HIV therapy Flashcards
HIV protease inhibitor that inhibits cytochrome P-450
Ritonavir
Suffix for Protease inhibitors
-navir
Mechanism of NRTIs
Inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain in 3’ to 5’ direction
NRTIs lack what that leads to DNA chain termination
3’ OH group needed for phosphodiester bond formation in 3’ to 5’ direction
Only NRTI that is a nucleotide
Tenofovir - all others are nucleosides
This is needed to activate NRTIs
Phosphorylation
All NRTIs are associated with these side effects
Mitochondrial toxicity, lactic acidosis
NRTIs that may cause peripheral neuropathy
Lamivudine, stavudine, didanosine
NRTIs that treat Hepatitis B
Lamivudine and tenofovir
NRTI that does not require phosphorylation for activation
Tenofovir
NRTI used in pregnancy and breastfeeding to reduce vertical transmission
Zidovudine
Zidovudine side effect
Myelosuppression leading to anemia and neutropenia, and lipodystrophy
NRTIs that cause lipodystrophy (central adiposity)
Zidovudine and Stavudine
Side-effect of didanosine
Pancreatitis
NRTI contraindicated in HLA-B57:01 allele mutation
Abacavir
Complication of Abacavir in HLA-B57:01 mutation
Delayed type IV hypersensitivity reaction resulting in rash
NRTI that causes hyperpigmentation of palms and soles
Emtricitabine
NNRTIs
Delavirdine, Efavirenz, Nevirapine (DEN)
NNRTIs contraindicated in pregnancy
Delavirdine and Efavirenz (ED)
NNRTI that causes vivid dreams and CNS symptoms
Efavirenz
Complication common to all NNRTIs
Rash (SJS-TEN) and hepatotoxicity
Do NNRTIs require activation
No - phosphorylation not needed
Mechanism of NNRTIs
Direct binding and allostering inhibtion of HIV reverse transcriptase halting DNA polymerase activity
Jaundiced yellow glow and liver spots within 6 weeks indicates treatment with these HIV drugs
NNRTIs
Protease inhibitor mechanism
Inhibit HIV POL genes that make HIV proteases needed to cleave polypeptide products of HIV and mRNA into functional parts
Protease inhibitor side effects
Hyperglycemia from insulin resistance, dysliipidemia, lipodystrophy
Protease inhibitor that causes nephrolithiasis
Indinavir
Protease inhibitor that boosts the concentration of other drugs
Ritonovir
CYP450 inducer used in TB, reduces protease inhibitor concentrations
Rifampin
Alternate drug used in TB to avoid lowering protease inhibitor concentrations in HIV patients
Rifabutin
Cells infected in HIV
CD4+ T-cells, macrophages, and dendritic cells
What gene codes for virion core proteins
gag structural gene
Core proteins coded by gag structural gene
p24 and p7
HIV viral proteins needed for infiltratrion
gp41 and gp120 envelope proteins
Gene that codes for gp41, gp120 envelope proteins
env structural gene
gp120 mechanism for entry into host cell
Binds to host cell CD4 molecule and chemokine receptor CXCR4 or CCR5
Entry inhibitor that binds CCR5
Maraviroc
Maraviroc mechanism
Binds CCR5 on CD4 host cell preventing gp120 binding
HIV envelope protein that facilitates fusion to host cell
gp41
Fusion inhibitor that binds gp41
Enfuvirtide
Enfuvirtide mechanism
Binds gp41 inhibiting viral entry
Envelope proteins gp41 and gp120 are sent to what cell structure before exiting infected cell
Endoplasmic reticulum
HIV therapy drugs that inhibit reverse transcriptase
NRTIs and NNRTIs
Resistance to NRTIs and NNRTIs is due to what
Mutations in the viral pol gene that produce enzymes resistant to binding
Integrase inhibitors
Raltegravir, Elvitegravir, Dolutegravir
Prevents transcription of viral mRNA
Integrase inhibitors
HIV therapy drugs that increase creatine kinase levels
Integrase inhibitors
Mutations in pol gene can lead to…
Resistance to NRTIs, NNRTIs, integrase and protease inhibitors
Side effect of integrase inhibitors
Rhabdomyolysis (increased CK levels)