Nursing Pharmacology: Antiviral Drugs

**Sites of Antiretroviral Drug Actions⁷**

a: The lifecycle of HIV-1, showing the step at which enfuvirtide acts, and also the steps targeted by other drugs.⁷ b: "Simplified schematic of the mechanism by which enfuvirtide inhibits viral entry into host cells.⁷ The envelope glycoprotein of HIV-1 consists of two non-covalently associated subunits, gp120 and gp41. After attachment of HIV-1 to its target cells carrying the CD4 receptor, gp120 interacts with the CD4 receptor, which initiates a series of conformational changes in gp41 and gp120 that lead to the insertion of a region of gp41 into the membrane of the host cell, and formation of a ' pre-hairpin intermediate' (top). Further changes in the confirmation of gp41 bring the viral and cellular membranes into close enough proximity for membrane fusion (bottom left). Abbreviations: NNRTI, non-nucleoside reverse transcriptase inhibitor; NRTI, nucleoside reverse transcriptase inhibitor; PI, protease inhibitor" Attribution: Slight modification of Figure 1 from: LaBonte J Lebbos J Kirkpatrick nature Reviews Drug Discovery 2, 345-346 (May 2003).⁷

References
Wang F Kieff E Medical Viriology, Cahpter 177 Section 11: Viral Diseases: General Considerations (in Harrison's Principles of Internal Medicine, 18th edition, Longo DF Fauci AS Kasper DL Hauser SL Jameson JL Loscalzo J, eds) McGraw-Hill, New York, 2012, pp 1432-1433. Lu K Gulick RM (Based on a presentation at PRN by Roy M. Gulick, MD, MPH New antiretrovirals for the treatment of HIV; the view in 2006. The PRN Notebook 11(2) October 2006. The figure corresponds to Figure 2 in this reference and was derived by the authors from an original image by Robert W. Doms, MD, Ph.D. The figure in on this page has been slightly modified from its original form in reference 8. Flexner C Chapter 59. Antiretroviral Agents and Treatment of HIV Infection (in Goodman & Gilman's The Pharmacological Basis of Therapeutics, 12 e, Brunton LL Chabner BA Knollmann BC, eds) The McGraw-Hill Companies, Inc, 2011. Safrin S Chapter 49: Antiviral Agents: Antiretroviral Agents in Basic & Clinical Pharmacology 13e (Katzung BG Trevor AJ, eds) 2015, online edition. AIDSinfo: Guidelines for the Use of Antriretroviral Agents in HIV-1-Infected Adults and Adolescents https://aidsinfo.nih.gov/guidelines (2015) Tsibris AMN Hirsch MS Chapter 130 Antiretroviral Therapy for Human Immunodeficiency Virus Infection in Mandell, Douglas, and Bennett's Principles and Practice of Infectious Diseases, 8e (Bennett JE Bolin R Blaser, eds) Elsevier, Inc/Saunders 2015, online version. LaBonte J Lebbos J Kirkpatrick nature Reviews Drug Discovery 2, 345-346 (May 2003). (Slight modification of Fig. 1) http://www.nature.com/nrd/journal/v2/n5/fig_tab/nrd1091_F1.html; Original figure attribution: Kilby JM Hopkins S Venetta TM Woster PM Antiviral Agents and Protease Inhibitors. Chapter 43 in Foye's Principles of Medicinal Chemistry, 6e Lemke TL; Williams DA, eds; Roche VF Zito SW, asst. eds), Lippincott Williams & Wilkins, a Wolters Kluwer business, 1219, 2008. Swaminathan J and MSD staff at the European Bioinformatics Institute (http://www.ebi.ac.uk/) Renin: molecular structure registered with 2rn code. https://commons.wikimedia.org/wiki/File:PDB_2ren_EBI.jpg Renin: https://en.wikipedia.org/wiki/Renin Haggstrom M "Overview of the renin-angiotensin system" https://commons.wikimedia.org/wiki/File:Renin-angiotensin_system_in_man_shadow.svg Flexner C HIV-Protease Inhibitors The New England Journal of Medicine 338(18) 1281-1292, April 30, 1998. http://www.ncbi.nlm.nih.gov/pubmed/9562584 MLGProGamer123 "Cartoon structure of HIV enzyme" "HIV-1 Protease with Active Site" https://commons.wikimedia.org/wiki/File:HIV-1_Protease_with_Active_Site.png HIV-1 Protease https://en.wikipedia.org/wiki/HIV-1_protease Jaskolski M Tomasselli AG Sawyer TK Staples DG Heinrikson RL Schneider J Kent SBH Wlodawer Structure at 2.5 A Resolution of Chemically Synthesized Human Immunodeficiency Virus Type I Protease Complexed with a Hydroxyethylene-Based Inhibitor. Biochemistry 30, 1600-1609, 1991. http://www.ncbi.nlm.nih.gov/pubmed/1993177

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