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PT3 ID 1 (HIV) > HIV pharmacology/med chem > Flashcards

HIV pharmacology/med chem Flashcards

1
Q

HIV has what kind of nucleic acid structure

A

ssRNS with reverse transcriptase

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2
Q

CD4 role in HIV life cycle

A

CD4 is on surface of T cells/macrophage and the HIV virion attaches to CD4, allowing entrance into the cell

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3
Q

sequence of events in HIV life cycle

A
  1. fusion of HIV to host cell
  2. RNA, RT, integrase, and proteins enter
  3. viral DNA is formed by RT
  4. DNA is integrated with host DNA
  5. new viral RNA is made, and viral proteins come as result
  6. viral RNA and proteins moves to surface
  7. virus is released and protease makes mature proteins
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4
Q

classes of HIV drugs

A
  • NRTIs
  • NNRTIs
  • protease inhibitors
  • integrase inhibitors
  • entry inhibitors
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5
Q

NRTIs MoA

A

replace DNA/RNa components, but lack 3’ OH so they terminate the elongation chain

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6
Q

NRTI resistance

A

associated with mutations in pol gene that encodes for RT

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7
Q

NRTI adverse effects

A

mitochondrial toxicity leading to:

  • neuropathy
  • myopathy
  • hepatic steatosis with lactic acidosis
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8
Q

NRTI drugs

A 
zidovudine*not as important*
lamivudine
abacavir
tenofovir
emtricitabine
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9
Q

zidovudine features

A

very short half life so dosing is 2-6 times per day

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10
Q

lamivudine features

A
  • once daily dosing
  • can reverse zidovudine resistance
  • renal dosing is very important
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11
Q

emtricitabine features

A

more potent than lamivudine with less severe side effects

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12
Q

tenofovir features

A
  • nucleoTIDE analog, not nucleoside
  • prodrug
  • poor outcomes when combined with other drugs
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13
Q

NNRTI MoA

A

inhibit RT allosterically by binding noncompetitively at a distinct site from NRTIs

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14
Q

notable ADME for NNRTI

A

all are metabolized by p450s so they are prone to drug interactions

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15
Q

NNRTI resistance

A

RT mutations

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16
Q

NNRTI side effects

A

severe rash

CNS symptoms

17
Q

NNRTI drugs

A

efavirenz
etravirine
rilpivirine

18
Q

efavirenz features

A

don’t use with GERD drugs

19
Q

etravirine features

A
  • no cross resistance with other NNRTIs

- pregnancy class B

20
Q

rilpivirine features

A

-pregnancy class B

21
Q

protease inhibitors MoA

A

inhibit the protease that matures viral proteins at the end of the life cycle

22
Q

protease inhibitors ADME

A

metabolized by 3A4

23
Q

protease inhibitors adverse effects

A
  • GI intolerance

- lipodystrophy

24
Q

protease inhibitor drugs

A

ritonavir
atazanavir
darunavir

25
Q

ritonavir use

A

because it is the most potent 3A4 inhibitor it is used to keep other drugs going longer, and not so much for its antiviral activity

26
Q

drugs used as 3A4 inhibitors to increase half life of other drugs

A

ritonavir

cobicistat

27
Q

atazanavir features

A

good tolerability with once daily dosing

28
Q

darunavir features

A

1st line option due to its high antiviral activity

29
Q

integrase inhibitors MoA

A

prevents transfer of viral DNA into host DNA (specifically inhibits strand transfer)

30
Q

integrase inhibitor ADME

A

not 3A4 inhibitors

31
Q

integrase inhibitor adverse effects

A 
insomnia
fatigue
headache
altered cholesterol
hypersensitivity reactions
32
Q

integrase inhibitor drugs

A

raltegravir

dolutegravir

33
Q

drug that can cause stevens johnsons

A

raltegravir

34
Q

entry inhibitor MoA

A

prevents viral entry by blocking gp120 attachment to CCR5

35
Q

entry inhibitor drug

A

maraviroc

36
Q

why is combo therapy most effective in HIV

A

HIV has a very high mutation rate

37
Q

what modification is needed to make NRTIs active

A

phosphorylation (3 phosphates needed)

38
Q

when using multiple NRTIs what consideration must be made when choosing

A

the bases they mimic, double dipping doesn’t add any benefit

PT3 ID 1 (HIV) (5 decks)

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