Exam 4 - Anti-HIV Flashcards

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1
Q

Anti-HIV

6 classes

A
  • nucleoside reverse transcriptase inhibitors (NRTIs)
  • non-NRTIs (NNRTIs)
  • protease inhibitors
  • fusion inhibitors
  • integrase inhibitors
  • CCR5 receptor entry agonists
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2
Q

Anti-HIV

DRUG LIST

A
  • NRTIs: abacavir, lamivudine/emtricitibine
  • NtRTIs: tenofovir
  • NNRTIs: efavirenz
  • HIV protease inhibs: ritonavir, darunavir, atazanavir
  • Fusion/entry/integration inhibs: enfuvirtide, maraviroc, dolutegravir
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3
Q

Anti-HIV
NRTIs
toxicities

A

-mitochondrial toxicity
-hyperlipidemia, insulin resistance, lactic acidosis,
hepatic steatosis

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4
Q

Anti-HIV
NRTIs
Abacavir
mechanism

A

-guanosine analog

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5
Q

Anti-HIV
NRTIs
Abacavir
administratio

A

-combo with lamivudine

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6
Q

Anti-HIV
NRTIs
Abacavir
toxicities

A
  • MI, hypsersensitivity rxns

- skin rash

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7
Q

Anti-HIV
NRTIs
Abacavir
contraindications

A
  • heart dz (extreme caution)

- HL-B*5701 absolute contraindication

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8
Q

Anti-HIV
NRTIs
lamivudine/emtricitabine
mechanism

A

-cytosine analog, inhibits reverse transcriptase

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9
Q

Anti-HIV
NRTIs
lamivudine/emtricitabine
administration

A

-combo with tenofovir (“truvada)

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10
Q

Anti-HIV
NtRTIs
tenofovir
mechanism

A
  • adenosine nucleoTide analog pro-drug

- competitively inhibits HIV RT, chain termination

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11
Q

Anti-HIV
NtRTIs
tenofovir
administration

A

-co-adm w/ emtricitabine (truvada)

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12
Q

Anti-HIV
NtRTIs
tenofovir
toxicities

A
  • the farts
  • muscle weakness, fatigue, renal dysfx’n
  • osteopenia
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13
Q

Anti-HIV
NNRTIs
efavirenz
mechanism

A
  • binds directly to HIV-1 reverse transcriptase
  • inhibits RNA/DNA polymerase activity
  • doesn’t require phosporylation
  • no in vitro HIV2 activity
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14
Q

Anti-HIV
NNRTIs
efavirenz
contraindications

A

-extensive drug-drug; limited use in HAART

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15
Q

Anti-HIV
NNRTIs
efavirenz
toxicity

A
  • nightmares! psychiatric distrurbances!

- these sx resolve over time

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16
Q

Anti-HIV
PIs
mechanism

A
  • peptidomimetics, inhibits cleavage of Gag/Gag-Pol

- does not require intracellular activation

17
Q

Anti-HIV
PIs
Ritonavir
administration

A

-PI with “Boosting” potential

co-adm w/ atazanavir or darunavir

18
Q

Anti-HIV
PIs
toxicities

A
  • Ritonavir: TAG/LDL-emia, paresthesisas, altered tase
  • Atazanavir: bilirubinemia, rash, kidney stones, PR prolong
  • Darunavir: rash, esp with sulfa allergy
19
Q

Anti-HIV
Entry Inhibitors
Maraviroc
mechanism

A
  • inhibits at CCR5

- specific to CCR5 strains

20
Q

Anti-HIV
Entry Inhibitors
Maraviroc
toxicity

A

hepaptotoxicity; used for resistant HIV-1

21
Q

Anti-HIV
Entry/Fusion Inhibitors
Enfuvirtide
mechanism

A
  • binds G41 subunit of viral envelope, preventing fusion

- no entry pore formed

22
Q

Anti-HIV
Entry/Fusion Inhibitors
enfuvirtide
administration

A
  • subcutaneous

- for tx-experienced Pts w/ ongoing replication

23
Q

Anti-HIV
Integrase Inhibitors
Dolutegravir
Mechanism

A

-binds integrase, inhibits viral DNA strand

integration into host genome

24
Q

Anti-HIV
Integrase Inhibitors
Dolutegravir
administration

A

-combo tx for resistant HIV

25
Q

Anti-HIV
Integrase Inhibitors
Dolutegravir
Toxicities

A
  • well tolerated
  • hypersens rxns
  • elevated liver enzymes
26
Q

Anti-HIV
post-exposure
prophylaxis

A

Raltegravir + Truvada