Anti-Retroviral Drugs

Question 1

Name the NRTIs.

Answer 1

Abacavir
Lamivudine
Tenofovir
Emtricitabine
Zidovudine
Didanosine
Stavudine

Question 2

Name the NNRTIs.

Answer 2

Nevirapine

Efavirenz

Question 3

Name the protease inhibitors.

Answer 3

any drug that ends in "-navir": 
Atazanavir
Ritonavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Saquinavir

Question 4

Name the fusion inhibitors.

Answer 4

Enfuvirtide

Maraviroc

Question 5

Name the integrase inhibitor.

Answer 5

Raltegravir

Question 6

Describe the route, metabolism, and elimination of the NRTIs.

Answer 6

Route: oral 1-2x/day
Metabolism: minimal/no CYPs, some are glucuronide metabolites
Elimination: in urine as drug and metabolite

Question 7

Describe the route, metabolism, and elimination of the NNRTIs.

Answer 7

Route: oral 1-2x/day
Metabolism: CYP interaction
Elimination: urine/stool as metabolites

Question 8

What is the metabolism of Delavirdine?

Answer 8

3A4/2D6 substrate.

Inhibits 3A4, 2D6, 2C9, 2C10

Question 9

What is the metabolism of Efavirenz?

Answer 9

Induces 3A4/2B6

Question 10

What is the metabolism of Nevirapine?

Answer 10

Induces 3A4/2B6

Question 11

Describe the route, metabolism, and elimination of the protease inhibitors.

Answer 11

Route: oral 1-2x/day
Metabolism: serious CYP interaction
Elimination: stool mostly as metabolites

Question 12

What is the metabolism of Atazanavir?

Answer 12

Inhibits 3A4/UGT

Question 13

What is the metabolism of Saquinavir?

Answer 13

Inhibits 3A4/UGT

Question 14

What is the metabolism of Indinavir?

Answer 14

Inhibits 3A4; substrate of 3A4/P-gp

Question 15

What is the metabolism of Fosamprenavir?

Answer 15

Inhibits 3A4; substrate of 3A4/2D6/2C9/P-gp

Question 16

What is the metabolism of Ritonavir?

Answer 16

Inhibits 3A4/2D6/P-gp/UGT

Question 17

What is the metabolism of Lopinavir?

Answer 17

substrate for 3A4

Question 18

What is the metabolism of Darunavir?

Answer 18

substrate for 3A4

Question 19

What is the special HAART drug that is NOT given orally, and how is it given?

Answer 19

Enfuvirtide - given subcutaneously

Question 20

Describe the route, metabolism, and elimination of the integrase/fusion inhibitors.

Answer 20

Route: orally 1-2x/day (except enfuvirtide)
Metabolism: different, only Maraviroc has CYP interactions
Elimination: stool/urine as drug and metabolites (except enfuvirtide)

Question 21

What is the metabolism of Enfuvirtide?

Answer 21

catabolized to amino acids

Question 22

What is the metabolism of Maraviroc?

Answer 22

3A4/P-gp substrate

Question 23

What is the metabolism of Raltegravir?

Answer 23

glucuronide metabolite

Question 24

What is cobicistat and what is it used for?

Answer 24

it’s an orally active 3A4 inhibitor and it’s used as a pharmacokinetic enhancer to increase the serum concentration of CYP3A substrates, such as the protease inhibitors atazanavir and darunavir

Question 25

What is Atripla?

Answer 25

a once daily pill that constitutes a complete ART drug regimen; includes tenofovir, emtricitabine, and efavirenz

Question 26

What are the contraindications/BBW of Abacavir?

Answer 26

contra: hypersensitivity and hepatic disease BBW: lactic acidosis

Question 27

What are the BBW of Didanosine?

Answer 27

hepatic disease, lactic acidosis, neuropathy, pancreatitis

Question 28

What are the BBW of Emtricitabine?

Answer 28

hepatic disease, lactic acidosis, neuropathy

Question 29

What are the BBW of Lamivudine?

Answer 29

hepatic disease, lactic acidosis, neuropathy

Question 30

What are the BBW of Stavudine?

Answer 30

hepatic disease, lactic acidosis, neuropathy (MOST), pancreatitis

Question 31

What are the BBW of Tenofovir?

Answer 31

hepatic disease, lactic acidosis, neuropathy, pancreatitis

Question 32

What are the BBW of Zidovudine?

Answer 32

anemia, myopathy, neutropenia

Question 33

What NNRTI has the most BBWs and what are they?

Answer 33

Nevirapine - hepatic disease (X), hypersensitivity (X), hepatitis, serious rash, females

Question 34

Rash and hepatotoxicity are common to all members of what class?

Answer 34

NNRTIs

Question 35

Efavirenz carries what weird toxicities?

Answer 35

CNS toxicities and vivid dreams

Question 36

What 2 HAART drugs are contraindicated in pregnancy?

Answer 36

Delavirdine and Efavirenz

Question 37

What are the major side effects of protease inhibitors?

Answer 37

GI intolerance, lipodystrophy, hyperglycemia/DM, dyslipidemia, nephrolithiasis (most common with indinavir), severe rash including SJS

Question 38

Describe the role of peripheral neuropathy in HIV and HAART.

Answer 38

its a consequence of HIV infection of macrophages in the DRG and neuronal injury related to gp120; toxic peripheral neuropathy is a long term side effect of HAART (NNRTIs, NRTIs, and some PIs)

Question 39

What are the recommended agents to prevent pneumo jiroveci?

Answer 39

Trimethoprim-Sulfamethoxazole

Question 40

What are the recommended agents to prevent m. TB?

Answer 40

Isoniazid and Pyridoxine

Question 41

What are the recommended agents to prevent toxoplasmosis?

Answer 41

Trimethoprim-Sulfamethoxazole

Question 42

What are the recommended agents to prevent CMV?

Answer 42

val/gangciclovir

Question 43

What are the recommended agents to prevent fungal infections?

Answer 43

Fluconazole

Question 44

What drugs are used against CMV?

Answer 44

valganciclovir (PO), ganciclovir, foscarnet, cidofovir (last 3 = IV)

Question 45

What are side effects of valganciclovir?

Answer 45

leukopenia, neutropenia, renal toxicity

Question 46

What is the MOA and major toxicity of foscarnet?

Answer 46

viral DNA polymerase inhibitor; nephrotoxicity (hydrate patient before administration)

Question 47

What is vidarabine and what is it used to treat?

Answer 47

nucleoside analog; treats EBV infection, applied to eye as ointment

Question 48

What drug is given to treat KSHV?

Answer 48

Cidofovir, IV | also other anti-virals: ganciclovir, valganciclovir,