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HIV/AIDS > ANTI RETROVIRAL DRUGS > Flashcards

ANTI RETROVIRAL DRUGS Flashcards

1
Q

Classes of antiretrovirals

A 
CCR5 co-receptor antagonists
fusion inhibitors
nucleoside analogs (NRTIs)
non-nucleoside analogs (NNRTIs)
integrase inhibitors
protease inhibitors
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2
Q

CCR5 inhibitor

A

maraviroc

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3
Q

maraviroc moa

A

interferes with entry of HIV1 into cells by binding CCR5 receptor and blocking the interaction between HIV gp120 and CCR5

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4
Q

maraviroc metabolism

A

not an inhibitor or inducer of cyp3A4, but concentration altered by co administration of drugs that are

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5
Q

maraviroc tox

A

allergic reactions

rash, hypersensativity

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6
Q

marviroc limitations

A

requires viral tropism assay for resistance screening

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7
Q

fusion inhibitors

A

enfuvirtide

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8
Q

enfurvirtide moa

A

inhibits fusion of viral and cellular membranes

prevents conformational changes by binding to gp41

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9
Q

enfurvirtide metabolism

A

no interactions

no renal/hepatic adjustment

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10
Q

enfurvirtide tox

A

SC injection–> injection site rxn
bacterial pneumonia
hypersensativity rxn
mutations have developed in gp41–>resistance

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11
Q

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

A 
Zidovudine
Didanosine
Stavudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine
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12
Q

NRTIs moa

A

Triphosphorylated intracellularly to active form, tenofovir diphos by thymidine kinase
compete with natural nucleosides and terminate the growing DNA chain

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13
Q

NRTIs metabolism/interaction

A

Zidovudine antagonizes phosphorylation of Stavudine- DONT USE TOGETHER
Dose reduce didanosine when given with tenofovir

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14
Q

NRTI class tox

A

mitochodrial tox with lactic acidosis and hepatic steatosis
lipodystrophy/fat atrophy
hepatoxicity

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15
Q

zidovudine tox

A

bone marrow suppression
GI distress
megaloblastic anemia
lactic acidosis

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16
Q

abacavir tox

A

hypersensativity

lactic acidosis

17
Q

lamuvudine tox

A

minimal-none

18
Q

tenofovir tox

A

nausea, vomiting, diarrhea, gas
renal tox
lactic acidosis

19
Q

Mutation in multidrug resistance for NRTIs

A

Q151M

K65R

20
Q

Non-nucleoside Reverse Transcriptase Inhibitors (nnrti’s)

A

efavirenz
nevirapine
delavirdine

21
Q

efavirenz moa

A

No phosphorylation needed to be active, reversible non-comp inhibitor of HIV RT at the RNA dep/DNA dep DNA pol
fucks up enzyme at dif’t site than NRTIs

22
Q

NNRTIs metabolism

A

drug-drug interaction with PI’s
no adjustment for renal, adjust for hepatic
DO NOT USE: rifampin, rifamycin, sedatives, St. John’s Wort

23
Q

NNRTIs class tox

A

skin rash
steven johnson/TEN
hepatotoxicity

24
Q

efavirez tox

A

CNS tox
hyperlipidemia
avoid in pregnancy

25
Q

NNRTIs multidrug resistance

A

K103N

26
Q

integrase inhibitor

A

raltegravir

27
Q

raltegravir moa

A

inhibits catalytic activity of HIV1 integrase

can’t form HIV provirus

28
Q

raltegravir tox

A

CPK elevations, myositis, rhadomyolysis
hypercholesterolemia
increase trunk fat

29
Q

Protease Inhibitors

A 
atazanavir
darunavir
lopinavir
atazanavir
fosamprenavir
saquinavir
ritonavir
30
Q

atazanavir/darunavir MOA

A

blocks protease cleavage of viral gag and gag-pol polyproteins–>non-infectious viral particles

31
Q

Protease Inhibitors metabolism

A

adjust for hepatotoxicity
simultaneous dosing may require adjustmant
inhibit cyp3A4- boost other drugs
not one mutation that can cause class resistance- highest barrier to resistance
DO NOT USE: rifa-‘s, BZDs

32
Q

Protease Inhibitors class tox

A 
hpyerglycemia
GI intolerance
lipodystrophy, hyperlipidemia
bleeding in hemophiliacs
CV
33
Q

Key HIV dosing notes

A

avoid all monotherapies!
avoid zidovudine-stavudine
avoid nevirapine if women > 250 CD4, or men > 400
avoid efavirenz in 1st trimester preg

HIV/AIDS (1 decks)

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