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28 Cards in this Set
- Front
- Back
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What is the goal of anti-retroviral therapy?
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The reduce the viral load and maintain as much immune function as possible.
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What RNA level must a patient's HIV RNA be at for the HIV to be virologically suppressed?
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Less than 50 copies/ml.
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At what level of CD4 cells must HAART be started at?
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CD4 count< 350cells/mm3
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What is an HIV-2 infection?
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It is an HIV strain endemic to west Africa.
Generally shows longer asymptomatic stage, lower viral loads and mortality. |
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What test is approved for differentiating between HIV-1 and HIV-2?
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Monospot Rapid test.
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Why are NNRTI's so effective against HIV-2?
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They are NOT effective you dummy.
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What are the six major drug classes for treatment of HIV-infection?
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CCR5 antagonists
Fusion inhibitors Protease inhibitors NNRTIs NRTIs Integrase inhibitors |
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What is the mechanism of action of Abacavir, Zidovudine (AZT),
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ABC, and AZT are NRTIs. They are nucleoside or nucleotide analogs that terminate proviral DNA when incorporated.
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What drug class is associated with lactic acidosis-hepatic steatosis syndrome.
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NRTIs
(stavudine, zidovudine, didanosine, and zalcitabine). |
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What is a contraindication for Abacavir?
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Patients with an HLA-B5701 genotype. These patients have hypersensitivity issues with this drug.
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True or false. Abacavir is effective for HIV-1 and HIV-2.
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False. HIV-1
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What are the major adverse effects of Zidovudine (AZT)?
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Anemia and neutropenia.
AZT is OK for children or adults and in pregnancy. |
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What is the mechanism of action of NNRTIs?
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They are noncompetitive inhibitors that bind to reverse transcriptase and induce a conformational change that greatly reduces enzyme activity.
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What is a disadvantage to using NNRTIs? Advantage?
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The prevalence of resistant virus, low genetic barrier to resistance.
The advantage is that you can hold off on the protease inhibitors. |
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What are the two FDA approved NNRTIs?
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Efavirenz and Nevirapine.
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Can Enfavirenz be used in women planning to conceive?
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No.
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Do NNRTIs influence CYP activity?
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Yes, both Enfavirenz and Nevirapine are CYP inducers.
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How do protease inhibitors work?
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Specifically and reversibly inhibit the HIV aspartyl protease and thereby block post-translational processing of viral proteins required to produce a mature viral particle.
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All protease inhibitors have poor bioavailability and are metabolized by CYP system. What is given to help boost protease inhibitors?
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Ritonavir.
It is a protease inhibitor that is a potent CYP3A4 inhibitor. |
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Fact: Protease inhibitors are generally not well tolerated at doses required for antiviral activity.
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They can also cause PI-induced metabolic syndrome.
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Which Integrase inhibitor is used and how does it work.
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Reltegravir blocks the insertion of reverse-transcribed viral DNA into the host DNA.
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What is Enfuvirtide and how does it work?
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EnFUvirtide is and FUsion inhibitor that works by binding HIV surface glycoprotein gp41 to block conformation required for membrane fusion with host cell.
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CCR5 antagonists interact with what part of the HIV virus?
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Maraviroc is an antagonist of the CCR5 interaction with gp120.
Blocks CCR5-tropic HIV-1 entry. |
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What are the major side affects of Maraviroc?
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Hepatoxicity and possibly hypersensitivity.
NOTE: Maraviroc is a CYP substrate, so beware of CYP inhibitors or inducers. |
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What is the recommended starting regimen of combination ARTs?
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1 NNRTI + 2 NRTIs
or 1 PI + 2 NRTIs |
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Fact about protease inhibitors.
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They all end in "navir"
Ritonavir Atazanavir Darunavir Fosamprenavir Lopinavir |
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Why is Tuberculosis treatment for HIV-infected patients important?
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Rifampin is a potent CYP inducer and should not be used with PI's or NNRTIs except efavirenz.
Bottom Line: coadministration of rifabutin and HAART will require monitoring and dose adjustment. |
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What protease inhibitor is associated with parathesias?
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Ritonavir.
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