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Dose adjustment of the non-nucleoside reverse transcriptase inhibitors during concurrent rifampicin-containing tuberculosis therapy: one size does not fit all

, MD, MPHTM, , PhD (Scientist C) & , MD (Scientist F)
Pages 55-68 | Published online: 07 Dec 2009

Bibliography

  • WHO. Global tuberculosis control–epidemiology, strategy, financing. WHO Report 2009. WHO/HTM/TB/2009411 2009. Available from: http://www.who.int/tb/publications/global_report/2009/pdf/full_report.pdf. [Last accessed 13 August 2009]
  • Dheda K, Lampe FC, Johnson MA, Lipman MC. Outcome of HIV-associated tuberculosis in the era of highly active antiretroviral therapy. J Infect Dis 2004;190(9):1670-6
  • Manosuthi W, Chottanapand S, Thongyen S, Survival rate and risk factors of mortality among HIV/tuberculosis-coinfected patients with and without antiretroviral therapy. J Acquir Immune Defic Syndr 2006;43(1):42-6
  • Velasco M, Castilla V, Sanz J, Effect of simultaneous use of highly active antiretroviral therapy on survival of HIV patients with tuberculosis. J Acquir Immune Defic Syndr 2009;50(2):148-52
  • Burman WJ. Issues in the management of HIV-related tuberculosis. Clin Chest Med 2005;26(2):283-94, vi-vii
  • Kwara A, Flanigan TP, Carter EJ. Highly active antiretroviral therapy (HAART) in adults with tuberculosis: current status. Int J Tuberc Lung Dis 2005;9(3):248-57
  • Brinkhof MW, Egger M, Boulle A, Tuberculosis after initiation of antiretroviral therapy in low-income and high-income countries. Clin Infect Dis 2007;45(11):1518-21
  • Lawn SD, Myer L, Bekker LG, Wood R. Burden of tuberculosis in an antiretroviral treatment programme in sub-Saharan Africa: impact on treatment outcomes and implications for tuberculosis control. AIDS 2006;20(12):1605-12
  • Lawn SD, Harries AD, Anglaret X, Early mortality among adults accessing antiretroviral treatment programmes in sub-Saharan Africa. AIDS 2008;22(15):1897-908
  • Lawn SD, Lipman MC, Easterbrook PJ. Immune reconstitution disease associated with mycobacterial infections. Curr Opin HIV AIDS 2008;3(4):425-31
  • Wilkinson GR. Drug metabolism and variability among patients in drug response. N Engl J Med 2005;352(21):2211-21
  • Xu C, Li CY, Kong AN. Induction of phase I, II and III drug metabolism/transport by xenobiotics. Arch Pharm Res 2005;28(3):249-68
  • WHO. Antiretroviral therapy for HIV infection in adults and adolescents in resource-limited settings: towards universal access. Geneva, Switzerland: World Health Organization; 2006
  • Desta Z, Saussele T, Ward B, Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitro. Pharmacogenomics 2007;8(6):547-58
  • Ward BA, Gorski JC, Jones DR, The cytochrome P450 2B6 (CYP2B6) is the main catalyst of efavirenz primary and secondary metabolism: implication for HIV/AIDS therapy and utility of efavirenz as a substrate marker of CYP2B6 catalytic activity. J Pharmacol Exp Ther 2003;306(1):287-300
  • Mutlib AE, Chen H, Nemeth GA, Identification and characterization of efavirenz metabolites by liquid chromatography/mass spectrometry and high field NMR: species differences in the metabolism of efavirenz. Drug Metab Dispos 1999 Nov;27(11):1319-33
  • Belanger AS, Caron P, Harvey M, Glucuronidation of the antiretroviral drug efavirenz by UGT2B7 and an in vitro investigation of drug-drug interaction with zidovudine. Drug Metab Dispos 2009;37(9):1793-6
  • di Iulio J, Fayet A, Arab-Alameddine M, In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function. Pharmacogenet Genomics 2009;19(4):300-9
  • Faucette SR, Wang H, Hamilton GA, Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metab Dispos 2004;32(3):348-58
  • Hesse LM, Sakai Y, Vishnuvardhan D, Effect of bupropion on CYP2B6 and CYP3A4 catalytic activity, immunoreactive protein and mRNA levels in primary human hepatocytes: comparison with rifampicin. J Pharm Pharmacol 2003;55(9):1229-39
  • Madan A, Graham RA, Carroll KM, Effects of prototypical microsomal enzyme inducers on cytochrome P450 expression in cultured human hepatocytes. Drug Metab Dispos 2003;31(4):421-31
  • Benedeck IH, Joshi A, Fiske WD, Pharmacokinetic interaction between efavirenz and rifampin in healthy volunteers. 12th World AIDS Conference; June 28–July 3 1998; Geneva, Switzerland
  • Lopez-Cortes LF, Ruiz-Valderas R, Viciana P, Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis. Clin Pharmacokinet 2002;41(9):681-90
  • Friedland G, Khoo S, Jack C, Lalloo U. Administration of efavirenz (600 mg/day) with rifampicin results in highly variable levels but excellent clinical outcomes in patients treated for tuberculosis and HIV. J Antimicrob Chemother 2006;58(6):1299-302
  • Matteelli A, Regazzi M, Villani P, Multiple-dose pharmacokinetics of efavirenz with and without the use of rifampicin in HIV-positive patients. Curr HIV Res 2007;5(3):349-53
  • Blumberg HM, Burman WJ, Chaisson RE, American Thoracic Society/Centers for Disease Control and Prevention/Infectious Diseases Society of America: treatment of tuberculosis. Am J Respir Crit Care Med 2003;167(4):603-62
  • CDC. Managing drug interactions in the treatment of HIV-related tuberculosis. [online] 2007. Available from: http://www.cdc.gov/tb/TB_HIV_Drugs/default.htm. [Last accessed 10 July 2009]
  • Pozniak AL, Miller RF, Lipman MC, BHIVA treatment guidelines for tuberculosis (TB)/HIV infection 2005. HIV Med 2005;6(Suppl 2):62-83
  • Csajka C, Marzolini C, Fattinger K, Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin Pharmacol Ther 2003;73(1):20-30
  • Marzolini C, Telenti A, Decosterd LA, Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS 2001;15(1):71-5
  • Stahle L, Moberg L, Svensson JO, Sonnerborg A. Efavirenz plasma concentrations in HIV-infected patients: inter- and intraindividual variability and clinical effects. Ther Drug Monit 2004;26(3):267-70
  • Langmann P, Weissbrich B, Desch S, Efavirenz plasma levels for the prediction of treatment failure in heavily pretreated HIV-1 infected patients. Eur J Med Res 2002;7(7):309-14
  • Kwara A, Lartey M, Sagoe KW, Pharmacokinetics of efavirenz when co-administered with rifampin in TB/HIV co-infected patients: pharmacogenetic effect of CYP2B6 variation. J Clin Pharmacol 2008;48(9):1032-40
  • Ramachandran G, Hemanth Kumar AK, Rajasekaran S, CYP2B6 G516T polymorphism but not rifampin coadministration influences steady-state pharmacokinetics of efavirenz in human immunodeficiency virus-infected patients in South India. Antimicrob Agents Chemother 2009;53(3):863-8
  • Brennan-Benson P, Lyus R, Harrison T, Pharmacokinetic interactions between efavirenz and rifampicin in the treatment of HIV and tuberculosis: one size does not fit all. AIDS 2005;19(14):1541-3
  • Lopez-Cortes LF, Ruiz-Valderas R, Ruiz-Morales J, Efavirenz trough levels are not associated with virological failure throughout therapy with 800 mg daily and a rifampicin-containing antituberculosis regimen. J Antimicrob Chemother 2006;58(5):1017-23
  • Manosuthi W, Kiertiburanakul S, Sungkanuparph S, Efavirenz 600 mg/day versus efavirenz 800 mg/day in HIV-infected patients with tuberculosis receiving rifampicin: 48 weeks results. AIDS 2006;20(1):131-2
  • Cabrera SE, Cordero M, Iglesias A, Efavirenz-rifampicin interaction: therapeutic drug monitoring to efavirenz dosage optimization in HIV/TBC patients. AIDS 2008;22(18):2549-51
  • Patel A, Patel K, Patel J, Safety and antiretroviral effectiveness of concomitant use of rifampicin and efavirenz for antiretroviral-naive patients in India who are coinfected with tuberculosis and HIV-1. J Acquir Immune Defic Syndr 2004;37(1):1166-9
  • DiGiacinto JL, Chan-Tack KM, Robertson SM, Are literature references sufficient for dose recommendations? An FDA case study of efavirenz and rifampin. J Clin Pharmacol 2008;48(4):518-23
  • Ren Y, Nuttall JJ, Eley BS, Effect of rifampicin on efavirenz pharmacokinetics in HIV-infected children with tuberculosis. J Acquir Immune Defic Syndr 2009;50(5):439-43
  • Cabrera SE, Santos D, Valverde MP, Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. Antimicrob Agents Chemother 2009;53(7):2791-8
  • Kappelhoff BS, Huitema AD, Yalvac Z, Population pharmacokinetics of efavirenz in an unselected cohort of HIV-1-infected individuals. Clin Pharmacokinet 2005;44(8):849-61
  • Arab-Alameddine M, Di Iulio J, Buclin T, Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals. Clin Pharmacol Ther 2009;85(5):485-94
  • Motsinger AA, Ritchie MD, Shafer RW, Multilocus genetic interactions and response to efavirenz-containing regimens: an adult AIDS clinical trials group study. Pharmacogenet Genomics 2006;16(11):837-45
  • Burger D, van der Heiden I, la Porte C, Interpatient variability in the pharmacokinetics of the HIV non-nucleoside reverse transcriptase inhibitor efavirenz: the effect of gender, race, and CYP2B6 polymorphism. Br J Clin Pharmacol 2006;61(2):148-54
  • Kappelhoff BS, van Leth F, MacGregor TR, Nevirapine and efavirenz pharmacokinetics and covariate analysis in the 2NN study. Antivir Ther 2005;10(1):145-55
  • Pfister M, Labbe L, Hammer SM, Population pharmacokinetics and pharmacodynamics of efavirenz, nelfinavir, and indinavir: Adult AIDS Clinical Trial Group Study 398. Antimicrob Agents Chemother 2003;47(1):130-7
  • Stohr W, Back D, Dunn D, Factors influencing efavirenz and nevirapine plasma concentration: effect of ethnicity, weight and co-medication. Antivir Ther 2008;13(5):675-85
  • Kwara A, Lartey M, Sagoe KW, CYP2B6 (c.516G–>T) and CYP2A6 (*9B and/or *17) polymorphisms are independent predictors of efavirenz plasma concentrations in HIV-infected patients. Br J Clin Pharmacol 2009;67(4):427-36
  • Haas DW, Ribaudo HJ, Kim RB, Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study. Aids 2004;18(18):2391-400
  • Lang T, Klein K, Fischer J, Extensive genetic polymorphism in the human CYP2B6 gene with impact on expression and function in human liver. Pharmacogenetics 2001;11(5):399-415
  • Tsuchiya K, Gatanaga H, Tachikawa N, Homozygous CYP2B6 *6 (Q172H and K262R) correlates with high plasma efavirenz concentrations in HIV-1 patients treated with standard efavirenz-containing regimens. Biochem Biophys Res Commun 2004;319(4):1322-6
  • Wyen C, Hendra H, Vogel M, Impact of CYP2B6 983T>C polymorphism on non-nucleoside reverse transcriptase inhibitor plasma concentrations in HIV-infected patients. J Antimicrob Chemother 2008;61(4):914-8
  • Rotger M, Tegude H, Colombo S, Predictive value of known and novel alleles of CYP2B6 for efavirenz plasma concentrations in HIV-infected individuals. Clin Pharmacol Ther 2007;81(4):557-66
  • Nyakutira C, Roshammar D, Chigutsa E, High prevalence of the CYP2B6 516G–>T(*6) variant and effect on the population pharmacokinetics of efavirenz in HIV/AIDS outpatients in Zimbabwe. Eur J Clin Pharmacol 2008;64(4):357-65
  • Rodriguez-Novoa S, Barreiro P, Rendon A, Influence of 516G>T polymorphisms at the gene encoding the CYP450-2B6 isoenzyme on efavirenz plasma concentrations in HIV-infected subjects. Clin Infect Dis 2005;40(9):1358-61
  • Rotger M, Colombo S, Furrer H, Influence of CYP2B6 polymorphism on plasma and intracellular concentrations and toxicity of efavirenz and nevirapine in HIV-infected patients. Pharmacogenet Genomics 2005;15(1):1-5
  • Saitoh A, Fletcher CV, Brundage R, Efavirenz pharmacokinetics in HIV-1-infected children are associated with CYP2B6-G516T polymorphism. J Acquir Immune Defic Syndr 2007;45(3):280-5
  • ter Heine R, Scherpbier HJ, Crommentuyn KM, A pharmacokinetic and pharmacogenetic study of efavirenz in children: dosing guidelines can result in subtherapeutic concentrations. Antivir Ther 2008;13(6):779-87
  • Klein K, Lang T, Saussele T, Genetic variability of CYP2B6 in populations of African and Asian origin: allele frequencies, novel functional variants, and possible implications for anti-HIV therapy with efavirenz. Pharmacogenet Genomics 2005;15(12):861-73
  • Mehlotra RK, Bockarie MJ, Zimmerman PA. CYP2B6 983T>C polymorphism is prevalent in West Africa but absent in Papua New Guinea: implications for HIV/AIDS treatment. Br J Clin Pharmacol 2007;64(3):391-5
  • Riska P, Lamson M, MacGregor T, Disposition and biotransformation of the antiretroviral drug nevirapine in humans. Drug Metab Dispos 1999;27(8):895-901
  • Lamson MJ, Cort S, Sabo JP, Assessment of Nevirapine oral bioavailability in healthy volunteers following oral and intravenous administration. Pharmacol Res 1995;12:S-415
  • Lamson MJ, Cort S, Sabo JP, Effects of gender on the single and multiple dose pharmacokinetics of nevirapine. Pharmacol Res 1995;12:S-101
  • Ofotokun I, Chuck SK, Hitti JE. Antiretroviral pharmacokinetic profile: a review of sex differences. Gend Med 2007;4(2):106-19
  • Combalbert J, Fabre I, Fabre G, Metabolism of cyclosporin A. IV. Purification and identification of the rifampicin-inducible human liver cytochrome P-450 (cyclosporin A oxidase) as a product of P450IIIA gene subfamily. Drug Metab Dispos 1989;17(2):197-207
  • Erickson DA, Mather G, Trager WF, Characterization of the in vitro biotransformation of the HIV-1 reverse transcriptase inhibitor nevirapine by human hepatic cytochromes P-450. Drug Metab Dispos 1999;27(12):1488-95
  • Burman WJ, Jones BE. Treatment of HIV-related tuberculosis in the era of effective antiretroviral therapy. Am J Respir Crit Care Med 2001;164(1):7-12
  • Cohen K, van Cutsem G, Boulle A, Effect of rifampicin-based antitubercular therapy on nevirapine plasma concentrations in South African adults with HIV-associated tuberculosis. J Antimicrob Chemother 2008;61(2):389-93
  • Alexander CS, Asselin JJ, Ting LS, Antiretroviral concentrations in untimed plasma samples predict therapy outcome in a population with advanced disease. J Infect Dis 2003;188(4):541-8
  • de Vries-Sluijs TE, Dieleman JP, Arts D, Low nevirapine plasma concentrations predict virological failure in an unselected HIV-1-infected population. Clin Pharmacokinet 2003;42(6):599-605
  • Gonzalez de Requena D, Bonora S, Garazzino S, Nevirapine plasma exposure affects both durability of viral suppression and selection of nevirapine primary resistance mutations in a clinical setting. Antimicrob Agents Chemother 2005;49(9):3966-9
  • Veldkamp AI, Weverling GJ, Lange JM, High exposure to nevirapine in plasma is associated with an improved virological response in HIV-1-infected individuals. AIDS 2001;15(9):1089-95
  • Kappelhoff BS, Crommentuyn KM, de Maat MM, Practical guidelines to interpret plasma concentrations of antiretroviral drugs. Clin Pharmacokinet 2004;43(13):845-53
  • Dean GL, Back DJ, de Ruiter A. Effect of tuberculosis therapy on nevirapine trough plasma concentrations. AIDS 1999;13(17):2489-90
  • Elsherbiny D, Cohen K, Jansson B, Population pharmacokinetics of nevirapine in combination with rifampicin-based short course chemotherapy in HIV- and tuberculosis-infected South African patients. Eur J Clin Pharmacol 2009;65(1):71-80
  • Ramachandran G, Hemanthkumar AK, Rajasekaran S, Increasing nevirapine dose can overcome reduced bioavailability due to rifampicin coadministration. J Acquir Immune Defic Syndr 2006;42(1):36-41
  • Ribera E, Pou L, Lopez RM, Pharmacokinetic interaction between nevirapine and rifampicin in HIV-infected patients with tuberculosis. J Acquir Immune Defic Syndr 2001;28(5):450-3
  • Boulle A, Van Cutsem G, Cohen K, Outcomes of nevirapine- and efavirenz-based antiretroviral therapy when coadministered with rifampicin-based antitubercular therapy. JAMA 2008;300(5):530-9
  • Oliva J, Moreno S, Sanz J, Co-administration of rifampin and nevirapine in HIV-infected patients with tuberculosis. AIDS 2003;17(4):637-8
  • Autar RS, Wit FW, Sankote J, Nevirapine plasma concentrations and concomitant use of rifampin in patients coinfected with HIV-1 and tuberculosis. Antivir Ther 2005;10(8):937-43
  • Manosuthi W, Ruxrungtham K, Likanonsakul S, Nevirapine levels after discontinuation of rifampicin therapy and 60-week efficacy of nevirapine-based antiretroviral therapy in HIV-infected patients with tuberculosis. Clin Infect Dis 2007;44(1):141-4
  • Manosuthi W, Sungkanuparph S, Thakkinstian A, Plasma nevirapine levels and 24-week efficacy in HIV-infected patients receiving nevirapine-based highly active antiretroviral therapy with or without rifampicin. Clin Infect Dis 2006;43(2):253-5
  • Avihingsanon A, Manosuthi W, Kantipong P, Pharmacokinetics and 48-week efficacy of nevirapine: 400 mg versus 600 mg per day in HIV-tuberculosis coinfection receiving rifampicin. Antivir Ther 2008;13(4):529-36
  • Manosuthi W, Sungkanuparph S, Tantanathip P, A randomized trial comparing plasma drug concentrations and efficacies between 2 nonnucleoside reverse-transcriptase inhibitor-based regimens in HIV-infected patients receiving rifampicin: the N2R Study. Clin Infect Dis 2009;48(12):1752-9
  • Soumya Swaminathan PC, Venkatesan P, Once-daily nevirapine vs efavirenz in the treatment of HIV-infected patients with TB: a Randomized Clinical Trial. Abstract # 35. Presented at the 16th Conference on Retroviruses and Opportunistic Infections (CROI 2009); 2009
  • L'Homme R, Warris A, Gibb D, Burger D. Children with HIV are not small adults: what is different in pharmacology? Curr Opin HIV AIDS 2007;2(5):405-9
  • Anderson GD, Lynn AM. Optimizing pediatric dosing: a developmental pharmacologic approach. Pharmacotherapy 2009;29(6):680-90
  • Chokephaibulkit K, Plipat N, Cressey TR, Pharmacokinetics of nevirapine in HIV-infected children receiving an adult fixed-dose combination of stavudine, lamivudine and nevirapine. AIDS 2005;19(14):1495-9
  • Ellis JC, L'Homme RF, Ewings FM, Nevirapine concentrations in HIV-infected children treated with divided fixed-dose combination antiretroviral tablets in Malawi and Zambia. Antivir Ther 2007;12(2):253-60
  • O'Brien DP, Sauvageot D, Zachariah R, Humblet P. In resource-limited settings good early outcomes can be achieved in children using adult fixed-dose combination antiretroviral therapy. AIDS 2006;20(15):1955-60
  • L'Homme RF, Kabamba D, Ewings FM, Nevirapine, stavudine and lamivudine pharmacokinetics in African children on paediatric fixed-dose combination tablets. AIDS 2008;22(5):557-65
  • Saitoh A, Sarles E, Capparelli E, CYP2B6 genetic variants are associated with nevirapine pharmacokinetics and clinical response in HIV-1-infected children. AIDS 2007;21(16):2191-9
  • Kamateeka MML, Mudiope P, Mubiru M, Immunological and virological response to fixed-dose nevirapine based highly active antiretroviral therapy (HAART) in HIV-infected Ugandan children with concurrent active tuberculosis infection on rifampicin-based anti-TB treatment. Abstract MOPEB089 presented at the 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention, Cape Town, July 2009
  • Oudijk JMMH, Mulenga V, Chintu C, Pharmacokinetics of nevirapine in young children during combined ART and rifampicin-containing antituberculosis treatment. Abstract LBPEB10 presented at the 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention, Cape Town, July 2009
  • Penzak SR, Kabuye G, Mugyenyi P, Cytochrome P450 2B6 (CYP2B6) G516T influences nevirapine plasma concentrations in HIV-infected patients in Uganda. HIV Med 2007;8(2):86-91
  • Ramachandran G, Ramesh K, Hemanth Kumar AK, Association of high T allele frequency of CYP2B6 G516T polymorphism among ethnic south Indian HIV-infected patients with elevated plasma efavirenz and nevirapine. J Antimicrob Chemother 2009;63(4):841-3
  • Bakshi S, Ramachandran G, Ramesh K, Study of ABCB1 polymorphism (C3435T) in HIV-1-infected individuals from South India. Br J Clin Pharmacol 2008 May;65(5):791-2
  • Bonnet M BN, Jani IV, Slawuski A, Pharmacokinetic parameters of nevirapine when given without 2-weeks leading dose in tuberculosis -HIV coinfected patients receiving rifamocin: substudy of the CARINE 12146 trial in Maputo. Abstract presented at the 5th IAS Conference on HIV Pathogenesis, Treatment and Prevention, Cape Town, July 2009

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