tolmetin / Generic mfg. - LARVOL DELTA

Combination of solid-liquid hollow fiber liquid phase microextraction method with electromembrane extraction for extraction of Tolmetin and its determination followed by high performance liquid chromatography-ultraviolet detection. (PubMed, Ecotoxicol Environ Saf) - "This approach offers high sensitivity, short extraction time, and excellent selectivity and reproducibility, making it well suited for trace analysis of tolmetin in complex matrices."

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Fabrication of tolmetin/cyclodextrin nanofibers for potential wound healing applications: Physicochemical, in vitro characterization, and scratch assay. (PubMed, Int J Pharm) - "Cultured cells treated with TMN-CD-IC-NFs were well proliferated towards the scratched area and the wound closure rate was higher (80-90 %) compared to the control. Thus, fabricated TMN-CD-IC-NFs have potential as sustained drug nanocarriers for wound treatment."

Journal • Preclinical • Inflammation

Spectrofluorometric Turn-Off Sensing Probe for Tolmetin Determination Using Cerium and Nitrogen Codoped Carbon Dots. (PubMed, Luminescence) - "The developed sensing strategy was successfully applied for TOL detection as an active pharmaceutical ingredient in pharmaceutical formulation and as a potential pollutant in environmental water samples, such as tap and river water, with acceptable recovery and considerable selectivity. Thus, the direct single-step spectrofluorometric determination of TOL was enabled without extensive processing or chemical derivatization."

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Potential-Modulated Surface-Enhanced Raman Spectroscopy of Tolmetin at Gold Nanoparticle Film Functionalized Polarizable Liquid-Liquid Interfaces. (PubMed, J Phys Chem C Nanomater Interfaces) - "Intense SERS signals are observed at the polarizable liquid-liquid interface when micromolar concentrations of tolmetin, a nonsteroidal anti-inflammatory drug, are entrapped in the AuNP fractal film. The change in the signal intensity, averaged over multiple spectra, with respect to the concentration of tolmetin, depends on the polarization conditions and suggests the presence of chemical-induced damping effects on the surface plasmons of the gold film."

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Systematic review and network meta-analysis of different non-steroidal anti-inflammatory drugs for juvenile idiopathic arthritis. (PubMed, World J Clin Cases) - "In summary, celecoxib (6 mg/kg bid) was found to be the most effective NSAID for treating JIA. Rofecoxib, piroxicam, and meloxicam may be safer options, but further research is needed to confirm these findings in larger trials with higher quality studies."

Journal • Retrospective data • Review • Idiopathic Arthritis • Immunology • Rheumatoid Arthritis • Rheumatology

Modification of cellulose substrate by in situ synthesis of metal-organic framework-5 for thin film microextraction of some non-steroidal anti-inflammatory drugs and their measurement by high-performance liquid chromatography-ultraviolet detector. (PubMed, J Chromatogr A) - "The thin film prepared by MOF-5 modified cellulose substrate was utilized in thin film microextraction (TFME) method for the extraction and preconcentration of naproxen, aspirin, tolmetin, and celecoxib. Moreover, relative recoveries varied from of 94 % to 108 %, indicating the absence of matrices effect in the proposed method. Eventually, the TFME was successfully used for the extraction of selected analytes from urine samples."

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Recent Advancements in Refashioning of NSAIDs and their Derivatives as Anticancer Candidates. (PubMed, Curr Pharm Des) - "This review summarizes the antiproliferative activity of derivatives of NSAIDs such as Diclofenac, Etodolac, Celecoxib, Ibuprofen, Tolmetin, and Sulindac, published between 2017 and 2023. Their mechanism of action and structural activity relationships (SARs) were also discussed to set the path for potential future repositioning of NSAIDs for clinical deployment in the treatment of cancer."

Journal • Oncology

Surface-enhanced Raman spectroscopy of drugs at water-oil interfaces: Impact of electrochemical polarization induced by background electrolytes (ACS-Fall 2023) - "Therefore, our method is very adaptive and easy to use for analytical purposes and also to study in situ the physicochemical characteristics of this fascinating interface between two immiscible liquids. Schematic representation of SERS detection of tolmetin drug at a free-floating assemblies of gold nanoparticles at water-oil interfaces"

Transcriptional Profiling of a Patient-Matched Cohort of Glioblastoma (IDH-Wildtype) for Therapeutic Target and Repurposing Drug Identification. (PubMed, Biomedicines) - "Top-ranking target compounds that may be effective against GSC and GBM recurrence were rosiglitazone, nizatidine, pantoprazole, and tolmetin. Our translational bioinformatics pipeline provides an approach to identify target compounds for repurposing that may add clinical benefit in addition to standard therapies against resistant cancers such as GBM."

IO biomarker • Journal • Brain Cancer • CNS Tumor • Glioblastoma • Glioma • Oncology • Solid Tumor

Forty years experience in Bartter's syndrome (IPNA 2022) - "19/19 received prostaglandin inhibitors (NSAIDs) indomethacin (maximum 2.04±0.68 mg/kg/day) or tolmetin (maximum 31.2±14mg/kg/day), with no significant adverse effects, permitting treatment to be maintained throughout the course of the disease. At the end of the follow-up only 1 has a lower height -2SD. Renal function is deteriorated in only those with nephrocalcinosis, although we are uncertain about the role of NSAID use in the long-term."

Chronic Kidney Disease • Gastrointestinal Disorder • Metabolic Disorders • Nephrology • Rare Diseases • Renal Disease

Oxalate Oxidase for In Situ H2O2-generation in Unspecific Peroxygenase-Catalysed Drug Oxyfunctionalisations. (PubMed, Angew Chem Int Ed Engl) - "Furthermore, oxidation of the drug tolmetin was achieved on a 50 mg scale (TON UPO 25,664) with 84% yield, which was further improved via enzyme immobilization. This one-pot approach ensures adequate H 2 O 2 levels, enabling rapid access to industrially relevant molecules that are difficult to obtain by other routes."

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Tolmetin Sodium Fast Dissolving Tablets for Rheumatoid Arthritis Treatment: Preparation and Optimization Using Box-Behnken Design and Response Surface Methodology. (PubMed, Pharmaceutics) - "For optimizing and analyzing the effect of super-disintegrants and sublimating agents in the TLM-FDTs formula, the three-factor, three-level full factorial design is a suitable tool. TLM-FDTs are a possible drug delivery system for enhancing TLM bioavailability and could be used to treat rheumatoid arthritis."

Journal • Gastrointestinal Disorder • Immunology • Inflammation • Inflammatory Arthritis • Orthopedics • Rheumatoid Arthritis • Rheumatology

A universal methodology for reliable predicting the non-steroidal anti-inflammatory drug solubility in supercritical carbon dioxide. (PubMed, Sci Rep) - "The considered NSAIDs are Fenoprofen, Flurbiprofen, Ibuprofen, Ketoprofen, Loxoprofen, Nabumetone, Naproxen, Nimesulide, Phenylbutazone, Piroxicam, Salicylamide, and Tolmetin. Experimental measurements, model predictions, and relevancy analyses justified that the drug solubility in SCCO increases by increasing temperature and pressure. The results show that Ibuprofen and Naproxen are the most soluble and insoluble drugs in SCCO, respectively."

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Design, synthesis, anticancer evaluation, and molecular modelling studies of novel tolmetin derivatives as potential VEGFR-2 inhibitors and apoptosis inducers. (PubMed, J Enzyme Inhib Med Chem) - "Compound 5b arrested the cell cycle in the G0/G1 phase. Furthermore, the ADME studies showed that compound 5b possessed promising pharmacokinetic properties."

Journal • Oncology • KDR

Molecularly Imprinted Micelles for Fluorescent Sensing of Nonsteroidal Anti-Inflammatory Drugs (NSAIDs). (PubMed, React Funct Polym) - "A thiourea-based fluorescent functional monomer was identified in this work to enable highly efficient synthesis of molecularly imprinted nanoparticle (MINP) sensors for NSAIDs such as Indomethacin or Tolmetin. Micromolar binding affinities were obtained in aqueous solution, with binding selectivities comparable to those reported for polyclonal antibodies. The detection limit was ~50 ng/mL in aqueous solution, and common carboxylic acids such as acetic acid, benzoic acid, and citric acid showed negligible interference."

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Crystal structure of the non-steroidal anti-inflammatory drug (NSAID) tolmetin sodium. (PubMed, Acta Crystallogr E Crystallogr Commun) - "As a result, a two-dimensional polymer is formed in the crystal. Hirshfeld surface analysis and two-dimensional fingerprint plots were used to analyze the inter-molecular contacts present in the crystal."

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[VIRTUAL] Concomitant use of direct oral anticoagulants and nonsteroidal anti-inflammatory drugs: a review of the literature (ASHP 2020) - "Purpose: Direct oral anticoagulants were developed to provide an alternative to warfarin with less stringent monitoring requirements...The direct oral anticoagulants were apixaban, edoxaban, dabigatran, rivaroxaban, and betrixaban. The nonsteroidal anti-inflammatory drugs included ibuprofen, ketoprofen, meloxicam ketorolac, diclofenac, indomethacin, celecoxib, naproxen, diflunisal, etodolac, fenoprofen, flurbiprofen, mefenamic acid, nabumetone, oxaprozin, piroxicam, sulindac, and tolmetin... Overall, the studies found that the difference in the risk of bleeding is not statistically significant between patients who used NSAIDs while on particular DOACs and those who did not. These DOACs include rivaroxaban, dabigatran, and apixaban. Other pharmacokinetic and pharmacodynamic studies found slight increases in bleeding time but nothing significant as well."

Review • Atrial Fibrillation • Cardiovascular

Dispersive micro-solid phase extraction combined with switchable hydrophilicity solvent-based homogeneous liquid-liquid microextraction for enrichment of non-steroidal anti-inflammatory drugs in environmental water samples. (PubMed, J Chromatogr A) - "To demonstrate the applicability of proposed method, three non-steroidal anti-inflammatory drugs including ketoprofen, naproxen and tolmetin in water samples were enriched and purified prior to HPLC-UV analysis. The method exhibits good linearity (0.1-50 ng/mL), low limits of detection (0.02-0.05 ng/mL), high precision (RSDs<9.3%) and acceptable accuracy (97.2%-105.7%). Therefore, the presented procedure is fast, sensitive, simple and suitable for determination of non-steroidal anti-inflammatory drugs from aqueous matrices."

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Using static method to measure tolmetin solubility at different pressures and temperatures in supercritical carbon dioxide. (PubMed, Sci Rep) - "The correlated solubility data revealed that the KJ model was the most accurate one with an average absolute relative deviation percent (AARD%) of 6.9. Moreover, the carried out self-consistency analysis utilizing these correlations illustrated great potential of these models to extrapolate the solubility of tolmetin beyond the measured conditions."

Journal • Immunology • Osteoarthritis • Pain • Rheumatoid Arthritis • Rheumatology

Design, synthesis of celecoxib-tolmetin drug hybrids as selective and potent COX-2 inhibitors. (PubMed, Bioorg Chem) - "Three novel series of diarylpyrazole 10b-d and triarylpyrazole derivatives 11a-d &12a-d were synthesized through Vilsmier-Haack condition. All compounds were more selective for COX-2 isozyme than COX-1 isozyme and with excellent anti-inflammatory activity. Compounds 11b, 11d and 12b showed the highest anti-inflammatory activity (67.4%, 62.7%, 61.4% respectively), lower ulcerogenic liability (UI = 2.00, 2.75, 3.25 respectively) than indomethacin (UI = 14) and comparable to celecoxib (UI = 1.75) which were confirmed from the histopatholgical study."

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Drug repurposing for schistosomiasis: molecular docking and dynamics investigations. (PubMed, J Biomol Struct Dyn) - "Its treatment relies on the use of praziquantel or oxamniquine but there are reported cases of treatment failures due to resistance or tolerance...Tolmetin was predicted as potential antischistosomal drug with binding energies of -231.064 ± 18.550 and -338.636 ± 36.900 KJ/mol for sulfotransferase and thioredoxin glutathione reductase (TGR) respectively...Confirmation of covalent interactions and in vitro validations are recommended. Communicated by Ramaswamy H. Sarma."

Journal • GSR

Spectroscopic Studies as a Toolbox for Biophysical and Chemical Characterization of Lipid-Based Nanotherapeutics. (PubMed, Front Chem) - "The least observed quenching effect suggested that Tolmetin is probably located at the polar headgroup region of the lipid nanocarriers and this superficial location may translate in a fast drug release from the nanocarriers. Finally the cellular uptake of lipid nanocarriers loaded with Daunorubicin was investigated in cancer cells using fluorescence lifetime imaging microscopy. From the images obtained it was possible to conclude that even at short incubation times (15 min) there was a distribution of the drug in the cytoplasm, whereas for longer incubation periods (4 h) the drug has reached the nucleus."

Journal • Biosimilar • Oncology

Sensitive spectrofluorimetric and mass spectroscopic methods for the determination of nucleic acid damage induced by photosensitized anti-inflammatory drugs: Comparative study. (PubMed, J Pharm Biomed Anal) - "Five commonly used anti-inflammatory drugs; diclofenac, ketoprofen, leflunomide, piroxicam and tolmetin, were studied. Results show that DNA-damage occurred via photoinduced oxidative mechanism. Also, the potency of the studied drugs was examined on calf-thymus real DNA samples using TbCl fluorescence with ketoprofen and leflunomide being the most photogenotoxic anti-inflammatory drugs."

Journal • Oncology

[A choice of a nonsteroidal anti-inflammatory drug with regard to gastrointestinal and cardiovascular' risks]. (PubMed) - Zh Nevrol Psikhiatr Im S S Korsakova - "The potential negative risks of using NSAIDs promote an active research on creation of ne...y medicinal substances which are able to minimize NSAID-induced complications. The use of oxide-nitrogen-associated NSAIDs, in particular amtolmetin guacil1in patients with risk factors of side-effects from the gastrointestinal tract and cardiovascular system seems to be promising.It is noted that amtolmetin guacil has balanced analgesic and anti-inflammatory effects and is well tolerated."

Journal • Biosimilar • Pain

Polymeric ionic liquid immobilized onto paper as sorptive phase in microextraction. (PubMed, Anal Chim Acta) - "The method detection limits were 3.8, 7.2, 6.8, 9.4, 15.7, and 5.1 μg/L for indomethacin, diclofenac, tolmetin, ketoprofen, naproxen, and ibuprofen, respectively. The accuracy, calculated as relative recovery, was in the range from 72 to 95%, thus being considered appropriate. The easiness of polymeric ionic liquid paper synthesis and the multi-sample extraction protocol designed allows the processing of a high number of samples at the same time."

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