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Ketoprofen toxic

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https://www.readbyqxmd.com/read/29705907/impact-of-selected-drugs-and-their-binary-mixtures-on-the-germination-of-sorghum-bicolor-sorgo-seeds
#1
Monika Wieczerzak, Błażej Kudłak, Jacek Namieśnik
The aim of this study was to assess the toxicological potential of binary drug mixtures and individual drugs under different pH conditions with different inorganic ion additions on the germination of Sorghum bicolor (sorgo) seeds. To assess whether the given drug mixtures were more phytotoxic than the individual compounds, concentration addition (CA) and independent action (IA) approaches were applied to estimate the predicted phytotoxicity values, followed by calculations of the MDR (model deviation factor) to determine the deviation from the predicted values...
April 29, 2018: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/29702595/optical-detection-of-ketoprofen-by-its-electropolymerization-on-an-indium-tin-oxide-coated-optical-fiber-probe
#2
Robert Bogdanowicz, Paweł Niedziałkowski, Michał Sobaszek, Dariusz Burnat, Wioleta Białobrzeska, Zofia Cebula, Petr Sezemsky, Marcin Koba, Vitezslav Stranak, Tadeusz Ossowski, Mateusz Śmietana
In this work an application of optical fiber sensors for real-time optical monitoring of electrochemical deposition of ketoprofen during its anodic oxidation is discussed. The sensors were fabricated by reactive magnetron sputtering of indium tin oxide (ITO) on a 2.5 cm-long core of polymer-clad silica fibers. ITO tuned in optical properties and thickness allows for achieving a lossy-mode resonance (LMR) phenomenon and it can be simultaneously applied as an electrode in an electrochemical setup. The ITO-LMR electrode allows for optical monitoring of changes occurring at the electrode during electrochemical processing...
April 27, 2018: Sensors
https://www.readbyqxmd.com/read/29626791/biotransformation-and-oxidative-stress-responses-in-rat-hepatic-cell-line-h4iie-exposed-to-racemic-ketoprofen-rs-kp-and-its-enantiomer-dexketoprofen-s-kp
#3
Elvira Mennillo, Åse Krøkje, Carlo Pretti, Valentina Meucci, Augustine Arukwe
Pharmaceuticals such as racemate ketoprofen (RS-KP) and its enantiomer, dexketoprofen (S(+)-KP) are highly detectable non-steroidal anti-inflammatory drugs (NSAIDs) in the aquatic environment and therefore are designated as one of the most emerging groups of pollutants that can affect environmental and human health. The potential impact of these pharmaceuticals was assessed for the first time in vitro using a rat hepatocellular carcinoma cell line (H4IIE). Cells were exposed to low and high concentrations of these drugs...
March 30, 2018: Environmental Toxicology and Pharmacology
https://www.readbyqxmd.com/read/29524877/impact-of-inorganic-ions-and-ph-variations-on-toxicity-and-endocrine-potential-of-selected-environmentally-relevant-pharmaceuticals
#4
Monika Wieczerzak, Błażej Kudłak, Galina Yotova, Stefan Tsakovski, Vasil Simeonov, Jacek Namieśnik
Assessment of the impact of pharmaceutical residues on living organisms is a very complex subject. Apart from taking into account the toxicity of individual compounds, environmental factors should also be taken into account. In this paper, attempts were made to assess the impact of coexisting inorganic ions and changes in pH on the toxicity of ten selected pharmaceuticals. Two bioassays were used to measure the estrogenic and androgenic effects (XenoScreen YES/YAS - Saccharomyces cerevisiae) and acute toxicity (Microtox® - Vibrio fischeri)...
June 2018: Environmental Pollution
https://www.readbyqxmd.com/read/29417856/gastrointestinal-safety-and-tolerability-of-oral-non-aspirin-over-the-counter-analgesics
#5
REVIEW
Nicholas Moore, James M Scheiman
Over-the-counter (OTC) analgesics are routinely used worldwide for self-management of various painful conditions. Despite this, there has been little in-depth review of the safety of non-aspirin analgesics at OTC doses. This paper reviews the available literature on the gastrointestinal (GI) and hepatic safety of non-aspirin OTC analgesics, including nonsteroidal anti-inflammatory drugs (NSAIDs; ibuprofen, ketoprofen, diclofenac, and naproxen) and acetaminophen; safety in overdose is also reviewed. Each non-aspirin OTC analgesic has a distinct adverse event (AE) profile, with GI AE rates for OTC dosing in one study ranging from 37% for diclofenac to 7...
March 2018: Postgraduate Medicine
https://www.readbyqxmd.com/read/29174986/correlation-between-glucuronidation-and-covalent-adducts-formation-with-proteins-of-nonsteroidal-anti-inflammatory-drugs
#6
Hiroaki Shimada, Yuri Kobayashi, Sakiko Tanahashi, Atsushi Kawase, Taro Ogiso, Masahiro Iwaki
Nonsteroidal anti-inflammatory drugs (NSAIDs) can cause idiosyncratic liver injury. Mechanisms involved in NSAID-induced liver injury are complex. Previous studies have suggested that acyl glucuronide of NSAIDs (NSAIDs-Glu) plays an important role in the development of liver injury via covalently binds to proteins and the resultant adduct induces immunological toxicity. As only some NSAIDs-Glu are commercially available, the evaluation of covalent protein adduct formation using ready-made NSAIDs-Glu is difficult and inconvenient...
January 15, 2018: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29043859/gastrointestinal-bleeding-associated-with-chronic-excessive-use-overdosing-with-topical-ketoprofen-patch-in-elderly-patient
#7
Sakiko Hirose, Kana Matsuura, Hiroko Kato-Hayashi, Akio Suzuki, Koichi Ohata, Ryo Kobayashi, Takashi Ibuka, Hiroshi Araki, Masahito Shimizu, Yoshinori Itoh
PURPOSE: Topical ketoprofen patch has been developed to reduce the risk of systemic adverse effects such as gastrointestinal injury and renal toxicity. MATERIALS AND METHODS: We reported here a case of lower intestinal bleeding associated with chronic excessive use of topical ketoprofen patch in an elderly patient. RESULTS: A 74-year-old female visited to the outpatient clinic of the Gifu University Hospital and admitted thereafter. She had fecal occult blood and anemia...
January 2018: Scandinavian Journal of Gastroenterology
https://www.readbyqxmd.com/read/28946474/solid-lipid-nanoparticles-for-the-controlled-delivery-of-poorly-water-soluble-non-steroidal-anti-inflammatory-drugs
#8
Raj Kumar, Ashutosh Singh, Neha Garg, Prem Felix Siril
Non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen (IBP) are among the most prescribed drugs across the globe. However, most NSAIDs are insoluble in water leading them to have poor bioavailability and erratic absorption. Moreover, NSAIDs such as IBP and ketoprofen (KP) have to be administered very frequently due to their short plasma half-life leading to side effects. Controlled release formulations of IBP, KP and nabumetone (NBT) based on solid lipid nanoparticles (SLNs) were successfully synthesised in the present study to solve the above-mentioned challenges that are associated with NSAIDs...
January 2018: Ultrasonics Sonochemistry
https://www.readbyqxmd.com/read/28894363/ketoprofen-loaded-polymer-carriers-in-bigel-formulation-an-approach-to-enhancing-drug-photostability-in-topical-application-forms
#9
Velichka Andonova, Petya Peneva, George S Georgiev, Vencislava T Toncheva, Elisaveta Apostolova, Zhivko Peychev, Stela Dimitrova, Mariana Katsarova, Nadia Petrova, Margarita Kassarova
The purpose of the study was to investigate the stability and biopharmaceutical characteristics of ketoprofen, loaded in polymeric carriers, which were included into a bigel in a semisolid dosage form. The polymer carriers with in situ-included ketoprofen were obtained by emulsifier-free emulsion polymerization of the monomers in aqueous medium or a solution of the polymers used. The morphological characteristics of the carriers, the in vitro release and the photochemical stability of ketoprofen were evaluated...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28796322/ecotoxicological-properties-of-ketoprofen-and-the-s-enantiomer-dexketoprofen-bioassays-in-freshwater-model-species-and-biomarkers-in-fish-plhc-1-cell-line
#10
Elvira Mennillo, Augustine Arukwe, Gianfranca Monni, Valentina Meucci, Luigi Intorre, Carlo Pretti
The increased use of nonsteroidal anti-inflammatory drugs (NSAIDs) has resulted in their ubiquitous presence in the environment. The toxicological properties of these 2 widely prescribed NSAIDs, namely racemic ketoprofen and its enantiomer S(+)-ketoprofen (dexketoprofen), were evaluated, firstly, by acute and chronic toxicity tests using 3 representative model organisms (Vibrio fischeri, Pseudokirchneriella subcapitata, and Ceriodaphnia dubia) and, secondly, by evaluating the responses of biotransformation systems and multidrug resistance-associated proteins (MRP1/MRP2) using the Poeciliopsis lucida hepatocellular carcinoma 1 (PLHC-1) fish hepatic cell line...
January 2018: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28745761/study-of-the-simulated-sunlight-photolysis-mechanism-of-ketoprofen-the-role-of-superoxide-anion-radicals-transformation-byproducts-and-ecotoxicity-assessment
#11
Yingfei Wang, Wen Deng, Fengliang Wang, Yuehan Su, Yiping Feng, Ping Chen, Jingshuai Ma, Haiying Su, Kun Yao, Yang Liu, Wenying Lv, Guoguang Liu
The aim of this study was to investigate the photolysis mechanism of ketoprofen (KET) under simulated sunlight. The results demonstrated that the photolysis of KET aligned well with pseudo first-order kinetics. Radical scavenging experiments and dissolved oxygen experiments revealed that the superoxide anion radical (O2 ˙- ) played a primary role in the photolytic process in pure water. Bicarbonate slightly increased the photodegradation of KET through generating carbonate radicals, while DOM inhibited the photolysis via both attenuating light and competing radicals...
September 20, 2017: Environmental Science. Processes & Impacts
https://www.readbyqxmd.com/read/28732306/photostability-testing-using-online-reactor-hplc-hyphenation-and-mass-spectrometric-compound-identification-illustrated-by-ketoprofen-as-model-compound
#12
Jaber Assaf, Diego Zulkiewicz Gomes, Bernhard Wuest, Maria Kristina Parr
Investigations on the photochemical stability of pharmaceutical substances are mandatory in drug development and licensing as photo-induced degradation of an active pharmaceutical ingredient (API) may not only lead to decreased API concentrations but also to toxic or reactive products. Thus, the US Food and Drug Administration (FDA) and the International Council for Harmonisation of Technical Requirements for Pharmaceuticals for Human Use (ICH) issued Guidance for Industry Q1B "Photostability Testing of New Drug Substances and Products" for testing of pure but also packed drugs...
October 25, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28718961/photodegradation-kinetics-transformation-and-toxicity-prediction-of-ketoprofen-carprofen-and-diclofenac-acid-in-aqueous-solutions
#13
Jian Li, Li-Yun Ma, Lu-Shuang Li, Li Xu
Photodegradation of 3 commonly used nonsteroidal anti-inflammatory drugs, ketoprofen, carprofen, and diclofenac acid, was conducted under ultraviolet (UV) irradiation. The kinetic results showed that the 3 pharmaceuticals obeyed the first-order reaction with decreasing rate constants of 1.54 × 10-4 , 5.91 × 10-5 , and 7.78 × 10-6  s-1 for carprofen, ketoprofen, and diclofenac acid, respectively. Moreover, the main transformation products were identified by ion-pair liquid-liquid extraction combined with injection port derivatization-gas chromatography-mass spectrometry and high-performance liquid chromatography-quadrupole-time of flight mass spectrometric analysis...
December 2017: Environmental Toxicology and Chemistry
https://www.readbyqxmd.com/read/28635050/prediction-of-sustained-fetal-toxicity-induced-by-ketoprofen-based-on-pk-pd-analysis-using-human-placental-perfusion-and-rat-toxicity-data
#14
Shingo Tanaka, Takeshi Kanagawa, Kazuo Momma, Satoko Hori, Hiroki Satoh, Takeshi Nagamatsu, Tomoyuki Fujii, Tadashi Kimura, Yasufumi Sawada
AIM: We encountered a case of fetal toxicity due to ductus arteriosus (DA) constriction in a 36-week pregnant woman who had applied multiple ketoprofen patches. The aim of the present study was to present the case and develop a model to predict quantitatively the fetal toxicity risk of transdermal administration of ketoprofen. METHODS: Human placenta perfusion studies were conducted to estimate transplacental pharmacokinetic (PK) parameters. Using a developed model and these parameters, human fetal plasma concentration profiles of ketoprofen administered to mothers were simulated...
November 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28480594/nanostructured-dpa-mpc-dpa-triblock-copolymer-gel-for-controlled-drug-release-of-ketoprofen-and-spironolactone
#15
Bahaa Azmy, Guy Standen, Petra Kristova, Andrew Flint, Andrew L Lewis, Jonathan P Salvage
OBJECTIVE: Uncontrolled rapid release of drugs can reduce their therapeutic efficacy and cause undesirable toxicity; however, controlled release from reservoir materials helps overcome this issue. The aims of this study were to determine the release profiles of ketoprofen and spironolactone from a pH-responsive self-assembling DPA-MPC-DPA triblock copolymer gel and elucidate underlying physiochemical properties. METHODS: Drug release profiles from DPA50 -MPC250 -DPA50 gel (pH 7...
May 7, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28381310/biochemical-histopathologic-physiologic-and-behavioral-effects-of-nonsteroidal-antiinflammatory-drugs-in-rainbow-trout-oncorhynchus-mykiss
#16
Amy L Rizzo, Gregory A Wooster, Luce E Guanzini, Christine M Peterson, Karryssas Fenderson, Hollis N Erb, Paul R Bowser, Mary E Martin
Because the number of fish being used in research is increasing rapidly, evaluating the analgesic and pathologic effects of NSAID in fish is essential. To determine the biochemical, histopathologic, physiologic and behavioral effects of 3 NSAID, 48 rainbow trout underwent anesthesia with tricaine methanesulfonate and exploratory celiotomy and were randomly assigned to receive flunixin (0.5 mg/kg IM), ketorolac (0.5 mg/kg IM), ketoprofen (2 mg/kg IM), or saline. Clinical pathologic variables were assessed 1 wk before surgery and 48 h after surgery...
March 1, 2017: Comparative Medicine
https://www.readbyqxmd.com/read/28285173/peptide-dendrimer-conjugates-of-ketoprofen-synthesis-and-ex-vivo-and-in-vivo-evaluations-of-passive-diffusion-sonophoresis-and-iontophoresis-for-skin-delivery
#17
Aswathi R Hegde, Prarthana V Rewatkar, Jyothsna Manikkath, Karnaker Tupally, Harendra S Parekh, Srinivas Mutalik
The aim of this study was to evaluate skin delivery of ketoprofen when covalently tethered to mildly cationic (2+ or 4+ ) peptide dendrimers prepared wholly by solid phase peptide synthesis. The amino acids glycine, arginine and lysine formed the dendrimer with ketoprofen tethered either to the lysine side-arm (Nε ) or periphery of dendrimeric branches. Passive diffusion, sonophoresis- and iontophoresis-assisted permeation of each peptide dendrimer-drug conjugate (D1-D4) was studied across mouse skin, both in vitro and in vivo...
May 1, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28266283/biochemical-histopathologic-physiologic-and-behavioral-effects-of-nonsteroidal-antiinflammatory-drugs-in-rainbow-trout-oncorhynchus-mykiss
#18
Amy L Rizzo Gregory A Wooster Luce E Guanzini Christine M Peterson Karryssa S Fenderson Hollis N Erb Paul R Bowser And Mary E Martin
Because the number of fish being used in research is increasing rapidly, evaluating the analgesic and pathologic effects of NSAIDin fish is essential. To determine the biochemical, histopathologic, physiologic and behavioral effects of 3 NSAID, 48 rainbow trout underwent anesthesia with tricaine methanesulfonate and exploratory celiotomy and were randomly assigned to receive flunixin(0.5 mg/kg IM), ketorolac (0.5 mg/kg IM), ketoprofen (2 mg/kg IM), or saline. Clinical pathologic variables were assessed 1 wk before surgery and 48 h after surgery...
March 6, 2017: Comparative Medicine
https://www.readbyqxmd.com/read/28254731/remediation-of-a-mixture-of-analgesics-in-a-stirred-tank-photobioreactor-using-microalgal-bacterial-consortium-coupled-with-attempt-to-valorise-the-harvested-biomass
#19
Maha M Ismail, Tamer M Essam, Yasser M Ragab, Abo El-Khair B El-Sayed, Fathia E Mourad
An artificial microalgal-bacterial consortium was used to remediate a mixture of analgesics (ketoprofen, paracetamol and aspirin) in a stirred-tank photobioreactor. A hydraulic retention time (HRT) of 3days supported poor treatment because of the formation of p-aminophenol (paracetamol toxic metabolite). Increasing the HRT to 4days enhanced the bioremediation efficiency. After applying an acclimatization regime, 95% removal of the analgesics mixture, p-aminophenol and COD reduction were achieved. However, shortening the HRT again to 3days neither improved the COD reduction nor ketoprofen removal...
May 2017: Bioresource Technology
https://www.readbyqxmd.com/read/28163223/influence-of-peptide-dendrimers-and-sonophoresis-on-the-transdermal-delivery-of-ketoprofen
#20
Jyothsna Manikkath, Aswathi R Hegde, Guruprasad Kalthur, Harendra S Parekh, Srinivas Mutalik
The aim of this study was to determine the individual and combined effects of peptide dendrimers and low frequency ultrasound on the transdermal permeation of ketoprofen. Arginine terminated peptide dendrimers of varying charges (4(+), 8(+) and 16(+), named as A4. A8 and A16 respectively) were synthesized and characterized. Ketoprofen was subjected to passive, peptide dendrimer-assisted and sonophoretic permeation studies (with and without dendrimer application) across Swiss albino mouse skin, both in vitro and in vivo...
April 15, 2017: International Journal of Pharmaceutics
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