References
- Holtgrave DR . Causes of the decline in AIDS deaths, United States, 1995–2002. Prevention, treatment or both? Int. J. STD AIDS16 , 777–781 (2005).
- Palella FJ , DelaneyKM, MoormanAC et al. Declining morbidity and mortality among patients with advanced human immunodeficiency virus infection. N. Engl. J. Med. 338 , 853–860 (1998).
- Sabin CA , SmithCJ, YouleM et al. Deaths in the era of HAART: contribution of late presentation, treatment exposure, resistance and abnormal laboratory markers. AIDS 20 , 67–71 (2006).
- Trotta MP , AmmasariA, MelziS et al. Treatment-related factors and highly active antiretroviral therapy adherence. J. Acquir. Immune Defic. Syndr. 31 , S128–S131 (2002).
- Johnson MO , StalworthT, NeilandsTB. Three drugs or the disease? Causal attributions of symptoms held by HIV positive adults on HAART. AIDS Behav.7 , 109–117 (2003).
- Carr A , CooperDA. Adverse effects of antiretroviral therapy. Lancet3356 , 1423–1430 (2000).
- O‘Brien ME , ClarkRA, BeschCL, MyersL, KissingerP. Patterns and correlates of discontinuation of the initial HAART regimen in an urban outpatient cohort. J. Acquir. Inmune Defic. Syndr.34 , 407–414 (2003).
- Staszewski S , Morales-RamirezJ, TashimaKT et al. EFV plus zidovudine and lamivudine, EFV plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. N. Engl. J. Med. 341 , 1865–1873 (1999).
- Wynn H , BrundageR, FletcherC. Clinical implications of central nervous system penetration of antiretroviral drugs. CNS Drugs6 , 595–609 (2002).
- von Giesen HJ , KöllerH, TheisenA, ArendtG. Therapeutic effects of nonnucleoside reverse transcriptase inhibitors on the central nervous system in HIV-1-infected patients. J. Acquir. Immune Defic. Syndr.29 , 363–367 (2002).
- Adkins JC , NobleS. EFV. Drugs56 , 1055–1066 (1998).
- Clifford DB , EvansS, YangY et al. Impact of efavirenz on neuropsychological performance and symptoms in HIV-infected individuals. Ann. Intern. Med. 143 , 714–721 (2005).
- Pérez-Molina JA . Safety and tolerance of efavirenz in different antiretroviral regimens: results from a national multicenter prospective study in 1,033 HIV-infected patients. HIV Clin. Trials3 , 279–286 (2002).
- Hartmann M , RumpA, BrustJ et al. Evaluation of an efavirenz-containing regimen: an open-label, multicenter study. HIV Clin. Trials 2 , 421–428 (2001).
- Fumaz CR , TuldràA, FerrerMJ et al. Quality of life, emotional status, and adherence of HIV-1-infected patients treated with efavirenz versus protease inhibitor-containing regimens. J. Acquir. Immune Defic. Syndr. 29 , 244–253 (2002).
- Gutiérrez F , NavarroA, PadillaS et al. Prediction of neuropsychiatric adverse events associated with long-term efavirenz therapy, using plasma drug level monitoring. Clin. Infect. Dis. 41 , 1648–1653 (2005).
- Lochet P , PeyrièreH, LotthéA, MauboussinJM, DelmasB, ReynesJ. Long-term assessment of neuropsychiatric adverse reactions associated with efavirenz. HIV Med.4 , 62–66 (2003).
- Fumaz CR , Muñoz-MorenoJA, MoltóJ et al. Long-term neuropsychiatric disorders on efavirenz-based approaches: quality of life, psychologic issues, and adherence. J. Acquir. Immune. Defic. Syndr. 38(5) , 560–565 (2005).
- Marzolini C , TelentiA, DecosterdLA, GreubG, BiollazJ, BuclinT. Efavirenz plasma levels can predict treatment failure and central nervous system side effects in HIV-1-infected patients. AIDS15 , 71–75 (2001).
- Núñez M , González de Requeda D, Gallego L, Jiménez-Nácher I, González-Lahoz J, Soriano V. Higher efavirenz plasma levels correlate with development of insomnia. J. Acquir. Immune Defic. Syndr.28 , 399–400 (2001).
- Fuertes A , CabreraS, ValverdeMP, Domínguez-GilA. Hyperhidrosis in association with efavirenz. AIDS Patient Care STDS23 , 143–145 (2009).
- Gallego L , BarreiroP, del Río R et al. Analyzing sleep abnormalities in HIV-infected patients treated with efavirenz. Clin. Infect. Dis.38 , 430–432 (2004).
- Cabrera Figueroa S , Iglesias Gómez A, Sánchez Martín A, de la Paz Valverde Merino M, Domínguez-Gil Hurlé A, Cordero Sánchez M. Long-term efficacy and safety of efavirenz dose reduction to 200 mg once daily in a Caucasian patient with HIV. Clin. Drug. Investig.30 , 405–411 (2010).
- Haas DW , RibaudoHJ, KimRB et al. Pharmacogenetics of efavirez and central nervous system side effects: an adult AIDS clinical trials group study. AIDS 18 , 2391–2400 (2004).
- Puzantian T . Central nervous system adverse effects with EFV: case report and review. Pharmacotherapy22 , 930–933 (2002).
- Brundage RC , YongFH, FentonT, SpectorSA, StarrSE, FletcherCV. Intrapatient variability of efavirenz concentrations as a predictor of virologic response to antiretroviral therapy. Antimicrob. Agents Chemother.48 , 979–984 (2004).
- Pfister M , LabbeL, HammerSM et al. Population pharmacokinetics and pharmacodynamics of efavirenz, nelfinavir and indinavir. Antimicrob. Agents Chemother. 47 , 130–137 (2003).
- Lubomirov R , CsajkaC, TelentiA. ADME pathway approach for pharmacogenetic studies of anti-HIV therapy. Pharmacogenomics28 , 623–633 (2007).
- Ward BA , GorskiJC, JonesDR, HallSD, FlockhartDA, DestaZ. 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.306 , 287–300 (2003).
- Desta Z , SausseleT, WardB et al. Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitro. Pharmacogenomics 8 , 547–558 (2007).
- Di Iulio J , FayetA, Arab-AlameddineM et al. In vivo analysis of efavirenz metabolism in individuals with impaired CYP2A6 function. Pharmacogenet. Genomics19 , 300–309 (2009).
- Kwara A , LarteyM, SagoeKW, KenuE, CourtMH. CYP2B6, CYP2A6 and UGT2B7 genetic polymorphisms are predictors of efavirenz mid-dose concentration in HIV-infected patients. AIDS23 , 2101–2106 (2009).
- Kwara A , LarteyM, SagoeKW, RzekNL, CourtMH. 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.67 , 427–436 (2009).
- Arab-Alameddine M , Di Iulio J, Buclin T et al. Pharmacogenetics-based population pharmacokinetic analysis of efavirenz in HIV-1-infected individuals. Clin. Pharmacol. Ther.85 , 485–494 (2009).
- Sánchez A , CabreraS, SantosD et al. Population pharmacokinetic/pharmacogenetic model for optimization of efavirenz therapy in Caucasian HIV-infected patients. Antimicrob. Agents Chemother. 55(11) , 5314–5324 (2011).
- Fellay J , MarzoliniC, MeadenER et al. Response to antiretroviral treatment in HIV-1-infected individuals with allelic variants of the multidrug resistance transporter 1: a pharmacogenetics study. Lancet 359 , 30–36 (2002).
- Tsuchiya K , GatanagaH, TachikawaN et al. 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. 319 , 1322–1326 (2004).
- Motsinger AA , RitchieMD, ShaferRW et al. Multilocus genetic interactions and response to efavirenz-containing regimens: an adult AIDS clinical trials group study. Pharmacogenet. Genomics 16 , 837–845 (2006).
- Saitoh A , SinghKK, PowellCA et al. An MDR1-3435 variant is associated with higher plasma nelfinavir levels and more rapid virologic response in HIV-1 infected children. AIDS 19 , 371–380 (2005).
- Rotger M , TegudeH, ColomboS et al. Predictive value of known and novel alleles of CYP2B6 for efavirenz plasma concentrations in HIV-infected individuals. Clin. Pharmacol. Ther. 81 , 557–566 (2007).
- Ribaudo HJ , LiuH, SchwabM et al. Effect of CYP2B6, ABCB1, and CYP3A5 polymorphisms on efavirenz pharmacokinetics and treatment response: an AIDS clinical trials group study. J. Infect. Dis. 202 , 717–722 (2010).
- Leger P , DillinghamR, BeauharnaisCA et al. CYP2B6 variants and plasma efavirenz concentrations during antiretroviral therapy in Port-au-Prince, Haiti. J. Infect. Dis.200 , 955–964 (2009).
- Haas DW , GebretsadikT, MayoG et al. Associations between CYP2B6 polymorphisms and pharmacokinetics after a single dose of nevirapine or efavirenz in African Americans. J. Infect. Dis. 199 , 872–880 (2009).
- Alex KD , PehekEA. Pharmacologic mechanisms of serotonergic regulation of dopamine neurotransmission. Pharmacol. Ther.113 , 296–320 (2007).
- Manji HK , DrevetsWC, CharneyDS. The cellular neurobiology of depression. Nat. Med.7(5) , 541–547 (2001).
- Varga G , SzekelyA, Sasvari-SzekelyM. Candidate gene studies of dopaminergic and serotonergic polymorphisms. Neuropsychopharmacol. Hung.13 , 93–101 (2011).
- Knobel H , AlonsoJ, CasadoJL et al. Validation of a simplified medication adherence questionnaire in a large cohort of HIV-infected patients: the GEEMA Study. AIDS 16 , 605–613 (2002).
- Beal SL , SheinerLB, BoeckmannAJ. NONMEM Users Guides. Icon Development Solutions MD, USA (1989–2006).
- Cabrera S , SantosD, ValverdeMP et al. Influence of the cytochrome P450 2B6 genotype on population pharmacokinetics of efavirenz in human immunodeficiency virus patients. Antimicrob. Agents Chemother. 53 , 2791–2798 (2009).
- Gonzalez JR , ArmengolL, SoleX et al. SNPassoc: an R package to perform whole genome association studies. Bioinformatics 23 , 644–645 (2007).
- Wyen C , HendraH, SiccardiM et al. Cytochrome P450 2B6 (CYP2B6) and constitutive androstane receptor (CAR) polymorphisms are associated with early discontinuation of efavirenz-containing regimens. J. Antimicrob. Chemother. 66 , 2092–2098 (2011).
- Fayet Mello A , BuclinT, DecosterdLA et al. Successful efavirenz dose reduction guided by therapeutic drug monitoring. Antivir. Ther. 16 , 189–197 (2011).
- Gatanaga H , HayashidaT, TsuchiyaK et al. Successful efavirenz dose reduction in HIV type 1-infected individuals with cytochrome P450 2B6 *6 and *26. Clin. Infect. Dis. 45 , 1230–1237 (2007).
- Ribera E , López-CortésLF, SorianoV, CasadoJL, MallolasJ. Therapeutic drug monitoring and the inhibitory quotient of antiretroviral drugs: can they be applied to the current situation? Enferm. Infecc. Microbiol. Clin.23 , 41–67 (2005).
- Kharasch ED , CampbellS, StubbertK et al. Mechanism of efavirenz influence on methadone pharmacokinetics and pharmacodynamics II: hepatic and intestinal CYP2B6, CYP3A and transporter activities. Clin. Pharmacol. Ther. 91 , 673–684 (2012).
- Weiss J , HerzogM, Sonja König S et al. Induction of multiple drug transporters by efavirenz. J. Pharmacol. Sci.109 , 242–250 (2009).
▪ Websites
- Panel on Antiretroviral Guidelines for Adult and Adolescents. Guidelines for the use of antiretroviral agents in HIV-1-infected adults and adolescents. Department of Health and Human Services. AIDSinfo website (10 January 2011) www.aidsinfo.nih.gov/ContentFiles/AdultandAdolescentGL.pdf (Accessed 19June2012).
- British HIV Association guidelines for the treatment of HIV-1-infected adults with antiretroviral therapy 2008. British HIV Association BHIVA website, 9 June 2008. www.bhiva.org/TreatmentofHIV1_2008.aspx (Accessed 22December2012)
- US FDA. Sustiva label information, approved 18 August 2008. www.accessdata.fda.gov/drugsatfda_docs/label/2008/020972s030,021360s019lbl.pdf (Accessed 22December2012)
- HapMap project. http://hapmap.ncbi.nlm.nih.gov/downloads/encode1.html.en
- HIV Pharmacology. USA: HIVPharmacology.com Editorial Board: Editor; 2006. Updated Guidelines 2006. www.hivpharmacology.com (Accessed 17January2013)