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ID Review > Antiretroviral Medications > Flashcards

Antiretroviral Medications Flashcards

1
Q

ART that will exacerbate Hep B if discontinued? [3]

A

TAF, TDF, lamivudine, emtricitabine.

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2
Q

What is 3TC/FTC?

A

Lamivudine, emtricitabine.

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3
Q

FTC side effect?

A

Skin hyperpigmentation

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4
Q

What CD4 and viral load can abacavir be started at?

A

CD4 >200, viral load <100,000

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5
Q

What HLA needs to be tested prior to abacavir use?

A

B*5701

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6
Q

Abacavir has what side effect?

A

MI in cohort studies

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7
Q

ABC?

A

Abacavir

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8
Q

Name the NRTIs [6]

A

Lamivudine, emtricitabine, abacavir, TAF, TDF, zidovudine

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9
Q

Name the 3 NNRTIs

A

Efavirenz, rilpivirine, doravirine

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10
Q

EFV

A

Efavirenz

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11
Q

RPV

A

rilpivirine

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12
Q

DOR

A

doravirine

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13
Q

Efavirenz side effects?

A

Vivid dreams, dizziness, somnolence, insomnia, hallucinations, [50% with CNS toxicity] depression, SI, rash

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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

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15
Q

Rilpivirine side effects?

A

QT prolongation, neuropsychiatric.

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16
Q

Name the 4 INSTIs [integrase strand transfer inhibitors]

A

Raltegravir, Dolutegravir, bictegravir [preferred]. Elvitegravir [alt].

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17
Q

RAL

A

Raltegravir

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18
Q

DTG

A

Dolutegravir

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19
Q

BIC

A

Bictegravir

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20
Q

Raltegravir side effects

A

CPK elevation, weakness, rhabdo

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21
Q

Dolutegravir claim to fame?

A

Higher barrier to resistance than RAL or ETG. If there is preexisting INSTI resistance BID dosing

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22
Q

DTG dosing considerations?

A

Calcium, iron, zinc, antacids reduce DTGs efficacy and caution is needed regarding timing.

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23
Q

DTG pregnancy considerations?

A

Neural tube defects. Ensure adequate birth control.

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24
Q

BIC claim to fame?

A

Does not need boosting, high barrier to resistance with activity to most INSTI-resistant variants

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25
Q

ETG

A

Elvitegravir

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26
Q

Which INSTI needs boosting and with what?

A

ETG [Elvitegravir] with cobicistat

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27
Q

Name the 3 protease inhibitors

A

Ritonavir, darunavir [DRV] [preferred], atazanavir [ATV] [alt]

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28
Q

DRV

A

darunavir

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29
Q

ATV

A

atazanavir

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30
Q

Darunavir side effects

A

Sulfa drug, rash in 10%, erythema multiforme, SJS, TEN

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31
Q

Atazanavir side effects

A

Kidney and gall stones, PR prolongation, indirect hyperbilirubinemia.

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32
Q

Atazanavir dosing considerations

A

Needs acid, do not use with PPI, boosting is preferred. MUST be boosted with TAF

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33
Q

MVC

A

Maraviroc

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34
Q

Maraviroc contraindications?

A

Avoid in dual/mixed CXCR4-tropic HIV-1 infection.

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35
Q

T20?

A

Enfuvirtide

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36
Q

What is Enfuvirtide?

A

Fusion inhibitor, BID injection.

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37
Q

Didanosine SE [DDI] (Not frequently used)

A

Pancreatitis, peripheral neuropathy, lactic acidosis [life threatening]

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38
Q

Stavudine SE [d4T] (Not frequently used)

A

Lipodystrophy, peripheral neuropathy, lactic acidosis, pancreatitis

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39
Q

Zidovudine SE [AZT] (Not frequently used)

A

Anemia, neutropenia, myopathy, lipodystrophy

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40
Q

Etravirine [ETR] SE (Not frequently used)

A

Rash - this can be a life threatening hypersensitivity reacation

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41
Q

Nevirapine [NPV] SE (Not frequently used)

A

Hepatotoxicity

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42
Q

Fosamprenavir [FPV] SE (Not frequently used)

A

SJS

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43
Q

Indinavir [IDV] SE (Not frequently used)

A

Renal stones

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44
Q

Lopinavir [LPV] SE (Not frequently used)

A

Diarrhea

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45
Q

Nelfinavir [NFV] SE (Not frequently used)

A

ONLY UNBOOSTED PI. Hepatoxicity in moderate to severe liver disease

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46
Q

Saquinavir [SQV] SE (Not frequently used)

A

Arrhythmia

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47
Q

Tipranavir [TPV] SE (Not frequently used)

A

ICH, hepatotoxicity

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48
Q

Maraviroc [MVC] SE (Not frequently used)

A

Hepatotoxicity preceded by severe rash or system allergic reaction.

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49
Q

Four empiric regiments for HAART recommended.

A 
INSTI + 2 NRTIs
BIC/TAF/FTC
DTG/ABC/3TC
DTG + TAF/FTC
RAL + TAF/FTC
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50
Q

What is virologic failure?

A

Inability to achieve or maintain HIV RNA <200

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51
Q

Most common type of HIV resistance mutation?

A

NNRTI mutations

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52
Q

Class side effect of NRTI? [4]

A

Lactic acidosis, hepatitis steatosis, lipoatrophy

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53
Q

Class SE of NNRTI? [1]

A

Rash [TEN, SJS]

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54
Q

Class SE of INSTI? [1]

A

Rarely depression or SI

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55
Q

Class SE of PI? [4]

A

Dyslipidemia, hyperglycemia, insulin resistance, lipodystrophy

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56
Q

MOA of NRTI?

A

Structural analogs of normal nucleosides or nucleotides that terminate HIV DNA synthesis by targeting reverse transcriptase

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57
Q

MOA Of NNRTI?

A

Binds noncompetitively to reverse transcriptase and blocks polymerization of the viral DNA

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58
Q

MOA of INSTI?

A

Binds to HIV integrase and blocks the insertion of HIV pro viral DNA into host cells thus inhibiting HIV-catalyzed strand transfer

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59
Q

MOA of PI?

A

Binds to HIV protease preventing the packaging of virions

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60
Q

In general what are the drug classes in an initial regimen for HIV treatment?

A

2 NRTI + INSTI

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61
Q

Name the 4 most common starting regimens for treatment of HIV

A
  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]
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62
Q

When should HIV resistance testing be done?

A

If there is virologic failure while patient is taking failing regimen or within 4 weeks of discontinuing.

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63
Q

If a patient has a suppressed viral load but CD4 count has not recovered what medication change should be made?

A

None.

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64
Q

What is the prevalence of HIV resistance at baseline? What is the most common type of resistance?

A

5-15%

NNRTI resistance

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65
Q

What type of resistance testing should be done on all patients prior to starting ART?

A
  1. Protease Inhibitors

2. Reverse Transcriptase

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66
Q

What is genotypic resistance testing?

A

Looks for viral genetic mutations associated with specific HIV drugs.

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67
Q

What is phenotypic resistance testing?

A

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
Q

What is TAMS?

A

Thymidine analogue mutations

69
Q

What are the type 1 TAMS?

A

M41L, L210W, T215F/Y

70
Q

What are the type 2 TAMS?

A

D67N, K70R, K219Q/E

71
Q

What drugs may lead to TAMS? [2]

A

Zidovudine

Stavudine

72
Q

What is the significance of TAMS?

A

Reduces effectiveness of all NRTIs

73
Q

What mutation does Lamivudine/Emtricitabine select for?

74
Q

In M184V/I what medications is HIV resistant to?

A

abacavir, Lamivudine/Emtricitabine

75
Q

In M184V/I what medications is HIV more susceptible to? [2]

A

tenofovir and zidovudine

76
Q

What medications select for K65R mutation? [4]

A

Tenofovir
Abacavir
Didanosine
Lamivudine [rare]

77
Q

What medications do not work in K65R mutation? [4]

A

Tenofovir
Abacavir
Didanosine
Stavudine

78
Q

What medication works better in K65R mutation

A

Zidovudine

79
Q

What medications select for a T69 insertion? [2]

A

Didanosine

Stavudine

80
Q

What medication do not work in T69 insertion?

A

tenofovir, abacavir, didanosine high-level resistance

lamivudine and emtricitabine work worse.

81
Q

What medication induce Q151M mutation? [2]

A

Didanosine

Zidovudine

82
Q

What resistance does Q151M mutation cause?

A

High-level resistance to abacavir, didanosine, and the thymidine analogs
↓ susceptibility to lamivudine, emtricitabine
Low-level resistance to tenofovir

83
Q

What medications induce L74V mutation? [2]

A

Abacavir

Didanosine

84
Q

What medications do not work as well with an L74V mutation?

A

didanosine

abacavir

85
Q

What medications work better with L74V mutation

A

tenofovir

zidovudine

86
Q

What medications induce K103N mutation? [2]

A

Efavirenz
Nevirapine
–> NNRTIs

87
Q

What medications do not work in K103N mutation? [2]

A

efavirenz and nevirapine

88
Q

What medications induce a Y181C mutation?

A

Nevirapine

89
Q

What medications do not work in Y181C mutation?

A

All NNRTIs, especially Nevirapine

90
Q

What medication induce a E138K mutation?

A

Rilpivirine

–>NNRTIs

91
Q

Combination of E138K with what other mutation can lead to rilpivirine treatment failure?

92
Q

What medications induce a Q148R mutation [2]

A

Raltegravir

Elvitegravir

93
Q

What medications do not work as well with s Q148R mutation? [2]

A

Raltegravir

Elvitegravir

94
Q

What INSTI still works against Q148R mutations

A

dolutegravir BID

95
Q

What medications do not work as well with N155H mutation [2]

A

raltegravir and elvitegravir

96
Q

Combination of Q148R and what other mutation cause resistance to dolutegravir and bictegravir

97
Q

What medication induces I50L mutation?

A

Atazanavir

98
Q

What medication does not work as well with I50L mutation? What medications work better?

A

Atazanavir - not as well

Other PIs work better

99
Q

What HIV drug class should not be used with benzos? Why?

A

PI due to increased benzo concentration

100
Q

What HIV medications decrease bupropion/sertraline concentration?

101
Q

What HIV medications increase bupropion/sertraline concentration?

102
Q

What HIV medications cannot be used with a PPI?

103
Q

Can ATV or RPV be used with H2 blockers

A

Yes, but only if dosing is separated by 10 hours.

104
Q

How does carbamazepine interact with PI?

A

Increases carbamazepine levels

Decreases PI levels

105
Q

How does Phenobarbital interact with PI?

A

Reduces PI levels

106
Q

How does Lamotrigine interact with PI?

A

PIs decrease lamotrigine levels

107
Q

What HIV medications interact with itrazonazole and how?

A

PI and COBI lead to increased itrazonazole levels

108
Q

What HIV medications interact with Posaconazole and how?

A

Posaconazole increase ATV levels

109
Q

What HIV medications interact with Voriconazole and how?

A

Contraindicated with EFV

RTV reduces levels

110
Q

What medications are contraindicated with ritonavir?

A

Fluticasone, budesonide, Mometasone, Triamcinolone

111
Q

NOTE:

A

ritonavir boosted PIs and cobicistat have risk for iatrogenic cushings with inhaled, intranasal AND intraarticular steroids.

112
Q

As a rule what classes of HIV medications do azoles interact with?

A

PIs and NNRTIs

113
Q

Which two HIV medications need an acidic environment for absorption?

114
Q

With what HIV medications is Rifampin/rifapentine contraindicated with? [4]

A

PIs, ETG/COBI containing regimens and MVC

ALL NNRTIs except EFV [and EFV needs close monitoring of RNA levels]

115
Q

Which HIV medications need dose alteration when taken with Rifampin/rifapentine?

A

DTG and RAL

116
Q

What class of HIV medications prompts reduced rifabutin dosing?

117
Q

What class of HIV medications prompts increased rifabutin dosing?

118
Q

What HIV medications are contraindicated with rifabutin?

119
Q

What HIV medication should be avoided with OCP?

120
Q

How do PI effect methadone?

A

Decreases methadone concentration

121
Q

How do polyvalent cations interact with HIV medications

A

INSTIs should be given 2 hours before or 6 hours after polyvalent cations

122
Q

How do PIs effect Phosphodiesterase type 5 inhibitors

A

Increases Phosphodiesterase type 5 inhibitors concentration

123
Q

Describe the drug interaction between TAF and the rifamycin class

A

Rifamycins induce intestinal efflux transporter P-glycoprotein. TAF uses this and is therefore contraindicated when a patient is on a rifamycin.

124
Q

What are the 2 booster medications?

A

Ritonavir

Cobicistat

125
Q

Who should get PrEP?

A

HIV negative patients with..

  1. IVDU
  2. Risky sexual behavior
126
Q

What is the current PrEP regimen?

A

TDF/FTC daily or before and after sexual encounter

127
Q

What infection should be excluded prior to starting PrEP?

128
Q

Who should get PEP?

A
  1. Sexual or needle sharing from known HIV positive source presenting within 72 hours
  2. High risk exposure from HIV unknown person
129
Q

What is the PEP regimen and for how long? [2]

A
  1. TDF/FTC + RAL or DTG
  2. TDF/FTC + DRV/r [alt]

28 days of therapy

130
Q

If a health care professional is exposed to body fluids what baseline testing should they have done? [3]

131
Q

How often should the health care profession be tested for HIV if it is a positive source exposure?

A

6 weeks
12 weeks
16 weeks

132
Q

When should pregnant women have HIV resistance testing performed?

A
  1. Untreated HIV

2. RNA >500

133
Q

What NRTIs are safe in pregnancy? [4]

A

ABC
TDF
3TC
FTC

134
Q

What PIs are safe in pregnancy? [2]

A

ATV/r

DRV/r

135
Q

Which INSTIs are safe in pregnancy?

136
Q

Side effect of DTG in pregnancy?

A

Neural tube defects. Avoid in women in child bearing age. Make sure they are on birth control.

137
Q

What is the role of IV AZT in pregnancy?

A

Administer if HIV RNA is >1000 copies or if RNA is unknown

138
Q

When should an HIV positive woman have a C-section

A

38 weeks if RNA is >1000

139
Q

Which HIV medications are active against HBV? [3]

A

Lamivudine
Emtricitabine
Tenofovir

140
Q

HBV medication entecavir may induce HIV resistance to what medications [2]

141
Q

What medication classes is HIV-2 intrinsically resistant to? [2]

A

NNRTIs

T20 [fusion inhibitor]

142
Q

What is ibalizumab?

A

CD4 post-attachment inhibitor [auto antibody]

143
Q

What 2 medications need a viral load <100,000 and CD4 >200 to start?

A

Abacavir

Rilpivirine

144
Q

Two second line integrase based HIV regimens?

A

Elvitegravir/cobicistat/TAF/FTC

RAL + ABA/3TC

145
Q

Three second line PI based therapy

A

Darunavir/ritonavir + TAF + FTC
Atazanavir/ritonavir + TAF + FTC
Darunavir/ritonavir + ABA/3TC

–> Ritonavir may be subbed for cobicistat

146
Q

Second line NNRTI based HIV therapy?

A

Doravirine/TDF/3TC

Efavirenz/TAF/FTC

147
Q

What are alternative HIV regimens to be considered when ABC, TAF, and TDF cannot be used?

A

Dolutegravir + Lamivudine
Darunavir/ritonavir + Raltegravir
Darunavir/ritonavir + Lamivudine

148
Q

Describe the progression of tenofovir associated fanconi’s syndrome?

A
  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
Q

SE of doravirine?

A

CNS toxicity
Lipid abnormalities
–> Less so than EFV

150
Q

Why is darunavir recommended over atazanavir?

A

Darunavir is active against PI resistant viral strains

151
Q

SE of atazanavir?

A

Elevated indirect bilirubin like Gilbert’s syndrome which may lead to jaundice. NO alk or AST/ALT elevation
Renal stones

152
Q

Which HIV medications will cause creatinine bump due to impaired excretion of creatinine?

A

Bictegravir
Dolutegravir
Cobicistat

153
Q

Which integrase inhibitors have a high barrier to resistance? [2]

A

Bictegravir

Dolutegravir

154
Q

NOTE

A

Most NNRTIs [EFV, ETR, RPV] are P450 induces causing levels of other drugs to fall.
–> DOR is an exception.

155
Q

Medications to NNRTIs will likely effect, causing decreased levels?

A
  1. Rifampin
  2. Ketoconazole/itraconazole
  3. Seizure medications
  4. Benzos
  5. PIs
  6. Maraviroc
156
Q

How do PI’s effect the cytochrome system?

A

They are INHIBITORS
Ritonavir is the most potent inhibitor ever described
This will increase levels of other drugs [Same list as NNRTIs]

157
Q

What entire HIV medication drug class CANNOT be used with rifampin?

158
Q

HIV medications that are teratogens?

A

Dolutegravir –> Neural tube defects

159
Q

Which HIV drug class has been a/w increased cardiac events?

A

PI except atazanavir

160
Q

If you are on a 3 drug regimen and HIV is suppressed what 2 drug regimens may be effective to switch to?

A

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
Q

HIV RNA copies can increase, when does this become concerning?

A

RNA >200.

If <200 - even if it is increased - repeat RNA next visit.

162
Q

What viral load level is concerning for drug resistance?

A

VL persistently >200
VL >500
–> Perform resistance testing
–> Change therapy

163
Q

What is HIV therapy immunologic failure?

A

This is when VL is suppressed but CD4 counts are not increasing.

164
Q

What coinfections may lead to HIV therapy immunologic failure?

A

HCV

HTLV-1

165
Q

Mgmt of immunologic failure?

A

Reassurance

If there is VL suppression ART is working, no need to change treatment.

166
Q

How much HIV copies are needed to undergo genotyping for resistance?

A

> 1000 copies

167
Q

What is the most common mutation in transmitted drug resistance?

A

K103N

NNRTI resistance

ID Review (25 decks)

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