ANTI RETROVIRAL DRUGS

Question 1

Classes of antiretrovirals

Answer 1

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

Question 2

CCR5 inhibitor

Answer 2

maraviroc

Question 3

maraviroc moa

Answer 3

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

Question 4

maraviroc metabolism

Answer 4

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

Question 5

maraviroc tox

Answer 5

allergic reactions

rash, hypersensativity

Question 6

marviroc limitations

Answer 6

requires viral tropism assay for resistance screening

Question 7

fusion inhibitors

Answer 7

enfuvirtide

Question 8

enfurvirtide moa

Answer 8

inhibits fusion of viral and cellular membranes

prevents conformational changes by binding to gp41

Question 9

enfurvirtide metabolism

Answer 9

no interactions

no renal/hepatic adjustment

Question 10

enfurvirtide tox

Answer 10

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

Question 11

Nucleoside Reverse Transcriptase Inhibitors (NRTIs)

Answer 11

Zidovudine
Didanosine
Stavudine
Lamivudine
Abacavir
Tenofovir
Emtricitabine

Question 12

NRTIs moa

Answer 12

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

Question 13

NRTIs metabolism/interaction

Answer 13

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

Question 14

NRTI class tox

Answer 14

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

Question 15

zidovudine tox

Answer 15

bone marrow suppression
GI distress
megaloblastic anemia
lactic acidosis

Question 16

abacavir tox

Answer 16

hypersensativity

lactic acidosis

Question 17

lamuvudine tox

Answer 17

minimal-none

Question 18

tenofovir tox

Answer 18

nausea, vomiting, diarrhea, gas
renal tox
lactic acidosis

Question 19

Mutation in multidrug resistance for NRTIs

Answer 19

Q151M

K65R

Question 20

Non-nucleoside Reverse Transcriptase Inhibitors (nnrti’s)

Answer 20

efavirenz
nevirapine
delavirdine

Question 21

efavirenz moa

Answer 21

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

Question 22

NNRTIs metabolism

Answer 22

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

Question 23

NNRTIs class tox

Answer 23

skin rash
steven johnson/TEN
hepatotoxicity

Question 24

efavirez tox

Answer 24

CNS tox
hyperlipidemia
avoid in pregnancy

Question 25

NNRTIs multidrug resistance

Answer 25

K103N

Question 26

integrase inhibitor

Answer 26

raltegravir

Question 27

raltegravir moa

Answer 27

inhibits catalytic activity of HIV1 integrase | can't form HIV provirus

Question 28

raltegravir tox

Answer 28

CPK elevations, myositis, rhadomyolysis hypercholesterolemia increase trunk fat

Question 29

Protease Inhibitors

Answer 29

``` atazanavir darunavir lopinavir atazanavir fosamprenavir saquinavir ritonavir ```

Question 30

atazanavir/darunavir MOA

Answer 30

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

Question 31

Protease Inhibitors metabolism

Answer 31

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

Question 32

Protease Inhibitors class tox

Answer 32

``` hpyerglycemia GI intolerance lipodystrophy, hyperlipidemia bleeding in hemophiliacs CV ```

Question 33

Key HIV dosing notes

Answer 33

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