HIV drugs Flashcards
HIV drugs map
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side effects of NRTIs
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Unique side effects of NRTIs
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HART therapy regimens
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MOA of NRTI ?
These are pro-drugs converted to their active form intracellularly by the cellular kinases.NRTIs lack a 3’-hydroxyl group at the 2’-deoxyribosyl moiety. This prevents the formation of a 3’-5’-phosphodiester bond in growing DNA chains which prevent replication of the virus.
MOA of NNRTIs?
Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are the second class of reverse transcriptase inhibitors. The primary mechanism of action is through the binding of the NNRTI to the reverse transcriptase and the creation of a hydrophobic pocket proximal to the active site. This pocket creates a new spatial configuration of the substrate-binding site to reduce the overall polymerase activity. By creating a different configuration, DNA synthesis becomes slowed overall. Because of the non-competitive inhibitor action of NNRTI, it is not effective against HIV-2 reverse transcriptase