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rifampicin AND pharmacokinetics

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https://www.readbyqxmd.com/read/28303006/short-course-high-dose-rifampicin-achieves-wolbachia-depletion-predictive-of-curative-outcomes-in-preclinical-models-of-lymphatic-filariasis-and-onchocerciasis
#1
Ghaith Aljayyoussi, Hayley E Tyrer, Louise Ford, Hanna Sjoberg, Nicolas Pionnier, David Waterhouse, Jill Davies, Joanne Gamble, Haelly Metugene, Darren A N Cook, Andrew Steven, Raman Sharma, Ana F Guimaraes, Rachel H Clare, Andrew Cassidy, Kelly L Johnston, Laura Myhill, Laura Hayward, Samuel Wanji, Joseph D Turner, Mark J Taylor, Stephen A Ward
Lymphatic filariasis (LF) and onchocerciasis are priority neglected tropical diseases targeted for elimination. The only safe drug treatment with substantial curative activity against the filarial nematodes responsible for LF (Brugia malayi, Wuchereria bancrofti) or onchocerciasis (Onchocerca volvulus) is doxycycline. The target of doxycycline is the essential endosymbiont, Wolbachia. Four to six weeks doxycycline therapy achieves >90% depletion of Wolbachia in worm tissues leading to blockade of embryogenesis, adult sterility and premature death 18-24 months post-treatment...
March 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28254951/examination-of-the-human-cytochrome-p4503a4-induction-potential-of-pf-06282999-an-irreversible-myeloperoxidase-inactivator-integration-of-preclinical-in-silico-and-biomarker-methodologies-in-the-prediction-of-the-clinical-outcome
#2
Jennifer Dong, James Gosset, Odette Fahmi, Zhiwu Lin, Jeffrey Chabot, Steven Terra, Vu Le, Kristin Chidsey, Parya Nouri, Albert Kim, Leonard Buckbinder, Amit S Kalgutkar
The propensity for cytochrome P450 (CYP)3A4 induction by 2-(6-(5-chloro-2-methoxyphenyl)-4-oxo-2-thioxo-3,4-dihydropyrimidin-1(2H)-yl)acetamide (PF-06282999), an irreversible inactivator of myeloperoxidase, was examined in the present work. Studies using human hepatocytes revealed moderate increases in CYP3A4 messenger RNA (mRNA) and midazolam-1'-hydroxylase activity in a PF-06282999 dose-dependent fashion. At the highest tested concentration of 300 μM, PF-06282999 caused maximal induction in CYP3A4 mRNA and enzyme activity ranging from 56% - 86% and 47% - 72%, respectively, of rifampicin response across the three hepatocyte donor pools...
March 2, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/28213941/population-pharmacokinetic-and-exposure-simulation-analysis-for-cediranib-azd2171-in-pooled-phase-i-ii-studies-in-patients-with-cancer
#3
Jianguo Li, Nidal Al-Huniti, Anja Henningsson, Weifeng Tang, Eric Masson
AIMS: A population pharmacokinetic (PPK) model was developed for cediranib to simulate cediranib exposure for different doses, including co-medication with strong UGT/Pgp inducers such as rifampicin, in cancer patients. METHODS: Plasma concentrations and covariates from 625 cancer patients after single or multiple oral cediranib administrations ranging from 0.5 to 90 mg in 19 Phase I and II studies were included in the analysis. Stepwise covariate modelling was used to develop the PPK model...
February 18, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28205025/the-multistate-tuberculosis-pharmacometric-model-a-semi-mechanistic-pharmacokinetic-pharmacodynamic-model-for-studying-drug-effects-in-an-acute-tuberculosis-mouse-model
#4
Chunli Chen, Fatima Ortega, Joaquin Rullas, Laura Alameda, Iñigo Angulo-Barturen, Santiago Ferrer, Ulrika Sh Simonsson
The Multistate Tuberculosis Pharmacometric (MTP) model, a pharmacokinetic-pharmacodynamic disease model, has been used to describe the effects of rifampicin on Mycobacterium tuberculosis (M. tuberculosis) in vitro. The aim of this work was to investigate if the MTP model could be used to describe the rifampicin treatment response in an acute tuberculosis mouse model. Sixty C57BL/6 mice were intratracheally infected with M. tuberculosis H37Rv strain on Day 0. Fifteen mice received no treatment and were sacrificed on Days 1, 9 and 18 (5 each day)...
February 15, 2017: Journal of Pharmacokinetics and Pharmacodynamics
https://www.readbyqxmd.com/read/28193650/interaction-of-rifampicin-and-darunavir-ritonavir-or-darunavir-cobicistat-in-vitro
#5
Owain Roberts, Saye Khoo, Andrew Owen, Marco Siccardi
Treatment of HIV patients co-infected with tuberculosis (TB) is challenging due to drug-drug interactions (DDIs) between antiretrovirals (ARVs) and anti-TB drugs. The aim of this study was to quantify the effects of cobicistat (COBI), or ritonavir (RTV), in modulating DDIs between darunavir (DRV) and rifampicin (RIF) in a human hepatocyte-based in vitro model. Human primary hepatocyte cultures were incubated with RIF alone, or in combination with either COBI or RTV for three days, followed by co-incubation with DRV for one hour...
February 13, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28192070/predicting-effects-of-antibiotic-combinations-using-mics-determined-at-pharmacokinetically-derived-concentration-ratios-in-vitro-model-studies-with-linezolid-and-rifampicin-exposed-staphylococcus-aureus
#6
Maria V Golikova, Elena N Strukova, Yury A Portnoy, Svetlana A Dovzhenko, Mikhail B Kobrin, Stephen H Zinner, Alexander A Firsov
To predict the effects of combined use of antibiotics on their pharmacodynamics, the susceptibility of Staphylococcus aureus to linezolid-rifampicin combinations was tested at concentration ratios equal to the ratios of 24-area under the concentration-time curve (AUC24) simulated in an in vitro dynamic model. The linezolid MICs in combination with rifampicin decreased 8- to 67-fold. The rifampicin MICs were similar with or without linezolid. The enhanced activity of linezolid combined with rifampicin increased the AUC24/MIC ratios and provided more pronounced antibacterial effects compared with single treatments...
February 13, 2017: Journal of Chemotherapy
https://www.readbyqxmd.com/read/28160272/suboptimal-exposure-to-anti-tb-drugs-in-a-tbm-hiv-population-is-not-related-to-anti-retroviral-therapy
#7
M E Török, G Aljayyoussi, D Waterhouse, Tth Chau, Nth Mai, N H Phu, T T Hien, W Hope, J J Farrar, S A Ward
A placebo-controlled trial that compares the outcomes of immediate versus deferred initiation of antiretroviral therapy in HIV+ve Tuberculous Meningitis (TBM) patients was conducted in Vietnam in 2011. Here, the pharmacokinetics of Rifampicin, Isoniazid, Pyrazinamide and Ethambutol were investigated in the presence and absence of anti-HIV treatment in 85 patients. Pharmacokinetic analyses show that HIV therapy has no significant impact upon the pharmacokinetics of TB drugs in this cohort. The same population, however, displayed generally low CSF and systemic exposures to rifampicin compared to previously reported HIV -ve cohorts...
February 4, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28101656/off-label-use-of-antimicrobials-in-neonates-in-a-tertiary-children-s-hospital
#8
Niina Laine, Ann Marie Kaukonen, Kalle Hoppu, Marja Airaksinen, Harri Saxen
PURPOSE: Off-label (OL) use of drugs for hospitalized children is very common. OL use occurs especially in the youngest patients, neonates. This study focused on the OL use of antimicrobials in neonates. To our knowledge, only few studies have focused on the prevalence of OL use of antimicrobials in neonates. METHODS: We investigated the OL use of antimicrobials in neonates in a tertiary children's hospital. First, we investigated what were the most consumed OL antimicrobials in defined daily doses according to hospital's registry data from neonatal intensive care unit (NICU) during 2009-2014...
January 18, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28063154/pharmacological-indices-and-pulmonary-distribution-of-rifampicin-after-repeated-oral-administration-in-healthy-foals
#9
S Berlin, A Kirschbaum, L Spieckermann, S Oswald, M Keiser, M Grube, M Venner, W Siegmund
BACKGROUND: The treatment of equine lung infections by Rhodococcus equi with rifampicin is empirically based because pharmacokinetic/pharmacodynamic (PK/PD) indices and pivotal clinical outcome data are not available. OBJECTIVES: To evaluate the pharmacokinetics and pulmonary distribution of rifampicin into epithelial lining fluid (ELF) and bronchoalveolar lavage cells (BALC) to predict antimicrobial activity in the lung using PK/PD indices. STUDY DESIGN: Controlled, randomised, two-period, crossover, repeated-dose study with an initial arm to measure disposition after i...
January 7, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/27943222/clinical-pharmacokinetics-and-pharmacodynamics-of-cediranib
#10
REVIEW
Weifeng Tang, Alex McCormick, Jianguo Li, Eric Masson
Cediranib potently and selectively inhibits all three vascular endothelial growth factor receptors (VEGFR-1, -2 and -3), and clinical studies have shown that it is effective in patients with ovarian cancer at a dose of 20 mg/day. Cediranib is absorbed moderately slowly; a high-fat meal reduced the cediranib area under the plasma concentration-time curve (AUC) by 24% and maximum plasma concentration (C max) by 33%. Cediranib binds to serum albumin and α1-acid glycoprotein; protein binding in human plasma is approximately 95%...
December 9, 2016: Clinical Pharmacokinetics
https://www.readbyqxmd.com/read/27934638/comparative-evaluation-of-dehydroepiandrosterone-sulfate-dheas-potential-to-predict-hepatic-oatp-transporter-based-drug-drug-interactions
#11
Kei Nishizawa, Takeo Nakanishi, Ikumi Tamai
Pharmacokinetic drug-drug interactions (DDIs) on hepatic organic anion transporting polypeptides (OATPs) are important clinical issues. Previously we reported that plasma dehydroepiandrosterone sulfate (DHEAS) could serve as an endogenous probe to predict OATP-based DDIs in monkeys using rifampicin as an OATP inhibitor. However, since the contribution of hepatic OATPs to the changes of plasma DHEAS by rifampicin remains unclear, here, we evaluated by an in vivo pharmacokinetic study. Since plasma DHEAS concentrations were unexpectedly low in our rat model, disposition of externally administered DHEAS was evaluated...
December 1, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27889832/effects-of-cytochrome-p450-cyp3a4-and-cyp2c19-inhibition-and-induction-on-the-exposure-of-selumetinib-a-mek1-2-inhibitor-in-healthy-subjects-results-from-two-clinical-trials
#12
RANDOMIZED CONTROLLED TRIAL
Angela W Dymond, Karen So, Paul Martin, Yifan Huang, Paul Severin, David Mathews, Eleanor Lisbon, Gabriella Mariani
PURPOSE: Two phase I, open-label trials in healthy subjects assessed whether co-administration with CYP3A4/CYP2C19 inhibitors, itraconazole/fluconazole (study A), or CYP3A4 inducer, rifampicin (study B), affects the exposure, safety/tolerability and pharmacokinetics of selumetinib and its metabolite N-desmethyl selumetinib. METHODS: In study A (n = 26), subjects received a single dose of selumetinib 25 mg and, after 4 days of washout, were randomized to treatment 1 (itraconazole 200 mg twice daily on days 1-11) or treatment 2 (fluconazole 400 mg on day 1 then 200 mg/day on days 2-11) plus co-administration of single-dose selumetinib 25 mg on day 8 (selumetinib staggered 4 h after itraconazole/fluconazole dose); Twenty-one days after discharge/washout, subjects received the alternate treatment...
February 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27813241/population-pharmacokinetics-of-rifampicin-in-adult-patients-with-osteoarticular-infections-interaction-with-fusidic-acid
#13
A Marsot, A Ménard, J Dupouey, C Muziotti, R Guilhaumou, O Blin
AIMS: Rifampicin represents the key antibiotic for management of osteoarticular infections. An important pharmacokinetic variability has already been described, incriminating notably absorption and metabolism. All previous pharmacokinetic studies were only focused on patient treated for tuberculosis. The objective of this study was to describe a population pharmacokinetic model of rifampicin in patients with staphylococcal osteoarticular infections, data which have not been investigated to date...
November 4, 2016: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/27795624/rifampicin-and-anti-hypertensive-drugs-in-chronic-kidney-disease-pharmacokinetic-interactions-and-their-clinical-impact
#14
A Agrawal, S K Agarwal, T Kaleekal, Y K Gupta
Patients on dialysis have an increased incidence of tuberculosis (TB). Rifampicin, a first-line antitubercular therapy (ATT) drug, is a potent inducer of hepatic cytochrome P450 (CYP). There is potential for pharmacokinetic interaction between rifampicin and anti-hypertensives that are CYP substrates: amlodipine and metoprolol. Therefore, hypertensive patients receiving rifampicin-based ATT are at risk for worsening of hypertension. However, this hypothesis has not yet been systematically studied. In this prospective study, hypertensive CKD 5D patients with TB were followed after rifampicin initiation...
September 2016: Indian Journal of Nephrology
https://www.readbyqxmd.com/read/27748167/pharmacokinetically-based-prediction-of-the-effects-of-antibiotic-combinations-on-resistant-staphylococcus-aureus-mutants-in-vitro-model-studies-with-linezolid-and-rifampicin
#15
Alexander A Firsov, Maria V Golikova, Elena N Strukova, Yury A Portnoy, Svetlana A Dovzhenko, Mikhail B Kobrin, Stephen H Zinner
To explore if combinations of linezolid (L) with rifampicin (R) are able to restrict Staphylococcus aureus resistance, the enrichment of L- and R-resistant mutants was studied in an in vitro dynamic model. L- and R-resistant mutants were enriched in all single drug treatments. In contrast, L-resistant mutants were not enriched and R-resistant mutants were similar to baseline amounts with only minimal regrowth at the end of the combination treatments. These effects appear to be explained by lowering the mutant prevention concentration (MPC) for L+R combinations (MPCL+R) compared to the MPCs of L and R alone (MPCL and MPCR) and thereby the longer times above MPCL+R (73-100% of the dosing interval for L and 42-58% for R) compared to the times above MPCL (0-44%) and MPCR (0%)...
October 17, 2016: Journal of Chemotherapy
https://www.readbyqxmd.com/read/27724114/the-challenges-of-pharmacokinetic-variability-of-first-line-anti-tb-drugs
#16
REVIEW
Bella Devaleenal Daniel, Geetha Ramachandran, Soumya Swaminathan
Inter-individual variations in the pharmacokinetics (PK) of anti-TB drugs are known to occur, which could have important therapeutic implications in patient management. Areas covered: We compiled factors responsible for PK variability of anti-TB drugs reported from different settings that would give a better understanding about the challenges of PK variability of anti-TB medications. We searched PubMed data base and Google scholar from 1976 to the present using the key words 'Pharmacokinetics', 'pharmacokinetic variability', 'first-line anti-TB therapy', 'Rifampicin', 'Isoniazid', 'Ethambutol', 'Pyrazinamide', 'food', 'nutritional status', 'HIV', 'diabetes', 'genetic polymorphisms' and 'pharmacokinetic interactions'...
January 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/27693756/nqo1-and-cyp450-reductase-decrease-the-systemic-exposure-of-rifampicin-quinone-and-mediate-its-redox-cycle-in-rats
#17
Fuguo Shi, Xiaobing Li, Hong Pan, Li Ding
Rifampicin (RIF) is used in regimens for infections caused by Mycobacteria accompanied by serious adverse reactions. Rifampicin-quinone (RIF-Q) is a major autoxidation product of RIF. It is not clear whether RIF-Q plays a role in RIF induced adverse reactions. Investigation of the systemic exposure of RIF-Q is helpful to better understand the role of RIF-Q in RIF induced adverse reactions. In this study, a simple and reproducible high performance liquid chromatography-mass spectrometry (LC-MS) method involving a procedure to prevent the RIF from oxidation for simultaneous quantification of RIF and RIF-Q in rat plasma has been developed and validated, and applied to elucidate the systemic exposure of RIF-Q in rats...
January 5, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27648490/transporter-mediated-hepatic-uptake-plays-an-important-role-in-the-pharmacokinetics-and-drug-drug-interactions-of-montelukast
#18
M V Varma, E Kimoto, R Scialis, Y Bi, J Lin, H Eng, A S Kalgutkar, A F El-Kattan, A D Rodrigues, L M Tremaine
Montelukast, a leukotriene receptor antagonist commonly prescribed for treatment of asthma, is primarily metabolized by cytochrome P450 (CYP)2C8, and has been suggested as a probe substrate for investigating CYP2C8 activity in vivo. We evaluated the quantitative role of hepatic uptake transport in its pharmacokinetics and drug-drug interactions (DDIs). Montelukast was characterized with significant active uptake in human hepatocytes, and showed affinity towards organic anion transporting polypeptides (OATPs) in transfected cell systems...
September 20, 2016: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/27637290/effect-of-cholecystectomy-on-bile-acids-as-well-as-relevant-enzymes-and-transporters-in-mice-implication-for-pharmacokinetic-changes-of-rifampicin
#19
Fan Zhang, Hongyan Qin, Yanshu Zhao, Yuhui Wei, Lili Xi, Zhi Rao, Jianping Zhang, Yanrong Ma, Yingting Duan, Xinan Wu
BACKGROUND AND PURPOSE: Long-term medical consequences of cholecystectomy are believed to be uncommon. It has been reported that bile acids (BAs) changed after cholecystectomy. As important signaling molecules, the alternations of BAs might favour the regulatory effect on enzymes and transporters involved in BAs physiological homeostasis at the transcriptional level, which could lead to pharmacokinetic changes of drugs. Here, we determined the effect of cholecystectomy on BAs, relevant enzymes and transporters and pharmacokinetic parameters of rifampicin, and explored the potential mechanisms at the transcriptional regulatory level via nuclear receptors...
January 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/27603548/pre-incubation-with-cyclosporine-a-potentiates-its-inhibitory-effects-on-pitavastatin-uptake-mediated-by-recombinantly-expressed-cynomolgus-monkey-hepatic-organic-anion-transporting-polypeptide
#20
Tsuyoshi Takahashi, Tatsuyuki Ohtsuka, Yasuhiro Uno, Masahiro Utoh, Hiroshi Yamazaki, Toshiyuki Kume
Cyclosporine A, an inhibitor of hepatic organic anion transporting polypeptides (OATPs), reportedly increased plasma concentrations of probe substrates, although its maximum unbound blood concentrations were lower than the experimental half-maximal inhibitory (IC50 ) concentrations. Pre-incubation with cyclosporine A in vitro before simultaneous incubation with probes has been reported to potentiate its inhibitory effects on recombinant human OATP-mediated probe uptake. In the present study, the effects of cyclosporine A and rifampicin on recombinant cynomolgus monkey OATP-mediated pitavastatin uptake were investigated in pre- and simultaneous incubation systems...
November 2016: Biopharmaceutics & Drug Disposition
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