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rifampicin AND pharmacokinetics

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https://www.readbyqxmd.com/read/29771932/a-multi-center-preclinical-study-of-gadoxetate-dce-mri-in-rats-as-a-biomarker-of-drug-induced-inhibition-of-liver-transporter-function
#1
Anastassia Karageorgis, Stephen C Lenhard, Brittany Yerby, Mikael F Forsgren, Serguei Liachenko, Edvin Johansson, Mark A Pilling, Richard A Peterson, Xi Yang, Dominic P Williams, Sharon E Ungersma, Ryan E Morgan, Kim L R Brouwer, Beat M Jucker, Paul D Hockings
Drug-induced liver injury (DILI) is a leading cause of acute liver failure and transplantation. DILI can be the result of impaired hepatobiliary transporters, with altered bile formation, flow, and subsequent cholestasis. We used gadoxetate dynamic contrast-enhanced magnetic resonance imaging (DCE-MRI), combined with pharmacokinetic modelling, to measure hepatobiliary transporter function in vivo in rats. The sensitivity and robustness of the method was tested by evaluating the effect of a clinical dose of the antibiotic rifampicin in four different preclinical imaging centers...
2018: PloS One
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
#2
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/29742964/efficient-generation-of-cynomolgus-monkey-induced-pluripotent-stem-cell-derived-intestinal-organoids-with-pharmacokinetic-functions
#3
Daichi Onozato, Misaki Yamashita, Ryosuke Fukuyama, Takumi Akagawa, Yuriko Kida, Akiko Koeda, Tadahiro Hashita, Takahiro Iwao, Tamihide Matsunaga
In preclinical studies, the cynomolgus monkey (CM) model is frequently used to predict the pharmacokinetics of drugs in the human small intestine, because of its evolutionary closeness to humans. Intestinal organoids that mimic the intestinal tissue have attracted attention in regenerative medicine and drug development. In this study, we generated intestinal organoids from CM induced pluripotent stem (CMiPS) cells and analysed their pharmacokinetic functions. CMiPS cells were induced into the hindgut; then, the cells were seeded on microfabricated culture vessel plates to form spheroids...
May 10, 2018: Stem Cells and Development
https://www.readbyqxmd.com/read/29718390/greater-early-bactericidal-activity-at-higher-rifampicin-doses-revealed-by-modeling-and-clinical-trial-simulations
#4
Robin J Svensson, Elin M Svensson, Rob E Aarnoutse, Andreas H Diacon, Rodney Dawson, Stephen H Gillespie, Mischka Moodley, Martin J Boeree, Ulrika S H Simonsson
Background: The current rifampicin dose (10 mg/kg) is sub-optimal for treating tuberculosis. The PanACEA HIGHRIF1 trial evaluated pharmacokinetics and early bactericidal activity with rifampicin doses up to 40 mg/kg. Conventional statistics revealed no significant exposure-response relationship. Our objective was to explore exposure-response for high dose rifampicin using pharmacokinetic-pharmacodynamic modeling and to predict early bactericidal activity of 50 mg/kg rifampicin. Methods: Data included time-to-positivity of sputum in liquid culture from 83 tuberculosis patients treated with 10 (n=8), 20, 25, 30, 35 or 40 (n=15/group) mg/kg rifampicin for 7 days (clinicaltrials...
April 28, 2018: Journal of Infectious Diseases
https://www.readbyqxmd.com/read/29709589/effect-of-the-alkyl-group-in-the-piperazine-n-substitution-on-the-therapeutic-action-of-rifamycins-a-drug-membrane-interaction-study
#5
Emílio V Lage, Joana Magalhães, Marina Pinheiro, Salette Reis
In this work, we studied the effects of the N-alkyl group (methyl, cyclopentyl) in the piperazine ring of, respectively, rifampicin (RIF) and rifapentine (RPT) to correlate this substitution with their differential pharmacokinetic properties and overall clinical performance. Since this group is their only structural change, and given that they share the same pharmacological target, differences in their therapeutic behavior may respond to this asset, particularly in their interaction with lipid membranes across the organism...
April 27, 2018: Chemico-biological Interactions
https://www.readbyqxmd.com/read/29701775/pharmacokinetics-of-rifampicin-in-adult-tb-patients-and-healthy-volunteers-a-systematic-review-and-meta-analysis
#6
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/29697766/intermediate-susceptibility-dose-dependent-breakpoints-for-high-dose-rifampicin-isoniazid-and-pyrazinamide-treatment-in-multidrug-resistant-tuberculosis-programmes
#7
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/29686169/risk-factors-for-multidrug-resistant-tuberculosis
#8
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/29643253/in-vitro-in-vivo-extrapolation-of-oatp1b-mediated-drug-drug-interactions-in-cynomolgus-monkey
#9
Ayse Ufuk, Rachel E Kosa, Hongying Gao, Yi-An Bi, Sweta Modi, Dana Gates, A David Rodrigues, Larry M Tremaine, Manthena V S Varma, J Brian Houston, Aleksandra Galetin
Hepatic organic anion transporting polypeptides (OATP) 1B1 and 1B3 are clinically relevant transporters associated with significant drug-drug interactions (DDIs) and safety concerns. Given that OATP1Bs in cynomolgus monkey share >90% degree of gene and amino acid sequence identity with human orthologs, we evaluated the in vitro-in vivo translation of OATP1B-mediated DDI risk using this preclinical model. In vitro studies using cynomolgus monkey hepatocytes showed active uptake Km values of 2.0 and 3.9 µM for OATP1B probe substrates, pitavastatin and rosuvastatin, respectively...
April 11, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29624706/pharmacokinetics-of-efavirenz-in-patients-on-antituberculosis-treatment-in-high-hiv-and-tuberculosis-burden-countries-a-systematic-review
#10
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/29600438/functionalization-of-plga-nanoparticles-with-1-3-%C3%AE-glucan-enhances-the-intracellular-pharmacokinetics-of-rifampicin-in-macrophages
#11
Matshawandile Tukulula, Luis Gouveia, Paulo Paixao, Rose Hayeshi, Brendon Naicker, Admire Dube
PURPOSE: Mycobacterium tuberculosis which causes tuberculosis, is primarily resident within macrophages. 1,3-β-glucan has been proposed as a ligand to target drug loaded nanoparticles (NPs) to macrophages. In this study we characterized the intracellular pharmacokinetics of the anti-tubercular drug rifampicin delivered by 1,3-β-glucan functionalized PLGA NPs (Glu-PLGA). We hypothesized that Glu-PLGA NPs would be taken up at a faster rate than PLGA NPs, and consequently deliver higher amounts of rifampicin into the macrophages...
March 29, 2018: Pharmaceutical Research
https://www.readbyqxmd.com/read/29555827/a-clinical-quantitative-evaluation-of-hepatobiliary-transport-of-11c-dehydropravastatin-in-humans-using-positron-emission-tomography
#12
Ken-Ichi Kaneko, Masaaki Tanaka, Akira Ishii, Yumiko Katayama, Takayoshi Nakaoka, Satsuki Irie, Hideki Kawahata, Takashi Yamanaga, Yasuhiro Wada, Takeshi Miyake, Kota Toshimoto, Kazuya Maeda, Yilong Cui, Masaru Enomoto, Etsushi Kawamura, Norifumi Kawada, Joji Kawabe, Susumu Shiomi, Hiroyuki Kusuhara, Yuichi Sugiyama, Yasuyoshi Watanabe
Various positron emission tomography (PET) probes have been developed to assess the in vivo activities of drug transporters in humans, that aid in the prediction of pharmacokinetic properties of drugs and the impact of drug-drug interactions. We developed a new PET probe, [11C ]dehydropravastatin ([11 C]DPV), and demonstrated its usefulness for the quantitative investigation of Oatps/SLCO and Mrp2/ABCC2 in rats. To further analyze the species differences and verify the pharmacokinetic parameters in humans, serial PET scanning of the abdominal region with [11 C]DPV was performed in six healthy volunteers with and without an OATP1Bs and MRP2 inhibitor, rifampicin (600 mg, oral), in a crossover fashion...
March 19, 2018: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29529504/synthesis-and-antimycobacterial-activity-of-1-%C3%AE-d-ribofuranosyl-4-coumarinyloxymethyl-coumarinyl-1-2-3-triazole
#13
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/29505119/exposure-of-nursed-infants-to-maternal-treatment-with-ethambutol-and-rifampicin
#14
Falko Partosch, Hans Mielke, Ralf Stahlmann, Ursula Gundert-Remy
Mycobacterial diseases remain a significant cause of morbidity and mortality worldwide. Rifampicin and ethambutol are among the drugs recommended by WHO as first-line treatment. In this work, we addressed the question whether doses of the two anti-tuberculosis agents ethambutol and rifampicin transferred to a nursed infant could be of health concerns when the mother is under treatment. We used the approach of pharmacokinetic modelling using a structural model with two interconnected organisms: the first one being the organism of the nursing mother and the second one being the organism of the nursed child...
March 5, 2018: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29500603/effects-of-ketoconazole-and-rifampicin-on-the-pharmacokinetics-of-nintedanib-in-healthy-subjects
#15
Doreen Luedtke, Kristell Marzin, Arvid Jungnik, Ute von Wangenheim, Claudia Dallinger
BACKGROUND: Nintedanib is a substrate for p-glycoprotein which can impact bioavailability. We investigated the effects of ketoconazole, a p-glycoprotein inhibitor, and rifampicin, a p-glycoprotein inducer, on the pharmacokinetics of nintedanib. METHODS: In the ketoconazole study, 34 healthy subjects received nintedanib 50 mg orally alone and 1 h after the last dose of ketoconazole given orally at a dose of 400 mg once daily for 3 days in 1 of 2 randomized sequences...
March 2, 2018: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/29470228/amiodarone-rifampicin-drug-drug-interaction-management-with-therapeutic-drug-monitoring
#16
Thijs H Oude Munnink, Anna Demmer, Roel H J Slenter, Kris L L Movig
The authors present a case of a 69-year-old man with arrhythmogenic right ventricular cardiomyopathy controlled with amiodarone and an infected orthopedic prosthesis requiring treatment with rifampicin. This combination involves a pharmacokinetic drug-drug interaction leading to subtherapeutic drug concentrations of amiodarone and its active metabolite. The long half-life of amiodarone and its active metabolite in combination with the late onset and offset of cytochrome P4503A (CYP3A4) induction by rifampicin makes this a challenging drug-drug interaction to cope with in clinical practice...
April 2018: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29468841/development-verification-and-prediction-of-osimertinib-drug-drug-interactions-using-pbpk-modeling-approach-to-inform-drug-label
#17
Venkatesh Pilla Reddy, Michael Walker, Pradeep Sharma, Peter Ballard, Karthick Vishwanathan
Osimertinib is a potent, highly selective, irreversible inhibitor of epidermal growth factor receptor (EGFR) and T790M resistance mutation. In vitro metabolism data suggested osimertinib is a substrate of cytochrome P450 (CYP)3A4/5, a weak inducer of CYP3A, and an inhibitor of breast cancer resistance protein (BCRP). A combination of in vitro data, clinical pharmacokinetic data, and drug-drug interaction (DDI) data of osimertinib in oncology patients were used to develop the physiologically based pharmacokinetic (PBPK) model and verify the DDI data of osimertinib...
February 22, 2018: CPT: Pharmacometrics & Systems Pharmacology
https://www.readbyqxmd.com/read/29463541/verapamil-targets-membrane-energetics-in-mycobacterium-tuberculosis
#18
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/29440136/problems-in-anticoagulation-of-a-patient-with-antibiotic-treatment-for-endocarditis-interaction-of-rifampicin-and-vitamin-k-antagonists
#19
Lars Mizera, Tobias Geisler, Klaus Mörike, Meinrad Gawaz, Martin Steeg
The cytochrome P450 is a superfamily of isoenzymes that are responsible for the metabolism of many drugs. Significant changes in pharmacokinetics and drug interactions may be due to induction of hepatic cytochrome P450 enzymes. Rifampicin is a common inducer of CYP3A4. We report a case of a 57-year-old woman who was suspected for endocarditis and therefore treated with rifampicin. Due to previous mechanical aortic valve replacement, she also received phenprocoumon for anticoagulation. Although continuing anticoagulant therapy, antibiotic coadministration led to normal international normalised ratio (INR) level...
February 12, 2018: BMJ Case Reports
https://www.readbyqxmd.com/read/29381826/the-effect-of-itraconazole-and-rifampicin-on-the-pharmacokinetics-of-osimertinib
#20
Karthick Vishwanathan, Paul A Dickinson, Karen So, Karen Thomas, Yuh-Min Chen, Javier De Castro Carpeño, Anne-Marie C Dingemans, Hye Ryun Kim, Joo-Hang Kim, Matthew G Krebs, James Chih-Hsin Yang, Khanh Bui, Doris Weilert, R Donald Harvey
AIMS: We investigated the effects of a strong CYP3A4 inhibitor (itraconazole) or inducer (rifampicin) on the pharmacokinetics of the epidermal growth factor receptor-tyrosine kinase inhibitor osimertinib, in patients with advanced non-small cell lung cancer in two Phase I, open-label, two-part clinical studies. Part one of both studies is reported. METHODS: In the itraconazole study (NCT02157883), patients received single-dose osimertinib 80 mg on Days 1 and 10 and itraconazole (200 mg twice daily) on Days 6-18 orally...
January 30, 2018: British Journal of Clinical Pharmacology
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