[ASAP] Selectivity Engineering in One-Pot Selective Synthesis of Drug Nabumetone over Novel Ni-Promoted La-Mg Oxide/Mesoporous Cellular Foam as Catalyst and Kinetic Modeling
Industrial& Engineering Chemistry ResearchDOI: 10.1021/acs.iecr.9b06210 (Source: Industrial and Engineering Chemical Research)
Source: Industrial and Engineering Chemical Research - February 10, 2020 Category: Chemistry Authors: Devendra S. Pisal and Ganapati D. Yadav* Source Type: research

A metabolic pathway for the prodrug nabumetone to the pharmacologically active metabolite, 6-methoxy-2-naphthylacetic acid (6-MNA) by non-cytochrome P450 enzymes.
Abstract 1. The pathway for the transformation of the prodrug nabumetone, 4-(6-methoxynaphthalen-2-yl)butan-2-on, to the active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA), a potent cyclooxygenase-2 inhibitor, has not yet been clarified in humans.2. To confirm the activation pathway, authentic standards of the nabumetone intermediates, 2-(6-methoxynaphthalen-2-yl)ethyl acetate (6-MNEA), 2-(6-methoxynaphthalen-2-yl)ethan-1-ol (6-MNE-ol) and 2-(6-methoxynaphthalen-2-yl)acetaldehyde (6-MN-CHO) were synthesized. High performance liquid-chromatography and gas chromatography-mass spectrometry on nabumetone oxidat...
Source: Xenobiotica - December 19, 2019 Category: Research Authors: Matsumoto K, Hasegawa T, Ohara K, Takei C, Kamei T, Koyanagi J, Takahashi T, Akimoto M Tags: Xenobiotica Source Type: research

Identification of antiparkinsonian drugs in the 6-hydroxydopamine zebrafish model
Publication date: Available online 28 November 2019Source: Pharmacology Biochemistry and BehaviorAuthor(s): Rita L. Vaz, Sara Sousa, Diana Chapela, Herma C. van der Linde, Rob Willemsen, Ana D. Correia, Tiago F. Outeiro, Nuno D. AfonsoAbstractParkinson's disease (PD) is known as a movement disorder due to characteristic motor features. Existing therapies for PD are only symptomatic, and their efficacy decreases as disease progresses. Zebrafish, a vertebrate in which parkinsonism has been modelled, offers unique features for the identification of molecules with antiparkinsonian properties. Here, we developed a screening ass...
Source: Pharmacology Biochemistry and Behavior - November 28, 2019 Category: Biochemistry Source Type: research

Preparation, characterization and in vitro cytotoxicity of Fenofibrate and Nabumetone loaded solid lipid nanoparticles
Publication date: January 2020Source: Materials Science and Engineering: C, Volume 106Author(s): Raj Kumar, Ashutosh Singh, Kajal Sharma, Divya Dhasmana, Neha Garg, Prem Felix SirilAbstractThere is an increasing attention on solid lipid nanoparticles (SLNs) due to their high biocompatibility and ability to enhance bioavailability for poorly water-soluble drugs. Preparation of SLNs that are capable of high drug loading and sustained drug release through hot melt sonication method is reported here. SLNs of palmitic acid and stearic acid loaded with poorly water-soluble drugs, viz. fenofibrate (FF) and nabumetone (NBT) having...
Source: Materials Science and Engineering: C - October 6, 2019 Category: Materials Science Source Type: research

Does medication administration affect the rate of orthodontic tooth movement and root resorption development in humans? A systematic review.
CONCLUSIONS: The aforementioned substances may show varying effects on the rate of orthodontic tooth movement and root resorption development in human subjects. Despite the observed limitations, the orthodontist should be able to identify patients taking pharmaceuticals and consider any implications related to orthodontic treatment. REGISTRATION: PROSPERO (CRD42017078208). PMID: 31421637 [PubMed - as supplied by publisher] (Source: European Journal of Orthodontics)
Source: European Journal of Orthodontics - August 18, 2019 Category: Dentistry Authors: Kaklamanos EG, Makrygiannakis MA, Athanasiou AE Tags: Eur J Orthod Source Type: research

Gut microbiota metabolizes nabumetone in vitro: Consequences for its bioavailability in vivo in the rodents with altered gut microbiome.
Abstract 1. The underlying microbial metabolic activity toward xenobiotics is among the least explored factors contributing to the inter-individual variability in drug response. 2. Here, we analyzed the effect of microbiota on a non-steroidal anti-inflammatory drug nabumetone. 3. First, we cultivated the drug with the selected gut commensal and probiotic bacteria under both aerobic and anaerobic conditions and analyzed its metabolites by high-performance liquid chromatography (HPLC) with UV detection. To analyze the effect of microbiota on nabumetone pharmacokinetics in vivo, we administered a single oral dose of ...
Source: Xenobiotica - February 22, 2019 Category: Research Authors: Jourova L, Anzenbacher P, Matuskova Z, Vecera R, Strojil J, Kolar M, Nobilis M, Hermanova P, Hudcovic T, Kozakova H, Kverka M, Anzenbacherova E Tags: Xenobiotica Source Type: research

Determination of the Absolute Configuration of the Nabumetone Metabolite 4-(6-Methoxy-2-naphthyl)butan-2-ol Using the Chiral Derivatizing Agent, 1-Fluoroindan-1-carboxylic Acid.
Abstract The absolute configuration of (+)-4-(6-methoxy-2-naphthyl)butan-2-ol ((+)-MNBO), a nabumetone metabolite, was determined using 1-fluoroindan-1-carboxylic acid (FICA). Both enantiomers of the FICA methyl esters were derivatized to diastereomeric esters of (+)-MNBO by an ester exchange reaction. The results of 1H- and 19F-NMR spectroscopy of the diastereomeric FICA esters of (+)-MNBO confirmed the absolute configuration of (+)-MNBO was (S). PMID: 30606953 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - January 6, 2019 Category: Drugs & Pharmacology Authors: Kamei T, Kimura Y, Koyanagi J, Matsumoto K, Hasegawa T, Akimoto M, Takahashi T Tags: Chem Pharm Bull (Tokyo) Source Type: research

The importance of the structure similarity of drugs used for depression and inflammation, two comorbid diseases.
Abstract Growing evidence links inflammation to depression and the combination of anti-inflammatory drugs with antidepressant to treat depressive symptoms is currently suggested. There is only few studies concerning the molecular mechanism underlying this comorbidity and many of them point out the importance of the tryptophan pathway. There is yet no data that analyzes the structural similarity of the molecules used for the treatment of these comorbid diseases. This review aimed first to classify current antidepressant drugs and non-steroidal anti-inflammatory drugs (NSAIDs) according to their structure. Molecules...
Source: Current Topics in Medicinal Chemistry - August 21, 2018 Category: Chemistry Authors: Bayram FEO, Reis R, Tuncer B, Sipahi H Tags: Curr Top Med Chem Source Type: research

Determining the Molecular Pathways Underlying the Protective Effect of Non-Steroidal Anti-Inflammatory Drugs for Alzheimer's Disease: A Bioinformatics Approach
In this study, we use pathway enrichment and fuzzy logic to identify pathways (KEGG database) simultaneously affected in both AD and by NSAIDs (Sulindac, Piroxicam, Paracetamol, Naproxen, Nabumetone, Ketoprofen, Diclofenac and Aspirin). Gene expression signatures were derived for disease from both blood (n = 344) and post-mortem brain (n = 690), and for drugs from immortalised human cell lines exposed to drugs of interest as part of the Connectivity Map platform. Using this novel approach to combine datasets we find striking overlap between AD gene expression in blood and NSAID induced changes in KEGG p...
Source: Computational and Structural Biotechnology Journal - July 10, 2018 Category: Biotechnology Source Type: research

Thiodipeptides targeting the intestinal oligopeptide transporter as a general approach to improving oral drug delivery.
Abstract The broad substrate capacity of the intestinal oligopeptide transporter, PepT1, has made it a key target of research into drug delivery. Whilst the substrate capacity of this transporter is broad, studies have largely been limited to small peptides and peptide-like drugs. Here, we demonstrate for the first time that a diverse range of drugs can be targeted towards transport by PepT1 using a hydrolysis resistant carrier. Eleven prodrugs were synthesized by conjugating modified dipeptides containing a thioamide bond to the approved drugs ibuprofen, gabapentin, propofol, aspirin, acyclovir, nabumetone, ateno...
Source: European Journal of Medicinal Chemistry - June 30, 2018 Category: Chemistry Authors: Foley DW, Pathak RB, Phillips TR, Wilson GL, Bailey PD, Pieri M, Senan A, Meredith D Tags: Eur J Med Chem Source Type: research

Development of Microemulsion Based Nabumetone Transdermal Delivery For Treatment of Arthritis.
Conclusion Nabumetone microemulgel exhibiting good in-vitro and ex-vivo controlled drug release was optimized. PMID: 29485013 [PubMed - as supplied by publisher] (Source: Recent Patents on Drug Delivery and Formulation)
Source: Recent Patents on Drug Delivery and Formulation - March 1, 2018 Category: Drugs & Pharmacology Tags: Recent Pat Drug Deliv Formul Source Type: research

Moving towards fast characterization of polymorphic drugs by solid-state NMR spectroscopy
Publication date: 30 January 2018 Source:Journal of Pharmaceutical and Biomedical Analysis, Volume 148 Author(s): Rosalynn Quiñones, Robbie J. Iuliucci, Grayce Behnke, Ryanne Brown, Deben Shoup, Taylor M. Riedel, Christine Plavchak, Brooke E. Lininger, Jonathan M. Spehar Solid-state nuclear magnetic resonance (SS-NMR) spectroscopy has become a common technique to study polymorphism in pharmaceutical solids at high-resolution. However, high-throughput application of high resolution SS-NMR spectroscopy is severely limited by the long 1H spin-lattice relaxation (T1) that is common to solid phase compounds. Here, we de...
Source: Journal of Pharmaceutical and Biomedical Analysis - October 14, 2017 Category: Drugs & Pharmacology Source Type: research

Analysis of inappropriate medication use and drug interactions in older people in South Korea 
CONCLUSION: Our findings demonstrated that PIM use and pDDIs were common in older people in the community setting, suggesting that optimal medication use and supportive interventions are necessary in this population.
. PMID: 28853697 [PubMed - as supplied by publisher] (Source: International Journal of Clinical Pharmacology and Therapeutics)
Source: International Journal of Clinical Pharmacology and Therapeutics - September 1, 2017 Category: Drugs & Pharmacology Tags: Int J Clin Pharmacol Ther Source Type: research

Celecoxib for rheumatoid arthritis.
CONCLUSIONS: Celecoxib may improve clinical symptoms, alleviate pain and contribute to little or no difference in physical function compared with placebo. Celecoxib was associated with fewer numbers of participant withdrawals. Results for incidence of gastroduodenal ulcers (≥ 3 mm) and short-term serious adverse events were uncertain; however, there were few reported events for either.Celecoxib may slightly improve clinical symptoms compared with tNSAIDs. Results for reduced pain and improved physical function were uncertain. Particpants taking celecoxib had lower incidence of gastroduodenal ulcers (≥ 3 mm) and there...
Source: Cochrane Database of Systematic Reviews - June 9, 2017 Category: General Medicine Authors: Fidahic M, Jelicic Kadic A, Radic M, Puljak L Tags: Cochrane Database Syst Rev Source Type: research

Coxibs Refocus Attention on the Cardiovascular Risks of Non-Aspirin NSAIDs
This article explains how coxibs refocused attention on the cardiovascular safety of NSAIDs and the general implications of that. COX-2 activity/specificity is one factor associated with increased cardiovascular risks; however, these risks cannot be attributed to coxibs alone. The traditional NSAIDs (i.e., meloxicam, etodolac, and nabumetone) have significant COX-2 specificity, but naproxen and ibuprofen have less specificity. All NSAIDs, whether traditional or a coxib, pose some cardiovascular risks. It is possible that clinicians continue to focus more on decreasing the immediate gastric risks than preventing the later c...
Source: American Journal of Cardiovascular Drugs - March 28, 2017 Category: Cardiology Source Type: research

Adverse and Hypersensitivity Reactions to Prescription Nonsteroidal Anti-Inflammatory Agents in a Large Health Care System
Conclusions NSAID therapeutic use can be limited by ADRs; about 1 in 5 NSAID ADRs is an HSR. Both patient and drug factors contribute to HSR risk and are important to guide patient counseling. (Source: The Journal of Allergy and Clinical Immunology: In Practice)
Source: The Journal of Allergy and Clinical Immunology: In Practice - January 19, 2017 Category: Allergy & Immunology Source Type: research

Conformational and entropy analyses of extended molecular dynamics simulations of [small alpha]-, [small beta]- and [gamma]-cyclodextrins and of the [small beta]-cyclodextrin/nabumetone complex
Phys. Chem. Chem. Phys., 2017, Advance Article DOI: 10.1039/C6CP06107A, PaperDimas Suarez, Natalia Diaz The conformational entropies of cyclodextrins and of the [small beta]-CD/nabumetone complex are assessed by means of extensive MD simulations. To cite this article before page numbers are assigned, use the DOI form of citation above. The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Phys. Chem. Chem. Phys. latest articles)
Source: RSC - Phys. Chem. Chem. Phys. latest articles - December 16, 2016 Category: Chemistry Authors: Dimas Suarez Source Type: research

Conformational and Entropy Analyses of Extended Molecular Dynamics Simulations of [small alpha]-, [small beta]- and [gamma]-Cyclodextrin and of the [small beta]-Cyclodextrin/Nabumetone Complex
Phys. Chem. Chem. Phys., 2016, Accepted Manuscript DOI: 10.1039/C6CP06107A, PaperDimas Suarez, Natalia Diaz Herein we report the results of 5.0 [small mu ]s molecular dynamics simulations of native [small alpha]-, [small beta]- and [gamma]-cyclodextrin (CD) in explicit water solvent that are useful to describe, in a comparative... The content of this RSS Feed (c) The Royal Society of Chemistry (Source: RSC - Phys. Chem. Chem. Phys. latest articles)
Source: RSC - Phys. Chem. Chem. Phys. latest articles - December 6, 2016 Category: Chemistry Authors: Dimas Suarez Source Type: research

Nabumetone and 6-MNA Pharmacokinetics, Assessment of Intrasubject Variability and Gender Effect
In this open-label, laboratory-blinded, 2-way single dose study in 24 volunteers of both sexes we found that (1) nabumetone reaches mean Cmax ± SD of 0.56 ± 0.20 mg·L−1 at mean tmax of 8.63 ± 7.05 hours, and mean area under the curve (AUC)last of 18.07 ± 7.19 h·mg·L−1; (2) there are no statistically significant differences between both sexes in pharmacokinetics of nabumetone; (3) 6-methoxy-2-naphthylacetic acid (6-MNA) reaches higher AUClast in men compared with women (mean ± SD, 721.23 ± 185.53 h·mg·L−1 and 545.27 ± 97.69...
Source: American Journal of Therapeutics - November 1, 2016 Category: Drugs & Pharmacology Tags: Original Articles Source Type: research

Pharmacokinetic and Pharmacodynamic Interaction of Andrographolide and Standardized Extract of Andrographis paniculata (Nees) with Nabumetone in Wistar Rats
The aim of the study was to investigate the herb–drug interaction of Andrographis paniculata Nees (Acanthaceae) and Andrographolide (AN) with nabumetone (NAB) in wistar rats. Pharmacokinetic and pharmacodynamic interactions were studied after co‐administration of APE and AN with NAB in Wistar rats. In pharmacokinetic studies, significant decrease in Cmax, AUC0–t and AUC0–∞ of 6‐MNA after co‐administration with pure AN and APE has been observed. Tmax of 6‐MNA has been increased to 2 h from 1.5 h in AN + NAB treated group. Changes in mean residential time, clearance...
Source: Phytotherapy Research - October 1, 2016 Category: Biochemistry Authors: Aishwarya Balap, Sathiyanarayanan Lohidasan, Arulmozhi Sinnathambi, Kakasaheb Mahadik Tags: Research Article Source Type: research

Polymorphic properties of micronized mefenamic acid, nabumetone, paracetamol and tolbutamide produced by rapid expansion of supercritical solutions (RESS)
Publication date: October 2016 Source:The Journal of Supercritical Fluids, Volume 116 Author(s): Michael Türk, Dennis Bolten The rapid expansion of a supercritical solution (RESS) process was used to produce submicron Paracetamol (=Acetaminophen), Mefenamic acid, Nabumetone and Tolbutamide particles. These model drugs have been chosen since different numbers of polymorphs (I & II, I–III and I–V) have been reported in literature. Thus, the aim of this investigation was twofold: to examine the possibility of using the RESS process to produce submicron drug particles and to control the polymorphic...
Source: The Journal of Supercritical Fluids - July 5, 2016 Category: Chemistry Source Type: research

Fixed Drug Eruption Due to Selective Hypersensitivity to Naproxen with Tolerance to other Propionic Acid NSAIDs.
CONCLUSION: In our patient PT confirmed the diagnosis and allowed us to study the cross-reactivity between NSAIDs of the same group, and confirmed by SBOCT. Cross-reactivity between propionic acid derivatives was studied. This is a case of hypersensitivity to naproxen with good tolerance to other propionic acids NSAIDs (ibuprofen and ketoprofen) and nabumetone, confirmed by PT and SBOCT. Some relavent patents for fixed drug eruption are discussed. PMID: 27041368 [PubMed - as supplied by publisher] (Source: Recent Patents on Inflammation and Allergy Drug Discovery)
Source: Recent Patents on Inflammation and Allergy Drug Discovery - April 7, 2016 Category: Allergy & Immunology Tags: Recent Pat Inflamm Allergy Drug Discov Source Type: research

Nabumetone use and risk of acute pancreatitis in a case-control study
It remains unknown whether nabumetone increases or decreases acute pancreatitis risk. To investigate this, we conducted a population-based case–control study using the database from the Taiwan National Health Insurance Program. (Source: Pancreatology)
Source: Pancreatology - March 11, 2016 Category: Gastroenterology Authors: Shih-Chang Hung, Kuan-Fu Liao, Hung-Chang Hung, Cheng-Li Lin, Shih-Wei Lai, Chih-Hsueh Lin Tags: Original Article Source Type: research

The modulation of carbonyl reductase 1 by polyphenols.
Authors: Boušová I, Skálová L, Souček P, Matoušková P Abstract Carbonyl reductase 1 (CBR1), an enzyme belonging to the short-chain dehydrogenases/reductases family, has been detected in all human tissues. CBR1 catalyzes the reduction of many xenobiotics, including important drugs (e.g. anthracyclines, nabumetone, bupropion, dolasetron) and harmful carbonyls and quinones. Moreover, it participates in the metabolism of a number of endogenous compounds and it may play a role in certain pathologies. Plant polyphenols are not only present in many human food sources, but are als...
Source: Drug Metabolism Reviews - February 16, 2016 Category: Drugs & Pharmacology Tags: Drug Metab Rev Source Type: research

Network Meta-Analysis Comparing Relatively Selective COX-2 Inhibitors Versus Coxibs for the Prevention of NSAID-Induced Gastrointestinal Injury
This study included 36 trials with a total of 112,351 participants. Network meta-analyses indicated no significant difference between relatively selective COX-2 inhibitors and coxibs regarding ulcer complications (RR, 1.38; 95% CI, 0.47–3.27), symptomatic ulcer (RR, 1.02; 95% CI, 0.09–3.92), and endoscopic ulcer (RR, 1.18; 95% CI, 0.37–2.96). Network meta-analyses adjusting potential influential factors (age, sex, previous ulcer disease, and follow-up time), and sensitivity analyses did not reveal any major change to the main results. Network meta-analyses suggested that relatively selective COX-2 inhibit...
Source: Medicine - October 1, 2015 Category: Internal Medicine Tags: Research Article: Systematic Review and Meta-Analysis (PRISMA Compliant) Source Type: research

Single dose oral analgesics for acute postoperative pain in adults - an overview of Cochrane reviews.
CONCLUSIONS: There is a wealth of reliable evidence on the analgesic efficacy of single dose oral analgesics. Fast acting formulations and fixed dose combinations of analgesics can produce good and often long-lasting analgesia at relatively low doses. There is also important information on drugs for which there are no data, inadequate data, or where results are unreliable due to susceptibility to publication bias. This should inform choices by professionals and consumers. PMID: 26414123 [PubMed - as supplied by publisher] (Source: Cochrane Database of Systematic Reviews)
Source: Cochrane Database of Systematic Reviews - September 28, 2015 Category: Journals (General) Authors: Moore RA, Derry S, Aldington D, Wiffen PJ Tags: Cochrane Database Syst Rev Source Type: research

Reductive metabolism of nabumetone by human liver microsomal and cytosolic fractions: exploratory prediction using inhibitors and substrates as marker probes
Abstract The metabolic reduction of nabumetone was examined by inhibition and correlation studies using human liver microsomes and cytosol. This reduction was observed in both fractions, with the V max values for reduction activity being approximately fourfold higher, and the V max /K m values approximately three-fold higher, in the microsomes than in the cytosol. The reduction of nabumetone was inhibited by 18β-glycyrrhetinic acid, an 11β-hydroxysteroid dehydrogenase (11β-HSD) inhibitor, in the microsomal fraction. The reduction activity was also inhibit...
Source: European Journal of Drug Metabolism and Pharmacokinetics - May 10, 2015 Category: Drugs & Pharmacology Source Type: research

A novel injection strategy of flurbiprofen axetil by inhibiting protein binding with 6-methoxy-2-naphthylacetic acid
This study focused on 6-methoxy-2-naphthylacetic acid (6-MNA), the active metabolite of nabumetone (a prodrug of NSAID). We performed ultrafiltration experiments and pharmacokinetics analysis in rats to investigate whether the inhibitory effect of 6-MNA on FP binding to albumin increased the free FP concentration in vitro and in vivo. Results indicated that 6-MNA inhibited the binding of FP to albumin competitively. When 6-MNA was injected in rats, there was a significant increase in the free FP concentration and the area under concentration–time curve (AUC) calculated from the free FP concentration, while there was ...
Source: European Journal of Drug Metabolism and Pharmacokinetics - December 24, 2014 Category: Drugs & Pharmacology Source Type: research

Concentration of non-steroidal anti-inflammatory drugs in the pelvic floor muscles: an experimental comparative rat model.
CONCLUSION: Diclofenac potassium had the highest disposition in pelvic floor muscle in a rat model. The finding implies that diclofenac potassium might be the choice for pain relief in pelvic muscle. PMID: 24954342 [PubMed - in process] (Source: Yonsei Medical Journal)
Source: Yonsei Medical Journal - June 29, 2014 Category: Universities & Medical Training Authors: Chin HY, Changchien E, Lin MF, Chiang CH, Wang CJ Tags: Yonsei Med J Source Type: research

Hypersensitivity to nabumetone: cross reactivity with naproxen.
tos A PMID: 23806470 [PubMed - as supplied by publisher] (Source: Annals of Allergy, Asthma and Immunology)
Source: Annals of Allergy, Asthma and Immunology - June 30, 2013 Category: Allergy & Immunology Authors: Rojas Perez-Ezquerra P, Sanchez-Morillas L, Laguna Martinez JJ, Gonzalez Mendiola R, Gomez-Traseira C, Carrasco Garcia I, Herranz Mañas M, Rubio Matos A Tags: Ann Allergy Asthma Immunol Source Type: research

A diclofenac suppository–nabumetone combination therapy for arthritic pain relief and a monitoring method for the diclofenac binding capacity of HSA site II in rheumatoid arthritis
ABSTRACT Diclofenac suppository , a non‐steroidal anti‐inflammatory drug (NSAID), is used widely in rheumatoid arthritis (RA) patients with severe arthritic pain. As the binding percentage of diclofenac to serum proteins is high, its free (unbound) concentration after rectal administration is low. To increase temporarily the free concentration of diclofenac and to enhance its analgesic effect by inhibiting the protein binding of diclofenac, the analgesic effect of diclofenac was examined before and after the start of an inhibitor administration to RA patients with insufficient control of arthritic pain, and the protein...
Source: Biopharmaceutics and Drug Disposition - January 24, 2013 Category: Drugs & Pharmacology Authors: Nao Setoguchi, Norito Takamura, Ken‐ichi Fujita, Kenji Ogata, Jin Tokunaga, Toyotaka Nishio, Etsuo Chosa, Kazuhiko Arimori, Keiichi Kawai, Ryuichi Yamamoto Tags: Original Paper Source Type: research