Drug exposure of first-line anti-tuberculosis drugs in China: A prospective pharmacological cohort study.
antituberculosis drugs
dosing strategy
drug exposure
population pharmacokinetics
Journal
British journal of clinical pharmacology
ISSN: 1365-2125
Titre abrégé: Br J Clin Pharmacol
Pays: England
ID NLM: 7503323
Informations de publication
Date de publication:
03 2021
03 2021
Historique:
received:
29
11
2019
revised:
27
07
2020
accepted:
03
08
2020
pubmed:
20
1
2021
medline:
27
7
2021
entrez:
19
1
2021
Statut:
ppublish
Résumé
Exploring the need for optimization of drug exposure to improve tuberculosis (TB) treatment outcome is of great importance. We aimed to describe drug exposure at steady state as well as the population pharmacokinetics (PK) of rifampicin (RIF), isoniazid (INH) and pyrazinamide (PZA) in Chinese TB patients. A prospective multicentre PK study of RIF, INH and PZA was conducted in China between January 2015 and December 2017. Six blood samples were collected from each subject for drug concentration measurement. Nonlinear mixed effect analyses were used to develop population PK models. In total, 217 patients were included. Positive correlations between body weight, clearance and volume of distribution were identified for RIF and PZA, whereas body weight only influenced clearance for INH. In addition, males had higher RIF clearance and thus lower RIF exposure than women. Acetylator status was significantly associated with INH clearance as INH exposure in intermediate and fast acetylators was significantly lower than in slow acetylators, especially in low-weight bands. Simulations also showed significantly lower drug exposures in low-weight bands for all three drugs. Patients weighing <38 kg were respectively exposed to 30.4%, 45.9% and 18.0% lower area under the concentration-time curve of RIF, INH and PZA than those weighing ≥70 kg. Higher doses by addition of one fixed-dose combination tablet or 150 mg INH were simulated and found to be effective in improving INH drug exposures, especially in low-weight bands. PK variability of first-line anti-TB drugs is common in Chinese TB patients. The developed population PK models can be used to optimize drug exposures in Chinese patients. Moreover, standard dosing needs to be adjusted to increase target attainment.
Substances chimiques
Antitubercular Agents
0
Pharmaceutical Preparations
0
Isoniazid
V83O1VOZ8L
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1347-1358Subventions
Organisme : National Natural Science Foundation of China
ID : 81874273
Organisme : Natural Science Foundation of Henan Province
ID : 182300410385
Organisme : Sweden-China project
ID : VR-grant No. 54020138797
Organisme : Sweden-China project
ID : NSFC No. 81361138019
Organisme : Fourth Round of Three-Year Public Health Action Plan of Shanghai, China
ID : 15GWZK0101
Informations de copyright
© 2020 The British Pharmacological Society.
Références
World Health Organization. Global tuberculosis report 2019. Geneva, Switzerland: World Health Organization; 2019.
Uplekar M, Weil D, Lonnroth K, et al. WHO's new end TB strategy. Lancet. 2015;385(9979):1799-1801.
Kumar AK, Chandrasekaran V, Kannan T, et al. Anti-tuberculosis drug concentrations in tuberculosis patients with and without diabetes mellitus. Eur J Clin Pharmacol. 2017;73(1):65-70.
Maze MJ, Paynter J, Chiu W, Hu R, Nisbet M, Lewis C. Therapeutic drug monitoring of isoniazid and rifampicin during anti-tuberculosis treatment in Auckland, New Zealand. Int J Tuberc Lung Dis. 2016;20(7):955-960.
Kumar AK, Kannan T, Chandrasekaran V, et al. Pharmacokinetics of thrice-weekly rifampicin, isoniazid and pyrazinamide in adult tuberculosis patients in India. Int J Tuberc Lung Dis. 2016;20(9):1236-1241.
Tostmann A, Mtabho CM, Semvua HH, et al. Pharmacokinetics of first-line tuberculosis drugs in Tanzanian patients. Antimicrob Agents Chemother. 2013;57(7):3208-3213.
World Health Organization. Treatment of tuberculosis: guidelines. 4th ed. Geneva, Switzerland: World Health Organization; 2010.
Park JS, Lee JY, Lee YJ, et al. Serum levels of antituberculosis drugs and their effect on tuberculosis treatment outcome. Antimicrob Agents Chemother. 2016;60(1):92-98.
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):1464-1473.
Srivastava S, Pasipanodya JG, Meek C, Leff R, Gumbo T. Multidrug-resistant tuberculosis not due to noncompliance but to between-patient pharmacokinetic variability. J Infect Dis. 2011;204(12):1951-1959.
Alffenaar J-WC, Tiberi S, Verbeeck RK, Heysell SK, Grobusch MP. Therapeutic drug monitoring in tuberculosis: practical application for physicians. Clin Infect Dis. 2017;64(1):104-105.
van den Elsen SHJ, Sturkenboom MGG, Akkerman OW, et al. Limited sampling strategies using linear regression and the Bayesian approach for therapeutic drug monitoring of moxifloxacin in tuberculosis patients. Antimicrob Agents Chemother. 2019;63(7):e00384-e00319.
van den Elsen SHJ, Sturkenboom MGG, Van't Boveneind-Vrubleuskaya N, et al. Population pharmacokinetic model and limited sampling strategies for personalized dosing of levofloxacin in tuberculosis patients. Antimicrob Agents Chemother. 2018;62:e01092-e01018.
Kamp J, Bolhuis MS, Tiberi S, et al. Simple strategy to assess linezolid exposure in patients with multi-drug-resistant and extensively-drug-resistant tuberculosis. Int J Antimicrob Agents. 2017;49(6):688-694.
Jing Y, Zhu LQ, Yang JW, Huang SP, Wang Q, Zhang J. Population pharmacokinetics of rifampicin in Chinese patients with pulmonary tuberculosis. J Clin Pharmacol. 2016;56(5):622-627.
Zhang M, Wang S, Wilffert B, et al. The association between the NAT2 genetic polymorphisms and risk of DILI during anti-TB treatment: a systematic review and meta-analysis. Br J Clin Pharmacol. 2018;84(12):2747-2760.
Dompreh A, Tang X, Zhou J, et al. Effect of genetic variation of NAT2 on isoniazid and SLCO1B1 and CES2 on rifampin pharmacokinetics in Ghanaian children with tuberculosis. Antimicrob Agents Chemother. 2018;62:e02099-e02017.
Kuznetsov IB, McDuffie M, Moslehi R. A web server for inferring the human N-acetyltransferase-2 (NAT2) enzymatic phenotype from NAT2 genotype. Bioinformatics. 2009;25(9):1185-1186.
Alsultan A, Peloquin CA. Therapeutic drug monitoring in the treatment of tuberculosis: an update. Drugs. 2014;74(8):839-854.
Seng KY, Hee KH, Soon GH, Chew N, Khoo SH, Lee LS. Population pharmacokinetic analysis of isoniazid, acetylisoniazid, and isonicotinic acid in healthy volunteers. Antimicrob Agents Chemother. 2015;59(11):6791-6799.
Lalande L, Bourguignon L, Bihari S, et al. Population modeling and simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of isoniazid in lungs. Antimicrob Agents Chemother. 2015;59(9):5181-5189.
Denti P, Jeremiah K, Chigutsa E, et al. Pharmacokinetics of isoniazid, pyrazinamide, and ethambutol in newly diagnosed pulmonary TB patients in Tanzania. Plos One. 2015;10(10):1-19, e0141002.
Chang MJ, Chae JW, Yun HY, et al. Effects of type 2 diabetes mellitus on the population pharmacokinetics of rifampin in tuberculosis patients. Tuberculosis. 2015;95(1):54-59.
Medellin-Garibay SE, Milan-Segovia Rdel C, Magana-Aquino M, Portales-Perez DP, Romano-Moreno S. Pharmacokinetics of rifampicin in Mexican patients with tuberculosis and healthy volunteers. J Pharm Pharmacol. 2014;66(10):1421-1428.
Milan Segovia RC, Dominguez Ramirez AM, Jung Cook H, et al. Population pharmacokinetics of rifampicin in Mexican patients with tuberculosis. J Clin Pharm Ther. 2013;38(1):56-61.
Wilkins JJ, Langdon G, McIlleron H, Pillai G, Smith PJ, Simonsson US. Variability in the population pharmacokinetics of isoniazid in south African tuberculosis patients. Br J Clin Pharmacol. 2011;72(1):51-62.
Chirehwa M, McIlleron H, Rustomjee R, et al. Pharmacokinetics of pyrazinamide and optimal dosing regimens for drug-sensitive and -resistant tuberculosis. Antimicrob Agents Chemother. 2017;61:e00490-e00417.
Alsultan A, Savic R, Dooley KE, et al. Population pharmacokinetics of pyrazinamide in patients with tuberculosis. Antimicrob Agents Chemother. 2017;61(6):1-11, e02625-16.
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):3298-3306.
Anderson BJ, Holford NHG. Mechanistic basis of using body size and maturation to predict clearance in humans. Drug Metab Pharmacokinet. 2009;24(1):25-36.
Wilkins JJ, Savic RM, Karlsson MO, et al. Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption. Antimicrob Agents Chemother. 2008;52(6):2138-2148.
Schwartz JB. The influence of sex on pharmacokinetics. Clin Pharmacokinet. 2003;42(2):107-121.
Chen B, Li J-H, Xu Y-M, Wang J, Cao X-M. The influence of NAT2 genotypes on the plasma concentration of isoniazid and acetylisoniazid in Chinese pulmonary tuberculosis patients. Clin Chim Acta. 2006;365(1-2):104-108.
Pasipanodya JG, Srivastava S, Gumbo T. Meta-analysis of clinical studies supports the pharmacokinetic variability hypothesis for acquired drug resistance and failure of antituberculosis therapy. Clin Infect Dis. 2012;55(2):169-177.
Azuma J, Ohno M, Kubota R, et al. NAT2 genotype guided regimen reduces isoniazid-induced liver injury and early treatment failure in the 6-month four-drug standard treatment of tuberculosis: a randomized controlled trial for pharmacogenetics-based therapy. Eur J Clin Pharmacol. 2013;69(5):1091-1101.
Pasipanodya JG, Gumbo T. Clinical and toxicodynamic evidence that high-dose pyrazinamide is not more hepatotoxic than the low doses currently used. Antimicrob Agents Chemother. 2010;54(7):2847-2854.
Aarnoutse RE, Kibiki GS, Reither K, et al. Pharmacokinetics, tolerability, and bacteriological response of rifampin administered at 600, 900, and 1,200 milligrams daily in patients with pulmonary tuberculosis. Antimicrob Agents Chemother. 2017;61:e01054-e01017.
Boeree MJ, Diacon AH, Dawson R, 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):1058-1065.
Ruslami R, Nijland HM, Adhiarta IG, et al. Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes. Antimicrob Agents Chemother. 2010;54(3):1068-1074.
Hanneke MJN, Rovina R, Janneke ES, et al. Exposure to rifampicin is strongly reduced in patients with tuberculosis and type 2 diabetes. Clin Infect Dis. 2006;43:848-854.
Niemi M, Backman J, Fromm M, Neuvonen P, Kivistö K. Pharmacokinetic interactions with rifampicin: clinical relevance. Clin Pharmacokinet. 2003;42(9):819-850.
Ruslami R, Nijland HM, Alisjahbana B, Parwati I, van Crevel R, Aarnoutse RE. Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients. Antimicrob Agents Chemother. 2007;51(7):2546-2551.
Sturkenboom MGG, Akkerman OW, van Altena R, et al. Dosage of isoniazid and rifampicin poorly predicts drug exposure in tuberculosis patients. Eur Respir J. 2016;48(4):1237-1239.
Daskapan A, Idrus LR, Postma MJ, et al. A systematic review on the effect of HIV infection on the pharmacokinetics of first-line tuberculosis drugs. Clin Pharmacokinet. 2019;58(6):747-766.