ID exam 4 Flashcards
Abacavir MOA
inhibits the activity of HIV-1 reverse transcriptase by competing with the natural substrate leading to chain termination
Abacavir DDIs
co admin with ethanol
Abacavir ADE
hypersensitivity syndrome
maculopapular rash
respiratory
Lamivudine MOA
inhibits reverse transcriptase competitively and acts as a chain terminator of viral DNA synthesis
Lamivudine DDIs
co admin with sorbitol
Lamivudine ADRs
headache, nausea, malaise
Tenofovir Disoproxil Fumarate MOA
competitive inhibitor of viral reverse transcriptase and chain termination
Tenofovir Disoproxil Fumarate ADME
low protein binding
take with high fat food
Tenofovir Disoproxil Fumarate DDI
Didanosine
Atazanavir
Lopinavir/ritonavir
Tenofovir Disoproxil Fumarate ADR
rash, diarrhea, headache, pain, nausea
Emtricitabine MOA
inhibit HIV-reverse transcriptase and chain terminates
Emtricitabine ADME
low protein bound
Emtricitabine DDIs
CYP3A4 and many others
Emtricitabine ADEs
hyperpigmentation of skin
Tenofovir Alafenamide MOA
competitive inhibitor of viral reverse transcriptase and cause chain termination
Tenofovir Alafenamide ADME
high protein bound
hydrolyzed within cells
uncleaved prodrug
Tenofovir Alafenamide ADRs
headache, ab pain, fatigue, cough, nausea, back pain
Zidovudine MOA
inhibit reverse transcriptase via chain termination
Zidovudine ADME
hepatic glucuronidation
Zidovudine DDIs
ganciclovir
doxorubicin
ribavirin
Zidovudine ADE
myalgia, bone marrow suppression, myopathy
Etravirine MOA
non-competitive inhibitor of reverse transcriptase
Etravirine AMDE
high protein bound
administer following a meal
Etravirine DDIs
CYP3A4
Etravirine ADR
rash
peripheral neuropathy
Rilpivirine MOA
non-competitive inhibitor of reverse transcriptase
Rilpivirine DDI
do not co admin with other NNRRIs
CYP3A4
Rilpivirine ADR
depression, insomnia, headache, rash
QT prolongation
Doravirine MOA
non-competitive inhibitor of reverse transcriptase
Doravirine ADE
nausea, dizziness, headache, fatigue, diarrhea, ab pain, abnormal dreams
Ritonavir MOA
prvent proteolytic cleavage of HIV polypeptides and maturation of viral particles
Ritonavir ADME
high protein bound
rapid absorption
Ritonavir DDIs
midazolam, triazolam, fentanyl, ergot derivatives
Ritonavir ADRs
GI, neurologic disorders, rash, fatigue
Atazanavir MOA
prevent proteolytic cleavage of HIV precursor polypeptides and maturation of viral particles
Atazanavir DDIs
PPIs
Atazanavir ADRs
GI, insomnia, peripheral neurologic symptoms, myalgia, depression, fever
Darunavir MOA
prevent proteolytic cleavage of HIV precursor polypeptides and maturation of viral particles
Darunavir ADME
high protein bound
Darunavir ADR
GI, headahce, ab pain
Raltegravir MOA
inhibit viral integrase enzyme blocking viral DNA into host genome
Raltegravir DDI
rifampin
Raltegravir ADE
insomnia, headache, nausea, asthenia, fatigue
Elvitegravir MOA
inhibit viral integrase enzyme blocking viral DNA into host genome
Elvitegravir ADME
high protein bound
Elvitegravir DDI
protease inhibitors
ritonavir
Elvitegravir ADRs
N/D
Dolutegravir MOA
inhibit integrase enzyme by binding to amino acids in active site and block strand of transfer step
Dolutegravir ADME
high protein bound
UGT1A1 metabolization
Dolutegravir DDIs
metabolic inducers
2 hours before or 6 hours after cations
Dolutegravir ADRs
insomnia and headache
Bictegravir MOA
targets HIV integrase and prevents strand transfer activity and integration of provirus into host genome
Bictegravir ADME
not for severe hepatic impairment
Bictegravir DDIs
rifampin
antacids
Bictegravir ADRs
lactic acidosis, liver problems, new or worsening kidney problems
Cabotegravir MOA
integrase strand transfer inhibitor
Cabotegravir ADME
IM slow absorption
high protein bound
Cabotegravir DDIs
other antiretroviral HIV meds
UGT1A1 or 1A9 inducers
-rifampicin, carbamazepine, oxcarbazepine, phenytoin, phenobarbital
Cabenuva
Cabotegravir ADRs
IM: inj site rxn, headache, fever
Oral: headache, hot
both: depressive, insomnia, rash
Cobicistat MOA
inhibit P450 3A4
Cobicistat ADME
high protein bound
Cobicistat DDI
CYP3A4, CYP2D6
Cobicistat DDIs
atazanavir causes jaundice and rash
Lenacapavir MOA
interfere with essential steps in viral replication by binding between viral capsid protein subunits and hexamers
Lenacapavir ADME
sub q: long absorption
high protein bound
Lenacapavir DDI
p-gp, UGT1A1
Lenacapavir ADR
itching, swelling, redness, pain, hardened skin, small mass/lumps at injection site
Enduvirtide MOA
disrupt gp41 rendering it incapable of mediating membrane fusion to allow viral entry into host cell
Enduvirtide ADME
sub q inj
high protein bound
undergoes catabolism
Enduvirtide DDI
lots of CYPs
ritonavir, rifampin
Enduvirtide ADR
inj site rxn
pneumonia
hypersensitivity rxn
respiratory, nephritis, guillain-barre syndrome
Maraviroc MOA
block HIV outer envelope binding of gp120 to CCR5
Maraviroc DDIs
CYP3A4 and Pgp
Maraviroc ADRs
pyrexia, upper rti, rash, musculoskeletal, ab pain, dizziness
Ibalizumab MOA
block HIV from binding to CCR5 and CXCR4 on CD4 cells
Ibalizumab ADME
need loading dose
Ibalizumab ADR
diarrhea, dizziness, nausea, rash
Fostemsavir MOA
dephosphorylated product that binds directly to gp120 and inhibits viral interaction with CD4 receptors
Fostemsavir ADME
hydrolysis, oxidation, and UGT
Fostemsavir DDIs
temsavir increase plasma concentration of grazoprevir and voxilaprevir
rifampin
Fostemsavir ADR
n/v/d
ab pain
dyspepsia
fatigue
sleep disturbance
immune reconstitution inflammatory syndrome
PrEP
TDF, FTC
TAF, FTC (M, TGF only)
Cabotegravir (IM q8w)
Lenacapavir
capsid inhibitor
purpose-1 (cis-women)
purpose-2 (MSM and trans-women)
sq 6 months
PrEP indications
All sexually active adults and adolescents should be informed about PrEP
For sexually active adults and adolescents
Goal of therapy for HIV
reduce acquisition of HIV infection with resulting morbidity, mortality and cost to individuals and society
What to monitor every 3 months for PrEP
HIV and HIV RNA test
sign/symptoms
pregnancy test
STI testing
What to monitor every 6 months for PrEP
renal toxicities
STI testing
What to monitor every 12 months for PrEP
Cr/CrCl
Follow up and monitoring for cabotegravir IM 1 month and 2 months
1: HIV, HIV RNA, signs, administer CAB
2: HIV, HIV RNA, signs, administer CAB
Follow up and monitoring for cabotegravir IM 4, 6, 12 months
4: STI
6: STI
12: evaluate need for PrEP
PEP HIV treatment
ART to prevent HIV infection after a potential exposure
medical emergency
HIV - baseline, 4-6 wk, 3 months
Pregnancy test for women
Who to consider for PEP
HIV-negative or HIV status unknown within the last 72 hours
May have a known or known exposure to HIV through:
-sex/sexual assalt
-shared needles
-occupational exposure