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rifampicin AND pharmacokinetics

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https://www.readbyqxmd.com/read/29326367/organic-anion-transporter-2-mediates-hepatic-uptake-of-tolbutamide-a-cytochrome-p450-2c9-probe-drug
#1
Yi-An Bi, Sumathy Mathialagan, Laurie Tylaska, Myra Fu, Julie Keefer, Anna Vildhede, Chester Costales, A David Rodrigues, Manthena Varma
Tolbutamide is primarily metabolized by cytochrome P450 (CYP)2C9, and thus, frequently applied as a clinical probe substrate for CYP2C9 activity. However, there is a marked discrepancy in the in vitro-in vivo extrapolation of its metabolic clearance implying potential for additional clearance mechanisms. The goal of this study was to evaluate the role of hepatic uptake transport in the pharmacokinetics of tolbutamide and identify the molecular mechanism thereof. Transport studies using singly-transfected cells expressing six major hepatic uptake transporters showed that tolbutamide is a substrate to organic anion transporter (OAT)2 alone -- with transporter affinity (Km) of 19...
January 11, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29277691/genetic-polymorphisms-of-drug-metabolizing-cytochrome-p450-enzymes-in-cynomolgus-and-rhesus-monkeys-and-common-marmosets-in-preclinical-studies-for-humans
#2
REVIEW
Yasuhiro Uno, Shotaro Uehara, Hiroshi Yamazaki
Cynomolgus monkeys (Macaca fascicularis, Old World Monkeys) and common marmosets (Callithrix jacchus, New World Monkeys) have been widely, and expectedly, used as non-human primate models in drug development studies. Major drug-metabolizing cytochrome P450 (P450) enzymes information is now available that supports these primate species as animal models, and it is established that multiple forms of cynomolgus monkey and common marmoset P450 enzymes have generally similar substrate recognition functionality to human P450 enzymes...
December 22, 2017: Biochemical Pharmacology
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
#3
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/29243231/gaining-mechanistic-insight-into-coproporphyrin-i-as-endogenous-biomarker-for-oatp1b-mediated-drug-drug-interactions-using-population-pharmacokinetic-modelling-and-simulation
#4
Shelby Barnett, Kayode Ogungbenro, Karelle Ménochet, Hong Shen, Yurong Lai, W Griffith Humphreys, Aleksandra Galetin
This study evaluates coproporphyrin I (CPI) as a selective endogenous biomarker of OATP1B-mediated drug-drug interactions (DDIs) relative to clinical probe rosuvastatin using nonlinear mixed-effect modelling. Plasma and urine CPI data in the presence/absence of rifampicin were modelled to describe CPI synthesis, elimination clearances and obtain rifampicin in vivo OATP Ki. The biomarker showed stable inter-occasion baseline concentrations and low inter-individual variability (<25%) in subjects with wild type SLCO1B1...
December 15, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29239016/intestinal-and-hepatic-contributions-to-the-pharmacokinetic-interaction-between-gamithromycin-and-rifampicin-after-single-dose-and-multiple-dose-administration-in-healthy-foals
#5
S Berlin, S Wallstabe, E Scheuch, S Oswald, M Hasan, D Wegner, M Grube, M Venner, A Ullrich, W Siegmund
BACKGROUND: Standard treatment of foals with severe abscessing lung infection caused by Rhodococcus equi using rifampicin and a macrolide antibiotic can be compromised by extensive inhibition and/or induction of drug metabolising enzymes (e.g. CYP3A4) and transport proteins (e.g. P-glycoprotein), as has been shown for rifampicin and clarithromycin. The combination of rifampicin with the new, poorly metabolised gamithromycin, a long-acting analogue of azithromycin and tulathromycin with lower pharmacokinetic interaction potential, might be a suitable alternative...
December 14, 2017: Equine Veterinary Journal
https://www.readbyqxmd.com/read/29226732/pharmacokinetics-and-pharmacogenetics-of-anti-tubercular-drugs-a-tool-for-treatment-optimization
#6
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/29120971/a-systematic-review-of-salivary-versus-blood-concentrations-of-anti-tuberculosis-drugs-and-their-potential-for-salivary-therapeutic-drug-monitoring
#7
Simone H J van den Elsen, Lisette M Oostenbrink, Scott K Heysell, Daiki Hira, Daan J Touw, Onno W Akkerman, Mathieu S Bolhuis, Jan-Willem C Alffenaar
BACKGROUND: Therapeutic drug monitoring is useful in the treatment of tuberculosis to assure adequate exposure, minimize antibiotic resistance, and reduce toxicity. Salivary therapeutic drug monitoring could reduce the risks, burden, and costs of blood-based therapeutic drug monitoring. This systematic review compared human pharmacokinetics of anti-tuberculosis drugs in saliva and blood to determine if salivary therapeutic drug monitoring could be a promising alternative. METHODS: On December 2, 2016, PubMed and the Institute for Scientific Information Web of Knowledge were searched for pharmacokinetic studies reporting human salivary and blood concentrations of anti-tuberculosis drugs...
November 8, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29117990/simultaneous-physiologically-based-pharmacokinetic-pbpk-modeling-of-parent-and-active-metabolites-to-investigate-complex-cyp3a4-drug-drug-interaction-potential-a-case-example-of-midostaurin
#8
Helen Gu, Catherine Dutreix, Sam Rebello, Taoufik Ouatas, Lai Wang, Dung Yu Chun, Heidi J Einolf, Handan He
Midostaurin (PKC412) is being investigated for the treatment of acute myeloid leukemia (AML) and advanced systemic mastocytosis (advSM). It is extensively metabolized by cytochrome P450 (CYP) 3A4 to form 2 major active metabolites, CGP52421 and CGP62221. In vitro and clinical drug-drug interaction (DDI) studies indicated that midostaurin and its metabolites are substrates, reversible and time-dependent inhibitors, and inducers of CYP3A4. A simultaneous pharmacokinetic model of parent and active metabolites was initially developed by incorporating data from in vitro, preclinical, and clinical pharmacokinetic studies in healthy volunteers and in patients with AML or advSM...
November 8, 2017: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/29098603/development-of-guanfacine-extended-release-dosing-strategies-in-children-and-adolescents-with-adhd-using-a-physiologically-based-pharmacokinetic-model-to-predict-drug-drug-interactions-with-moderate-cyp3a4-inhibitors-or-inducers
#9
Aiqun Li, Karen Yeo, Devin Welty, Haojing Rong
BACKGROUND: Guanfacine extended-release (GXR) is an orally administered, non-stimulant treatment for children and adolescents with attention-deficit/hyperactivity disorder (ADHD) and is primarily metabolized by the 3A4 isozyme of cytochrome P450 (CYP3A4). The results of clinical pharmacokinetic (PK) studies indicate that guanfacine is sensitive to drug-drug interactions (DDIs) perpetrated by strong inhibitors and inducers of CYP3A4. OBJECTIVE: The aim was to provide guidance on the possible requirement for GXR dose adjustment in children and adolescents with ADHD by predicting DDIs following co-administration with moderate CYP3A4 inhibitors and inducers...
November 2, 2017: Paediatric Drugs
https://www.readbyqxmd.com/read/29076107/pharmacokinetic-evaluation-of-the-interactions-of-amenamevir-asp2151-with-ketoconazole-rifampicin-midazolam-and-warfarin-in-healthy-adults
#10
Tomohiro Kusawake, Martin den Adel, Dorien Groenendaal-van de Meent, Alberto Garcia-Hernandez, Akitsugu Takada, Kota Kato, Yoshiaki Ohtsu, Masataka Katashima
INTRODUCTION: Amenamevir is a nonnucleoside antiherpes virus compound available for treating herpes zoster infections. Four studies aimed to determine any potential interactions between amenamevir and ketoconazole, rifampicin, midazolam, or warfarin in healthy male participants. METHODS: Two studies were open-label studies that evaluated the effects of multiple doses of ketoconazole (400 mg) and rifampicin (600 mg) on the pharmacokinetics of a single oral dose of amenamevir...
October 26, 2017: Advances in Therapy
https://www.readbyqxmd.com/read/29066867/clinical-and-pharmacological-hallmarks-of-rifapentine-s-use-in-diabetes-patients-with-active-and-latent-tuberculosis-do-we-know-enough
#11
REVIEW
Chunlan Zheng, Xiufen Hu, Li Zhao, Minhui Hu, Feng Gao
Rifapentine is a rifamycin derivate approved by the US Food and Drug Administration in 1998 for the treatment of active, drug-susceptible tuberculosis (TB). In 2014, rifapentine was approved for the treatment of latent TB infection in patients at high risk of progression to active disease and is currently under evaluation by the European Medicines Agency. Expanding indications of rifapentine largely affect diabetes patients, since about one-third of them harbor latent TB. Clinical consequences of rifapentine use in this population and potentially harmful interactions with hypoglycemic agents are widely underexplored and generally considered similar to the ones of rifampicin...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29063794/critical-physicochemical-and-biological-attributes-of-nanoemulsions-for-pulmonary-delivery-of-rifampicin-by-nebulization-technique-in-tuberculosis-treatment
#12
Kifayatullah Shah, Lai Wah Chan, Tin Wui Wong
The study investigated aerosolization, pulmonary inhalation, intracellular trafficking potential in macrophages and pharmacokinetics profiles of rifampicin-oleic acid first-generation nanoemulsion and its respective chitosan- and chitosan-folate conjugate-decorated second and third-generation nanoemulsions, delivered via nebulization technique. The nanoemulsions were prepared by conjugate synthesis and spontaneous emulsification techniques. They were subjected to physicochemical, drug release, aerosolization, inhalation, cell culture and pharmacokinetics analysis...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/29027654/pharmacokinetic-drug-drug-interactions-in-the-intensive-care-unit-single-centre-experience-and-literature-review
#13
Piotr Łój, Aleksanda Olender, Weronika Ślęzak, Łukasz J Krzych
BACKGROUND: Drug-drug interactions constitute a serious health hazard in everyday clinical practice in critically ill patients. Drug-drug interactions may be pharmacokinetic or pharmacodynamic in their nature. We aimed to investigate the quantity and quality of possible drug-drug interactions, and their possible side effects in intensive care unit patients in a 12-month period. METHODS: This retrospective study covered data on pharmacological treatment of 43 consecutive patients (11 females, 32 males) aged 62 ± 15 years, hospitalized between January 2015 and February 2016...
2017: Anaesthesiology Intensive Therapy
https://www.readbyqxmd.com/read/28993217/mechanistic-pbpk-modeling-of-the-dissolution-and-food-effect-of-a-bcs-iv-compound-the-venetoclax-story
#14
Arian Emami Riedmaier, David J Lindley, Jeffrey A Hall, Steven Castleberry, Russell T Slade, Patricia Stuart, Robert A Carr, Thomas B Borchardt, Daniel A J Bow, Marjoleen Nijsen
PURPOSE: Venetoclax, a selective B-cell lymphoma-2 inhibitor, is a biopharmaceutics classification system (BCS) class IV compound. The aim of this study was to develop a physiologically-based pharmacokinetic (PBPK) model to mechanistically describe absorption and disposition of an amorphous solid dispersion (ASD) formulation of venetoclax in humans. METHODS: A mechanistic PBPK model was developed incorporating measured amorphous solubility, dissolution, metabolism and plasma protein binding...
October 6, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28993169/anti-tuberculosis-drug-combination-for-controlled-oral-delivery-using-3d-printed-compartmental-dosage-forms-from-drug-product-design-to-in-vivo-testing
#15
Natalja Genina, Johan Peter Boetker, Stefano Colombo, Necati Harmankaya, Jukka Rantanen, Adam Bohr
The design and production of an oral dual-compartmental dosage unit (dcDU) was examined in vitro and in vivo with the purpose of physically isolating and modulating the release profile of an anti-tuberculosis drug combination. Rifampicin (RIF) and isoniazid (ISO) are first line combination drugs for treatment of tuberculosis (TB) that negatively interact with each other upon simultaneous release in acidic environment. The dcDUs were designed in silico by computer aided design (CAD) and fabricated in two steps; first three-dimensional (3D) printing of the outer structure, followed by hot-melt extrusion (HME) of the drug-containing filaments...
October 6, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28960401/prediction-of-drug-drug-interactions-using-physiologically-based-pharmacokinetic-models-of-cyp450-modulators-included-in-simcyp-software
#16
Niloufar Marsousi, Jules A Desmeules, Serge Rudaz, Youssef Daali
In recent years, Physiologically-Based PharmacoKinetic (PBPK) modeling has received growing interest as a useful tool for assessment of drug PK. It has demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio-pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug-drug interactions (DDIs). In this paper, the prediction success of DDIs involving various cytochrome P450 isoenzyme (CYP) modulators namely ketoconazole (a competitive inhibitor of CYP3A), itraconazole (a competitive inhibitor of CYP3A), clarithromycin (a mechanism-based inhibitor of CYP3A), quinidine (a competitive inhibitor of CYP2D6), paroxetine (a mechanism-based inhibitor of CYP2D6), ciprofloxacin (a competitive inhibitor of CYP1A2), fluconazole (a competitive inhibitor of CYP2C9/2C19) and rifampicin (an inducer of CYP3A) were assessed using Simcyp® software...
September 28, 2017: Biopharmaceutics & Drug Disposition
https://www.readbyqxmd.com/read/28948652/pharmacokinetic-changes-of-antibiotic-antiviral-antituberculosis-and-antifungal-agents-during-extracorporeal-membrane-oxygenation-in-critically-ill-adult-patients
#17
REVIEW
J Hahn, J H Choi, M J Chang
WHAT IS KNOWN AND OBJECTIVE: Extracorporeal membrane oxygenation (ECMO) is a life-saving system used for critically ill patients with cardiac and/or respiratory failure. The pharmacokinetics (PK) of drugs can change in patients undergoing ECMO, which can result in therapeutic failure or drug toxicity requiring further management of drug complications. In this review, we discussed changes in the PK of antibiotic, antiviral, antituberculosis and antifungal agents administered to adult patients on ECMO...
December 2017: Journal of Clinical Pharmacy and Therapeutics
https://www.readbyqxmd.com/read/28885219/recognition-of-possible-risk-factors-for-clinically-significant-drug-drug-interactions-among-indian-people-living-with-hiv-receiving-highly-active-antiretroviral-therapy-and-concomitant-medications
#18
Poka Siva Sai Lakshmi Priyanka, Danturulu Muralidhar Varma, Kavyasri Immadisetti, Radhakrishnan Rajesh, Sudha Vidyasagar, Vasudeva Guddattu
BACKGROUND: Greatest challenges for clinician is to recognize risk factors for clinically significant drug interactions (CSDIs). There is a lack of awareness about CSDIs among healthcare professionals in India. OBJECTIVE: To recognize all possible risk factors for drug-drug interactions (DDIs) and to identify clinically significant drug interactions (CSDIs), the prevalence, pattern of occurrence of DDIs in People Living with HIV (PLW-HIV) receiving highly active antiretroviral therapy (HAART) and concomitant medications...
2017: International Journal of Risk & Safety in Medicine
https://www.readbyqxmd.com/read/28862186/food-significantly-reduces-plasma-concentrations-of-first-line-anti-tuberculosis-drugs
#19
Agibothu Kupparam Hemanth Kumar, Vedachalam Chandrasekaran, Angadi Kiran Kumar, M Kawaskar, J Lavanya, Soumya Swaminathan, Geetha Ramachandran
BACKGROUND & OBJECTIVES: Concomitant feeding and anti-tuberculosis (TB) drug administration are likely to reduce nausea and enhance compliance to treatment. However, food could lower plasma drug concentrations. This study was undertaken to examine the effect of food on two-hour plasma concentrations of rifampicin (RMP), isoniazid (INH) and pyrazinamide (PZA), and pharmacokinetics of these drugs in adult TB patients. METHODS: Newly diagnosed adult TB patients were recruited from the Revised National Tuberculosis Control Programme (RNTCP) treatment centres in Chennai Corporation, Chennai, India...
April 2017: Indian Journal of Medical Research
https://www.readbyqxmd.com/read/28843937/determination-of-protein-unbound-active-rifampicin-in-serum-by-ultrafiltration-and-ultra-performance-liquid-chromatography-with-uv-detection-a-method-suitable-for-standard-and-high-doses-of-rifampicin
#20
Eleonora W J van Ewijk-Beneken Kolmer, Marga J A Teulen, Erik C A van den Hombergh, Nielka E van Erp, Lindsey H M Te Brake, Rob E Aarnoutse
Rifampicin is the most important antibiotic in use for the treatment of tuberculosis (TB). Preclinical and clinical data suggest that higher doses of rifampicin, resulting in disproportionally higher systemic exposures to the drug, are more effective. Serum concentrations of rifampicin are the intermediary link between the dose administered and eventual response and only protein-unbound (free) rifampicin is pharmacologically active. The objective of this work was to develop an ultra performance liquid chromatography assay for protein-unbound rifampicin in serum with ultrafiltration, carried out at a sample temperature of 37°C, suitable for measurement of concentrations achieved after currently used and higher doses of rifampicin...
September 15, 2017: Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences
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