Term
| TAT (nonstructural HIV protein) does what? |
|
Definition
| regulates HIV transcription (regulates production of spliced or unspliced HIV transcripts) |
|
|
Term
| REV (nonstructural HIV protein) does what? |
|
Definition
| regulates HIV RNA transport (regulates transport of spliced or unspliced HIV RNA transcripts) |
|
|
Term
| NEF (nonstructural HIV protein) does what? |
|
Definition
| downregulates CD4 and MHC class I expression (reduce CD4 to prevent reinfection and reduce MHC1 to protect against cytotoxic t cells) |
|
|
Term
| VPU (nonstructural HIV protein) does what? |
|
Definition
| downregulates CD4 expression (lacking in HIV-2) |
|
|
Term
| VPR (nonstructural HIV protein) does what? |
|
Definition
| arrests host cell in proliferation in the G2 phase (LTR most active in G2) |
|
|
Term
| VIF (nonstructural HIV protein) does what? |
|
Definition
| blocks the activation of an endogenous antiviral protein in host cell |
|
|
Term
|
Definition
| HIV med. (entry inhibitor) block gp41-mediated fusion of either the gp120-CCR5 or CD4-pg120-CXCR4 complex (has to be injected subcutaneously) |
|
|
Term
|
Definition
| HIV med (entry inhibitor) blocks the binding of the CD4-gp120 complex with CCR5 |
|
|
Term
| what are the 3 nucleoside reverse transcriptase inhibitors used in HIV therapy? |
|
Definition
| zidovidine (AZT), lamivudine (3TC), emtricitabine |
|
|
Term
| which two nucleoside reverse transcriptase inhibitors are helpful when used together? |
|
Definition
| zidovudine and lamivudine (resistance to lamivudine reverses inhibition to zidovudine, together they have synergistic anti-viral activity) |
|
|
Term
| what other HIV-related problem does zidovudine help with? |
|
Definition
| HIV dementia bc it gets significant CNS levels |
|
|
Term
| what other diseases is lamivudine effective against? |
|
Definition
|
|
Term
| what is responsible for lamivudine resistance? |
|
Definition
| a specific mutation in HIV reverse transcriptase at codon 184 (may result in increased susceptibility to zidovudine) |
|
|
Term
| what is responsible for resistance to emtricitabine? |
|
Definition
| mutation in HIV RT at codon 184 (cross-reactive with lamivudine) |
|
|
Term
| what is the common nucleoTide RT inhibitor used in HIV therapy? |
|
Definition
|
|
Term
| what are the common non-nucleoside HIV RT inhibitors used in HIV therapy? |
|
Definition
| nevirapine, delavirdine, efavirenz |
|
|
Term
| how do non-nucleoside HIV RT inhibitors work? |
|
Definition
| all bind to the same non-active binding site on RT --> allosteric modification of active site --> RT inhibited via conformational change |
|
|
Term
| which HIV therapy drugs are not active against HIV2? |
|
Definition
| non-nucleoside HIV RT inhibitors (nevirapine, delavirdine, efavirenz) |
|
|
Term
| what is the most common toxicity assoc with non-nucleoside HIV RT inhibitors? |
|
Definition
| rash (mild-moderate or sometimes severe) |
|
|
Term
| which HIV drugs are counterindicated in pregnant women? |
|
Definition
| delavirdine and efavirenz |
|
|
Term
| what 3 drugs are a part of the new 3 drug combination therapy in HIV? |
|
Definition
| emtricitabine, tenofovir and efavirenz |
|
|
Term
| what are the most common protease inhibitors in HIV therapy? |
|
Definition
| saquinavir, ritonavir, lopinavir/ritonovir |
|
|
Term
| what are the most common side effects associated with protease inhibitors? |
|
Definition
| GI disturbance, metabolic complilcations (increased uric acid, cholesterol, LDL, trig), lipodystrophy syndrome, diabetes mellitus |
|
|
Term
| what are the downsides of saquinavir? |
|
Definition
| less anti-viral activity than other protease inhibitors, low bioavailability, extensive first pass metabolism |
|
|
Term
| what are the downsides of ritonavir? |
|
Definition
| many many drug interactions |
|
|
Term
| what is the most common integrase inhibitor? |
|
Definition
|
|
