Drugs for HIV

Question 1

Name the 8 Nucleoside Reverse Transcriptase Inhibitors (NRTI)

Answer 1

• Zidovudine
• Lamivudine
• Emtricitabine
• Tenofovir
• Didanosine
• Zalcitabine
• Stavudine
• Abacavir

Question 2

MOA of Nucleoside Reverse Transcriptase Inhibitors (NRTI)

Answer 2

• Nucleoside analogue
• inhibits viral reverse transcriptase

Question 3

route of administration of Zidovudine

Answer 3

oral

Question 4

distribution of Zidovudine

Answer 4

good CNS penetration

Question 5

Use of Zidovudine

Answer 5

• lessen opportunistic infections
• safe in pregnancy: decreases risk of transmission during pregnancy and during labor

Question 6

Toxicity of Zidovudine

Answer 6

• CNS
• lactic acidosis or hepatotoxicity
• Myelosuppression: neutropenia, anemia

Question 7

If resistance develops to Zidovudine, what drug can be added to treatment regimen (alternate first choice)

Answer 7

Lamivudine

Question 8

MOA of Zidovudine

Answer 8

Thymidine analogue

Question 9

MOA of Lamivudine

Answer 9

• Cytosine analogue
• inhibits HIV reverse transcriptase

Question 10

route of administration of Lamivudine

Answer 10

oral

Question 11

toxicity of Lamivudine

Answer 11

low toxicity, very well tolerated

Question 12

MOA of Tenofovir

Answer 12

• Adenosine analogue
• inhibit reverse transcriptase

Question 13

MOA of Emtricitabine

Answer 13

• cytosine inhibitor
• inhibit reverse transcriptase

Question 14

route of administration of Tenofovir and Emtricitabine

Answer 14

oral

Question 15

DOC NRTI for treatment of HIV

Answer 15

Tenofovir and Emtricitabine

Question 16

side effects of Tenofovir and Emtricitabine

Answer 16

flatulence

Question 17

MOA of Didanosine

Answer 17

adenosine analogue

Question 18

Toxicity of Didanosine, Stavudine, and Zalcitabine

Answer 18

peripheral neuropathy

Question 19

toxicity of Abacavir

Answer 19

• serious hypersensitivity
  
  • discontinue drug and DO NOT restart

Question 20

what are serious side effects that can occur with all NRTIs

Answer 20

• lactic acidosis
• hepatotoxicity

Question 21

name the 3 non-nucleotide reverse transcriptase inhibitors

Answer 21

• Efavirenz
• Nevirapine
• Delavirdine

Question 22

MOA of non-nucleotide reverse transcriptase inhibitors

Answer 22

• bind directly to inhibit viral reverse transcriptase
• do not require phosphorylation for activity

Question 23

DOC: NNRTI for initial therapy of HIV

Answer 23

Efavirenz

Question 24

route of administration of Efavirenz

Answer 24

oral

Question 25

combine Efavirenz with ?

Answer 25

nucleoside analogues

Question 26

toxicities of Efavirenz

Answer 26

* Drug interaction: induces and inhibits CYP3A * teratogenic: avoid in pregnancy

Question 27

route of administration of Neviparine

Answer 27

oral

Question 28

DOC: NNRTI for intial therapy of HIV in pregnant females

Answer 28

Neviparine ## Footnote \*effective in the prevention of transmission of HIV from mother to newborn

Question 29

toxicities of Neviparine

Answer 29

* stevens-johnson syndrome * hepatitis

Question 30

route of administration of Delavirdine

Answer 30

oral

Question 31

toxicities of Delavirdine

Answer 31

* inhibits CYP3A4 * rash * teratogenic: avoid in pregnancy

Question 32

Name the 7 protease inhibitors used in treatment of HIV

Answer 32

* Atazanavir * Darunavir * Ritonavir * Saquinavir * Lopinavir/ritonavir * Indinavir * Tipranavir

Question 33

route of administration of protease inhibitors

Answer 33

oral

Question 34

combine protease inhibitors with?

Answer 34

1. **NRTIs** 2. **ritonavir**: bc protease inhibitors are metabolized by CYP3A4 and rionavir inhibits CYP3A4

Question 35

when giving your patient protease inhibitors, what should you specifically tell them to not take?

Answer 35

St. John's Wort

Question 36

common toxicities of protease inhibitors

Answer 36

* altered body fat distribution * insulin resistance * increases serum cholesterol: do not combine with statins * spontaneous bleeding: hemophilia A or B

Question 37

DOC: protease inhibitor in treatment of HIV

Answer 37

Atazenavir

Question 38

toxicity specific to Atazenavir

Answer 38

* increase biliruben * diarrhea, rash, nausea * less effect on body fat distribution

Question 39

DO second choice: protease inhibitor in treatment of HIV

Answer 39

Darunavir: combine with ritonavir

Question 40

contraindication of Darunavir

Answer 40

* contains a sulfonamide moiety: do not use in patients with sulfa allergy

Question 41

Use of Ritonavir

Answer 41

* inhibits CYP3A4: combined with other protease inhibitors to increase thier bioavailability

Question 42

Ritonavir should not be combined with which because together they cause QT elongation

Answer 42

Saquinavir

Question 43

Ritonavir contains alcohol and so should not be combined with

Answer 43

* disulfiram * metronidazole

Question 44

There is a cross resistance between ritonavir and ?

Answer 44

Indinavir

Question 45

toxicity of Indinavir

Answer 45

* nephrolithiasis * hyperbilirubinemia

Question 46

Use of Tipranavir

Answer 46

* non-peptide PI * indicated for use in treatment -experienced HIV-1-infected patients who harbor strains resistant to other PIs

Question 47

Tipranavir is combined with

Answer 47

ritonavir

Question 48

toxicity of Tipranavir + ritonavir

Answer 48

* intracranial hemorrhage - avoid in pts with head trauma * sulfonamide moiety * hepatotoxic

Question 49

MOA of Enfuvirtide

Answer 49

* fusion inhibitor * binds to **gp41** subunit of viral envelope glycoprotein

Question 50

route of administration of Enfuvirtide

Answer 50

subcutaneous: only parenteral antiretroviral agent

Question 51

good thing about Enfuvirtide

Answer 51

no cross resistance with other antiretroviral agents

Question 52

adverse effects of Enfuvirtide

Answer 52

increases likelihood of bacterial pneumonia

Question 53

MOA of Maraviroc

Answer 53

* inhibits virus fusion * binds to **CCR5 receptor** of CD4 T-cell

Question 54

use of Maraviroc

Answer 54

only use in patients with CCR5-tropic HIV infection in whom other treatment has not been effective

Question 55

MOA of Raltegravir

Answer 55

**integrase inhibitor**: inhibits transfer of viral DNA to host cell DNA

Question 56

MOA: zalcitabine

Answer 56

cytosine analogue

Question 57

MOA: stavudine

Answer 57

thymidine analogue

Question 58

MOA: abacavir

Answer 58

guanosine analogue