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isoniazid pharmacokinetics

Ana Requena-Méndez, Geraint Davies, David Waterhouse, Alison Ardrey, Oswaldo Jave, Sonia Llanet López-Romero, Stephen A Ward, David A J Moore
Background: Poor response to TB therapy might be attributable to subtherapeutic levels in drug-compliant patients. Pharmacokinetic parameters can be affected by comorbidities or the interaction of drugs with food. Objectives: This study aimed to determine the effect of food intake upon pharmacokinetics of rifampicin and isoniazid in a Peruvian population with TB. Methods: Rifampicin and isoniazid levels were analysed at 2, 4 and 6 h after drug intake in both fasting and non-fasting states using LC-MS methods...
November 8, 2018: Journal of Antimicrobial Chemotherapy
Alper Daskapan, Lusiana R Idrus, Maarten J Postma, Bob Wilffert, Jos G W Kosterink, Ymkje Stienstra, Daniel J Touw, Aase B Andersen, Adrie Bekker, Paolo Denti, Agibothu K Hemanth Kumar, Kidola Jeremiah, Awewura Kwara, Helen McIlleron, Graeme Meintjes, Joep J van Oosterhout, Geetha Ramachandran, Neesha Rockwood, Robert J Wilkinson, Tjip S van der Werf, Jan-Willem C Alffenaar
INTRODUCTION: Contrasting findings have been published regarding the effect of human immunodeficiency virus (HIV) on tuberculosis (TB) drug pharmacokinetics (PK). OBJECTIVES: The aim of this systematic review was to investigate the effect of HIV infection on the PK of the first-line TB drugs (FLDs) rifampicin, isoniazid, pyrazinamide and ethambutol by assessing all published literature. METHODS: Searches were performed in MEDLINE (through PubMed) and EMBASE to find original studies evaluating the effect of HIV infection on the PK of FLDs...
November 8, 2018: Clinical Pharmacokinetics
Awewura Kwara, Hongmei Yang, Sampson Antwi, Anthony Enimil, Fizza S Gillani, Albert Dompreh, Antoinette Ortsin, Theresa Opoku, Dennis Bosomtwe, Anima Sarfo, Lubbe Wiesner, Jennifer Norman, Wael A Alghamdi, Taimour Langaee, Charles A Peloquin, Michael H Court, David J Greenblatt
We compared efavirenz pharmacokinetic (PK) parameters in children with TB/HIV coinfection on and off first-line antituberculosis therapy to that in HIV-infected children. Children aged 3 to 14 years old with HIV infection with and without TB were treated with standard efavirenz-based antiretroviral therapy without any efavirenz dose adjustments. The new World Health Organization recommended antituberculosis drugs dosages were used in the co-infected participants. Steady-state efavirenz concentrations after 4 weeks of antiretroviral therapy were measured using validated LC/MS/MS assays...
November 5, 2018: Antimicrobial Agents and Chemotherapy
Feng Gao, Hua Yang, Tianyu Lu, Zijian Chen, Long Ma, Zhi Xu, Paul Schaffer, Guangming Lu
Herein we report the design and synthesis of a series of novel benzofuran-isatin hybrids, and in vitro evaluation of their anti-mycobacterial activity against both drug-susceptible and multi-drug resistant (MDR) Mycobacterium tuberculosis (MTB) strains. In parallel, cytotoxicity of these hybrids was also tested in VERO cells. Preliminary results indicated that all hybrids with acceptable cytotoxicity in VERO cells (CC50 : 128->1024 μg/mL) exhibited considerable anti-mycobacterial activities against MTB H37 Rv and MDR-TB with MIC ranging from 0...
November 5, 2018: European Journal of Medicinal Chemistry
Maxwell T Chirehwa, Helen McIlleron, Lubbe Wiesner, Dissou Affolabi, Oumou Bah-Sow, Corinne Merle, Paolo Denti
Objectives: To describe the pharmacokinetics of isoniazid and acetyl-isoniazid in TB/HIV-coinfected patients, and assess the effects of efavirenz co-administration and a 50% increase in the dose of rifampicin on the pharmacokinetic parameters of isoniazid and acetyl-isoniazid. Methods: TB/HIV-coinfected patients participating in the three-treatment-arm RAFA randomized controlled trial conducted in West Africa were recruited into the pharmacokinetics sub-study. Five serial blood samples were collected on a single visit between 4 and 8 weeks after initiation of antituberculosis treatment...
September 18, 2018: Journal of Antimicrobial Chemotherapy
Omamah Alfarisi, Vidya Mave, Sanjay Gaikwad, Tushar Sahasrabudhe, Geetha Ramachandran, Hemanth Kumar, Nikhil Gupte, Vandana Kulkarni, Sona Deshmukh, Sachin Atre, Swapnil Raskar, Rahul Lokhande, Madhusudan Barthwal, Arjun Kakrani, Sandy Chon, Amita Gupta, Jonathan E Golub, Kelly E Dooley
Diabetes mellitus (DM) and tuberculosis (TB) are two common diseases with increasing geographic overlap and clinical interactions. The effect of DM and hemoglobin A1c (HbA1c) values on the pharmacokinetics (PK) and pharmacodynamics (PD) of anti-TB drugs remains poorly characterized. Newly diagnosed TB patients with and without DM starting fixed-dose, thrice-weekly treatment underwent sampling for PK assessments (predose and 0.5, 2, and 6 h postdose) during the intensive and continuation phases of treatment...
November 2018: Antimicrobial Agents and Chemotherapy
Katarina Niward, Lina Davies Forsman, Judith Bruchfeld, Erja Chryssanthou, Oskar Carlström, Teba Alomari, Björn Carlsson, Anton Pohanka, Mikael Mansjö, Michaela Jonsson Nordvall, Anders G Johansson, Erik Eliasson, Jim Werngren, Jakob Paues, Ulrika S H Simonsson, Thomas Schön
Background: Therapeutic drug monitoring (TDM) could improve current TB treatment, but few studies have reported pharmacokinetic data together with MICs. Objectives: To investigate plasma concentrations of rifampicin, isoniazid, pyrazinamide and ethambutol along with MICs. Methods: Drug concentrations of rifampicin, isoniazid, pyrazinamide and ethambutol were analysed pre-dose and 2, 4 and 6 h after drug intake at week 2 in 31 TB patients and MICs in BACTEC 960 MGIT were determined at baseline...
August 14, 2018: Journal of Antimicrobial Chemotherapy
Maddalena Cerrone, Xinzhu Wang, Megan Neary, Christine Weaver, Serge Fedele, Isaac Day-Weber, Andrew Owen, Andrew Hill, Myra McClure, Marta Boffito
Background: The World Health Organization recommends efavirenz 400 mg (EFV400) as first-line antiretroviral therapy, with a disclaimer that no data with anti-tuberculosis (TB) treatment exist. Many people living with human immunodeficiency virus (PLWH) require TB treatment with isoniazid (INH) and rifampicin (RIF), which affect cytochrome P450 and antiretroviral exposure. Methods: PLWH receiving tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC)/EFV 600 mg with a viral load (VL) <50 copies/mL switched to TDF/FTC/EFV400...
August 6, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
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...
August 5, 2018: European Journal of Medicinal Chemistry
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
M M Parvez, Nazia Kaisar, Ho Jung Shin, Yoon Jae Lee, Jae-Gook Shin
The substrate potentials of antituberculosis drugs on solute carrier (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 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...
September 2018: Antimicrobial Agents and Chemotherapy
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
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
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 2 clinical trial of 180 adults with new smear-positive pulmonary tuberculosis, susceptible to isoniazid and rifampin...
September 1, 2018: American Journal of Respiratory and Critical Care Medicine
Yasuhiro Horita, Abdullah Alsultan, Awewura Kwara, Sampson Antwi, Antony Enimil, Antoinette Ortsin, Albert Dompreh, Hongmei Yang, Lubbe Wiesner, Charles A Peloquin
Optimal doses for antituberculosis (anti-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 dosage 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 predose and at 1, 2, 4, and 8 hours postdose...
September 2018: Antimicrobial Agents and Chemotherapy
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
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...
July 2018: International Journal of Antimicrobial Agents
Marlanka A Zuur, Jotam G Pasipanodya, Dick van Soolingen, Tjip S van der Werf, Tawanda Gumbo, Jan-Willem C Alffenaar
Background: 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 antituberculosis drugs. Pharmacokinetic/pharmacodynamic (PK/PD) target exposures, in tandem with Monte Carlo experiments, recently identified susceptibility breakpoints of 0.0312 mg/L for isoniazid, 0...
November 13, 2018: Clinical Infectious Diseases: An Official Publication of the Infectious Diseases Society of America
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...
August 2018: British Journal of Clinical Pharmacology
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
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