Exam 4 - Anti-HIV

Question 1

Anti-HIV

6 classes

Answer 1

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

Question 2

Anti-HIV

DRUG LIST

Answer 2

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

Question 3

Anti-HIV
NRTIs
toxicities

Answer 3

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

Question 4

Anti-HIV
NRTIs
Abacavir
mechanism

Answer 4

-guanosine analog

Question 5

Anti-HIV
NRTIs
Abacavir
administratio

Answer 5

-combo with lamivudine

Question 6

Anti-HIV
NRTIs
Abacavir
toxicities

Answer 6

• MI, hypsersensitivity rxns

- skin rash

Question 7

Anti-HIV
NRTIs
Abacavir
contraindications

Answer 7

• heart dz (extreme caution)

- HL-B*5701 absolute contraindication

Question 8

Anti-HIV
NRTIs
lamivudine/emtricitabine
mechanism

Answer 8

-cytosine analog, inhibits reverse transcriptase

Question 9

Anti-HIV
NRTIs
lamivudine/emtricitabine
administration

Answer 9

-combo with tenofovir (“truvada)

Question 10

Anti-HIV
NtRTIs
tenofovir
mechanism

Answer 10

• adenosine nucleoTide analog pro-drug

- competitively inhibits HIV RT, chain termination

Question 11

Anti-HIV
NtRTIs
tenofovir
administration

Answer 11

-co-adm w/ emtricitabine (truvada)

Question 12

Anti-HIV
NtRTIs
tenofovir
toxicities

Answer 12

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

Question 13

Anti-HIV
NNRTIs
efavirenz
mechanism

Answer 13

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

Question 14

Anti-HIV
NNRTIs
efavirenz
contraindications

Answer 14

-extensive drug-drug; limited use in HAART

Question 15

Anti-HIV
NNRTIs
efavirenz
toxicity

Answer 15

• nightmares! psychiatric distrurbances!

- these sx resolve over time

Question 16

Anti-HIV
PIs
mechanism

Answer 16

• peptidomimetics, inhibits cleavage of Gag/Gag-Pol

- does not require intracellular activation

Question 17

Anti-HIV
PIs
Ritonavir
administration

Answer 17

-PI with “Boosting” potential

co-adm w/ atazanavir or darunavir

Question 18

Anti-HIV
PIs
toxicities

Answer 18

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

Question 19

Anti-HIV
Entry Inhibitors
Maraviroc
mechanism

Answer 19

• inhibits at CCR5

- specific to CCR5 strains

Question 20

Anti-HIV
Entry Inhibitors
Maraviroc
toxicity

Answer 20

hepaptotoxicity; used for resistant HIV-1

Question 21

Anti-HIV
Entry/Fusion Inhibitors
Enfuvirtide
mechanism

Answer 21

• binds G41 subunit of viral envelope, preventing fusion

- no entry pore formed

Question 22

Anti-HIV
Entry/Fusion Inhibitors
enfuvirtide
administration

Answer 22

• subcutaneous

- for tx-experienced Pts w/ ongoing replication

Question 23

Anti-HIV
Integrase Inhibitors
Dolutegravir
Mechanism

Answer 23

-binds integrase, inhibits viral DNA strand

integration into host genome

Question 24

Anti-HIV
Integrase Inhibitors
Dolutegravir
administration

Answer 24

-combo tx for resistant HIV

Question 25

Anti-HIV
Integrase Inhibitors
Dolutegravir
Toxicities

Answer 25

• well tolerated
• hypersens rxns
• elevated liver enzymes

Question 26

Anti-HIV
post-exposure
prophylaxis

Answer 26

Raltegravir + Truvada