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OS1 - Heme > Anti-Retroviral Drugs > Flashcards

Anti-Retroviral Drugs Flashcards

1
Q

Name the NRTIs.

A 
Abacavir
Lamivudine
Tenofovir
Emtricitabine
Zidovudine
Didanosine
Stavudine
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2
Q

Name the NNRTIs.

A

Nevirapine

Efavirenz

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3
Q

Name the protease inhibitors.

A 
any drug that ends in "-navir": 
Atazanavir
Ritonavir
Darunavir
Fosamprenavir
Indinavir
Lopinavir
Saquinavir
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4
Q

Name the fusion inhibitors.

A

Enfuvirtide

Maraviroc

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5
Q

Name the integrase inhibitor.

A

Raltegravir

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6
Q

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

A

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

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7
Q

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

A

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

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8
Q

What is the metabolism of Delavirdine?

A

3A4/2D6 substrate.

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

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9
Q

What is the metabolism of Efavirenz?

A

Induces 3A4/2B6

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10
Q

What is the metabolism of Nevirapine?

A

Induces 3A4/2B6

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11
Q

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

A

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

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12
Q

What is the metabolism of Atazanavir?

A

Inhibits 3A4/UGT

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13
Q

What is the metabolism of Saquinavir?

A

Inhibits 3A4/UGT

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14
Q

What is the metabolism of Indinavir?

A

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

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15
Q

What is the metabolism of Fosamprenavir?

A

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

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16
Q

What is the metabolism of Ritonavir?

A

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

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17
Q

What is the metabolism of Lopinavir?

A

substrate for 3A4

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18
Q

What is the metabolism of Darunavir?

A

substrate for 3A4

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19
Q

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

A

Enfuvirtide - given subcutaneously

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20
Q

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

A

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

21
Q

What is the metabolism of Enfuvirtide?

A

catabolized to amino acids

22
Q

What is the metabolism of Maraviroc?

A

3A4/P-gp substrate

23
Q

What is the metabolism of Raltegravir?

A

glucuronide metabolite

24
Q

What is cobicistat and what is it used for?

A

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
Q

What is Atripla?

A

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

26
Q

What are the contraindications/BBW of Abacavir?

A

contra: hypersensitivity and hepatic disease
BBW: lactic acidosis

27
Q

What are the BBW of Didanosine?

A

hepatic disease, lactic acidosis, neuropathy, pancreatitis

28
Q

What are the BBW of Emtricitabine?

A

hepatic disease, lactic acidosis, neuropathy

29
Q

What are the BBW of Lamivudine?

A

hepatic disease, lactic acidosis, neuropathy

30
Q

What are the BBW of Stavudine?

A

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

31
Q

What are the BBW of Tenofovir?

A

hepatic disease, lactic acidosis, neuropathy, pancreatitis

32
Q

What are the BBW of Zidovudine?

A

anemia, myopathy, neutropenia

33
Q

What NNRTI has the most BBWs and what are they?

A

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

34
Q

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

A

NNRTIs

35
Q

Efavirenz carries what weird toxicities?

A

CNS toxicities and vivid dreams

36
Q

What 2 HAART drugs are contraindicated in pregnancy?

A

Delavirdine and Efavirenz

37
Q

What are the major side effects of protease inhibitors?

A

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

38
Q

Describe the role of peripheral neuropathy in HIV and HAART.

A

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
Q

What are the recommended agents to prevent pneumo jiroveci?

A

Trimethoprim-Sulfamethoxazole

40
Q

What are the recommended agents to prevent m. TB?

A

Isoniazid and Pyridoxine

41
Q

What are the recommended agents to prevent toxoplasmosis?

A

Trimethoprim-Sulfamethoxazole

42
Q

What are the recommended agents to prevent CMV?

A

val/gangciclovir

43
Q

What are the recommended agents to prevent fungal infections?

A

Fluconazole

44
Q

What drugs are used against CMV?

A

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

45
Q

What are side effects of valganciclovir?

A

leukopenia, neutropenia, renal toxicity

46
Q

What is the MOA and major toxicity of foscarnet?

A

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

47
Q

What is vidarabine and what is it used to treat?

A

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

48
Q

What drug is given to treat KSHV?

A

Cidofovir, IV

also other anti-virals: ganciclovir, valganciclovir,

OS1 - Heme (31 decks)

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