Antiretrovirals

Question 1

Abacavir

Answer 1

NRTI

MOA: They need to be phosphorylated into a triphosphate form by cellular enzymes before they are active. The triphosphate forms of the nucleoside/nucleotide inhibitors competitively inhibit the reverse transcriptase enzyme and cause premature chain termination when incorporated into the growing DNA strand.

Oral

Allergic Rxn: HLA-B5701 (do genetic testing)

Question 2

Lamivudine

Answer 2

NRTI

MOA: They need to be phosphorylated into a triphosphate form by cellular enzymes before they are active. The triphosphate forms of the nucleoside/nucleotide inhibitors competitively inhibit the reverse transcriptase enzyme and cause premature chain termination when incorporated into the growing DNA strand.

Oral

Question 3

Emtricitabine

Answer 3

NRTI

Fluorinated analogue of lamivudine

MOA: They need to be phosphorylated into a triphosphate form by cellular enzymes before they are active. The triphosphate forms of the nucleoside/nucleotide inhibitors competitively inhibit the reverse transcriptase enzyme and cause premature chain termination when incorporated into the growing DNA strand.

Oral

Question 4

Tenofovir

Answer 4

NRTI

MOA: They need to be phosphorylated into a triphosphate form by cellular enzymes before they are active. The triphosphate forms of the nucleoside/nucleotide inhibitors competitively inhibit the reverse transcriptase enzyme and cause premature chain termination when incorporated into the growing DNA strand.

Use prodrug

Question 5

Zidovudine

Answer 5

NRTI

MOA: They need to be phosphorylated into a triphosphate form by cellular enzymes before they are active. The triphosphate forms of the nucleoside/nucleotide inhibitors competitively inhibit the reverse transcriptase enzyme and cause premature chain termination when incorporated into the growing DNA strand.

Oral

Question 6

Efavirenz

Answer 6

NNRTI

MOA: binds to reverse transcriptase at site distinct from active site (only active against HIV1)

Question 7

Nevirapine

Answer 7

NNRTI

MOA: binds to reverse transcriptase at site distinct from active site (only active against HIV1)

Question 8

Atazanavir

Answer 8

Protease Inhibitor

MOA: mimics peptide target for protease -> blocks maturation of virion particles after budding

Inhibitor of CYP

Question 9

Ritonavir

Answer 9

Protease Inhibitor
MOA: mimics peptide target for protease -> blocks maturation of virion particles after budding

potent inhibitor of CYP3A4 cytochrome P450 enzyme

Question 10

Darunavir

Answer 10

Protease Inhibitor

MOA: mimics peptide target for protease -> blocks maturation of virion particles after budding

Question 11

Maraviroc

Answer 11

CCR5 Receptor Antagonist

MOA: Binds to the cellular CCR5 protein and prevents its interaction
with HIV gp120 envelop protein

Rx: Pts w/ CCR5 tropic virus

Resistance: tropism change (CCR4) / mutation in gp120

Question 12

Enfuvirtide

Answer 12

Fusion Inhibitor

MOA: Binds to the HIV gp41 fusion protein and prevents fusion w/ membrane

• Only delivered parenterally*
• Reserved for patients who have failed otehr antiretroviral Tx*

Question 13

Raltegravir

Answer 13

Integrase Inhibitor

MOA: inhibits the formation of covalent bonds between the host chromosomal DNA and the HIV proviral DNA, thereby preventing the provirus from being integrated into the host cell.

Question 14

Elvitegravir

Answer 14

Integrase Inhibitor

MOA: inhibits integrase -> provirus can’t integrate into host DNA

Question 15

Dolutegravir

Answer 15

Integrase Inhibitor

MOA: inhibits integrase -> provirus can’t integrate into host DNA

Question 16

ARV Tx Combination

Answer 16

1 Protease Inhibitor + 2 NRTIs

1 Integrase Inhibitor + 2 NRTIs