HIV Drugs

Question 1

Class: Tenofovir (TDF)

Answer 1

NRTI

Question 2

Class: Ritonavir

Answer 2

Protease inhibitor

Question 3

Class: Raltegravir

Answer 3

Integrase inhibitor

Question 4

Specific adverse effect for Zidovudine (NRTI)

Answer 4

Anemia

Question 5

HAART regimen generally consists of 3 drugs to prevent resistance: ___ and preferably a(n) ___.

Answer 5

2 NRTIs

Integrase inhibitor

Question 6

Specific side effects for Efavirenz (NNRTI)

Answer 6

Vivid dreams and CNS symptoms

Question 7

Mechanism: Protease inhibitors

Answer 7

Assembly of virions depends on HIV-1 protease (pol gene), which cleaves the polypeptide products of HIV mRNA into their functional parts. Thus, protease inhibitors prevent maturation of new viruses

Question 8

Toxicity: Protease inhibitors

Answer 8

Hyperglycemia

GI intolerance (nausea, diarrhea)

Lipodystrophy (Cushing-like syndrome)

Question 9

Class: Nevirapine

Answer 9

NNRTI

Question 10

Class: Didanosine (ddl)

Answer 10

NRTI

Question 11

Class: Lamivudine (3TC)

Answer 11

NRTI

Question 12

Toxicity: Enfuvirtide

Answer 12

Skin reaction at injection sites

Question 13

Mechanism: Enfuvirtide

Answer 13

Binds gp41 → inhibiting viral entry

(inhibits fusion)

Question 14

Toxicity: NNRTIs

Answer 14

Common to all NNRTIs:

1. Rash
2. Hepatotoxicity

Specific adverse effects:

1. Vivid dreams and CNS symptoms (Efavirenz)
2. Contraindicated in pregnancy: Delavirdine and Efavirenz

Question 15

Class: Saquinavir

Answer 15

Protease inhibitor

Question 16

Class: Darunavir

Answer 16

Protease inhibitor

Question 17

Class: Lopinavir

Answer 17

Protease inhibitor

Question 18

Class: Abacavir (ABC)

Answer 18

NRTI

Question 19

Toxicity: Integrase inhibitors

Answer 19

Increased creatine kinase

Question 20

Mechanism: NNRTIs

Answer 20

Bind to reverse transcriptase at site different from NRTIs (inhibits RT directly)

Do NOT require phosphorylation to be active

Do NOT compete with nucleotides (non-competitive)

Question 21

___ and ___ are NNRTIs that are contradicated in pregnancy

Answer 21

Delavirdine

Efavirenz

Question 22

Class: Elvitegravir

Answer 22

Integrase inhibitor

Question 23

Class: Fosamprenavir

Answer 23

Protease inhibitor

Question 24

Strongest indications for HAART [3]

Answer 24

AIDS-defining illness

Low CD4+ cell counts (<500 cells/mm³)

High viral load

Question 25

Tenofovir is a ___; other NRTIs are ___

Answer 25

Tenofovir - nucleoTIDE

Others - nucleoSIDES

Question 26

Class: Dolutegravir

Answer 26

Integrase inhibitor

Question 27

Mechanism: Maraviroc

Answer 27

Binds CCR-5 on surface of T-cells/monocytes → inhibiting interaction with gp120

(inhibits docking)

Question 28

Class: Delavirdine

Answer 28

NNRTI

Question 29

___ is a potent CYP/UGT inducer, which reduces protease inhibitor concentrations.

Use ___ instead.

Answer 29

Rifampin

Rifabutin

Question 30

Mechanism: NRTIs

Answer 30

Competitively inhibit nucleotide binding to reverse transcriptase

Incorporated into viral genome → terminating DNA synthesis (lacks 3’ OH group)

Question 31

All NRTIs need to be ___ to become activated

Answer 31

Phosphorylated

Question 32

Toxicity: NRTIs

Answer 32

1. Bone marrow suppression
   
   • Reversed with G-CSF and EPO
2. ​Lactic acidosis (nucleosides)
3. Anemia (Zidovudine)
4. Pancreatitis (Didanosine)

Question 33

Class: Maraviroc

Answer 33

Fusion inhibitor

Binds CCR-5 on surface of T-cells/monocytes → inhibiting interaction with gp120

Question 34

Class: Stavudine (d4T)

Answer 34

NRTI

Question 35

Class: Atazanavir

Answer 35

Protease inhibitor

Question 36

___ can “boost” other drug concentrations by inhibiting cytochrome P-450

Answer 36

Ritonavir

Question 37

Class: Indinavir

Answer 37

Protease inhibitor

Question 38

Class: Efavirenz

Answer 38

NNRTI

Question 39

Specific adverse effects for Indinavir (protease inhibitor)

Answer 39

1. Nephropathy → Hematuria
2. Thrombocytopenia

Question 40

Class: Enfuvirtide

Answer 40

Fusion inhibitor

Binds gp41 → inhibiting viral entry

Question 41

Class: Emtricitabine (FTC)

Answer 41

NRTI

Question 42

Class: Zidovudine (ZDV; formerly AZT)

Answer 42

NRTI

Question 43

___ is contraindicated if patient has HLA-B*5701 mutation due to increased risk of hypersensitivity

Answer 43

Abacavir

Question 44

___ can be used for general HIV prophylaxis and during pregnancy to decrease risk of fetal transmission

Answer 44

Zidovudine (ZDV)

Question 45

Specific adverse effect for Didanosine (NRTI)

Answer 45

Pancreatitis

Question 46

Mechanism: Integrase inhibitors

Answer 46

Inhibits HIV genome integration into host cell chromosome by reversibly inhibiting HIV integrase