Anti HIV Flashcards Preview

Pharmacology > Anti HIV > Flashcards

Flashcards in Anti HIV Deck (63):
1

Nucleoside Reverse Transcriptase Inhibitors (NRTI) MOA

Nucleoside analogues that require phosphorylation (from host cell) and are then incorporated into the DNA to inhibit viral reverse transcriptase.

2

NRTI common side effects

Hepatotoxicity and Lactic Acidosis

3

Zidovudine (retrovir) MOA

NRTI. Thymidine analogue

4

Zidovudine (retrovir) uses

Maintains CD4 counts, slows progression, used prophylactically, safe in pregnancy. Often combined with lamivudine.

5

Zidovudine (retrovir) toxicity

CNS (HA), myelosuppression (could be treated with epogen or neupogen), when used with acyclovir can cause lethary.

6

Lamivudine (epivir) MOA

NRTI. Cytosine analogue.

7

Lamivudine (epivir) uses

Often combined with zidovudine as an alternate to the first choice. Also used to treat HBV.

8

Lamivudine (epivir) toxicity

well tolerated. HA, fatigue, insomnia, GI.

9

Tenofovir (viread) + Emtricitabine (emtriva) use

This combination is the DOC for HIV infections.

10

Tenofovir (viread) MOA

NRTI. Adenosine analogue.

11

Emtricitabine (emtriva) MOA

NRTI. Cytosine analogue.

12

Tenofovir (viread) + Emtricitabine (emtriva) toxicity

flatulence

13

Didanosine (videx) MOA

NRTI. Adenosine analogue

14

Didanosine (videx) toxicity

Peripheral neuropathy, hyperuricemia, pancreatitis

15

Stavudine (zerit) MOA

NRTI. Thymidine analogue.

16

Stavudine (zerit) toxicity

peripheral neuropathy

17

Zalcitabine (hivid) MOA

NRTI. Cytosine analogue.

18

Zalcitabine (hivid) toxicity

peripheral neuropathy especially if diabetic, alcoholic or B12 deficient.

19

Drugs that cause peripheral neuropathy

NRTIs: Didanosine, stavudine, zalcitabine

20

Abacavir (ziagen) MOA

NRTI. Guanosine analogue.

21

Abacavir (ziagen) uses

often combined with lamivudine/zidovudine

22

Abacavir (ziagen) toxicity

hypersensitivity and GI disturbance

23

Non-nucleotide reverse transcriptase inhibitors (NNRTI) MOA

Bind directly to inhibit viral reverse transcriptase. Doesn't require any phosphorylation to be activated.

24

Efavirenz (sustiva) MOA

NNRTI

25

Efavirenz (sustiva) uses

DOC for initial therapy. Used in combination with NRTIs.

26

Non-nucleotide reverse transcriptase inhibitors (NNRTI) toxicity

inhibit and are metabolized by CYP3A4

27

Efavirenz (sustiva) toxicity

Teratogenic, dizziness, insomnia, HA

28

Neviparine (viramune) MOA

NNRTI.

29

Neviparine (viramune) uses

Used during pregnancy. A single dose is effective in preventing transmission to the new born.

30

Neviparine (viramune) toxicity

SJS, Hepatitis. Don't give with ketoconazole.

31

Delavirdine (rescriptor) MOA

NNRTI

32

Delaviridine uses

Oral. Absorption is decreased with antacids.

33

Delaviridine toxicity

teratogenic, rash, nausea, HA, elevated serum aminotransferase.

34

Protease inhibitors (PI) MOA

Bind to proteases and inhibit them from digesting long viral polypeptides into smaller functional proteins.

35

PI common toxicities

All are extensively metabolized by CYP3A4, altered body fat distribution, insulin resistance, increase in serum cholesterol (don't give with statins), spontaneous bleeding in those with hemophilia. Do not take with St. Johns Wort.

36

Atazenavir (reyataz) MOA

PI

37

Atazenavir (reyataz) uses

DOC for initial therapy due to low incidence of side effects.

38

Atazenavir (reyataz) Toxicity

less effect on body fat distribution. Can increase bilirubin due to inhibition of UGT. Diarrhea, rash, nausea.

39

Darunavir (prezista) MOA

PI

40

Darunavir (prezista) uses

Drug of second choice when combine with ritonavir (boosts it's bioavailability)

41

Darunavir (prezista) toxicity

sulfa moiety (hypersensitivity)

42

Ritonavir (norivir) MOA

PI

43

Ritonavir (norvir) use

inhibits CYP3A4 and is combined with other protease inhibitors to increase their bioavailability (allowing for less frequent dosing).

44

Ritonavir (norvir) toxicity

DO NOT combine with saquinavir due to QT prolongation. drug interaction, GI disturbance, increased liver enzymes, contains ethanol so don't give with disulfiram or metronidazole.

45

Saquinavir (invirase) MOA

PI

46

Saquinavir (invirase) toxicity

DO NOT combine with ritonavir due to QT prolongation.

47

Lopanvir/ritonavir (Kaletra) MOA

PI

48

Lopanvir/ritonavir (Kaletra) uses

This combination increases the bioavailability of lopinavir.

49

Lopanvir/ritonavir (Kaletra) toxicity

diarrhea, nausea, elevated liver enzymes.

50

Indinavir (crixivan) MOA

PI

51

Indinavir (crixivan) uses

Combine with ritonavir. Has cross resistance with ritonavir.

52

Indinavir (crixivan) toxicity

nephrolithiasis and hyperbilirubinemia (treat with hydration)

53

Tripanavir (aptivus) MOA

Non-peptide PI

54

Tripanavir (aptivus) uses

indicated in treatment-experience patients who harbor resistant strains. Can be given with ritonavir (causes increased risk of intracranial hemorrhage)

55

Tripanavir (aptivus) toxicity

sulfa moiety (hypersensitivity), GI, liver toxicity.

56

Enfuvirtide (fuzeon) MOA

Fusion inhibitor. Binds to gp41 on the viral envelope to prevent conformational change needed for fusion.

57

Enfuvirtide (fuzeon) uses

advanced disease and treatment-experienced patients. Give as a subcutaneous injection (only parenteral antiHIV drug).

58

Enfuvirtide (fuzeon) toxicity

Increased risk of bacterial pneumonia.

59

Maraviroc (selzentry) MOA

fusion inhibitor. Binds CCR5 receptor on the T cell. Have to analyze the strain because it is not useful against CXCR4 or mixed tropic infections.

60

Enfuvirtide (fuzeon) toxicity

rash. otherwise very well tolerated.

61

Raltegravir (isentress) MOA

Integrase inhibitor. Inhibits the transfer of viral DNA into host DNA

62

Raltegravir (isentress) uses

Cases of resistance

63

Raltegravir (isentress) toxicity

nausea, vomiting, HA, diarrhea