Topic 19 HIV Antiretroviral TreatmentP

Topic 19 HIV Antiretroviral TreatmentP -...

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Treating HIV-infected Individuals
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Targets for Licensed Anti-HIV  Chemotherapeutic Drugs Fusion inhibitor RT Inhibitors Protease Inhibitors Integrase Inhibitor * *  Restricted use Cytokine blocker *
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HIV Antiretroviral Drug Availability Antiretroviral Drug Class First Approved  Nucleoside/Nucleotide Reverse  Transcriptase Inhibitors 1987 Non-nucleoside Reverse  Transcriptase Inhibitors 1997 Protease Inhibitors 1995 Fusion Inhibitors 2003 Integrase Inhibitors 2007 Chemokine Blockers  [CCR5 Antagonist] 2007
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Antiviral drugs used to treat HIV infection:   NRTIs [N ucleoside R everse T ranscriptase I nhibitors] AZT (zidovudine) -   nucleoside analog, i.e., it  “looks like” dTTP used by a cell to make  deoxyribonucleotide -  lacks a 3’ (carbon) hydroxyl group -  once incorporated, DNA synthesis stops -  functions as a competitive inhibitor  [‘competes’ with dTTP]
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Deoxyribonucleotides are the Building  Blocks of DNA To continue synthesis, nucleotide must have a ‘free’ hydroxyl (-OH) group on C-3’ carbon Incorporation of AZT in elongating strand of DNA results in N 3  on C-3 [i.e., no –OH]
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RT Inhibitors:   Nucleotide analogs Nucleotide inhibitor: terminates  DNA synthesis NRTIs compete  with ‘real’  deoxyribonucleotides
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Antiviral drugs used to treat HIV infection: Non-NRTIs   Nevirapine - binds directly to RT enzyme (the viral DNA  polymerase) - binding ‘distorts’ RT, inhibiting its action - functions as a noncompetitive inhibitor
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Antiviral drugs used to treat HIV infection: Protease Inhibitor
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Topic 19 HIV Antiretroviral TreatmentP -...

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