Antiretroviral therapy for HIV Flashcards

1
Q

MOA of NRTI

A

competitive inhibition of reverse transcriptase to prevent formation of viral DNA from viral RNA
*DNA chain termination

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2
Q

ADRs of NRTIs

A

potential for lactic acidosis, hepatic steatosis, lipodystrophy
*No significant drug interactions

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3
Q

zidovudine (AZT)

A

nucleoside RTI

ADR: marrow suppression

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4
Q

didanosine (ddI)

A

nucleoside RTI

ADR: pancreatitis, neuropathy

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5
Q

stavudine (D4T)

A

nucleoside RTI

ADR: all shared ADRs of NRTIs increased; neuropathy

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6
Q

lamivudine (3TC)

A

nucleoside RTI

ADR: headache

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7
Q

emtricitabine (FTC)

A

nucleoside RTI

ADR: headache, diarrhea

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8
Q

abacavir (ABC)

A

nucleoside RTI

ADR: hypersensitivity reaction

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9
Q

tenofovir (TDF)

A

*nucleotide RTI
ADR: diarrhea, n/v, Fanconi syndrome (dz of prox renal tubules -> glucose, amino acids, uric acid, phosphate, bicarb passed into urine, instead of reabsorbed)

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10
Q

MOA of NNRTI

A

direct, non-nucleoside inhibitors of RT; doesn’t require metabolic conversion, not incorporated into viral DNA, additive effect to NRTI

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11
Q

ADR of NNRTI

A

rash, may -> Stevens-Johnson syndrome

significant drug interactions

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12
Q

nevirapine

A

NNRTI
ADR: rash, SJS, hepatotoxicity (esp CD4 > 250), modest CYP 3A4 inducer, may precipitate withdrawal in methadone maintenance patients

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13
Q

delaviridine

A

NNRTI
ADR: rash, SJS, HA, strong CYP 3A inhibitor
*rarely used d/t low potency

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14
Q

efavirenz

A

NNRTI

ADR: rash, SJS, neuropsych reaction, mod CYP 3A4 inducer, teratogenic

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15
Q

etravirine

A

NNRTI

ADR: rash, SJS, hyperlipidemia, modest CYP 3A4 inducer; CYP 2C9 and 2C19 inhibitor

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16
Q

rilpivirine

A

NNRTI

ADR: rash, HA, prolonged QT interval

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17
Q

MOA protease inhibitors

A

prevents viral protease from forming functional viral proteins necessary to mature viral particle and viral replication

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18
Q

ADR of protease inhibitors

A

GI distress, hyperglycemia, insulin resistance, hyperlipidemia, CAD, fat accumulation, hepatotoxicity
Metabolism by and inhibits CYP 3A4 (ritonavir most)
Metabolism induced by rifampin and phenytoin
Absorption reduced with rising gastric pH d/t H2-blockers and PPIs

19
Q

saquinavir

A

PI

ADR: n/v/d

20
Q

darunavir

A

PI

ADR: n/v, rash

21
Q

indinavir

A

PI

ADR: n/v, nephrolithiasis

22
Q

nelfinavir

A

PI

ADR: nausea, diarrhea

23
Q

fosamprenavir

A

PI

ADR: nausea, rash

24
Q

atazanavir

A

PI

ADR: increased bilirubin

25
Kaletra
AKA lopinavir + ritonavir PI used to boost levels of other PIs ADR: GI distress, hyperlipidemia
26
enfuviratide
fusion inhibitor; binds TM GP to prevent fusion of viral particle with CD4 cell membrane ADR: injection site rxn and HS rxns
27
maraviroc
entry inhibitor; antagonist of CCR5-R on CD4 necessary for HIV entry; active if resistance to other drug classes ADR: cough, rash, infections, substrate of CYP 3A4 (intx w PIs)
28
MOA integrase inhibitors
blocks integrase enzyme necessary for integration of viral DNA into cellular DNA INSTI = integrase strand transfer inhibitor
29
ADR integrase inhibitors
diarrhea, nausea, HA, myositis (monitor CPK)
30
Truvada
2NRTIs | emtricitabine + tenofovir
31
Combivir
2 NRTIs | AZT + lamivudine
32
Epizicom
2 NRTIs | ABC + lamivudine
33
Trizivir
3NRTIs (not recommended) | AZT + lamivudine + ABC
34
Atripla
NNRTI + 2NRTI | efavirenz + emtracitibine + tenofovir
35
Complera
NNRTI + 2NRTI | rilpivirine + emtracitibine + tenofovir
36
Who to test for HIV drug resistance and what to test for?
All HIV-infected people when they enter care Genotype testing for ARV-naive patients Look for mutations in RT and protease genes and INSTI resistance
37
Regimen for pregnant women
lopinavir/ritonavir (Kaletra) + AZT/lam (Combivir) | *PI may increase hyperglycemia risk
38
When is transmission of HIV from pregnant woman to infant most likely?
During labor/delivery
39
Regimen for infant of HIV+ mother
AZT for first 6 weeks of life
40
Teratogenic ARV drug
efavirenz
41
Pre-exposure prophylaxis for high-risk adults
Truvada
42
Post-exposure prophylaxis for occupational exposure
3 or more drugs | for all exposures
43
Post-exposure prophylaxis for non-occupational exposure (sex, drugs)
3 or more active drugs if source patient known to be HIV+ or exposure event high risk for transmission
44
When to start post-exposure prophylaxis
Within 72 hours of exposure and continue for 4 weeks | with follow-up HIV-Ab testing for 4-6 months post-exposure