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 - nucleo**TIDE** Others - nucleo**SIDES**

Question 26

Class: Dolu**tegravir**

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 (nucleo**_sides_**) 3. Anemia **(Zidovudine)** 4. Pancreatitis **(Didanosine)**

Question 33

Class: Maraviroc

Answer 33

Fusion inhibitor ## Footnote **Binds CCR-5 on surface of T-cells/monocytes → inhibiting interaction with gp120**

Question 34

Class: Stavudine (d4T)

Answer 34

NRTI

Question 35

Class: Ataza**navir**

Answer 35

Protease inhibitor

Question 36

\_\_\_ can "boost" other drug concentrations by inhibiting cytochrome P-450

Answer 36

Ritonavir

Question 37

Class: Indi**navir**

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 ## Footnote **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**