Exposure to Rifampicin and its Metabolite 25-Deacetylrifampicin Rapidly Decreases During Tuberculosis Therapy

Peloquin CA, Davies GR. The treatment of tuberculosis. Clin Pharmacol Ther. 2021;110(6):1455–66.

Article  PubMed  Google Scholar 

van Ingen J, Aarnoutse RE, Donald PR, Diacon AH, Dawson R, van Balen GP, et al. Why do we use 600 mg of rifampicin in tuberculosis treatment? Clin Infect Dis. 2011;52(9):e194–9.

Article  PubMed  Google Scholar 

Akkerman OW, Dijkwel RDC, Kerstjens HAM, van der Werf TS, Srivastava S, Sturkenboom MGG, et al. Isoniazid and rifampicin exposure during treatment in drug-susceptible TB. Int J Tuberc Lung Dis. 2023;27(10):772–7.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Trentalange A, Borgogno E, Motta I, Antonucci M, Pirriatore V, Costa C, et al. Rifampicin and isoniazid maximal concentrations are below efficacy-associated thresholds in the majority of patients: time to increase the doses? Int J Antimicrob Agents. 2021;57(3): 106297.

Article  CAS  PubMed  Google Scholar 

Pasipanodya JG, McIlleron H, Burger A, Wash PA, Smith P, Gumbo T. Serum drug concentrations predictive of pulmonary tuberculosis outcomes. J Infect Dis. 2013;208(9):1464–73.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Nahid P, Mase SR, Migliori GB, Sotgiu G, Bothamley GH, Brozek JL, et al. Treatment of drug-resistant tuberculosis: an official ATS/CDC/ERS/IDSA clinical practice guideline. Am J Respir Crit Care Med. 2019;200(10):e93-142.

Article  PubMed  PubMed Central  Google Scholar 

Zheng X, Bao Z, Forsman LD, Hu Y, Ren W, Gao Y, et al. Drug exposure and minimum inhibitory concentration predict pulmonary tuberculosis treatment response. Clin Infect Dis. 2021;73(9):e3520–8.

Article  CAS  PubMed  Google Scholar 

Sekaggya-Wiltshire C, von Braun A, Lamorde M, Ledergerber B, Buzibye A, Henning L, et al. Delayed sputum culture conversion in tuberculosis-human immunodeficiency virus-coinfected patients with low isoniazid and rifampicin concentrations. Clin Infect Dis. 2018;67(5):708–16.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Te Brake L, Dian S, Ganiem AR, Ruesen C, Burger D, Donders R, et al. Pharmacokinetic/pharmacodynamic analysis of an intensified regimen containing rifampicin and moxifloxacin for tuberculous meningitis. Int J Antimicrob Agents. 2015;45(5):496–503.

Article  Google Scholar 

Boeree MJ, Diacon AH, Dawson R, Narunsky K, du Bois J, Venter A, et al. A dose-ranging trial to optimize the dose of rifampin in the treatment of tuberculosis. Am J Respir Crit Care Med. 2015;191(9):1058–65.

Article  CAS  PubMed  Google Scholar 

Onorato L, Gentile V, Russo A, Di Caprio G, Alessio L, Chiodini P, et al. Standard versus high dose of rifampicin in the treatment of pulmonary tuberculosis: a systematic review and meta-analysis. Clin Microbiol Infect. 2021;27(6):830–7.

Article  CAS  PubMed  Google Scholar 

Marais S, Cresswell FV, Hamers RL, Te Brake LHM, Ganiem AR, Imran D, et al. High dose oral rifampicin to improve survival from adult tuberculous meningitis: a randomised placebo-controlled double-blinded phase III trial (the HARVEST study). Wellcome Open Res. 2019;4:190.

Article  PubMed  Google Scholar 

Perumal Kannabiran B, Palaniappan NA, Manoharan T, Paramasivam PK, Saini JK, Ansari MS, et al. Safety and efficacy of 25 mg/kg and 35 mg/kg vs 10 mg/kg rifampicin in pulmonary TB: a phase IIb randomized controlled trial. Open Forum Infect Dis. 2024;11(3):ofae034.

Article  PubMed  PubMed Central  Google Scholar 

Abulfathi AA, Decloedt EH, Svensson EM, Diacon AH, Donald P, Reuter H. Clinical pharmacokinetics and pharmacodynamics of rifampicin in human tuberculosis. Clin Pharmacokinet. 2019;58(9):1103–29.

Article  CAS  PubMed  Google Scholar 

Loos U, Musch E, Jensen JC, Mikus G, Schwabe HK, Eichelbaum M. Pharmacokinetics of oral and intravenous rifampicin during chronic administration. Klin Wochenschr. 1985;63(23):1205–11.

Article  CAS  PubMed  Google Scholar 

Vu DH, Koster RA, Bolhuis MS, Greijdanus B, Altena RV, Nguyen DH, et al. Simultaneous determination of rifampicin, clarithromycin and their metabolites in dried blood spots using LC-MS/MS. Talanta. 2014;121:9–17.

Article  CAS  PubMed  Google Scholar 

Bahuaud O, Genestet C, Hoffmann J, Dumitrescu O, Ader F. Opti-4TB: a protocol for a prospective cohort study evaluating the performance of new biomarkers for active tuberculosis outcome prediction. Front Med (Lausanne). 2022;9: 998972.

Article  PubMed  PubMed Central  Google Scholar 

Genestet C, Ader F, Pichat C, Lina G, Dumitrescu O, Goutelle S. Assessing the combined antibacterial effect of isoniazid and rifampin on four Mycobacterium tuberculosis strains using in vitro experiments and response-surface modeling. Antimicrob Agents Chemother. 2018;62(1):e01413-e1417.

Article  PubMed  Google Scholar 

Devine BJ. Gentamicin therapy. Drug Intell Clin Pharm. 1974;8:650–5.

Google Scholar 

James WPT, Waterlow JC. Research on obesity: a report of the DHSS/MRC Group. HM Stationery Office; 1976.

Gehan EA, Georges SL. Estimation of human body surface area from height and weight. Cancer Chemother Rep. 1970;54(4):225.

CAS  PubMed  Google Scholar 

Levey AS, Stevens LA, Schmid CH, Zhang YL, Castro AF 3rd, Feldman HI, et al. A new equation to estimate glomerular filtration rate. Ann Intern Med. 2009;150(9):604–12.

Article  PubMed  PubMed Central  Google Scholar 

van Buuren S, Groothuis-Oudshoorn K. Multivariate imputation by chained equations in R. J Stat Softw. 2011;45(3):1–67.

Article  Google Scholar 

Muda MR, Harun SN, Syed Sulaiman SA, Sheikh Ghadzi SM. Population pharmacokinetics analyses of rifampicin in adult and children populations: a systematic review. Br J Clin Pharmacol. 2022;88(7):3132–52.

Article  PubMed  Google Scholar 

Seng KY, Hee KH, Soon GH, Chew N, Khoo SH, Lee LS. Population pharmacokinetics of rifampicin and 25-deacetyl-rifampicin in healthy Asian adults. J Antimicrob Chemother. 2015;70(12):3298–306.

Article  CAS  PubMed  Google Scholar 

Loos U, Musch E, Jensen JC, Schwabe HK, Eichelbaum M. Influence of the enzyme induction by rifampicin on its presystemic metabolism. Pharmacol Ther. 1987;33(1):201–4.

Article  CAS  PubMed  Google Scholar 

Smythe W, Khandelwal A, Merle C, Rustomjee R, Gninafon M, Bocar Lo M, et al. A semimechanistic pharmacokinetic-enzyme turnover model for rifampin autoinduction in adult tuberculosis patients. Antimicrob Agents Chemother. 2012;56(4):2091–8.

Article  CAS  PubMed  PubMed Central  Google Scholar 

Svensson RJ, Aarnoutse RE, Diacon AH, Dawson R, Gillespie SH, Boeree MJ, et al. A population pharmacokinetic model incorporating saturable pharmacokinetics and autoinduction for high rifampicin doses. Clin Pharmacol Ther. 2018;103(4):674–83.

Article  CAS  PubMed  Google Scholar 

Chirehwa MT, Rustomjee R, Mthiyane T, Onyebujoh P, Smith P, McIlleron H, et al. Model-based evaluation of higher doses of rifampin using a semimechanistic model incorporating autoinduction and saturation of hepatic extraction. Antimicrob Agents Chemother. 2016;60(1):487–94.

Article  CAS  PubMed  Google Scholar 

Chang MJ, Chae JW, Yun HY, Lee JI, Choi HD, Kim J, et al. Effects of type 2 diabetes mellitus on the population pharmacokinetics of rifampin in tuberculosis patients. Tuberculosis (Edinb). 2015;95(1):54–9.

Article  CAS  PubMed  Google Scholar 

Kim ES, Kwon BS, Park JS, Chung JY, Seo SH, Park KU, et al. Relationship among genetic polymorphism of SLCO1B1, rifampicin exposure and clinical outcomes in patients with active pulmonary tuberculosis. Br J Clin Pharmacol. 2021;87(9):3492–500.

Article  CAS  PubMed  Google Scholar 

Gao Y, Davies Forsman L, Ren W, Zheng X, Bao Z, Hu Y, et al. Drug exposure of first-line anti-tuberculosis drugs in China: a prospective pharmacological cohort study. Br J Clin Pharmacol. 2021;87(3):1347–58.

Article  CAS  PubMed 

Comments (0)

No login
gif