Fitz - Pharm of HIV Inf Flashcards

1
Q

first line Nuceloside Reverse Transcriptase Inhibitors (NRTIs)

A
  • abacavir
  • emtracitabine
  • lamivudine
  • tenofovir
  • zidovudine > azidothymidine
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2
Q

first line non-NRTIs (NNRTIs)

A

efavirenz

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3
Q

what NNRTI do you want to avoid in pregnancy

A

efavirenz

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4
Q

first line HIV Protease Inhibitors (PIs)

A
  • atazanavir

- darunavir

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5
Q

adjunct PI drug always used with first line PIs

A

ritonavir

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6
Q

Integrase Strand Transfer Inhibitors (IIs)

A

raltegravir

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7
Q

CCR5 angtagonist Viral Fusion Inhibitor

A

maraviroc

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8
Q

GP41 antagonist Viral Fusion Inhibitor

A

enfuvirtide

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9
Q

MC initial HIV drug regimens

A

2 NRTIs +

  • NNRTI
  • PT
  • INSTI
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10
Q

NRTIs that penetrate CNS

A
  • zidovudine

- azidothymidine

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11
Q

NNRTI that penetrates CNS

A

nevirapine

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12
Q

MOA: NRTIs

A

modified versions of nucleosides > causes irreversible termination of DNA elongation > inhibits HIV DNA integration into host DNA

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13
Q

Purine NRTIs

A
  • abacavir
  • didanosine
  • tenofovir
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14
Q

Pyrimidine NRTIs

A
  • lamivudine
  • emtricitabine
  • zidovudine
  • stavudine
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15
Q

host enzyme that adds initial phosphate group to NRTIs

A

cytosine kinase

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16
Q

AEs: NRTIs

A
  • lactic acidosis syndrome

- lipoatrophy, lipodystrophy

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17
Q

s/s of lactic acidosis syndrome

A

nausea, vomiting, abd pain, wt loss, fatigue, myalgia, features of hepatic dysfunction

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18
Q

hallmark of NRTI toxicity

A

mitochondrial toxicity

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19
Q

mechanism of mitochodiral toxicity leading to lactic acidosis syndrome

A

mito DNA needed for ox phos proteins > def in proteins = impaired ox phos > anaerobic glucose metabolism > lactic acidosis

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20
Q

“not so bad” NRTIs

A
  • tenofovir
  • lamivudine
  • emtricitabine
  • abacavir
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21
Q

worst NRTIs

A

didanosin > stavudine > zidovudine

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22
Q

AE: tenofovir

A

nephrotoxicity

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23
Q

tenofovir elimnitation

A

glom filtration and active tubular secretion

24
Q

what NRTI should you use in a pt with kidney disease

25
s/s of abacavir hypersentivity
fever, rash, GI, respiratory s/s, lethargy, malaise
26
avoid used of abacavir in
HLA-B*5701 genotype pts > HSN rxn
27
NNRTI & PI elim
hepatic - CYP450
28
major NRTI combo to avoid
triple nucleoside analog combinations
29
preferred initial dual-NRTI therapy
tenofovir/emtricitabine
30
preferred initial dual NRTI therapy IN PREGNANCY
zidovudine/lamivudine
31
dual-NRTI therapies that tx Hep B too
- tenofovir/emtricitabine | - abacavir/lamivudine
32
dual-NRTI therapy that runs risk of ABC HSN
abacavir/lamivudine
33
NNRTI to use in preganacy
nevirapine
34
NNRTI to use with resistant HIV strains
etravirine
35
NNRTI prefered in treatment-experienced HIV pts
etravirine
36
MOA: NNRTIs
binds and distorts reverse transcriptase enzyme stopping viral DNA assembly > less HIV DNA > doesn't get integrated into host genome
37
pregnant women taking what drug should continue tx if their HIV viral load is managed?
efavirenz
38
hypersensitivity to NNRTIs can cause what? which one is the worst?
- steve-johnson syndrome | - nevirapime
39
NNRTI that induces drug-drug interactions
efavirenz
40
signature mutation that confirs resistance to NNRTIs
K103N
41
NNRTIthat has activity against HIV strains resistant to other NNRITs
etravirine
42
first line initial triple drug therapy NRTIs + NNRTI
tenofovir/emticitabine/efavirenz
43
PIs used in drug resistant HIV
- darunavir | - tiranavir
44
AE: indinavir
kidney stones
45
MOA: PIs
mimics peptide bond btwn pehnylalanine and proline at 167 and 168 to stop translation of functional proteins
46
role of ritonavir use with other PIs
"boosts" bioavailability of PI it's paired with by inhibiting CYP3A4 and prolonging their T1/2
47
AEs: PIs
- sulfonamide HSN - hepatotoxicity (acute) - lipodistrophy (LT)
48
Preferred dual-NRTI + PI
tenofovir/emtricitabine + ataxanavir/ritonavir
49
Alternative dual-NRTI + PI
tenofovir/emtricitabine + lopinavir/ritonavir
50
post exposure prophylaxis for HIV should be started within how many days
3
51
3 drug PEP recommended in pregnancy
- zidovudine + lamivudine - lopinavir + ritonavir - 2x/d
52
3 drug PEP recommended w/ chance of liver toxicity
- tnofovir + enmticitabine qd | - lopinavir + ritonavir
53
MOA: raltegravir
inhibition of HIV intrgrase > stops integration of HIV DNA into host DNA
54
AEs: raltrgravir
- myopathy - rhabdomyolysis - skin reactions
55
MOA: maraviroc
blocks gp120* binding to CCR5 > prevents gp41 exposure and viral fusion
56
what receptor is maraviroc ineffective against
CXCR4
57
MOA: Enfuvirtide
blocks gp41 fusion and inhibits HIV entry into host cell