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Antiretroviral agents
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34
Medical
Graduate
07/21/2012

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Term
Azidothymidine, Zidovudine class
Definition
NRTIs
Term
NRTIs
Definition
Azidothymidine, Zidovudine, Didanosine, Zalcitabine, Lamivudine, Stavudine, Emtricitabine,
Term
thymidine analogue. First phosphorylated by cellular thymidine kinase

______triphosphate terminates viral dNA synthesis by RT
Definition
Zidovudine
Term
Initial agent of choice for HIV infection w/ CD4 < 500 /mm3
Definition
Zidovudine
Term
combination w/ zalcitabine has shown higher survival
Definition
Zidovudine
Term
NRTI approved for treatment of advanced HIV infection in adults and children over 6 months
Definition
Didanosine,
Term
NRTI approved for treatment of advanced HIV infection in adults and children over 6 months INTOLERANT TO OTHER THERAPIES
Definition
Stavudine
Term
approved for HIV infection in combo with zidovudine in pts w/ CD4 counts <300mm3
Definition
Zalcitabine
Term
drugs that inhibit glucuronidation (fluconazole) may increase toxicity of this drug group
Definition
NRTIs
Term
Bone marrow suppression (granulocytopenia and anemia)
Definition
NRTIs
Term
painful sensory peripheral neruopathy
Definition
Stavudine, Zalcitabine
Term
guanine analogue NRTI useful in HIV infections. Used in viruses rsistant to 3TC (Lamivudine) and AZT(Zidovudine)
Definition
Abacavir
Term
NRTIs sometimes called NtRTIs
Definition
Tenofovir, Adefovir
Term
Nucleotide analogs approved for HIV as well as HBV infections
Definition
Tenofovir, Adefovir
Term
activation very selective for HIV-1 (not HIV 2) virus specific reverse transcriptase
Definition
NNRTIs
Term
NNRTIs that bind directly to a site on the viral RT that is near or distinct form the NRTIs. Do not compete with nucleoside triphosphate or require phospohrylation to be active.
Definition
Nevirapine, Delavirdine, Efavirenz
Term
block RNA dependent and DNA dependent DNA polymerases
Definition
Nevirapine, Delavirdine, Efavirenz
Term
second generation NNRTI shown t have low resistance when compared to others
Definition
Etravirine
Term
Second generation NNRTI.
Pyrimidine analogue.
high potentcy, long half life, reduced adverse effects compared to Efavirenz
Definition
Rilpivirine
Term
non peptide PI covers HIV protease variants resistant to other PIs and has shown to lower development of resistance
Definition
Tipranavir
Term
HIV aspartate protease inhibitor that inhibits cleavage of the polypeptide precursors that generate the structural proteins and enzymes of the virus
Definition
Tipranavir
Term
thrombocytopenia, hyperbilirubinemia, renal damage (hydration reduces
Definition
protease inhibitors (avirs)
Term
Use of these drugs with Rifampin is contraindicated (see resistance within a year)
Definition
protease inhibitors (avirs)
Term
Protease inhibitors contraindicated w/ use of
Definition
Rifampin
Term
36 amino acid peptide derived from HIV envelope glycoprotein gp41
Definition
Enfuvirtide
Term
prevents fusionof viral and cellular membranes blocking HIV 1 from entering
Definition
Enfuvirtide
Term
reserved for salvage therapy for those w/ advance disease or resistance to current treatments
Definition
Enfuvirtide
Term
binds to FIRST HEPTAD REPEAT in gp41
Definition
Enfuvirtide
Term
serious injection site reactions, increased bacterial infections, diarrhea and nasuea
Definition
Enfuvirtide
Term
inhibits HIV entry into human cells through CCR5 co-receptor on Th cells
Definition
Maroviroc
Term
Effective at reducing viral load in patients w/ CCR5-tropic HIV strains
Definition
Maraviroc
Term
not effective vs. virus targeting CXCR4 co receptor (CXCR4-tropic HIV) low therapeutic vs HIV w/ dual tropism
Definition
Maraviroc
Term
hepatotoxicity and symptoms of allergic reaction have reported
Definition
Maraviroc
Term
new class of antiretroviral drug that inhibits INTEGRATION
Definition
Raltegravir
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