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12 Cards in this Set
- Front
- Back
Lessons learned form monotherapy with HIV
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HIV rapidly develops resistance when one drug is used. Benefit lasted only two yeart.. Patients with lower HIV rna levels survived longer.
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HAART.
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Highly Active anti retroviral therapy. Aggressive treatment with many antivirals to keep RNA load down.
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Nucleoside Reverse Transcriptase inhibiors (nRTI) lack what?
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3'hydroxyl. All of these drugs require conversion to the triphosphate form. The triphophate causes chain termination.
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Zidovudine, emtricitabine, tenofovir, abacavir, didanosine, lamivudine
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nRTI
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nRTI toxicity
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Inhibition of mitochondrial function. Lactic acidosis, hepatic steatosis, peripheral neuropathy.
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Non-nucleoside reverse inhibitors (nnrti)
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Nevirapine and Efavirenz. Don't require metabolic activation. Noncompetitive inhibitor of RT. Cross resistance common.
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Protease Inhibitors
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Block action of proteases responsible for splitting viral DNA into functional pieces. Metabolize by or induced by CYP3A4. Lipodystrophy in extremities and depositied to buffalo hump and abdomen. Elevated fats and glucose.
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Protease inhibitor examples
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Atazanavir, fosamprenavir, darunavir, lopinavir, saquinavir.
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Ritonavir
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A protease but not really. It does something called protease boosting which is where we give a sub-therapeutic dose to inhibit P450 metabolism of other protease inhibitors.
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Raltegravir
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Integrase inhibitor so block insertion of HIV DNA into host cell.
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Enfurvirtide
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Fusion inhibitor. Targets gp41. Its a protein combined with other drugs. Only used when other options have failed.
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Maraviroc
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Entry inhibitor. Blocks CCR5 which is how HIV gets into the cell. Does not bind CXCR4.
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