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What are the 5 treatment goals for HIV?
- reduce HIV-related morbidity and prolong survival
- improve quality of life
- restore and preserve immunologic function
- maximally and durably suppress viral load
- prevent vertival transmission
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True or false. Antiretroviral regimens should contain at least 2, preferably 3 active drugs from multiple drug classes.
True
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When should you treat HIV (5 instances)?
- In patients with AIDS defining illnesses
- All HIV infected patients
- Pregnant women
- Patients with HIV-associated nephropathy
- Patients co-infected with HBV and undergoing treatment
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True or false. You should co-treat HIV with HAV.
False, you should co-treat HIV with HBV.
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What are the 6 different classes of drugs that are used in the treatment of HIV?
- nucleosides/nucleotide reverse transcriptase inhibitors (NRTIs)
- nonnucleoside reverse transcriptase inhibitors (NNRTIs)
- protease inhibitors (PIs)
- fusion inhibitors (FIs)
- CCR5 antagonists
- integrase inhibitor
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Which 2 classes of HIV drugs are used in resistant patients?
- fusion inhibitors
- CCR5 antagonists
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What is the general regimen for HIV treatment?
2 NRTIs plus 1 NNRTI, a "boosted" PI, or raltegravir
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What is the preferred NNRTI used in HIV treatment regimen? When should you use caution in administering this drug?
Efavirenz; in pregnancy (teratogenic)
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What is the mechanism of action for efavirenz (and other NNRTIs)? Why are these drugs considered to be detrimental?
non-competitive inhibitor of reverse transcriptase; long half-life, teratogenic, CNS symptoms
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What HIV drug can be used in pregnant patients? What is the most significant ADE?
Nevirapine; hepatoxicity
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What are the advantages and disadvantages of NNRTI based regimens?
- Advantagescan save PIs for duture use
- long half-lives (for less compliant patients)
- Disadvantages
- Resistance
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What does a PI based regimen consist of? What is the mechanism of action?
1 PI with a NRTI; binds to and inhibits HIV protease
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What the 3 preferred PI based regimen treatments?
- atazanavir with ritonavir
- darunavir with ritonavir
- lopinavir/ritonavir
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Why should you avoid using PIs in diabetic patients? and what is the main drug interaction?
Main side effect is dyslipidemia; inhibitor and substrates of CYP3A4
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What are the advantages and disadvantages of PI based regimens?
- Advantages
- Barrier against resistance
- Disadvantages
- metabolic complications
- GI side effects
- CYP3A4 issues
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What does a NRTI based regimen consist of? What is the mechanism of action? Adverse effects?
"backbone" of all HAART regimens, tenofovir/emtricitabine; chain terminator which inhibit reverse transcriptase; lactic acidosis and hepatic steatosis
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What is the specific adverse effect of Abacavir (NRTI)?
hypersensitivity, involves HLA-B*5701 allele
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Which NRTI is the most well tolerated in treating HIV?
lamivudine
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Which NRTI causes bone marrow suppression?
zidovudine
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What is the most common NRTI combo product?
Combivir (lamivudine with zidovudine)
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Which PI is most commonly used to treat HIV?
Kaletra (lopinavir/ritonavir)
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What is the mechanism of action for fusion inhibitors (FIs)? Route of administration? Adverse effects?
inhibits viral entry into cell; SubQ; injection site reactions, pneumonia, hypersensitivity
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What is the mechanism of action for Mirovac? Side effects? Drug interactions?
CCR5 antagonist; URI, dizziness, fever; CYP3A4 substrate
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What is the mechanism of action for Raltegravir? Side effects? Drug interactions?
blocks active site of HIV integrase; well-tolerated, may have CPK elevations, rhabdomyolysis; statins
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