Pharmacokinetics and Pharmacodynamics

Module 11, Version 4


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  • Bastiaans D, Cressey T, Vromans H, Burger D. The role of formulation on the pharmacokinetics of antiretroviral drugs. Expert Opin Drug Metab Toxicol. 2014;10:1019-1037.
  • Best GM, Capparelli EV, Diep H, et al. Pharmacokinetics of lopinavir/ritonavir crushed versus whole tablets in children. J Acquir Immune Defic Syndr. 2011;58:385-391.
  • Cahn P, Kaplan R, Sax P, et al. Raltegravir (RAL) 1200 mg once daily versus raltegravir 400 mg twice daily, with tenofovir disoproxil fumarate and emtricitabine, for previously untreated HIV-1 infection: a randomised, double-blind, parallel-group, phase 3, non-inferiority trial. Lancet HIV. 2017 Nov;4(11):e486-e494.
  • Cahn P, Sax PE, Squires K, et al. Raltegravir 1200 mg Once Daily vs 400 mg Twice Daily, with Emtricitabine and Tenofovir Disoproxil fumarate, for Previously Untreated HIV-1 Infection: Week 96 Results from ONCEMRK, a Randomized, Double-Blind, Noninferiority Trial. J Acquir Immune Defic Syndr. 2018 Aug 15;78(5):589-598.
  • Calcagno A, Di Perri G, Bonora S. Pharmacokinetics and pharmacodynamics of antiretrovirals in the central nervous system. Clin Pharmacokinet. 2014;53:891-906.
  • Caniglia EC, Cain LE, Justice A, et al. Antiretroviral penetration into the CNS and incidence of AIDS-defining neurologic conditions. Neurology. 2014;83:134-141.
  • Cattaneo D, Baldelli S, Castoldi S, et al. Is it time to revise antiretrovirals dosing? A pharmacokinetic viewpoint. AIDS. 2014;28:2477-2479.
  • Cattaneo D, Baldelli S, Cozzi V, et al. Impact of Therapeutic Drug Monitoring of Antiretroviral Drugs in Routine Clinical Management of People Living With HIV: A Narrative Review. Ther Drug Monit. 2020;42(1):64-74.
  • Crawford KW, Ripin DHB, Levin AD, et al. Optimising the manufacture, formulation, and dose of antiretroviral drugs for more cost-effective delivery in resource-limited settings: A consensus statement. Lancet Infect Dis. 2012;12:550-560.
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  • Ellis RJ, Letendre S, Vaida F, et al. Randomized trial of central nervous system-targeted antiretrovirals for HIV-associated neurocognitive disorder. Clin Infect Dis. 2014;58:1015-1022.
  • Emu B, Fessel J, Schrader S, et al. Phase 3 study of ibalizumab for multidrug-resistant HIV-1. N Engl J Med. 2018;379:645-654.
  • ENCORE1 Study Group. Efficacy and safety of efavirenz 400 mg daily versus 600 mg daily: 96-week data from the randomized, double-blind, placebo-controlled, non-inferiority ENCORE1 Study. Lancet Infect Dis. 2015;15:793-802.
  • Eron JJ, Rockstroh JK, Reynes J, et al. Raltegravir once daily or twice daily in previously untreated patients with HIV-1: A randomised, active-controlled, phase III non-inferiority trial. Lancet Infect Dis. 2011 Dec;11:907-915.
  • Flexner C, Hendrix CW. Pharmacology of antiretroviral agents. In: DeVita VT, Hellman S, Rosenberg SA, eds. AIDS: Etiology, Diagnosis, Treatment, and Prevention. 4th ed. Philadelphia, Pa: Lippincott-Raven Publishing; 1997:479-493.
  • Kakuda TN, Wade JR, Snoeck E, et al. Pharmacokinetics and pharmacodynamics of the non-nucleoside reverse-transcriptase inhibitor etravirine in treatment-experienced HIV-1-infected patients. Clin Pharmacol Ther. 2010;88:695-703.
  • Krummenacher I, Cavassini M, Bugnon O, Schneider MP. An interdisciplinary HIV-adherence program combining motivational interviewing and electronic antiretroviral drug monitoring. AIDS Care. 2011;23:550-561.
  • Larson KB, Wang K, Delille C, et al. Pharmacokinetic enhancers in HIV therapeutics. Clin Pharmacokinet. 2014;53:865-872.
  • Lecher SL, Shrestha RK, Botts LW, et al. Cost analysis of a novel HIV testing strategy in community pharmacies and retail clinics. J Am Pharm Assoc. 2015;55:488-492.
  • Letendre S. Central Nervous System Complications in HIV Disease: HIV-Associated Neurocognitive Disorder. Top Antivir Med. 2011; 19(4):137–142.
  • Leth FV, Kappelhoff BS, Johnson D, et al. Pharmacokinetic parameters of nevirapine and efavirenz in relation to antiretroviral efficacy. AIDS Res Hum Retroviruses. 2006;22:232-239.
  • Lucas GM, Ross MJ, Stock PG, et al. Clinical Practice Guideline for the Management of Chronic Kidney Disease in Patients Infected With HIV: 2014 Update by the HIV Medicine Association of the Infectious Diseases Society of America. Clin Infect Dis. 2014; 59(9): e96–e138.
  • Maitre T, Muret P, Blot M, et al. Benefits and Limits of Antiretroviral Drug Monitoring in Routine Practice. Curr HIV Res. 2019;17(3):190-197.
  • Marzolini C, Telenti A, Decosterd LA, et al. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS. 2001;15:71-75.
  • Mello AF, Buclin T, Decosterd LA, et al. Successful efavirenz dose-reduction guided by therapeutic drug monitoring. Antivir Ther. 2011;16:189-197.
  • Minuesa G, Huber-Ruano I, Pastor-Anglada M, et al. Drug uptake transporters in antiretroviral therapy. Pharmacol Ther. 2011;132:268-279.
  • Piscitelli SC, Flexner C, Minor JR, et al. Drug interactions in HIV-infected patients (review). Clin Infect Dis. 1996;23:685-693.
  • Podany AT, Scarsi KK, Fletcher CV. Comparative Clinical Pharmacokinetics and Pharmacodynamics of HIV-1 Integrase Strand Transfer Inhibitors. Clin Pharmacokinet. 2017; 56(1): 25–40.
  • Poggio ED, Hall PM. Estimation of glomerular filtration rate by creatinine-based formulas: Any room for improvement? NephSAP. 2006;5:131-140.
  • Pomerantz RJ. Reservoirs of human immunodeficiency virus type 1: The main obstacles to viral eradication. Clin Infect Dis. 2002;34:91-97.
  • Pretorius E, Klinker H, Rosenkranz B. The role of therapeutic drug monitoring in the management of patients with human immunodeficiency virus infection. Ther Drug Monit. 2011;33:265-274.
  • Renjifo B, van Wyk J, Salem AH, Bow D, Ng J, Norton M. Pharmacokinetic enhancement in HIV antiretroviral therapy: A comparison of ritonavir and cobicistat. AIDS Rev. 2015;17:37-46.
  • Rizk ML, Hang Y, Luo WL, et al. Pharmacokinetics and pharmacodynamics of once-daily versus twice-daily raltegravir in treatment-naïve HIV-infected patients. Antimicrob Agents Chemother. 2012;56:3101-3106.
  • Saberi P, Johnson MO. Technology-based self-care methods of improving antiretroviral adherence: A systematic review. PLOS ONE. 2011;6:e27533.
  • Sankatsing SUC, Beijnen JH, Schinkel AH, et al. P glycoprotein in human immunodeficiency virus type 1 infection and therapy. Antimicrob Agents Chemother. 2004;48:1073-1081.
  • Shah BM, Schafer JJ, Priano J, Squires KE. Cobicistat: A new boost for the treatment of human immunodeficiency virus infection. Pharmacotherapy. 2013;33:1107-1116.
  • Trezza CR, Kashuba AD. Pharmacokinetics of antiretrovirals in genital secretions and anatomic sites of HIV transmission: Implications for HIV prevention. Clin Pharmacokinet. 2014;53:611-624.
  • Tseng A, Seet J, Phillips EJ. The evolution of three decades of antiretroviral therapy: Challenges, triumphs and the promise of the future. Br J Clin Pharmacol. 2014;79:182-194.
  • Verbeeck RK, Musuamba FT. Pharmacokinetics and dosage adjustment in patients with renal dysfunction. Eur J Clin Pharmacol. 2009;65:757-773.
  • Wang X, Boffito M, Zhang J, et al. Effects of H2-receptor antagonist famotidine on the pharmacokinetics of atazanavir-ritonavir with or without tenofovir in HIV-infected patients. AIDS Patient Care STDS. 2011;25(9):509-515.
  • Williams PE, Crauwels HM, Basstanie ED. Formulation and pharmacology of long-acting rilpivirine. Curr Opin HIV AIDS. 2015;10:239-245.
  • American Society of Health Systems Pharmacists. (2015). ASHP Guidelines on Pharmacist Involvement in HIV Care. In: ASHP best practices. Position & Guidance Documents of ASHP 2015-2016 edition. Bethesda: American Society of Health Systems Pharmacists.
  • European AIDS Clinical Society. EACS Guidelines, version 10.1. October 2020. Available at: Accessed November 27, 2020.
  • Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the Use of Antiretroviral Agents in Adults and Adolescents with HIV. Department of Health and Human Services. December 18, 2019. Available at Accessed April 13, 2020.
  • Agarwala S, Gray K, Wang Y, Grasela D. Pharmacokinetic effect of omeprazole on atazanavir co-administered with ritonavir in healthy subjects. Program and abstracts of the 2005 Conference on Retroviruses and Opportunistic Infections; Feb 22-25, 2005; Boston, MA. Abstract 658. 
  • Crauwels HM, van Heeswijk RP, Kestens D, et al. The pharmacokinetic interaction between omeprazole and TMC 278, an investigational NNRTI. Program and abstracts of the 9th International Congress on Drug Therapy in HIV Infection; November 9-13, 2008; Glasgow, United Kingdom. Abstract P239.
  • Letendre S. HIV and the central nervous system. Impact of drug distribution. HIV Management. 2014: The New York Course.

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The American Academy of HIV Medicine is a professional organization that supports the HIV practitioner and promotes accessible, quality care for all Americans living with HIV disease. Our membership of HIV practitioners and credentialed HIV Specialists™, HIV Experts™, and HIV Pharmacists™ provide direct care to the majority of HIV patients in the US.