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Ketoprofen toxic

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)...
March 7, 2018: Environmental Pollution
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...
February 8, 2018: Postgraduate Medicine
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
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
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
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
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...
August 10, 2017: Environmental Toxicology and Chemistry
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
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
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
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
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
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
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...
March 8, 2017: European Journal of Pharmaceutical Sciences
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
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
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
Yao Lv, Qixia Pan, S W Annie Bligh, Heyu Li, Huanling Wu, Qingqing Sang, Li-Min Zhu
In this work, a smart drug delivery system of core-sheath nanofiber is reported. The core-sheath nanofibers were prepared with thermoresponsive poly-(N-isopropylacrylamide) (as core) and hydrophobic ethyl cellulose (as sheath) by coaxial electrospinning. Analogous medicated fibers were prepared by loading with a model drug ketoprofen (KET). The fibers were cylindrical without phase separation and have visible core-sheath structure as shown by scanning and transmission electron microscopy. X-ray diffraction patterns demonstrated the drug with the amorphous physical form was present in the fiber matrix...
May 2017: Journal of Pharmaceutical Sciences
Aleksandar Pantovic, Mihajlo Bosnjak, Katarina Arsikin, Milica Kosic, Milos Mandic, Biljana Ristic, Jelena Tosic, Danica Grujicic, Aleksandra Isakovic, Nikola Micic, Vladimir Trajkovic, Ljubica Harhaji-Trajkovic
We investigated the role of the intracellular energy-sensing AMP-activated protein kinase (AMPK)/mammalian target of rapamycin (mTOR) pathway in the in vitro antiglioma effect of the cyclooxygenase (COX) inhibitor indomethacin. Indomethacin was more potent than COX inhibitors diclofenac, naproxen, and ketoprofen in reducing the viability of U251 human glioma cells. Antiglioma effect of the drug was associated with p21 increase and G2M cell cycle arrest, as well as with oxidative stress, mitochondrial depolarization, caspase activation, and the induction of apoptosis...
February 2017: International Journal of Biochemistry & Cell Biology
Yu-Ting Cheng, Chi-Cheng Lu, Gow-Chin Yen
The gastrointestinal (GI) mucosa provides the first protective barrier for digested food and xenobiotics, which are easily attacked by toxic substances. Nonsteroidal anti-inflammatory drugs, including aspirin, diclofenac, indomethacin, and ketoprofen, are widely used in clinical medicine, but these drugs may cause oxidative stress, leading to GI damage such as ulcers. Lansoprazol, omeprazole, and other clinical drugs are widely used to treat duodenal and gastric ulcers and have been shown to have multiple biological functions, such as antioxidant activity and the ability to upregulate antioxidant enzymes in vivo...
June 2017: Molecular Nutrition & Food Research
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