(7) Antimicrobials: Antivirals HIV (6.1-6.4)

Question 1

How are NRTIs different from endogenous molecules?

Answer 1

Lack 3’ hydroxyl

Question 2

MOA: NRTIs: NRTIs

Answer 2

Incorporation into viral DNA ⇒ Premature chain termination

Question 3

How are nucleoside NRTIs activated?

Answer 3

Phosphorylation

Question 4

Adverse Effects (2) : All NRTIs

Answer 4

(1) Mitochondrial toxicity
(2) ⇒ Lactic acidosis

Question 5

Suffix: NRTIs

Answer 5

“-dine”

Question 6

Which NRTIs are used to treat Hepatitis B?

Answer 6

(1) Lamivudine
(2) Tenofovir

Question 7

Is Tenofovir a nucleoside or nucleotide?

Answer 7

Tenofovir = Nucleotide

Question 8

Which NRTI is first-line during pregnancy and breastfeeding?

Answer 8

Zidovudine

Question 9

Adverse Effect: Zidovudine

Answer 9

Myelosuppression

Question 10

Which NRTIs are associated with lipodystrophy?

Answer 10

(1) Zidovudine
(2) Stavudine

Question 11

Which NRTI is associated with pancreatitis?

Answer 11

Didanosine

Question 12

Which NRTI is most associated with hypersensitivity reactions?

Answer 12

Abacavir

Question 13

Which HLA allele has an association with hypersensitivity reactions with Abacavir?

Answer 13

HLA-B 57:01

Question 14

What type of hypersensitivity reaction is associated with Abacavir?

Answer 14

Type IV

Question 15

Which NRTI is associated with hyperpigmentation of palms and soles?

Answer 15

Emtricitabine

Question 16

Do NNRTIs require phosphorylation to be active?

Answer 16

No

Question 17

MOA: NNRTIs

Answer 17

Directly bind reverse transcriptase and inhibit enzyme

Question 18

Adverse Effects (2) : NNRTIs

Answer 18

(1) Liver failure
(2) Stevens-Johnson syndrome

Question 19

Which NNRTI is most associated with CNS side effects?

Answer 19

Efavirenz

Question 20

Which class of HIV drugs should be avoided in pregnancy?

Answer 20

NNRTIs

(Nevirapine is not contraindicated)

Question 21

What effect do NNRTIs have on CYP450 system?

Answer 21

Varying – some induce and others inhibit

Question 22

Which NNRTI is NOT contraindicated in pregnancy?

Answer 22

Nevirapine

(N in Nevirapine stands for No contraindication)

Question 23

Suffix: Protease inhibitors

Answer 23

“-navir”

Question 24

What HIV gene codes for proteases?

Answer 24

pol

Question 25

**Adverse Effects** - Metabolic (3) : Protease inhibitors

Answer 25

(1) Insulin resistance (2) Dyslipidemia (3) Central adiposity

Question 26

What drug used to treat HIV is associated with nephrolithiasis?

Answer 26

Indinavir

Question 27

What protease inhibitor is the strongest inhibitor of the CYP450 system?

Answer 27

Ritonavir

Question 28

What tuberculosis drug is contraindicated in people taking protease inhibitors?

Answer 28

Rifampin

Question 29

**MOA**: HIV Protease inhibitors

Answer 29

Inhibits cleavage of precursor protein into active units

Question 30

What does the HIV gag gene code for?

Answer 30

The STRUCTURAL proteins, (1) p24 (2) p7

Question 31

What does the HIV env gene code for?

Answer 31

The ENVELOPE proteins, (1) gp41 (2) gp120

Question 32

What HIV protein binds host CD4/CCR5?

Answer 32

gp120

Question 33

**MOA**: Maraviroc

Answer 33

Binds CCR5 ⇒ Inhibits interaction with gp120 ## Footnote *(Note: This is likely more effective during early infection when CCR5 receptor is preferred over CXCR4)*

Question 34

What HIV protein is responsible for fusion?

Answer 34

gp41

Question 35

**MOA**: Enfuvirtide

Answer 35

Binds gp41 ⇒ Inhibits fusion

Question 36

What does HIV *pol* gene code for?

Answer 36

(1) Protease (2) Reverse transcriptase (3) Integrase

Question 37

**MOA**: Raltegravir

Answer 37

HIV integrase inhibitor

Question 38

**Adverse Effect:** Integrase inhibitors

Answer 38

Rhabdomyolysis