF/FTC + DTG [NRTI/NRTI + INSTI]
4. TAF/FTC + RAL [NRTI/NRTI + INSTI]
62
When should HIV resistance testing be done?
If there is virologic failure while patient is taking failing regimen or within 4 weeks of discontinuing.
63
If a patient has a suppressed viral load but CD4 count has not recovered what medication change should be made?
None.
64
What is the prevalence of HIV resistance at baseline? What is the most common type of resistance?
5-15%
| NNRTI resistance
65
What type of resistance testing should be done on all patients prior to starting ART?
1. Protease Inhibitors
| 2. Reverse Transcriptase
66
What is genotypic resistance testing?
Looks for viral genetic mutations associated with specific HIV drugs.
67
What is phenotypic resistance testing?
Measures viral replication in the presence of ART, may be more instructive in heavily treatment-experienced PLWH with multiple resistance mutations on genotypic testing.
68
What is TAMS?
Thymidine analogue mutations
69
What are the type 1 TAMS?
M41L, L210W, T215F/Y
70
What are the type 2 TAMS?
D67N, K70R, K219Q/E
71
What drugs may lead to TAMS? [2]
Zidovudine
| Stavudine
72
What is the significance of TAMS?
Reduces effectiveness of all NRTIs
73
What mutation does Lamivudine/Emtricitabine select for?
M184V/I
74
In M184V/I what medications is HIV resistant to?
abacavir, Lamivudine/Emtricitabine
75
In M184V/I what medications is HIV more susceptible to? [2]
tenofovir and zidovudine
76
What medications select for K65R mutation? [4]
Tenofovir
Abacavir
Didanosine
Lamivudine [rare]
77
What medications do not work in K65R mutation? [4]
Tenofovir
Abacavir
Didanosine
Stavudine
78
What medication works better in K65R mutation
Zidovudine
79
What medications select for a T69 insertion? [2]
Didanosine
| Stavudine
80
What medication do not work in T69 insertion?
tenofovir, abacavir, didanosine high-level resistance
| lamivudine and emtricitabine work worse.
81
What medication induce Q151M mutation? [2]
Didanosine
| Zidovudine
82
What resistance does Q151M mutation cause?
High-level resistance to abacavir, didanosine, and the thymidine analogs
↓ susceptibility to lamivudine, emtricitabine
Low-level resistance to tenofovir
83
What medications induce L74V mutation? [2]
Abacavir
| Didanosine
84
What medications do not work as well with an L74V mutation?
didanosine
| abacavir
85
What medications work better with L74V mutation
tenofovir
| zidovudine
86
What medications induce K103N mutation? [2]
Efavirenz
Nevirapine
--> NNRTIs
87
What medications do not work in K103N mutation? [2]
efavirenz and nevirapine
88
What medications induce a Y181C mutation?
Nevirapine
89
What medications do not work in Y181C mutation?
All NNRTIs, especially Nevirapine
90
What medication induce a E138K mutation?
Rilpivirine
| -->NNRTIs
91
Combination of E138K with what other mutation can lead to rilpivirine treatment failure?
K103N
92
What medications induce a Q148R mutation [2]
Raltegravir
| Elvitegravir
93
What medications do not work as well with s Q148R mutation? [2]
Raltegravir
| Elvitegravir
94
What INSTI still works against Q148R mutations
dolutegravir BID
95
What medications do not work as well with N155H mutation [2]
raltegravir and elvitegravir
96
Combination of Q148R and what other mutation cause resistance to dolutegravir and bictegravir
Q148R
97
What medication induces I50L mutation?
Atazanavir
98
What medication does not work as well with I50L mutation? What medications work better?
Atazanavir - not as well
| Other PIs work better
99
What HIV drug class should not be used with benzos? Why?
PI due to increased benzo concentration
100
What HIV medications decrease bupropion/sertraline concentration?
PI, EFV
101
What HIV medications increase bupropion/sertraline concentration?
COBI
102
What HIV medications cannot be used with a PPI?
ATV, RPV
103
Can ATV or RPV be used with H2 blockers
Yes, but only if dosing is separated by 10 hours.
104
How does carbamazepine interact with PI?
Increases carbamazepine levels
| Decreases PI levels
105
How does Phenobarbital interact with PI?
Reduces PI levels
106
How does Lamotrigine interact with PI?
PIs decrease lamotrigine levels
107
What HIV medications interact with itrazonazole and how?
PI and COBI lead to increased itrazonazole levels
108
What HIV medications interact with Posaconazole and how?
Posaconazole increase ATV levels
109
What HIV medications interact with Voriconazole and how?
Contraindicated with EFV
| RTV reduces levels
110
What medications are contraindicated with ritonavir?
Fluticasone, budesonide, Mometasone, Triamcinolone
111
NOTE:
ritonavir boosted PIs and cobicistat have risk for iatrogenic cushings with inhaled, intranasal AND intraarticular steroids.
112
As a rule what classes of HIV medications do azoles interact with?
PIs and NNRTIs
113
Which two HIV medications need an acidic environment for absorption?
ATV, RPV
114
With what HIV medications is Rifampin/rifapentine contraindicated with? [4]
PIs, ETG/COBI containing regimens and MVC
| ALL NNRTIs except EFV [and EFV needs close monitoring of RNA levels]
115
Which HIV medications need dose alteration when taken with Rifampin/rifapentine?
DTG and RAL
116
What class of HIV medications prompts reduced rifabutin dosing?
PIs
117
What class of HIV medications prompts increased rifabutin dosing?
NNRTIs
118
What HIV medications are contraindicated with rifabutin?
ETG/COBI
119
What HIV medication should be avoided with OCP?
PI
120
How do PI effect methadone?
Decreases methadone concentration
121
How do polyvalent cations interact with HIV medications
INSTIs should be given 2 hours before or 6 hours after polyvalent cations
122
How do PIs effect Phosphodiesterase type 5 inhibitors
Increases Phosphodiesterase type 5 inhibitors concentration
123
Describe the drug interaction between TAF and the rifamycin class
Rifamycins induce intestinal efflux transporter P-glycoprotein. TAF uses this and is therefore contraindicated when a patient is on a rifamycin.
124
What are the 2 booster medications?
Ritonavir
| Cobicistat
125
Who should get PrEP?
HIV negative patients with..
1. IVDU
2. Risky sexual behavior
126
What is the current PrEP regimen?
TDF/FTC daily or before and after sexual encounter
127
What infection should be excluded prior to starting PrEP?
Hep B
128
Who should get PEP?
1. Sexual or needle sharing from known HIV positive source presenting within 72 hours
2. High risk exposure from HIV unknown person
129
What is the PEP regimen and for how long? [2]
1. TDF/FTC + RAL or DTG
2. TDF/FTC + DRV/r [alt]
28 days of therapy
130
If a health care professional is exposed to body fluids what baseline testing should they have done? [3]
HIV
HBV
HCV
131
How often should the health care profession be tested for HIV if it is a positive source exposure?
6 weeks
12 weeks
16 weeks
132
When should pregnant women have HIV resistance testing performed?
1. Untreated HIV
| 2. RNA >500
133
What NRTIs are safe in pregnancy? [4]
ABC
TDF
3TC
FTC
134
What PIs are safe in pregnancy? [2]
ATV/r
| DRV/r
135
Which INSTIs are safe in pregnancy?
RAL
136
Side effect of DTG in pregnancy?
Neural tube defects. Avoid in women in child bearing age. Make sure they are on birth control.
137
What is the role of IV AZT in pregnancy?
Administer if HIV RNA is >1000 copies or if RNA is unknown
138
When should an HIV positive woman have a C-section
38 weeks if RNA is >1000
139
Which HIV medications are active against HBV? [3]
Lamivudine
Emtricitabine
Tenofovir
140
HBV medication entecavir may induce HIV resistance to what medications [2]
3TC
| FTC
141
What medication classes is HIV-2 intrinsically resistant to? [2]
NNRTIs
| T20 [fusion inhibitor]
142
What is ibalizumab?
CD4 post-attachment inhibitor [auto antibody]
143
What 2 medications need a viral load <100,000 and CD4 >200 to start?
Abacavir
| Rilpivirine
144
Two second line integrase based HIV regimens?
Elvitegravir/cobicistat/TAF/FTC
| RAL + ABA/3TC
145
Three second line PI based therapy
Darunavir/ritonavir + TAF + FTC
Atazanavir/ritonavir + TAF + FTC
Darunavir/ritonavir + ABA/3TC
--> Ritonavir may be subbed for cobicistat
146
Second line NNRTI based HIV therapy?
Doravirine/TDF/3TC
| Efavirenz/TAF/FTC
147
What are alternative HIV regimens to be considered when ABC, TAF, and TDF cannot be used?
Dolutegravir + Lamivudine
Darunavir/ritonavir + Raltegravir
Darunavir/ritonavir + Lamivudine
148
Describe the progression of tenofovir associated fanconi's syndrome?
1. Presents with low phos and proteinuria
2. Progresses to glucosuria and renal failure
3. Usually presents >1 year on TAF/TDF
--> Reversible when tenofovir is stopped
149
SE of doravirine?
CNS toxicity
Lipid abnormalities
--> Less so than EFV
150
Why is darunavir recommended over atazanavir?
Darunavir is active against PI resistant viral strains
151
SE of atazanavir?
Elevated indirect bilirubin like Gilbert's syndrome which may lead to jaundice. NO alk or AST/ALT elevation
Renal stones
152
Which HIV medications will cause creatinine bump due to impaired excretion of creatinine?
Bictegravir
Dolutegravir
Cobicistat
153
Which integrase inhibitors have a high barrier to resistance? [2]
Bictegravir
| Dolutegravir
154
NOTE
Most NNRTIs [EFV, ETR, RPV] are P450 induces causing levels of other drugs to fall.
--> DOR is an exception.
155
Medications to NNRTIs will likely effect, causing decreased levels?
1. Rifampin
2. Ketoconazole/itraconazole
3. Seizure medications
4. Benzos
5. PIs
6. Maraviroc
156
How do PI's effect the cytochrome system?
They are INHIBITORS
Ritonavir is the most potent inhibitor ever described
This will increase levels of other drugs [Same list as NNRTIs]
157
What entire HIV medication drug class CANNOT be used with rifampin?
PI
158
HIV medications that are teratogens?
Dolutegravir --> Neural tube defects
159
Which HIV drug class has been a/w increased cardiac events?
PI except atazanavir
160
If you are on a 3 drug regimen and HIV is suppressed what 2 drug regimens may be effective to switch to?
DTG+RPV
Boosted PI [ATV, DRV, LPV] + 3TC or FTC
--> If you DROP one of the meds that is treating HBV infection this will cause flair
161
HIV RNA copies can increase, when does this become concerning?
RNA >200.
| If <200 - even if it is increased - repeat RNA next visit.
162
What viral load level is concerning for drug resistance?
VL persistently >200
VL >500
--> Perform resistance testing
--> Change therapy
163
What is HIV therapy immunologic failure?
This is when VL is suppressed but CD4 counts are not increasing.
164
What coinfections may lead to HIV therapy immunologic failure?
HCV
| HTLV-1
165
Mgmt of immunologic failure?
Reassurance
| If there is VL suppression ART is working, no need to change treatment.
166
How much HIV copies are needed to undergo genotyping for resistance?
>1000 copies
167
What is the most common mutation in transmitted drug resistance?
K103N
| NNRTI resistance
