Use LEFT and RIGHT arrow keys to navigate between flashcards;
Use UP and DOWN arrow keys to flip the card;
H to show hint;
A reads text to speech;
67 Cards in this Set
- Front
- Back
|
what drug inhibits GP41 fusion and penetration |
Enfuvirtide |
|
|
what inhibits the conformational change of the GP120-GP41 complex by competing for CCR5 binding site
|
Maraviroc |
|
|
what competes with each other for phosphorylation |
two NRTI's with the SAME base analog |
|
|
should two NRTI's with the SAME base analog be used together |
no |
|
|
why are two NRTI's given |
to combat resistance |
|
|
name the NRTI's mentioned in lectured |
Zidovudine
Stavudine Zalcitabine Lamivudine Emtricitabine Abacavir Tenofovir Didanosine |
|
|
how are NRTI's primarily excreted |
renal |
|
|
when would a NRTI dose be adjusted |
renal insufficiency |
|
|
what is the exception to the previous |
Abacavir |
|
|
which NTRI is MOST responsible for pancreatitis |
Didanosine |
|
|
which 2 NTRI's are MOST responsible for neuropathy |
Zalcitabine Stavudine |
|
|
which NTRI is responsible for myelodepression and leukopenia |
Zidovudine |
|
|
which NTRI is Least toxic and Least potent as well as responsible for neutropenia and GI |
Lamivudine |
|
|
which drug is responsible for Neuropathy AND hyperlipidemia |
Stavudine |
|
|
which NTRI is responsible for allergic reactions |
abacavir |
|
|
which NTRI causes hyperpigmentation of palms and sole plus GI |
Emtricitabine |
|
|
which NRTI RARELY causes renal problems |
tenofovir |
|
|
what are NRTI's used for |
treatment and prophylaxis of HIV |
|
|
which NRTI is used to prevent vertical transmission of HIV in pregnancy |
Zidovudine |
|
|
a NRTI can be combined with what |
a protease inhibitor |
|
|
what does HAART do |
DECREASES viral RNA reversal of decline in CD4 cells DECREASES opportunistic infections |
|
|
what do NRTI's and NNRTI's do |
inhibit the viral reverse transcriptase |
|
|
what does the previous inhibition do |
prevents the synthesis of the essential DNA intermediate |
|
|
what are NNRTI's |
highly selective, noncompetitive inhibitors of HIV-1 reverse transcriptase |
|
|
what do they do |
they bind to HIV-1 RT at an allosteric hydrophobic site which induces a confomational change that results in enzyme inhibition |
|
|
where is this allosteric site |
adjacent to the active site |
|
|
do NNRTI's require phosphorylation |
no |
|
|
what are NNRTI's metabolized by |
CYP450 |
|
|
what are the 4 NNRTI drugs |
Efavirenz Nevirapine Etravirine Delavirdine |
|
|
which NNRTI causes nightmares, insomnia, dizziness and headache |
Efavirenz |
|
|
which three NRTI's cause rash |
Nevirapine Etravirine Delavirdine |
|
|
which NNRIT causes rash AND hepatitis |
Nevirapine |
|
|
which NNRTI causes rash AND GI upset |
Etravirine |
|
|
which NNRTI SOLELY causes a rash |
delavirdine |
|
|
a specific protease is needed for what during the replication cycle of HIV |
to process gag and pol proteins into MATURE HIV components |
|
|
what happens if the protease is missing |
noninfectious HIV virions are produced |
|
|
why are HIV protease inhibitor specific to HIV protease |
it differs slightly from human protease |
|
|
type of protease resistance |
pol gene mutation (encode protease) |
|
|
what are the 9 protease inhibitors SINRAALTD |
1. Saquinavir 2. Indinavir 3. Nelfinavir 4. Ritonavir 5. Amprenavir 6. Atazanavir 7. Lopinavir 8. Tipranavir 9. Darunavir |
|
|
all protease inhibitors interact with other drugs due to what |
their effect on the drug metabolizing enzymes CYP450 |
|
|
all protease inhibitors cause what 6 |
glucose intolerance (type 2 diabetes) GI intolerance Paresthesia Dizziness Rash Headache |
|
|
which PI is the most potent inhibitor of CYP 3A4 |
4. Ritonavir |
|
|
which PI is the least toxic and has low bioavalability |
1. Saquinavir |
|
|
what should always be given with Saquinavir |
4. Ritonavir |
|
|
what are three very important adverse drug reactions of PI's |
Glucose intolerance Dyslipidemia Lipodystrophy |
|
|
Insulinresistance and lipodystrophy are less in which PI |
6. Atazanavir |
|
|
Ritonavir induces what and inhibits what |
induces CYP 1A2 Inhibits P450 3A4 and 2D6 |
|
|
what is Lipodystrophy |
loss of fat, especially in face, hands and limbs. can be disfiguring cosmetically. may reduce medical adherence |
|
|
what is kinetic boost |
using two drugs to increase bioavailability |
|
|
administering ritonavir with other anti HIV drugs does what |
increasesthe plasma concentration of those drugs |
|
|
which PI has LOW oral bioavailability |
7. Lopinavir |
|
|
which PI has LOW bioavailabilty and is quick to develop resistance |
1. Saquinavir |
|
|
which two PI's prolong Q-T |
1. Saquinavir and 4. Ritonavir |
|
|
which PI has Crystalluria and Nephrolithiasis toxicity |
2. Indinavir |
|
|
which PI has Indirect hyperbilirubinemia toxicity |
6. Atazanavir |
|
|
standard combination therapy care for patients with HIV |
HAART |
|
|
what combination is often recommended |
combination of PI or NNRTI with one or two NRTI's |
|
|
HIV prophylaxis for needle stick |
zidovudine + lamivudine for 1 month NRTI's |
|
|
HIV prophylaxis for pregnancy |
Zidovudine (AZT) full doese in 2nd and 3rd trimester plus 6 weeks neonate |
|
|
how do integrase inhibitors work |
inhibiting the insertion of proviral DNA into the host cell genome |
|
|
type if integrase inhibitor and how it works
|
Raltegravir BlocksHIV - encoded integrase preventing integration of virus DNA into the hostchromosome |
|
|
what does a fusion inhibitor do |
it binds to GP41 whichinhibits the fusion of HIV to the CD4 cells |
|
|
what kind of local reaction does it cause and what is it active against |
causes local skin reactions and is active against drug resistant HIV |
|
|
type of CCR5antagonist |
Maraviroc |
|
|
what is it
|
a Viral co-receptor antagonist |
|
|
how does it work
|
competes for binding at CCR5 co-receptors |
|
|
does it work on CXCR4 receptors |
NO |
