Sbl2: Pharmacological Management Of Hiv/aids, Clay

Front 1

5 approved classes of antiretrovirals

Back 1

reverse transcriptase inhibitors
integrase inhibitors
protease inhibitors
fusion inhibitors
CCR5 receptor antagonists

Front 2

ethnicity that currently has the highest incidence of HIV infection

Back 2

African Americans

Front 3

4 goals in the therapy for HIV

Back 3

suppression of viral load
restoration and/or preservation of immune function
improve quality of life
reduce morbidity and mortality

Front 4

3 major classes of entry inhibitors

Back 4

CD4 inhibitors
coreceptor inhibitors
fusion inhibitors

Front 5

antiretroviral that is a coreceptor inhibitor (receptor antagonist)

inhibits R5

Back 5

maraviroc

Front 6

antiretroviral that is a fusion inhibitor that is rarely used as a last resort due to extensive side effects

Back 6

enfuvirtide

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MoA of Maraviroc

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CCR5 inhibitor it does this by altering the coreceptor's (CCR5) shape so the virus cannot bind to it

Front 8

what molecules does HIV bind to on the cell surface?

two co-receptors on cell surfaces that are available to bind to the HIV virus

which cells are they associated w/?

Back 8

CD4 and a coreceptor

CCR5 (macrophages) and CXCR4 (T cells)

note: a coreceptor swith in HIV is associated w/ faster progression of the disease

Front 9

2 likely pathways of resistance of HIV to entry inhibitors

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pathway 1: co-receptor switch (usually R5 to X4)
pathway 2: evolution of HIV's ability to use the drug-bound confirmation of the co-receptor

Front 10

drug classes that are associated w/ resistance

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NRTI, NNRTI, PI, and enfuvirtide

Front 11

antiretroviral drug class that is associated w/ resistance to the whole class after a single point mutation?

classes that require multiple mutations before resistance occurs

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NNRTI

NRTI, PI

Front 12

when should CCR5 inhibitors (maraviroc) be used in the course of an HIV infection?

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early on

Note: in tx experienced patients and late stage, X4 use can be very common and CCR5 is not likley to be effective

Front 13

antiretroviral that is an integrase inhibitor

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raltegravir

Front 14

NRTI that is associated w/ a hypersensitivity syndrome

screening test that is used to establish likelihood of this syndrome

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abacavir

HLA-B*5701

Front 15

NRTI whose dosage must be adjusted to account for renal failure

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tenofovir

Front 16

antiretroviral drug class that as a class can cause hepatic steatosis and lactic acidosis

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NRTIs (but particularly stavudine, didanosine, zidovudine)

Front 17

antiretroviral that is most likely to cause hepatotoxicity

Back 17

nevirapine

Front 18

antiretroviral that is associated w/ bone marrow suppression

Back 18

zidovudine

Front 19

antiretrovirals that cause nephrotoxicity (2)

Back 19

indinavir and tenofovir

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antiretrovirals that are associated w/ pancreatitis (2)

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didanosine and stavudine

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specific antiviral regimens to avoid

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3 NRTI's (only one mechanism of action)
didanosine + (tenofovir or stavudine(increased risk of pancreatitis))
stavudine + zidovudine (work against each other)

Front 22

non-nucleoside RT inhibitors (2)

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efavirenz
nevirapine

Front 23

nucleoside reverse transcriptase inhibitors (5)

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abacavir
tenofovir
stavudine
zidovudine
didanosine

Front 24

NNRTI that has neurological side effects

possibly teratogenic

don't give to those w/ psychiatric hx

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efavirenz

Front 25

NNRTI that is associated w/ hepatotoxicity

run-in dosing (QD at first, then BID)

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nevirapine

Front 26

protease inhibitors (4)

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atazanavir
tipranavir
darunavir
indinavir

Front 27

unique side effect of atazanavir

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hyperbilirubinemia (indinavir can also cause this)

Front 28

protease inhibitor that can be given once daily

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atazanavir

Front 29

two protease inhibitors to work in the face of resistance

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tipranavir and darunavir (ADRs are almost identical so dosent matter which one you choose)

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side effects common to all PIs

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hyperlipidemia
fat redistribution
insulin resistance and diabetes

Front 31

PI that is NOT associated w/ cardiovascular side effects

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atazanavir

Front 32

two protease inhibitors that are associated w/ hyperbilirubinemia

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atazanavir and indinavir

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side effects of ritonavir

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GI intolerance, elevations in triglycerides, hepatitis

Front 34

major determinant of degree and duration of viral suppression

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adherence (optimal suppression requires 90-95% adherence

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most significant proven predictor of inadequate adherence

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fear of side effects

Front 36

antiretroviral that is the most significant inhibitor of CYP3A4

for this reason it is given low dose w/ other drugs to improve their efficacy

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ritonavir

Front 37

two statins that are recommended for use in patients w/ HIV

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atorvastatin and pravastatin (avoid others)

Front 38

two retrovirals that cannot be given w/ gastric acid altering agents

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atazanavir (PI) and didanosine (NRTI)

Front 39

drug that enhances the effects of the phosphodiesterase inhibitors

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ritonavir (CYP inhibitor)

Front 40

Mutations to the HIV virus usually occur to the drug binding site of the virus, what implications does this have on administration of the drug?

Back 40

Drug does not bind as well so more of the drug is needed to achieve inhibition (IC50 shift)

This happens w/ NRTI, NNRTI, PI and enfuvirtide

Front 41

Instead of IC50 shift, "Pleateu" results when the virus has mutated to overcome the effects of this drug, why does happen?

Back 41

The drug is a CCR5 inhibitor, Maraviroc, the drug binds to the host cell and not the the virus. HIV aquires the ability to use the drug bound receptor so adding more drug makes no difference.

Front 42

Patient was taking Abacavir and developed flu like symptomps so they stopped taking the medicine, what is the next step and why?

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Patient developed hypersensitivity syndrome and continuing to take the drug could of slowly lead to death, however, if they restart the drug they can experience and anaphylactic rxn and die w/in hrs

Front 43

What Antiretroviral do you give a patient w/ CV?

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Atazanavir

Front 44

Which antiretrovirals can cause hyperlipidemia

Back 44

all

Front 45

Lipidysrtophy is associated w/ which antiretrovirals

Back 45

PI's

stavudine

Front 46

This antiretroviral has diarrhea and pregancy category D as ADR's

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Nelfinavir