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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
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

Pharmacology (24 decks)

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