Antiretrovirals and HIV: Difference between revisions

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The goal of HIV medicines is to prevent HIV from multiplying. There are six classes of drugs used in antiretroviral therapy<ref>Kemnic TR, Gulick PG. [https://www.ncbi.nlm.nih.gov/books/NBK513308/ HIV antiretroviral therapy.] StatPearls [Internet]. 2020 Jun 23.</ref>:
* nucleoside reverse transcriptase inhibitors (NRTI): They compete with natural deoxynucleotides for incorporation into a growing viral DNA chain. However, NRTIs lack a 3'-hydroxyl group on the deoxyribose moiety. This difference results in incorporating an NRTI, and the next incoming deoxynucleotide cannot form the following 5', 3' phosphodiester bond needed to extend the DNA chain. The result is a chain termination in DNA synthesis. Names of FDA approved drugsAbacavir, emtricitabine, lamivudine; Tenofovir disoproxil fumarate, zidovudine
** non-nucleoside reverse transcriptase inhibitor (NNRTI):  They block reverse transcriptase (RT) by directly binding to the enzyme. Though NNRTIs do not get incorporated into the viral DNA, they inhibit the movement of protein domains of RT that are essential to carry out the DNA synthesis. Name of FDA approved drugs-Efavirenz, etravirine, nevirapine, rilpivirine
* protease inhibitor (PI): Bind HIV-1 protease and block proteolytic cleavage of protein precursors necessary for the production of viral particles. Name of FDA approved drugsAtazanavir, darunavir, fosamprenavir, ritonavir, saquinavir, tipranavir
* integrase inhibitor (II): Block the action of integrase, preventing the viral genome from inserting itself into the DNA of a host cell.Name of FDA approved drugs


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Introduction[edit | edit source]

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The goal of HIV medicines is to prevent HIV from multiplying. There are six classes of drugs used in antiretroviral therapy[1]:

  • nucleoside reverse transcriptase inhibitors (NRTI): They compete with natural deoxynucleotides for incorporation into a growing viral DNA chain. However, NRTIs lack a 3'-hydroxyl group on the deoxyribose moiety. This difference results in incorporating an NRTI, and the next incoming deoxynucleotide cannot form the following 5', 3' phosphodiester bond needed to extend the DNA chain. The result is a chain termination in DNA synthesis. Names of FDA approved drugsAbacavir, emtricitabine, lamivudine; Tenofovir disoproxil fumarate, zidovudine
    • non-nucleoside reverse transcriptase inhibitor (NNRTI): They block reverse transcriptase (RT) by directly binding to the enzyme. Though NNRTIs do not get incorporated into the viral DNA, they inhibit the movement of protein domains of RT that are essential to carry out the DNA synthesis. Name of FDA approved drugs-Efavirenz, etravirine, nevirapine, rilpivirine
  • protease inhibitor (PI): Bind HIV-1 protease and block proteolytic cleavage of protein precursors necessary for the production of viral particles. Name of FDA approved drugsAtazanavir, darunavir, fosamprenavir, ritonavir, saquinavir, tipranavir
  • integrase inhibitor (II): Block the action of integrase, preventing the viral genome from inserting itself into the DNA of a host cell.Name of FDA approved drugs

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Resources[edit | edit source]

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References[edit | edit source]

  1. Kemnic TR, Gulick PG. HIV antiretroviral therapy. StatPearls [Internet]. 2020 Jun 23.