19. HIV Agents

Question 1

burst of viral antigen > CD4 T cells decline > anti-HIV antibody gp120 increases > opportunistic infection

Answer 1

clinical progression of HIV disease

Question 2

attachment > fusion > reverse transcription > integration > genome replication > budding > protein cleavage > mature virion

Answer 2

human immunodeficiency virus life cycle

Question 3

inhibit attachment

Answer 3

co-receptor antagonist

Question 4

inhibit fusion

Answer 4

fusion inhibitors

Question 5

inhibit reverse transcription

Answer 5

nucleoside reverse transcriptase inhibitors / non-nucleoside transcriptase inhibitors

Question 6

blocks integration

Answer 6

integrase strand transfer inhibitors

Question 7

blocks protein cleavage

Answer 7

protease inhibitors

Question 8

combination of two or three antri-retroviral drugs, from at least two different classes

Answer 8

standard of care for HIV therapy

Question 9

abacavir, lamivudine, tenofovir disproxil fumarate, tenofovir alafenamide, emtrictiabine

Answer 9

nucleoside reverse transcriptase inhibitors

Question 10

efavirenz, doravirine, rilpivirine

Answer 10

non-nucleoside reverse transcriptase inhibitor

Question 11

darunavir, ritonavir, atanzanavir

Answer 11

protease inhibitors

Question 12

bictegravir, raltegravir, dolutegravir

Answer 12

integrase strand inhibitors

Question 13

enfuvirtide

Answer 13

fusion inhibitor

Question 14

maraviroc

Answer 14

co-receptor antagonist

Question 15

2 NRTI antivirals + 1 INSTI inhibitor

Answer 15

recommended initial treatment for HIV

Question 16

1 NRTI + 1 INSTI

Answer 16

new two drug regiment for HIV

Question 17

act at the active site of reverse transcriptase, require cellular kinases to converted to triphosphate form, approved for chronic hepatitis B, mitochondrial damage

Answer 17

NRTIs

Question 18

associated with lipodystrophy syndrome

Answer 18

zidovudine and stavudine

Question 19

cytosine analogue, single base change confers high level resistance, included in recommended initial treatment, can be used for heptatis b

Answer 19

lamuvidine

Question 20

flourinated analogue of lamivudine, longer half life, headache, nausea, diarrhea, resistance by single base pair change, recommended in initial treatment regiment for HIV

Answer 20

emtricitabine

Question 21

guanosine analogue, hypersensitivity in 4% of patients leading to fever, skin rash, fatigue, GI symptoms, associated with HLA-B5701, genetic screening must be done prior to treatment, resistance by multiple mutations, used in recommended initial treatment regimen

Answer 21

abacavir

Question 22

prodrug of tenofovir, analogue of adenosine, crosses the placenta, recommended for initial treatment, contraindicated in renal patients

Answer 22

tenofovir disoproxil fumarate

Question 23

phosphonoamidate prodrug of tenofovir, metabolized intracellularly by cathepsin A, higher concentrations in HIV replicating cells so more specific, bone and kidney toxicities

Answer 23

tenofovir alafenamide

Question 24

acts on integrase enzyme

Answer 24

integrase inhibitors

Question 25

analogue integrase strand transfer inhibitor, safe, resistance by single mutation

Answer 25

raltegravir

Question 26

integrase strand transfer inhibitor, nausea, diarrhea, headache, recommended initial treatment of HIV

Answer 26

bicetegravir

Question 27

integrase strand transfer inhibitor, combined with antiretroviral therapy in a single pill, insomnia, headache, still works if resistance against raltegravir and elvitegravir, increased risk of neural tube defects, contraindicated in pregnancy

Answer 27

dolutegravir

Question 28

boosted PI + 2 NRTIs, NNRTI + 2 NRTIs, INSTI + 2 NRTIs

Answer 28

recommended initial regimens in certain clinical situations - 2020

Question 29

target HIV protease by mimicing a peptide blocking maturation after budding, multiple mutations necessary for high level resistance

Answer 29

protease inhibitors

Question 30

non-peptidic protease inhibitor, given orally, coadminstered with pharmokinetic enhancer, skin rash, GI intolerance, headache, 90% are still susceptible, recommended initial regimen for HIV

Answer 30

darunavir

Question 31

peptide, once daily oral administration, requires acid for absorption so no antiacids, inhibitor of CYP3A4 and CYP2C9, multiple codon changes for high level resistance, included in recommended initial treatment for HIV

Answer 31

atanzavir

Question 32

peptidomimetic protease inhibitor, 1st of its class approved, given orally, most commonly used as pharmacokinetic booster, potent inhibitor of CYP3A4 and 2D6s, multiple mutations for high level resisance, recommended in initial treatment of HIV

Answer 32

ritonavir

Question 33

pharmacokinetic enhancer, inhibits CYP3A enzymes, no antiviral action on it’s own

Answer 33

cobicistat

Question 34

target reverse transcriptase, do not require phosphorylation, not active against HIV-2, single amino acid changes confer resistance

Answer 34

reverse transcriptase inhibitors

Question 35

non-nucleoside reverse transcriptase inhibitor, orally adminstered, induces CYP3A4s, associated with birth defects during pregnancy

Answer 35

efavirenz

Question 36

non-nucleoside reverse transcriptase inhibitor, given orally, CYP3A4 substrate, resistance to this drug can confer resistance to other NNRTIs

Answer 36

doravirine

Question 37

non-nucleoside reverse transcriptase inhibitor, administered orally, contraindicated with proton pump inhibitors, single base change confers resistance, recommended initial regimen in HIV treatment

Answer 37

rilpivirine

Question 38

drugs reserved for treatment experienced patients

Answer 38

CCR5 receptor antagonists,

Question 39

blocks co-receptor binding

Answer 39

CCR5 receptor antagonists

Question 40

co-receptor antagonist, given orally, resistance through changes in tropism or mutations in gp120 blocking binding to it, resistance also by HIV virions that enter through CCR4 pathway instead, screen for tropism before use

Answer 40

maraviroc

Question 41

blocks virus envelope fusion with plasma membrane, blocks confirmational change of gp41 preventing binding to gp120 by binding to prefusion complex

Answer 41

fusion inhibitors

Question 42

36 amino acid peptide fusion inhibitor, administered in twice daily subcutaneous injection, painful erythematous nodule at the site of infection, high level resistance requires multiple mutations in gp41 gene

Answer 42

enfuvirtide

Question 43

combination of TDF and emtricitibine, recommended for individuals in certain high risk groups for HIV infection like HIV negative individual with HIV positive partner, commericial sex workers, injection drug users, assess pregancy if women are pregnant

Answer 43

pre-exposure prophylaxis for HIV

Question 44

recommended in groups like blood transfusion, needle sharing during injection drug use, percutaneous needlestick, within 72 hours of exposure, 28 day treatment, similar 3 drug regiment as preferred combination antiretroviral therapy for initial therapy for most people with HIV, testing for HIV is included in management

Answer 44

post-exposure prophylaxis