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isoniazid pharmacokinetics

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https://www.readbyqxmd.com/read/30025351/design-synthesis-and-antimicrobial-evaluation-of-propylene-tethered-ciprofloxacin-isatin-hybrids
#1
Ruo Wang, Xueyang Yin, Yaohuan Zhang, Weitao Yan
Twelve novel propylene-tethered ciprofloxacin-isatin hybrids 3a-f and 4a-f were designed, synthesized and characterized by MS, HRMS, 1 H NMR and 13 C NMR. All hybrids were evaluated for their in vitro antimicrobial activities against representative Gram-positive, Gram-negative and mycobacterial pathogens, cytotoxicity in VERO cell line as well as metabolic stability and in vivo pharmacokinetic (PK) properties. The preliminary results indicated that all mono-isatin-ciprofloxacin hybrids exhibited excellent antibacterial activities with MIC ranging from ≤0...
July 16, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/30023583/s-enantiomer-of-the-antitubercular-compound-s006-830-complements-activity-of-frontline-tb-drugs-and-targets-biogenesis-of-mycobacterium-tuberculosis-cell-envelope
#2
Padam Singh, Shashi Kant Kumar, Vineet Kumar Maurya, Basant Kumar Mehta, Hafsa Ahmad, Anil Kumar Dwivedi, Vinita Chaturvedi, Tejender S Thakur, Sudhir Sinha
A synthetic molecule S006-830, belonging to the class of thiophene-containing trisubstituted methanes, had shown good in vitro and in vivo bactericidal activity against drug-sensitive and drug-resistant Mycobacterium tuberculosis (Mtb). The molecule had also shown good druglike pharmacokinetic properties. However, S006-830 is a racemic mixture of two enantiomers, one of which could possess a better pharmacological profile than the other. We purified both the enantiomers on a chiral column and observed that S-enantiomer has a significantly higher inhibitory and cidal activity against Mtb than the R-enantiomer...
November 30, 2017: ACS Omega
https://www.readbyqxmd.com/read/30012768/comprehensive-substrate-characterization-of-22-antituberculosis-drugs-for-multiple-solute-carrier-slc-uptake-transporters-in-vitro
#3
Md Masud Parvez, Nazia Kaisar, Ho Jung Shin, Yoon Jae Lee, Jae-Gook Shin
Substrate potential of antituberculosis drugs on SLC transporters are not well characterized to date, despite a well-established understanding of their drug dispositions and pharmacokinetics. In this study, we investigated comprehensively the substrate potentials of the 22 currently available antituberculosis drugs for solute carrier (SLC) family transporter-mediated uptake, using Xenopus laevis oocytes and stably transfected HEK-293 cells in vitro The result suggested that, ethambutol, isoniazid, amoxicillin, and prothionamide act as novel substrates for the SLC transporters...
July 16, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29991405/modelling-the-long-acting-administration-of-anti-tuberculosis-agents-using-pbpk-a-proof-of-concept-study
#4
R K R Rajoli, A T Podany, D M Moss, S Swindells, C Flexner, A Owen, M Siccardi
SETTING: Anti-tuberculosis formulations necessitate uninterrupted treatment to cure tuberculosis (TB), but are characterised by suboptimal adherence, which jeopardises therapeutic efficacy. Long-acting injectable (LAI) formulations or implants could address these associated issues. OBJECTIVE: niazid, rifapentine, bedaquiline and delamanid-in adults for treatment for latent tuberculous infection (LTBI). DESIGN: PBPK models were developed and qualified against available clinical data by integrating drug physicochemical properties and in vitro and population pharmacokinetic data into a mechanistic description of drug distribution...
August 1, 2018: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/29984757/pharmacokinetics-of-isoniazid-induced-rhabdomyolysis-in-a-girl
#5
Koyuru Kurane, Masahide Goto, Kazumi Sano, Kumiko Noguchi, Daisuke Tamura, Takanori Yamagata
No abstract text is available yet for this article.
July 6, 2018: Internal Medicine
https://www.readbyqxmd.com/read/29954183/efficacy-and-safety-of-high-dose-rifampin-in-pulmonary-tuberculosis-a-randomized-controlled-trial
#6
Gustavo E Velásquez, Meredith B Brooks, Julia M Coit, Henry Pertinez, Dante Vargas Vásquez, Epifanio Sánchez Garavito, Roger I Calderón, Judith Jiménez, Karen Tintaya, Charles A Peloquin, Elna Osso, Dylan B Tierney, Kwonjune J Seung, Leonid Lecca, Geraint R Davies, Carole D Mitnick
RATIONALE: We examined whether increased rifampin doses could shorten standard therapy for tuberculosis without increased toxicity. OBJECTIVES: To assess the differences across three daily oral doses of rifampin in change in elimination rate of Mycobacterium tuberculosis in sputum and frequency of rifampin-related adverse events. METHODS: We conducted a blinded, randomized, controlled Phase II clinical trial of 180 adults with new smear-positive pulmonary tuberculosis, susceptible to isoniazid and rifampin...
June 29, 2018: American Journal of Respiratory and Critical Care Medicine
https://www.readbyqxmd.com/read/29914960/evaluation-of-the-adequacy-of-who-revised-dosages-of-the-first-line-anti-tuberculosis-drugs-in-children-with-tuberculosis-using-population-pharmacokinetic-modeling-and-simulations
#7
Yasuhiro Horita, Abdullah Alsultan, Awewura Kwara, Sampson Antwi, Antony Enimil, Antoinette Orstin, Albert Dompreh, Hongmei Yang, Lubbe Wiesner, Charles A Peloquin
Optimal doses for anti-tuberculosis (TB) drugs in children have yet to be established. In 2010, the World Health Organization (WHO) recommended revised dosages of the first-line anti-TB drugs for children. Pharmacokinetic (PK) studies that investigated the adequacy of the WHO revised dosages to date have yielded conflicting results. We performed population PK modeling using data from one of these studies to identify optimal dosages ranges. Ghanaian children with tuberculosis on recommended therapy with rifampin (RIF), isoniazid (INH), pyrazinamide (PZA) and ethambutol (EMB) for at least 4 weeks had blood samples collected at pre-dose, 1, 2, 4, and 8-hours post-dose...
June 18, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29765372/is-iqg-607-a-potential-metallodrug-or-metallopro-drug-with-a-defined-molecular-target-in-mycobacterium-tuberculosis
#8
REVIEW
Bruno L Abbadi, Valnês da Silva Rodrigues-Junior, Adilio da Silva Dadda, Kenia Pissinate, Anne D Villela, Maria M Campos, Luiz G de França Lopes, Cristiano V Bizarro, Pablo Machado, Eduardo H S Sousa, Luiz A Basso
The emergence of strains of Mycobacterium tuberculosis resistant to isoniazid (INH) has underscored the need for the development of new anti-tuberculosis agents. INH is activated by the mycobacterial katG -encoded catalase-peroxidase, forming an acylpyridine fragment that is covalently attached to the C4 of NADH. This isonicotinyl-NAD adduct inhibits the activity of 2- trans -enoyl-ACP(CoA) reductase (InhA), which plays a role in mycolic acid biosynthesis. A metal-based INH analog, Na3 [FeII (CN)5 (INH)]·4H2 O, IQG-607, was designed to have an electronic redistribution on INH moiety that would lead to an intramolecular electron transfer to bypass KatG activation...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29751121/evaluation-of-dried-blood-spot-sampling-for-pharmacokinetic-research-and-therapeutic-drug-monitoring-of-anti-tuberculosis-drugs-in-children
#9
Lisa C Martial, Jordy Kerkhoff, Nilza Martinez, Mabel Rodríguez, Rosarito Coronel, Gladys Molinas, Myriam Roman, Roscio Gomez, Sarita Aguirre, Erwin Jongedijk, Justine Huisman, Daan J Touw, Domingo Pérez, Gilberto Chaparro, Felipe Gonzalez, Rob E Aarnoutse, Jan-Willem Alffenaar, Cecile Magis-Escurra
BACKGROUND: Dried blood spot (DBS) sampling for pharmacokinetic (PK) studies and therapeutic drug monitoring have unique advantages over venous sampling. This study aimed to evaluate a DBS method for first-line anti-tuberculosis drugs in children, and DBS sampling to assess PK parameters. METHODS: Paraguayan children were treated according to the revised paediatric dosing scheme of the World Health Organization. A PK curve was performed both with DBS sampling and conventional venous sampling for rifampicin, pyrazinamide and ethambutol...
May 8, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29697766/intermediate-susceptibility-dose-dependent-breakpoints-for-high-dose-rifampicin-isoniazid-and-pyrazinamide-treatment-in-multidrug-resistant-tuberculosis-programmes
#10
Marlanka A Zuur, Jotam G Pasipanodya, Dick van Soolingen, Tjip S van der Werf, Tawanda Gumbo, Jan-Willem C Alffenaar
Background: In infectious diseases, for some drugs, bacterial susceptibility is categorized as susceptible, intermediate-susceptible dose-dependent (ISDD), and resistant. The strategy is to use higher doses of first-line agents in the ISDD category, thereby preserving the use of these drugs. This system has not been applied to anti-tuberculosis drugs. Pharmacokinetics/pharmacodynamics (PK/PD) target exposures, in tandem with Monte Carlo experiments (MCE), recently identified susceptibility breakpoints of 0...
April 24, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29624706/pharmacokinetics-of-efavirenz-in-patients-on-antituberculosis-treatment-in-high-human-immunodeficiency-virus-and-tuberculosis-burden-countries-a-systematic-review
#11
REVIEW
Daniel Atwine, Maryline Bonnet, Anne-Marie Taburet
AIMS: Efavirenz (EFV) and rifampicin-isoniazid (RH) are cornerstone drugs in human immunodeficiency virus (HIV)-tuberculosis (TB) coinfection treatment but with complex drug interactions, efficacy and safety challenges. We reviewed recent data on EFV and RH interaction in TB/HIV high-burden countries. METHODS: We conducted a systematic review of studies conducted in the high TB/HIV-burden countries between 1990 and 2016 on EFV pharmacokinetics during RH coadministration in coinfected patients...
April 6, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29529504/synthesis-and-antimycobacterial-activity-of-1-%C3%AE-d-ribofuranosyl-4-coumarinyloxymethyl-coumarinyl-1-2-3-triazole
#12
Smriti Srivastava, Devla Bimal, Kapil Bohra, Balram Singh, Prija Ponnan, Ruchi Jain, Mandira Varma-Basil, Jyotirmoy Maity, M Thirumal, Ashok K Prasad
A series of β-d-ribofuranosyl coumarinyl-1,2,3-triazoles have been synthesized by Cu-catalyzed cycloaddition reaction between azidosugar and 7-O-/7-alkynylated coumarins in 62-70% overall yields. The in vitro antimycobacterial activity evaluation of the synthesized triazolo-conjugates against Mycobacterium tuberculosis revealed that compounds were bactericidal in nature and some of them were found to be more active than one of the first line antimycobacterial drug ethambutol against sensitive reference strain H37Rv, and 7 to 420 times more active than all four first line antimycobacterial drugs (isoniazid, rifampicin, ethambutol and streptomycin) against multidrug resistant clinical isolate 591...
April 25, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29514812/pharmacokinetic-study-of-isoniazid-and-pyrazinamide-in-children-impact-of-age-and-nutritional-status
#13
Rajeshwar Dayal, Yatish Singh, Dipti Agarwal, Manoj Kumar, Soumya Swaminathan, Geetha Ramachandran, Santosh Kumar, Shamrendra Narayan, Ankur Goyal, A K Hemant Kumar
OBJECTIVES: To evaluate pharmacokinetics of first-line antitubercular drugs, isoniazid (INH) and pyrazinamide (PZA), with revised WHO dosages and to assess its adequacy in relation to age and nutritional status. DESIGN: Observational study. SETTING: This study was conducted at Sarojini Naidu Medical College, Agra, and National Institute for Research in Tuberculosis, Chennai. PATIENTS: 40 subjects diagnosed with tuberculosis were registered in the study and started on daily first-line antitubercular regimen based on the revised WHO guidelines...
March 7, 2018: Archives of Disease in Childhood
https://www.readbyqxmd.com/read/29507756/integration-of-genome-scale-metabolic-networks-into-whole-body-pbpk-models-shows-phenotype-specific-cases-of-drug-induced-metabolic-perturbation
#14
Henrik Cordes, Christoph Thiel, Vanessa Baier, Lars M Blank, Lars Kuepfer
Drug-induced perturbations of the endogenous metabolic network are a potential root cause of cellular toxicity. A mechanistic understanding of such unwanted side effects during drug therapy is therefore vital for patient safety. The comprehensive assessment of such drug-induced injuries requires the simultaneous consideration of both drug exposure at the whole-body and resulting biochemical responses at the cellular level. We here present a computational multi-scale workflow that combines whole-body physiologically based pharmacokinetic (PBPK) models and organ-specific genome-scale metabolic network (GSMN) models through shared reactions of the xenobiotic metabolism...
2018: NPJ Systems Biology and Applications
https://www.readbyqxmd.com/read/29415190/cytokine-mediated-systemic-adverse-drug-reactions-in-a-drug-drug-interaction-study-of-dolutegravir-with-once-weekly-isoniazid-and-rifapentine
#15
Kristina M Brooks, Jomy M George, Alice K Pau, Adam Rupert, Carolina Mehaffy, Prithwiraj De, Karen M Dobos, Anela Kellogg, Mary McLaughlin, Maryellen McManus, Raul M Alfaro, Colleen Hadigan, Joseph A Kovacs, Parag Kumar
Background: Once-weekly isoniazid and rifapentine for 3 months is a treatment option in persons with human immunodeficiency virus and latent tuberculosis infection. This study aimed to examine pharmacokinetic drug-drug interactions between this regimen and dolutegravir, a first-line antiretroviral medication. Methods: This was a single-center, open-label, fixed-sequence, drug-drug interaction study in healthy volunteers. Subjects received oral dolutegravir 50 mg once-daily alone (Days 1-4) and concomitantly with once-weekly isoniazid 900 mg, rifapentine 900 mg, and pyridoxine 50 mg (Days 5-19)...
February 3, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
https://www.readbyqxmd.com/read/29247506/suboptimal-antituberculosis-drug-concentrations-and-outcomes-in-small-and-hiv-coinfected-children-in-india-recommendations-for-dose-modifications
#16
Benjamin Guiastrennec, Geetha Ramachandran, Mats O Karlsson, A K Hemanth Kumar, Perumal Kannabiran Bhavani, N Poorana Gangadevi, Soumya Swaminathan, Amita Gupta, Kelly E Dooley, Radojka M Savic
This work aimed to evaluate the once-daily antituberculosis treatment as recommended by the new Indian pediatric guidelines. Isoniazid, rifampin, and pyrazinamide concentration-time profiles and treatment outcome were obtained from 161 Indian children with drug-sensitive tuberculosis undergoing thrice-weekly dosing as per previous Indian pediatric guidelines. The exposure-response relationships were established using a population pharmacokinetic-pharmacodynamic approach. Rifampin exposure was identified as the unique predictor of treatment outcome...
December 16, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29244108/optimal-doses-of-rifampicin-in-the-standard-drug-regimen-to-shorten-tuberculosis-treatment-duration-and-reduce-relapse-by-eradicating-persistent-bacteria
#17
Yingjun Liu, Henry Pertinez, Fatima Ortega-Muro, Laura Alameda-Martin, Thomas Harrison, Geraint Davies, Anthony Coates, Yanmin Hu
Objectives: Although high-dose rifampicin holds promise for improving tuberculosis disease control by eradication of persistent bacteria, the optimal dose of rifampicin that kills persistent bacteria and shortens the treatment duration is unknown. Methods: The Cornell mouse model was used to test the efficacy of rifampicin at elevated doses combined with isoniazid and pyrazinamide to kill actively growing and persistent bacilli and to measure relapse rate. Persistent bacteria were evaluated using Mycobacterium tuberculosis culture supernatant containing resuscitation-promoting factors...
December 12, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29226732/pharmacokinetics-and-pharmacogenetics-of-anti-tubercular-drugs-a-tool-for-treatment-optimization
#18
REVIEW
Ilaria Motta, Andrea Calcagno, Stefano Bonora
WHO global strategy is to end tuberculosis epidemic by 2035. Pharmacokinetic and pharmacogenetic studies are increasingly performed and might confirm their potential role in optimizing treatment outcome in specific settings and populations. Insufficient drug exposure seems to be a relevant factor in tuberculosis outcome and for the risk of phenotypic resistance. Areas covered: This review discusses available pharmacokinetic and pharmacogenetic data of first and second-line antitubercular agents in relation to efficacy and toxicity...
January 2018: Expert Opinion on Drug Metabolism & Toxicology
https://www.readbyqxmd.com/read/29216273/isoniazid-concentrations-in-hair-and-plasma-area-under-the-curve-exposure-among-children-with-tuberculosis
#19
Vidya Mave, Aarti Kinikar, Anju Kagal, Smita Nimkar, Hari Koli, Sultanat Khwaja, Renu Bharadwaj, Roy Gerona, Anita Wen, Geetha Ramachandran, Hemanth Kumar, Peter Bacchetti, Kelly E Dooley, Nikhil Gupte, Amita Gupta, Monica Gandhi
We measured hair and plasma concentrations of isoniazid among sixteen children with tuberculosis who underwent personal or video-assisted directly observed therapy and thus had 100% adherence. This study therefore defined typical isoniazid exposure parameters after two months of treatment among fully-adherent patients in both hair and plasma (plasma area under the concentration-time curve, AUC, estimated using pharmacokinetic data collected 0, 2, 4, and 6 hours after drug administration). We found that INH levels in hair among highly-adherent individuals did not correlate well with plasma AUC or trough concentrations, suggesting that each measure may provide incremental and complementary information regarding drug exposure in the context of TB treatment...
2017: PloS One
https://www.readbyqxmd.com/read/29133558/pharmacokinetics-and-drug-drug-interactions-of-lopinavir-ritonavir-administered-with-first-and-second-line-antituberculosis-drugs-in-hiv-infected-children-treated-for-multidrug-resistant-tuberculosis
#20
Louvina E van der Laan, Anthony J Garcia-Prats, H Simon Schaaf, Tjokosela Tikiso, Lubbe Wiesner, Mine de Kock, Jana Winckler, Jennifer Norman, Helen McIlleron, Paolo Denti, Anneke C Hesseling
Lopinavir-ritonavir forms the backbone of current first-line antiretroviral regimens in young HIV-infected children. As multidrug-resistant (MDR) tuberculosis (TB) frequently occurs in young children in high-burden TB settings, it is important to identify potential interactions between MDR-TB treatment and lopinavir-ritonavir. We describe the pharmacokinetics of and potential drug-drug interactions between lopinavir-ritonavir and drugs routinely used for MDR-TB treatment in HIV-infected children. A combined population pharmacokinetic model was developed to jointly describe the pharmacokinetics of lopinavir and ritonavir in 32 HIV-infected children (16 with MDR-TB receiving treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 16 without TB) who were established on a lopinavir-ritonavir-containing antiretroviral regimen...
February 2018: Antimicrobial Agents and Chemotherapy
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