HIV Pharmacology

Question 1

NRTI

Answer 1

emtricitabine
tenofovir

nucleoside reverse transcripatase inhibitors

Question 2

NNRTI

Answer 2

efavirenz

Question 3

PI

Answer 3

ataanavir
darunavir
lopinavir
ritonavir

Question 4

INSTI

Answer 4

raltegravir

Question 5

CCR5 antagonist

Answer 5

maraviroc

Question 6

fusion inhibitors

Answer 6

enfuviritide

Question 7

antiretroviral treatment

Answer 7

backbone and a base

backbone - two NRTIs

base - NNRTI, PI, INSTI, CCR5 blocker

Question 8

backbone

Answer 8

emtricitabine

tenofovir

Question 9

pregnant women

Answer 9

polinavir/ritonavir and zidovudine/lamivudine BID

Question 10

preferred base drugs

Answer 10

efavirenz

ritonivir boosted atazanavir or darunavir

raltegravir

Question 11

HIV virus

Answer 11

RNA retrovirus

gp41, gp120, p24, p17

drug choice depends on genetic analysis of HIV virus patient has
-reverse transcriptase, protease, integrase, ribonuclease - important genetic targets (pol)

Question 12

coreceptor

Answer 12

CCR5 - allows fusion and entry of HIV

gp120, gp41 involved

Question 13

primary infection

Answer 13

initial viremia spike - then decreases

Question 14

eradication of HIV

Answer 14

cannot occur

Question 15

primary goal of antiretroviral therapy

Answer 15

reduce morbidity and increase duration of life

Question 16

combination drugs

Answer 16

minimize development of resistance

billions of copes of viral DNA produced per day - lots of mutations

Question 17

initiation of therapy

Answer 17

CD4 < 350 - 500

and all patients regardless of CD4 - pregnant, HIV associated nephropathy, and have hep B virus coinfection

Question 18

IV drug users

Answer 18

often hep B and HIV coinfection

Question 19

indicator of response

Answer 19

viral load

Question 20

drug resistance testing

Answer 20

genotypic assays
-to detect mutations

test all patients when first begin drug treatment

phenotypic assays - ability of virus to grow in antiretroviral drug presence

Question 21

ART

Answer 21

antiretroviral therapy

decrease risk of resistance

Question 22

HAART

Answer 22

highly active anti-retroviral therapy (old name)

Question 23

NRTI MOA

Answer 23

tenofovir, emtricitabine

nucleoside/nucleotide

reverse transcriptase inhibitor
-causes chain termination

only nucleotide - tenofovir

tenofovir - Hep B
emtricitabine - well tolerated
zidovudine (AZT) - first licensed

Question 24

NNRTI MOA

Answer 24

efavirenz

non-nucleoside

bind to reverse transcriptase blocking RNA and DNA dependent DNA polymerase activity

Question 25

not in pregnant women

Answer 25

efavirenz - embryotoxic

Question 26

ritonavir boosting

Answer 26

inhibit metabolism of other PIs by binding to CYP3A4

Question 27

PI MOA

Answer 27

gag and gag-pol gene product

prevent this viral protease

get immature noninfectious viral particles

Question 28

PI combination

Answer 28

this was a breakthrough drug - prolonged survival with even advanced HIV infection

Question 29

INSTI MOA

Answer 29

integrase strand transfer inhibitor

block integrase that catalyzes process of viral DNA insertion into host genome

-prevents viral DNA from integrating with cellular DNA

Question 30

CCR5 antagonists

Answer 30

co-receptors are CCR5 (early) and CXCR4 (later)

blocks receptor and prevents entry of virus into cell

can assay for CCR5 - coreceptor tropism assay

Question 31

fusion inhibitor

Answer 31

small peptide

reserved for pt on regimen and have developed resistance or tx failure

receptors for HIV virus - are CD4 and CCR5

MOA - binds gp41 subunit and preventionof conformation changes necessary for fusion

must be given BID subQ - drawback