Antiviral - HIV Flashcards
NRTI MOA
Competitive inhibition of reverse transcriptase by incorporating itself into DNA and cause premature chain termination
NRTI adverse effect?
Lactic acidosis
NRTI suffix
-dine
Lamivudine adverse
Peripheral neuropathy
Lamivudine treament
Hepatitis B infection
Tenofovir
Nucleotide analogue, does not need phosphorylation and treats Hep B
Zidovudine
Nucleoside analogue used during pregnancy to reduce vertical transmission
Zidovudine adverse
Myelosuppression
Granulocytopenia
Lipodystrophy
Staviduine adverse
Nucleoside analogue that can cause peripheral neuropathy
Didanosine adverse
Can cause dose dependent pancreatitis
Abacavir adverse
Hypersensitivity reaction (type 4) associated with HLA-B57
Emtricitabine adverse
Hyperpigmentation of palms and soles
Do nucleotide or nucleoside analogues need to be phosphorylated?
Nucleoside
These end with the suffix -dine
NNRTIs
Non-nucleoside reverse transcriptase inhibitors
NNRTI MOA
Do not need to be phosphorylated to bind directly to HIV reverse transcriptase causing chain termination
NNRTI adverse effects
Hepatic failure CNS issues Teratogenic CYP450 Steven Johnson Syndrome
NNRTI drugs
Delavirdine
Efavirenz
Nevirapine
Protease Inhibitors suffix
“-navir”
Protease Inhibitors MOA
Do not need to be phosphorylated to inhibit cleavage of virions
Protease inhibitors adverse effects
Hyperglycemia
Dyslipidemias
Lipodystrophy
Inhibit CYP450
Indinavir adverse effects
Nephrolithiasis, so patients must maintain adequate hydration
Ritonovir adverse effects?
Greatest inhibition of CYP450, especially with Rifampin
What cells do HIV target/infect?
CD4+ T cells
Macrophages
Dendritic Cells
HIV virion proteins
p24 and p7
HIV envelope proteins
gp41 and gp120
Entry inhibitors MOA
Maraviroc binds/blocks the CCR5 receptor inhibit gp120 binding
Entry inhibitor drug
Maraviroc
Fusion inhibitors MOA
Binds to gp41 envelope proteins to block their fusion
Fusion inhibitor drug
Enfuvirtide
What HIV gene encodes for protease, reverse transcriptase, and integrase?
Pol gene
Integrase inhibitors MOA
Binding viral integrase to not allow viral DNA to integrate into host chromosomes
Integrase inhibitor drug
Raltegravir
Integrase inhibitors adverse effect
Rhabdomyolysis