Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?

International Journal of Clinical Pharmacology and Therapeutics

Volumn 52, Issue 6, 2014, Pages 446-453

  Liu, Jiang ^a   Chan Tack, Kirk M ^a   Jadhav, Pravin ^a   Seo, Shirley ^a   Robertson, Sarah M ^a   Kraft, Jeffrey ^a   Singer, Mary E ^a   Struble, Kimberly A ^a   Arya, Vikram ^a  

^a CENTER FOR DRUG EVALUATION AND RESEARCH   (United States)

Author keywords

Drug interaction; Efavirenz; HIV; Rifampin; Tuberculosis

Indexed keywords

CYTOCHROME P450 2B6; EFAVIRENZ; RIFAMPICIN;

ANXIETY DISORDER; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DEPRESSION; DIZZINESS; DROWSINESS; DRUG APPROVAL; DRUG DOSE INCREASE; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG EXPOSURE; DRUG POTENTIATION; DRUG SAFETY; FOOD AND DRUG ADMINISTRATION; GENOTYPE; HALLUCINATION; HEADACHE; HEPATITIS; HUMAN; MAJOR CLINICAL STUDY; MAXIMUM PLASMA CONCENTRATION; RASH; RISK ASSESSMENT; SINGLE DRUG DOSE; SLEEP DISORDER; SOMNOLENCE; UNSPECIFIED SIDE EFFECT; VIVID DREAM;

ANTIBIOTICS, ANTITUBERCULAR; AREA UNDER CURVE; ARYL HYDROCARBON HYDROXYLASES; BENZOXAZINES; COINFECTION; COMPUTER SIMULATION; DRUG ADMINISTRATION SCHEDULE; DRUG APPROVAL; DRUG DOSAGE CALCULATIONS; DRUG INTERACTIONS; GENOTYPE; HIV INFECTIONS; HUMANS; MODELS, BIOLOGICAL; PHENOTYPE; POLYPHARMACY; REVERSE TRANSCRIPTASE INHIBITORS; RIFAMPIN; TUBERCULOSIS; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 84902190005     PISSN: 09461965     EISSN: None     Source Type: Journal    
DOI: 10.5414/CP202079     Document Type: Article

References (34)

1. World Health Organization Consolidated Guidelines on the Use of Antiretroviral Drugs for Treating and Preventing HIV Infection. Available at http://apps.who.int/iris/bitstream/1?06?65/?8?5?3?2?1?/?1?/?9?789241505727-eng. pdf. Accessed on November 15, 2013.
2. Panel on Antiretroviral Guidelines for Adults and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. Available at http://aidsinfo.nih.gov/ contentfiles/lvguidelines/AdultandAdolescentGL.pdf. Accessed on November 15, 2013.
3. Panel on Opportunistic Infections in HIV-Infected Adults and Adolescents. Guidelines for the prevention and treatment of opportunistic infections in HIV-infected adults and adolescents: recommendations from the Centers for Disease Control and Prevention, the National Institutes of Health, and the HIV Medicine Association of the Infectious Diseases Society of America. Available at http://aidsinfo.nih.gov/contentfiles/lvguidelines/adult-oi.pdf. Accessed on November 15, 2013.
4. Panel on Antiretroviral Therapy and Medical Management of HIV-Infected Children. Guidelines for the Use of Antiretroviral Agents in Pediatric HIV Infection. Available at http://aidsinfo.nih.gov/contentfiles/lvguidelines/ pediatricguidelines.pdf. Accessed on November 15, 2013.
5. Guidelines for the Prevention and Treatment of Opportunistic Infections Among HIV-Exposed and HIV-Infected Children. Available at http://www.aidsinfo. nih.gov/contentfiles/lvguidelines/oi-guidelines-pediatrics.pdf. Accessed on November 15, 2013.
6. Pozniak AL, Coyne KM, Miller RF, Lipman MC, Freedman AR, Ormerod LP, Johnson MA, Collins S, Lucas SB; BHIVA Guidelines Subcommittee. British HIV Association guidelines for the treatment of TB/HIV coinfection 2011. HIV Med. 2011; 12: 517-524. CrossRef PubMed
7. Harries AD, Lawn SD, Getahun H, Zachariah R, Havlir DV. HIV and tuberculosis - science and implementation to turn the tide and reduce deaths. J Int AIDS Soc. 2012; 15: 17396. CrossRef PubMed
8. Matteelli A, Regazzi M, Villani P, De Iaco G, Cusato M, Carvalho AC, Caligaris S, Tomasoni L, Manfrin M, Capone S, Carosi G. Multiple-dose pharmacokinetics of efavirenz with and without the use of rifampicin in HIV-positive patients. Curr HIV Res. 2007; 5: 349-353. CrossRef PubMed (Pubitemid 46785071)
9. López-Cortés LF, Ruiz-Valderas R, Viciana P, Alarcón-González A, Gómez-Mateos J, León-Jimenez E, Sarasanacenta M, López-Pua Y, Pachón J. Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis. Clin Pharmacokinet. 2002; 41: 681-690. CrossRef PubMed
10. Yenny N, Nafrialdi, Djoerban Z, Setiabudy R. Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers. Int J Clin Pharmacol Ther. 2011; 49: 162-168. CrossRef PubMed
11. Ngaimisi E, Mugusi S, Minzi O, Sasi P, Riedel KD, Suda A, Ueda N, Janabi M, Mugusi F, Haefeli WE, Bertilsson L, Burhenne J, Aklillu E. Effect of rifampicin and CYP2B6 genotype on long-term efavirenz autoinduction and plasma exposure in HIV patients with or without tuberculosis. Clin Pharmacol Ther. 2011; 90: 406-413. CrossRef PubMed
12. Haas DW, Ribaudo HJ, Kim RB, Tierney C, Wilkinson GR, Gulick RM, Clifford DB, Hulgan T, Marzolini C, Acosta EP. Pharmacogenetics of efavirenz and central nervous system side effects: an Adult AIDS Clinical Trials Group study. AIDS. 2004; 18: 2391-2400. PubMed (Pubitemid 40065906)
13. Gutiérrez F, Navarro A, Padilla S, Antón R, Masiá M, Borrás J, Martín-Hidalgo A. Prediction of neuropsychiatric adverse events associated with long-term efavirenz therapy, using plasma drug level monitoring. Clin Infect Dis. 2005; 41: 1648-1653. CrossRef PubMed (Pubitemid 41691605)
14. Marzolini C, Telenti A, Decosterd LA, Greub G, Biollaz J, Buclin T. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS. 2001; 15: 71-75. CrossRef PubMed (Pubitemid 32055781)
15. Rodriguez-Novoa S, Barreiro P, Rendón A, Jiménez-Nacher I, González-Lahoz J, Soriano V. 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: 1358-1361. CrossRef PubMed (Pubitemid 40570249)
16. Brennan-Benson P, Lyus R, Harrison T, Pakianathan M, Macallan D. Pharmacokinetic interactions between efavirenz and rifampicin in the treatment of HIV and tuberculosis: one size does not fit all. AIDS. 2005; 19: 1541-1543. CrossRef PubMed (Pubitemid 41400701)
17. Manosuthi W, Sungkanuparph S, Thakkinstian A, Vibhagool A, Kiertiburanakul S, Rattanasiri S, Prasithsirikul W, Sankote J, Mahanontharit A, Ruxrungtham K. Efavirenz levels and 24-week efficacy in HIV-infected patients with tuberculosis receiving highly active antiretroviral therapy and rifampicin. AIDS. 2005; 19: 1481-1486. CrossRef PubMed (Pubitemid 41400693)
18. Manosuthi W, Kiertiburanakul S, Sungkanuparph S, Ruxrungtham K, Vibhagool A, Rattanasiri S, Thakkinstian A. Efavirenz 600 mg/day versus efavirenz 800 mg/day in HIV-infected patients with tuberculosis receiving rifampicin: 48 weeks results. AIDS. 2006; 20: 131-132. CrossRef PubMed (Pubitemid 41818129)
19. 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: 1299-1302. CrossRef PubMed (Pubitemid 44884158)
20. Orrell C, Cohen K, Conradie F, Zeinecker J, Ive P, Sanne I, Wood R. Efavirenz and rifampicin in the South African context: is there a need to dose-increase efavirenz with concurrent rifampicin therapy? Antivir Ther. 2011; 16: 527-534. CrossRef PubMed
21. Villar J, Sánchez P, González A, Sorli L, Montero MM, Guelar A, Solé E, López JL, Knobel H. Use of non-nucleoside analogues together with rifampin in HIV patients with tuberculosis. HIV Clin Trials. 2011; 12: 171-174. CrossRef PubMed
22. González de Requena D, Gallego O, Corral A, Jiménez- Nácher I, Soriano V. Higher efavirenz concentrations determine the response to viruses carrying non-nucleoside reverse transcriptase resistance mutations. AIDS. 2004; 18: 2091-2094. CrossRef PubMed (Pubitemid 39463366)
23. Burger D, van der Heiden I, la Porte C, van der Ende M, Groeneveld P, Richter C, Koopmans P, Kroon F, Sprenger H, Lindemans J, Schenk P, van Schaik R. 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: 148-154. CrossRef PubMed (Pubitemid 43382608)
24. Gatanaga H, Hayashida T, Tsuchiya K, Yoshino M, Kuwahara T, Tsukada H, Fujimoto K, Sato I, Ueda M, Horiba M, Hamaguchi M, Yamamoto M, Takata N, Kimura A, Koike T, Gejyo F, Matsushita S, Shirasaka T, Kimura S, Oka S. Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6*6 and*26. Clin Infect Dis. 2007; 45: 1230-1237. CrossRef PubMed (Pubitemid 47580326)
25. Boulle A, Van Cutsem G, Cohen K, Hilderbrand K, Mathee S, Abrahams M, Goemaere E, Coetzee D, Maartens G. Outcomes of nevirapine- and efavirenz-based antiretroviral therapy when coadministered with rifampicin-based antitubercular therapy. JAMA. 2008; 300: 530-539. CrossRef PubMed
26. Manosuthi W, Mankatitham W, Lueangniyomkul A, Chimsuntorn S, Sungkanuparph S. Standarddose efavirenz vs. standard-dose nevirapine in antiretroviral regimens among HIV-1 and tuberculosis co-infected patients who received rifampicin. HIV Med. 2008; 9: 294-299. CrossRef PubMed (Pubitemid 351517276)
27. Khan FA, Minion J, Pai M, Royce S, Burman W, Harries AD, Menzies D. Treatment of active tuberculosis in HIV-coinfected patients: a systematic review and meta-analysis. Clin Infect Dis. 2010; 50: 1288-1299. CrossRef PubMed
28. DiGiacinto JL, Chan-Tack KM, Robertson SM, Reynolds KS, Struble KA. Are literature references sufficient for dose recommendations? An FDA case study of efavirenz and rifampin. J Clin Pharmacol. 2008; 48: 518-523. CrossRef PubMed (Pubitemid 351389117)
29. Bristol Myers Squibb. Efavirenz (Sustiva) product information, 2013.
30. Food and Drug Administration. Sustiva labeling update/dosing adjustment with rifampin. Jan 6, 2012. (http://www.natap.org/2012/newsUpdates/010612-06. htm).
31. Bristol Myers Squibb and Gilead Sciences, LLC. Efavirenz, Emtricitabine, and Tenofovir disoproxil fumarate (Atripla) product information, 2013.
32. Gengiah T, Abdool Karim S. Should efavirenz be dosed higher when coadministered with rifampin? Journal Watch HIV. AIDS Clin Care. 2012; 6. http://www.jwatch.org/ac2012?020?600?00?00?1/?20?12/02/06/should-efavirenz-be- dosed-higher-when
33. Csajka C, Marzolini C, Fattinger K, Décosterd LA, Fellay J, Telenti A, Biollaz J, Buclin T . Population pharmacokinetics and effects of efavirenz in patients with human immunodeficiency virus infection. Clin Pharmacol Ther. 2003; 73: 20-30. CrossRef PubMed (Pubitemid 36158483)
34. Tang C, Lin JH, Lu AY. Metabolism-based drug-drug interactions: what determines individual variability in cytochrome P450 induction? Drug Metab Dispos. 2005; 33: 603-613. CrossRef (Pubitemid 40593872)