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Anti HIV Flashcards

1
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTI) MOA

A

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

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2
Q

NRTI common side effects

A

Hepatotoxicity and Lactic Acidosis

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3
Q

Zidovudine (retrovir) MOA

A

NRTI. Thymidine analogue

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4
Q

Zidovudine (retrovir) uses

A

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

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5
Q

Zidovudine (retrovir) toxicity

A

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

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6
Q

Lamivudine (epivir) MOA

A

NRTI. Cytosine analogue.

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7
Q

Lamivudine (epivir) uses

A

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

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8
Q

Lamivudine (epivir) toxicity

A

well tolerated. HA, fatigue, insomnia, GI.

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9
Q

Tenofovir (viread) + Emtricitabine (emtriva) use

A

This combination is the DOC for HIV infections.

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10
Q

Tenofovir (viread) MOA

A

NRTI. Adenosine analogue.

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11
Q

Emtricitabine (emtriva) MOA

A

NRTI. Cytosine analogue.

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12
Q

Tenofovir (viread) + Emtricitabine (emtriva) toxicity

A

flatulence

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13
Q

Didanosine (videx) MOA

A

NRTI. Adenosine analogue

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14
Q

Didanosine (videx) toxicity

A

Peripheral neuropathy, hyperuricemia, pancreatitis

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15
Q

Stavudine (zerit) MOA

A

NRTI. Thymidine analogue.

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16
Q

Stavudine (zerit) toxicity

A

peripheral neuropathy

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17
Q

Zalcitabine (hivid) MOA

A

NRTI. Cytosine analogue.

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18
Q

Zalcitabine (hivid) toxicity

A

peripheral neuropathy especially if diabetic, alcoholic or B12 deficient.

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19
Q

Drugs that cause peripheral neuropathy

A

NRTIs: Didanosine, stavudine, zalcitabine

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20
Q

Abacavir (ziagen) MOA

A

NRTI. Guanosine analogue.

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21
Q

Abacavir (ziagen) uses

A

often combined with lamivudine/zidovudine

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22
Q

Abacavir (ziagen) toxicity

A

hypersensitivity and GI disturbance

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23
Q

Non-nucleotide reverse transcriptase inhibitors (NNRTI) MOA

A

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

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24
Q

Efavirenz (sustiva) MOA

A

NNRTI

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25
Q

Efavirenz (sustiva) uses

A

DOC for initial therapy. Used in combination with NRTIs.

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26
Q

Non-nucleotide reverse transcriptase inhibitors (NNRTI) toxicity

A

inhibit and are metabolized by CYP3A4

27
Q

Efavirenz (sustiva) toxicity

A

Teratogenic, dizziness, insomnia, HA

28
Q

Neviparine (viramune) MOA

29
Q

Neviparine (viramune) uses

A

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

30
Q

Neviparine (viramune) toxicity

A

SJS, Hepatitis. Don’t give with ketoconazole.

31
Q

Delavirdine (rescriptor) MOA

32
Q

Delaviridine uses

A

Oral. Absorption is decreased with antacids.

33
Q

Delaviridine toxicity

A

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

34
Q

Protease inhibitors (PI) MOA

A

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

35
Q

PI common toxicities

A

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
Q

Atazenavir (reyataz) MOA

37
Q

Atazenavir (reyataz) uses

A

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

38
Q

Atazenavir (reyataz) Toxicity

A

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

39
Q

Darunavir (prezista) MOA

40
Q

Darunavir (prezista) uses

A

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

41
Q

Darunavir (prezista) toxicity

A

sulfa moiety (hypersensitivity)

42
Q

Ritonavir (norivir) MOA

43
Q

Ritonavir (norvir) use

A

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

44
Q

Ritonavir (norvir) toxicity

A

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
Q

Saquinavir (invirase) MOA

46
Q

Saquinavir (invirase) toxicity

A

DO NOT combine with ritonavir due to QT prolongation.

47
Q

Lopanvir/ritonavir (Kaletra) MOA

48
Q

Lopanvir/ritonavir (Kaletra) uses

A

This combination increases the bioavailability of lopinavir.

49
Q

Lopanvir/ritonavir (Kaletra) toxicity

A

diarrhea, nausea, elevated liver enzymes.

50
Q

Indinavir (crixivan) MOA

51
Q

Indinavir (crixivan) uses

A

Combine with ritonavir. Has cross resistance with ritonavir.

52
Q

Indinavir (crixivan) toxicity

A

nephrolithiasis and hyperbilirubinemia (treat with hydration)

53
Q

Tripanavir (aptivus) MOA

A

Non-peptide PI

54
Q

Tripanavir (aptivus) uses

A

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

55
Q

Tripanavir (aptivus) toxicity

A

sulfa moiety (hypersensitivity), GI, liver toxicity.

56
Q

Enfuvirtide (fuzeon) MOA

A

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

57
Q

Enfuvirtide (fuzeon) uses

A

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

58
Q

Enfuvirtide (fuzeon) toxicity

A

Increased risk of bacterial pneumonia.

59
Q

Maraviroc (selzentry) MOA

A

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
Q

Enfuvirtide (fuzeon) toxicity

A

rash. otherwise very well tolerated.

61
Q

Raltegravir (isentress) MOA

A

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

62
Q

Raltegravir (isentress) uses

A

Cases of resistance

63
Q

Raltegravir (isentress) toxicity

A

nausea, vomiting, HA, diarrhea

Pharmacology (24 decks)

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