HIV Drugs Flashcards
Enfuvirtide/Fuzeon
Fusion inhibitor; Binds gp41
SubQ injection
AE: Injection site reaction, increased rate of bacterial pneumonia, hypersensitivity
Maraviroc
CCR5 antagonist (only works against CCR5-tropic virus)
Consider use if failed 2 regimens or other ART
Blocks co-receptor to viral entry
Metabolized by p450
AE: cough, fever, rash, URT infection, abdominal pain, postural dizziness
Raltegravir
Intregrase inhibitor
approved for patients that have failed other treatments
Rifampin can enhance elimination, Divalent cations may inhibit actions
Zidovudine (AZT), lamivudine (3TC), emtricitabine, abacavir (ABC)
Nucleoside analogues
Inhibit revers transcriptase
AE: Pancreatitis, peripheral neuropathy, myopathy, cardiomyopathy, heaptic steatosis, lipid dystrophy
Zidovudine- induced anemia and neutropenia
Abacavir- hypersensitivity (HLA dependent)
All are renal eliminated (dose adjusted w/ renal insufficiency)
p450 metabolism
Tenofovir
Nucleotide analogue
Does not require phosphorylation
Efavirenz, delavirdine, nevirapine
Non-Nucleoside reverse transcriptase inhibitors
inhibit reverse transcriptase but do not act at the active site
Nevirapine- Rash (steven-johnson syndrome reported), hepatitis (substrate for CYP450 and inducer of 3A)
Efavirenz- teratogenic in animals
Ritonavir, lopinavir, amprenavir
Protease inhibitor
AE: N/V/D, hyperglycemia, lipodystrophy, hyperlipidemia, hepatotoxicity, osteonecruses/osteopenia/osteoporosis
Inhibitor of p450 (ritonavir used to prolong action of other drugs)
NNRTI based regiments
Efavirenz + tenofovir/emtricitabine or zidovudine/lamivudine
except for pregnant women or women with pregnancy potential
PI based regiments
Lopinavir/Ritonavir+ (tenofovir/emtricitabine or zidovudine/lamivudine)
Integrase based regiments
Raltegravir + (tenofovir/emtricitabine or zidovudine/lamivudine)
