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

A

abacavir

25
Q

s/s of abacavir hypersentivity

A

fever, rash, GI, respiratory s/s, lethargy, malaise

26
Q

avoid used of abacavir in

A

HLA-B*5701 genotype pts > HSN rxn

27
Q

NNRTI & PI elim

A

hepatic - CYP450

28
Q

major NRTI combo to avoid

A

triple nucleoside analog combinations

29
Q

preferred initial dual-NRTI therapy

A

tenofovir/emtricitabine

30
Q

preferred initial dual NRTI therapy IN PREGNANCY

A

zidovudine/lamivudine

31
Q

dual-NRTI therapies that tx Hep B too

A
  • tenofovir/emtricitabine

- abacavir/lamivudine

32
Q

dual-NRTI therapy that runs risk of ABC HSN

A

abacavir/lamivudine

33
Q

NNRTI to use in preganacy

A

nevirapine

34
Q

NNRTI to use with resistant HIV strains

A

etravirine

35
Q

NNRTI prefered in treatment-experienced HIV pts

A

etravirine

36
Q

MOA: NNRTIs

A

binds and distorts reverse transcriptase enzyme stopping viral DNA assembly > less HIV DNA > doesn’t get integrated into host genome

37
Q

pregnant women taking what drug should continue tx if their HIV viral load is managed?

A

efavirenz

38
Q

hypersensitivity to NNRTIs can cause what? which one is the worst?

A
  • steve-johnson syndrome

- nevirapime

39
Q

NNRTI that induces drug-drug interactions

A

efavirenz

40
Q

signature mutation that confirs resistance to NNRTIs

A

K103N

41
Q

NNRTIthat has activity against HIV strains resistant to other NNRITs

A

etravirine

42
Q

first line initial triple drug therapy NRTIs + NNRTI

A

tenofovir/emticitabine/efavirenz

43
Q

PIs used in drug resistant HIV

A
  • darunavir

- tiranavir

44
Q

AE: indinavir

A

kidney stones

45
Q

MOA: PIs

A

mimics peptide bond btwn pehnylalanine and proline at 167 and 168 to stop translation of functional proteins

46
Q

role of ritonavir use with other PIs

A

“boosts” bioavailability of PI it’s paired with by inhibiting CYP3A4 and prolonging their T1/2

47
Q

AEs: PIs

A
  • sulfonamide HSN
  • hepatotoxicity (acute)
  • lipodistrophy (LT)
48
Q

Preferred dual-NRTI + PI

A

tenofovir/emtricitabine + ataxanavir/ritonavir

49
Q

Alternative dual-NRTI + PI

A

tenofovir/emtricitabine + lopinavir/ritonavir

50
Q

post exposure prophylaxis for HIV should be started within how many days

A

3

51
Q

3 drug PEP recommended in pregnancy

A
  • zidovudine + lamivudine
  • lopinavir + ritonavir
  • 2x/d
52
Q

3 drug PEP recommended w/ chance of liver toxicity

A
  • tnofovir + enmticitabine qd

- lopinavir + ritonavir

53
Q

MOA: raltegravir

A

inhibition of HIV intrgrase > stops integration of HIV DNA into host DNA

54
Q

AEs: raltrgravir

A
  • myopathy
  • rhabdomyolysis
  • skin reactions
55
Q

MOA: maraviroc

A

blocks gp120* binding to CCR5 > prevents gp41 exposure and viral fusion

56
Q

what receptor is maraviroc ineffective against

A

CXCR4

57
Q

MOA: Enfuvirtide

A

blocks gp41 fusion and inhibits HIV entry into host cell