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What are the 3 non-nucleoside RT inhibitors approved for use?
nevirapine, efavirenz, delavirdine
T/F: Non-nucleoside RTI's induce a 3D structure change and competively reduce enzyme activity
Are NNRTIs active against HIV-1, HIV-2, or both
NNRTIs have no activity against mammalian _____________
which 2 hepatic enzymes eliminate NNRTIs
CYP3A4 and CYP2B6
How can resistance to NNRTI occur? How is it avoided?
A single mutation can cause extensive resistance. To avoid use combinations of agents.
What is the most frequent ADR for nevirapine and the organ most affected by this drug
rash, liver (causes hepatitis)
T/F Nevirapine is approved for monotherapy in adults but not children infected with HIV.
False: combination only, adults AND children
Efavirenz triple therapy with ______ and ______ showed 70% of patients with non-detectable levels.
Which of the following is NOT a characteristic of NNRTIs
a. metabolized by CYP 3A4 and 2B6
b. binds to essential site
c. shows no activity against mammalian DNA polymerase
What ADR is most common with efavirenz and can occur with the first dose
HIV protease inhibitors are peptidomimetic that inhibit what?
HIV aspartyl protease
HIV protease inhibitors prefer cleavage between what 2 amino acids?
proline and phenylalanine
Renin and pepsin are examples of what? are these inhibited by HIV protease inhibitors?
Human aspartyl proteases, no
inhibition of the protease prevents cleavage of which 2 polyproteins
gag and pol
Which enzyme is most responsible for HIV protease inhibitor elimination?
which drug is often used to inhibit CYP3A4 to increase levels of other drugs?
T/F Resistance to one HIV protease inhibitor not cross-resistant to other protease inhibitors
What are the 7 HIV protease inhibitors from the lecture? (HINT: SARALIN)
In general, HIV protease inhibitors have effectiveness against HIV-1, HIV-2, or both?
T/F Resistance to saquinavir can be achieved by a single nucleotide mutation
False: requires multiple mutations
what is the most common ADR for saquinavir?
What is the dose-dependent ADR for ritonavir?
high cholesterol, TG, lipodystrophy
Food ____ oral bioavailability of indinavir, while food usually _____ bioavailability of HIV protease inhibitors
A unique ADR of indinavir is ______ and ________ due to poor solubility of drug at neutral pH
crystalluria and nephrolithiasis
This drug's metabolite from CYP2C19 oxidation is active, unlike all other HIV protease inhibitors
The prodrug of amprenavir is called what?
this HIV protease inhibitor is most likely to cause skin eruptions
This protease inhibitor is similar to ritonavir, but more potent against HIV-1 in vitro
Which 2 protease inhibitors may cause hyperbilirubinemia without clinical significance?
indinavir and atazanavir
Increase in circulating triglycerides can lead to what 3 effects?
increased central fat, increased breast fat in women, insulin resistance
what is the name of the only entry inhibitor, active against HIV-1
T/F enfuvirtide requires intramuscular injections 2x daily
Enfuvirtide blocks interaction between N36 and C34 sequences of the _______