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pharmacokinetics and TB

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https://www.readbyqxmd.com/read/29777407/modelling-the-delay-between-pharmacokinetics-and-eeg-effects-of-morphine-in-rats-binding-kinetic-versus-effect-compartment-models
#1
Wilhelmus E A de Witte, Vivi Rottschäfer, Meindert Danhof, Piet H van der Graaf, Lambertus A Peletier, Elizabeth C M de Lange
Drug-target binding kinetics (as determined by association and dissociation rate constants, k on and k off ) can be an important determinant of the kinetics of drug action. However, the effect compartment model is used most frequently instead of a target binding model to describe hysteresis. Here we investigate when the drug-target binding model should be used in lieu of the effect compartment model. The utility of the effect compartment (EC), the target binding kinetics (TB) and the combined effect compartment-target binding kinetics (EC-TB) model were tested on either plasma (ECPL , TBPL and EC-TBPL ) or brain extracellular fluid (ECF) (ECECF , TBECF and EC-TBECF ) morphine concentrations and EEG amplitude in rats...
May 18, 2018: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/29765372/is-iqg-607-a-potential-metallodrug-or-metallopro-drug-with-a-defined-molecular-target-in-mycobacterium-tuberculosis
#2
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
#3
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 sampling (DBS) for pharmacokinetic (PK) studies and Therapeutic Drug Monitoring has unique advantages over venous sampling. We aimed to evaluate a DBS method for first-line anti-TB drugs in children, implemented DBS to assess PK parameters. METHODS: Paraguayan children were treated according to the revised paediatric WHO dosing scheme. A PK curve was performed both with DBS and conventional venous sampling for rifampicin, pyrazinamide and ethambutol...
May 8, 2018: International Journal of Antimicrobial Agents
https://www.readbyqxmd.com/read/29701775/pharmacokinetics-of-rifampicin-in-adult-tb-patients-and-healthy-volunteers-a-systematic-review-and-meta-analysis
#4
K E Stott, H Pertinez, M G G Sturkenboom, M J Boeree, R Aarnoutse, G Ramachandran, A Requena-Méndez, C Peloquin, C F N Koegelenberg, J W C Alffenaar, R Ruslami, A Tostmann, S Swaminathan, H McIlleron, G Davies
Objectives: The objectives of this study were to explore inter-study heterogeneity in the pharmacokinetics (PK) of orally administered rifampicin, to derive summary estimates of rifampicin PK parameters at standard dosages and to compare these with summary estimates for higher dosages. Methods: A systematic search was performed for studies of rifampicin PK published in the English language up to May 2017. Data describing the Cmax and AUC were extracted. Meta-analysis provided summary estimates for PK parameter estimates at standard rifampicin dosages...
April 26, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29686171/influence-of-diabetes-mellitus-on-the-development-of-multi-drug-resistant-tuberculosis-in-yogyakarta
#5
Antonia Morita Iswari Saktiawati, Yanri Wijayanti Subronto
BACKGROUND: the correlation between diabetes mellitus (DM) and Multi-Drug-Resistant Tuberculosis (MDR-TB) has never been studied among patients with tuberculosis (TB) in Indonesia, while DM has been identified to alter immune response and pharmacokinetics of TB medications that may lead to a failure of TB treatment and develop MDR-TB. Our study aimed to analyze the influence of diabetes mellitus on the development of MDR-TB. METHODS: a retrospective cohort study was carried out on 356 TB patients at the Provincial Lung Clinics and Sardjito Hospital, Yogyakarta, Indonesia between 2010 and 2014...
January 2018: Acta Medica Indonesiana
https://www.readbyqxmd.com/read/29686169/risk-factors-for-multidrug-resistant-tuberculosis
#6
Cleopas Martin Rumende
In 2015, 10.4 million people developed tuberculosis (TB) and 580,000 amongst them suffered from multidrug-resistant TB (MDR-TB). From those 580,000 cases of MDR-TB, only 125,000 were detected and reported. A total of 111,000 people began to receive MDR-TB treatment in 2014 while 190,000 MDR-TB patients were estimated to have died, largely due to lack of access to effective treatment. The mechanism of drug resistance can be caused by genetic factors, factors related to previous treatment and other factors such as comorbidity with diabetes mellitus...
January 2018: Acta Medica Indonesiana
https://www.readbyqxmd.com/read/29673395/shorter-treatment-for-minimal-tuberculosis-tb-in-children-shine-a-study-protocol-for-a-randomised-controlled-trial
#7
Chishala Chabala, Anna Turkova, Margaret J Thomason, Eric Wobudeya, Syed Hissar, Vidya Mave, Marieke van der Zalm, Megan Palmer, Monica Kapasa, Perumal K Bhavani, Sarath Balaji, Priyanka A Raichur, Anne-Marie Demers, Graeme Hoddinott, Ellen Owen-Powell, Aarti Kinikar, Philippa Musoke, Veronica Mulenga, Rob Aarnoutse, Helen McIlleron, Anneke Hesseling, Angela M Crook, Mark Cotton, Diana M Gibb
BACKGROUND: Tuberculosis (TB) in children is frequently paucibacillary and non-severe forms of pulmonary TB are common. Evidence for tuberculosis treatment in children is largely extrapolated from adult studies. Trials in adults with smear-negative tuberculosis suggest that treatment can be effectively shortened from 6 to 4 months. New paediatric, fixed-dose combination anti-tuberculosis treatments have recently been introduced in many countries, making the implementation of World Health Organisation (WHO)-revised dosing recommendations feasible...
April 19, 2018: Trials
https://www.readbyqxmd.com/read/29665950/conducting-efficacy-trials-in-children-with-mdr-tb-what-is-the-rationale-and-how-should-they-be-done
#8
J A Seddon, E D Weld, H S Schaaf, A J Garcia-Prats, S Kim, A C Hesseling
Paediatric anti-tuberculosis treatment trials have traditionally been limited to Phase I/II studies evaluating the drug pharmacokinetics and safety in children, with assumptions about efficacy made by extrapolating data from adults. However, it is increasingly being recognised that, in some circumstances, efficacy trials are required in children. The current treatment for children with multidrug-resistant tuberculosis (MDR-TB) is long and toxic; shorter, safer regimens, using novel agents, require urgent evaluation...
May 1, 2018: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/29665949/current-status-of-pharmacokinetic-and-safety-studies-of-multidrug-resistant-tuberculosis-treatment-in-children
#9
A J Garcia-Prats, E M Svensson, E D Weld, H S Schaaf, A C Hesseling
After decades of neglect, data are finally becoming available on the appropriate, safe dosing of key second-line anti-tuberculosis drugs used for treating multidrug-resistant tuberculosis (MDR-TB) in children, including levofloxacin (LVX), moxifloxacin (MFX), linezolid (LZD) and delamanid (DLM). Much needed data on some novel and repurposed drugs are still lacking, including for bedaquiline (BDQ), pretomanid (PTM) and clofazimine (CFZ). We review the status of pharmacokinetic (PK) and safety studies of key anti-tuberculosis medications in children with MDR-TB, identify priority knowledge gaps and note ongoing work to address those gaps, in the context of planning for an efficacy trial in children with MDR-TB...
May 1, 2018: International Journal of Tuberculosis and Lung Disease
https://www.readbyqxmd.com/read/29661865/modeling-and-simulation-of-pretomanid-pharmacokinetics-in-pulmonary-tuberculosis-patients
#10
Michael A Lyons
Pretomanid is a nitroimidazole antibiotic in late phase clinical testing as a component of several novel antituberculosis (anti-TB) regimens. A population pharmacokinetic model for pretomanid was constructed using a Bayesian analysis of data from two phase 2 studies, PA-824-CL-007 and PA-824-CL-010, conducted with newly diagnosed adult (median age 27 years) pulmonary TB patients in Cape Town, South Africa. Combined, these studies included 63 males and 59 females administered once daily oral pretomanid doses of 50, 100, 150, 200, 600, 1000, or 1200 mg for 14 days...
April 16, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29624706/pharmacokinetics-of-efavirenz-in-patients-on-antituberculosis-treatment-in-high-hiv-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 HIV-tuberculosis (TB) co-infection 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 co-administration in co-infected patients...
April 6, 2018: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29618565/pharmacokinetics-of-rifapentine-and-rifampin-in-a-rabbit-model-of-tuberculosis-and-correlation-with-clinical-trial-data
#12
Dalin Rifat, Brendan Prideaux, Radojka M Savic, Michael E Urbanowski, Teresa L Parsons, Brian Luna, Mark A Marzinke, Alvaro A Ordonez, Vincent P DeMarco, Sanjay K Jain, Veronique Dartois, William R Bishai, Kelly E Dooley
In clinical trials of two rifamycin antibiotics (rifampin and rifapentine) for treating tuberculosis (TB), patients with cavitary lung lesions did not appear to derive benefit from rifapentine. Rifapentine was found not to outperform rifampin, despite a lower minimum inhibitory concentration against Mycobacterium tuberculosis in mouse models of TB. To understand these findings, we have developed a rabbit model of TB that reliably develops lung cavities with features similar to those of patients with pulmonary cavitary TB...
April 4, 2018: Science Translational Medicine
https://www.readbyqxmd.com/read/29584861/linezolid-pharmacokinetics-in-mdr-tb-a-systematic-review-meta-analysis-and-monte-carlo-simulation
#13
James Millard, Henry Pertinez, Laura Bonnett, Eva Maria Hodel, Véronique Dartois, John L Johnson, Maxine Caws, Simon Tiberi, Mathieu Bolhuis, Jan-Willem C Alffenaar, Geraint Davies, Derek J Sloan
Objectives: The oxazolidinone linezolid is an effective component of drug-resistant TB treatment, but its use is limited by toxicity and the optimum dose is uncertain. Current strategies are not informed by clinical pharmacokinetic (PK)/pharmacodynamic (PD) data; we aimed to address this gap. Methods: We defined linezolid PK/PD targets for efficacy (fAUC0-24:MIC >119 mg/L/h) and safety (fCmin <1.38 mg/L). We extracted individual-level linezolid PK data from existing studies on TB patients and performed meta-analysis, producing summary estimates of fAUC0-24 and fCmin for published doses...
March 23, 2018: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29579424/a-selective-and-sensitive-high-performance-liquid-chromatography-assay-for-the-determination-of-cycloserine-in-human-plasma
#14
A K Hemanth Kumar, Arun Kumar Polisetty, V Sudha, A Vijayakumar, Geetha Ramachandran
BACKGROUND: Cycloserine (CYC) is a second line antitubercular drug that is used for the treatment of multidrug resistant tuberculosis (MDR-TB) along with other antitubercular agents and is often used in developing countries. Monitoring CYC levels in plasma could be useful in the clinical management of patients with MDR-TB. A high performance liquid chromatography method for the determination of CYC in human plasma was developed. METHODS: The method involved extraction of the sample using solid phase extraction cartridges and analysis of the extracted sample using a reverse phase T3 column (150mm) and detection at 240nm with Photo Diode Array (PDA) detector...
April 2018: Indian Journal of Tuberculosis
https://www.readbyqxmd.com/read/29561515/effect-of-co-administration-of-lidocaine-on-the-pain-and-pharmacokinetics-of-intramuscular-amikacin-in-children-with-multidrug-resistant-tuberculosis-a-randomized-crossover-trial
#15
Anthony J Garcia-Prats, Penelope C Rose, Heather R Draper, James A Seddon, Jennifer Norman, Helen M McIlleron, Anneke C Hesseling, H Simon Schaaf
BACKGROUND: Currently recommended treatment for multidrug-resistant (MDR) tuberculosis (TB) includes 4-8 months of an injectable medication, which is poorly tolerated. We evaluated the impact of co-administering lidocaine on pain and pharmacokinetics of intramuscular injections of amikacin in children with MDR-TB. METHODS: Children 8-18 years of age, receiving amikacin for MDR-TB treatment in Cape Town, South Africa, were eligible for this randomized crossover trial...
March 14, 2018: Pediatric Infectious Disease Journal
https://www.readbyqxmd.com/read/29523331/the-utility-of-pharmacokinetic-studies-for-the-evaluation-of-exposure-response-relationships-for-standard-dose-anti-tuberculosis-drugs
#16
REVIEW
Christine Sekaggya-Wiltshire, Mohammed Lamorde, Agnes N Kiragga, Kelly E Dooley, Moses R Kamya, Andrew Kambugu, Jan Fehr, Yukari C Manabe, Barbara Castelnuovo
Tuberculosis (TB) is a major public health problem. Many countries still fall below the minimum World Health Organization (WHO) TB treatment target success rate. There is conflicting evidence about whether concentrations of anti-tuberculosis drugs given at standard doses have an effect on treatment outcomes. The current data correlating anti-TB drug concentrations and treatment outcome is limited. This article summarized the existing literature and their utility in evaluating the association between each anti-TB drug's concentrations using current target concentrations and treatment outcomes in patients with pulmonary tuberculosis receiving standard WHO-recommended dosing...
January 2018: Tuberculosis
https://www.readbyqxmd.com/read/29463541/verapamil-targets-membrane-energetics-in-mycobacterium-tuberculosis
#17
Chao Chen, Susana Gardete, Robert Sander Jansen, Annanya Shetty, Thomas Dick, Kyu Y Rhee, Véronique Dartois
Mycobacterium tuberculosis kills more people than any other bacterial pathogen and is becoming increasingly untreatable due to the emergence of resistance. Verapamil, an FDA-approved calcium channel blocker, potentiates the effect of several antituberculosis (anti-TB) drugs in vitro and in vivo This potentiation is widely attributed to inhibition of the efflux pumps of M. tuberculosis , resulting in intrabacterial drug accumulation. Here, we confirmed and quantified verapamil's synergy with several anti-TB drugs, including bedaquiline (BDQ) and clofazimine (CFZ), but found that the effect is not due to increased intrabacterial drug accumulation...
May 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29463539/pharmacokinetics-of-second-line-antituberculosis-drugs-in-children-with-multidrug-resistant-tuberculosis-in-india
#18
Agibothu Kupparam Hemanth Kumar, Alok Kumar, Thiruvengadam Kannan, Rakesh Bhatia, Dipti Agarwal, Santosh Kumar, Rajeshwar Dayal, Sheo Pratap Singh, Geetha Ramachandran
We studied the pharmacokinetics of levofloxacin (LFX), pyrazinamide (PZA), ethionamide (ETH), and cycloserine (CS) in children with multidrug-resistant tuberculosis (MDR-TB) who were being treated according to the Revised National TB Control Programme (RNTCP) guidelines in India. This observational, pharmacokinetic study was conducted in 25 children with MDR-TB at the Sarojini Naidu Medical College, Agra, India, who were being treated with a 24-month daily regimen. Serial blood samples were collected after directly observed administration of drugs...
May 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29335214/in-vivo-potent-bm635-analogue-with-improved-drug-like-properties
#19
Giovanna Poce, Martina Cocozza, Salvatore Alfonso, Sara Consalvi, Giulia Venditti, Raquel Fernandez-Menendez, Robert H Bates, David Barros Aguirre, Lluis Ballell, Alessandro De Logu, Giulio Vistoli, Mariangela Biava
BM635 is the hit compound of a promising anti-TB compound class. Herein we report systematic variations around the central pyrrole core of BM635 and we describe the design, synthesis, biological evaluation, pharmacokinetic analysis, as well as in vivo TB mouse efficacy studies of novel BM635 analogues that show improved physicochemical properties. This hit-to-lead campaign led to the identification of a new analogue, 4-((1-isopropyl-5-(4-isopropylphenyl)-2-methyl-1H-pyrrol-3-yl)methyl)morpholine (17), that shows excellent activity (MIC = 0...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29297422/steady-state-pharmacokinetics-of-cycloserine-in-patients-on-terizidone-for-multidrug-resistant-tuberculosis
#20
R Court, L Wiesner, A Stewart, N de Vries, J Harding, G Maartens, T Gumbo, H McIlleron
SETTING: Terizidone/cycloserine (TRD/CS) is included in standard treatment regimens for multidrug-resistant tuberculosis (MDR-TB) in many countries. The steady state pharmacokinetics (PKs) of CS after TRD administration are not known. OBJECTIVES AND DESIGN: We recruited in-patients treated with 250-750 mg oral TRD daily as part of standard treatment regimens for pulmonary MDR-TB in Cape Town, South Africa. Plasma CS assays were performed in samples taken pre-dose and at 2, 4, 6, 8 and 10 h post-dose...
January 1, 2018: International Journal of Tuberculosis and Lung Disease
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