Anti-Retroviral Drugs Flashcards Preview

OS1 - Heme > Anti-Retroviral Drugs > Flashcards

Flashcards in Anti-Retroviral Drugs Deck (48):
1

Name the NRTIs.

Abacavir
Lamivudine
Tenofovir
Emtricitabine
Zidovudine
Didanosine
Stavudine

2

Name the NNRTIs.

Nevirapine
Efavirenz

3

Name the protease inhibitors.

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

4

Name the fusion inhibitors.

Enfuvirtide
Maraviroc

5

Name the integrase inhibitor.

Raltegravir

6

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

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

7

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

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

8

What is the metabolism of Delavirdine?

3A4/2D6 substrate.
Inhibits 3A4, 2D6, 2C9, 2C10

9

What is the metabolism of Efavirenz?

Induces 3A4/2B6

10

What is the metabolism of Nevirapine?

Induces 3A4/2B6

11

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

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

12

What is the metabolism of Atazanavir?

Inhibits 3A4/UGT

13

What is the metabolism of Saquinavir?

Inhibits 3A4/UGT

14

What is the metabolism of Indinavir?

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

15

What is the metabolism of Fosamprenavir?

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

16

What is the metabolism of Ritonavir?

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

17

What is the metabolism of Lopinavir?

substrate for 3A4

18

What is the metabolism of Darunavir?

substrate for 3A4

19

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

Enfuvirtide - given subcutaneously

20

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

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

21

What is the metabolism of Enfuvirtide?

catabolized to amino acids

22

What is the metabolism of Maraviroc?

3A4/P-gp substrate

23

What is the metabolism of Raltegravir?

glucuronide metabolite

24

What is cobicistat and what is it used for?

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

25

What is Atripla?

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

26

What are the contraindications/BBW of Abacavir?

contra: hypersensitivity and hepatic disease
BBW: lactic acidosis

27

What are the BBW of Didanosine?

hepatic disease, lactic acidosis, neuropathy, pancreatitis

28

What are the BBW of Emtricitabine?

hepatic disease, lactic acidosis, neuropathy

29

What are the BBW of Lamivudine?

hepatic disease, lactic acidosis, neuropathy

30

What are the BBW of Stavudine?

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

31

What are the BBW of Tenofovir?

hepatic disease, lactic acidosis, neuropathy, pancreatitis

32

What are the BBW of Zidovudine?

anemia, myopathy, neutropenia

33

What NNRTI has the most BBWs and what are they?

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

34

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

NNRTIs

35

Efavirenz carries what weird toxicities?

CNS toxicities and vivid dreams

36

What 2 HAART drugs are contraindicated in pregnancy?

Delavirdine and Efavirenz

37

What are the major side effects of protease inhibitors?

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

38

Describe the role of peripheral neuropathy in HIV and HAART.

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)

39

What are the recommended agents to prevent pneumo jiroveci?

Trimethoprim-Sulfamethoxazole

40

What are the recommended agents to prevent m. TB?

Isoniazid and Pyridoxine

41

What are the recommended agents to prevent toxoplasmosis?

Trimethoprim-Sulfamethoxazole

42

What are the recommended agents to prevent CMV?

val/gangciclovir

43

What are the recommended agents to prevent fungal infections?

Fluconazole

44

What drugs are used against CMV?

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

45

What are side effects of valganciclovir?

leukopenia, neutropenia, renal toxicity

46

What is the MOA and major toxicity of foscarnet?

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

47

What is vidarabine and what is it used to treat?

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

48

What drug is given to treat KSHV?

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