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Igor V Ukrainets, Lidiya A Petrushova, Svitlana V Shishkina, Lina A Grinevich, Galina Sim
In order to obtain and then test pharmocologically any possible conformers of the new feasible analgesic N-benzyl-4-hydroxy-1-methyl-2,2-dioxo-1H-2λ⁶,1-benzothiazine-3-carboxamide, its 4-O-sodium salt was synthesized using two methods. X-ray diffraction study made possible to determine that, depending on the chosen synthesis conditions, the above-mentioned compound forms either monosolvate with methanol or monohydrate, where organic anion exists in the form of three different conformers. Pharmacological testing of the two known pseudo-enantiomeric forms of the original N-benzylamide and of the two solvates of its sodium salt was performed simultaneously under the same conditions and in equimolar doses...
October 19, 2016: Scientia Pharmaceutica
Ahmad Ainurofiq, Syaiful Choiri, Muhamad Ali Azhari, Chaterin Romauli Siagian, Bambang Budi Suryadi, Fea Prihapsara, Sholichah Rohmani
Purpose: The aim of this research was to formulate and develop an orally disintegrating tablet (ODT) that incorporated a MEL/β-CD complex, using a quality by design (QbD) approach to enhance solubility and drug release. Methods: Multiple regression linear analysis was conducted to develop the kneading process and ODT formulation. Mixing time and amount of solvent were used as independent variables in kneading process optimisation, while the superdisintegrants were used to obtain the desired formulation. Fourier transform infrared spectroscopy and differential scanning calorimetry were performed for complex characterization...
September 2016: Advanced Pharmaceutical Bulletin
J A Van Heerden, J R Burger, J J Gerber
BACKGROUND: Prescribing for older patients is a well-recognised problem, and inappropriate items are prescribed frequently. Several tools and criteria are available to promote rational prescribing in older patients. OBJECTIVE: To determine the prevalence of potentially inappropriate prescriptions (PIPs) in older South African patients. METHODS: A retrospective drug utilisation review was conducted using medicine claims data over a 1-year period...
September 9, 2016: South African Medical Journal, Suid-Afrikaanse Tydskrif Vir Geneeskunde
Daniel V Fredholm, Natalie D Mylniczenko, Butch KuKanich
Critically evaluating the pharmacokinetic behavior of a drug in the body provides crucial information about how to effectively treat a patient. Pharmacokinetic studies that exist in fish have primarily focused on drugs used to treat infectious disease, with minimal attention given to analgesic drugs. The objective of this study was to determine the pharmacokinetics of meloxicam (1 mg/kg) in Nile tilapia ( Oreochromis niloticus ) (n = 12). A single dose of meloxicam was administered either i.v. or i.m. Blood samples were obtained at predetermined times after drug injection...
September 2016: Journal of Zoo and Wildlife Medicine: Official Publication of the American Association of Zoo Veterinarians
Mujgan Gungor Hatipoglu, Sermet Inal, Sahin Kabay, Muhammet Kasim Cayci, Ayşenur Deger, Halil Isa Kuru, Sayit Altikat, Gizem Akkas
THE AIM: The aim of this study was to investigate the effect of dexketoprofen trometamol, meloxicam, diclofenac sodium on any untreated alveolar bone when they are used as drugs for another indication. MATERIALS AND METHODS: Twenty eight male Spraque-Dawley rats were randomized into four groups as dexketoprofen trometamol (Group I), meloxicam (Group II), diclofenac sodium (Group III) and control group. Nonsteroidal anti-inflammatory drugs (NSAID) were administered after a fibula fracture for 10 days...
December 2015: Acta Stomatologica Croatica
Yoshihiko Uehara, Yasuhiko Murata, Soichiro Shiga, Yoshio Hosoi
BACKGROUND: It is well known that radiation exposure to the heart and the use of non-steroidal anti-inflammatory drugs (NSAIDs) increase the risk of myocardial infarction (MI). Some NSAIDs are also known to act synergistically with ionizing radiation and have radio-sensitizing effects in radiotherapy. These evidences suggest that NSAIDs may affect the risk of MI after radiation exposure to the heart. In the present study, we investigated effects of NSAIDs on radiation-induced expression of cell adhesion molecules and COX-2, which are associated with inflammation and an increased risk of MI, in human endothelial cells...
October 28, 2016: Biochemical and Biophysical Research Communications
Benonio T Villalba, Francine R Ianiski, Ane G Vogt, Mikaela P Pinz, Angélica S Reis, Rodrigo A Vaucher, Mauro P Soares, Ethel A Wilhelm, Cristiane Luchese
This study determined whether meloxicam in nanocapsules modifies stomach and liver damage caused by free meloxicam in mice. Male Swiss mice were treated with blank nanocapsules or meloxicam in nanocapsules or free meloxicam (10 mg/kg, intragastrically, daily for five days). On the seventh day, blood was collected to determine biochemical markers (glutamic oxaloacetic transaminase, glutamic pyruvic transaminase, total bilirubin, unconjugated bilirubin, albumin and alkaline phosphatase). Stomachs and livers were removed for histological analysis...
September 21, 2016: Regulatory Toxicology and Pharmacology: RTP
M S Herskin, P Di Giminiani, K Thodberg
In many countries, piglets are tail docked to prevent tail biting. The aim of this study was 1) to evaluate the efficacy of a local anaesthetic and/or NSAID to reduce pain caused by tail docking; and 2) to examine interactions with docking length. This was examined in 295 piglets docked by hot iron cautery 2-4days after birth and based on behaviour during docking as well as the following 5h. The study involved three main factors: local anaesthetic (Lidocain), NSAID (Meloxicam) and docking length. Either 100%, 75%, 50% or 25% of the tails were left on the body of the piglets...
October 2016: Research in Veterinary Science
Alexandra Mikó, Nóra Füredi, Judit Tenk, Ildikó Rostás, Szilvia Soós, Margit Solymár, Miklós Székely, Márta Balaskó, Susanne M Brunner, Barbara Kofler, Erika Pétervári
Hypothalamic neuropeptides influence the main components of energy balance: metabolic rate, food intake, body weight as well as body temperature, by exerting either an overall anabolic or catabolic effect. The contribution of alarin, the most recently discovered member of the galanin peptide family to the regulation of energy metabolism has been suggested. Our aim was to analyze the complex thermoregulatory and food intake-related effects of alarin in rats. Adult male Wistar rats received different doses of alarin (0...
September 5, 2016: Neuropeptides
Edin Selimović, Lejla Ibrahimagić-Šeper, Ibrahim Šišić, Suad Sivić, Senad Huseinagić
Aim To assess prevention and reduction of trismus after surgically extracted impacted mandibular third molars with individual and combined therapy with corticosteroids and anti-inflammatory analgesics. Methods The research included 60 randomly selected patients (3 groups) attended to the Dental Oral Surgery of the Public Institution Healthcare Center Zenica during the period January-December 2008. Patients of both genders, 18-45 years of age, were presented without pain and other inflammatory symptoms at the time of surgery...
February 1, 2017: Medicinski Glasnik
Eniko Borbas, Balint Sinko, Oksana Tsinman, Konstantin Tsinman, Eva Kiserdei, Balazs Demuth, Attila Balogh, Brigitta Bodak, Andras Domokos, Gergo Dargo, György T Balogh, Zsombor K Nagy
The aim of this study was to investigate the impact of formulation excipients and solubilizing additives on dissolution, supersaturation and membrane transport of an active pharmaceutical ingredient (API). When a poorly water-soluble API is formulated to enhance its dissolution, additives, such as surfactants, polymers and cyclodextrins have an effect not only on dissolution profile, but also on the measured physicochemical properties (solubility, pKa, permeability) of the drug while the excipient is present, therefore also affect the driving force of membrane transport...
September 9, 2016: Molecular Pharmaceutics
A Montesinos, M Ardiaca, J A Gilabert, C Bonvehí, J Oros, T Encinas
Meloxicam is a nonsteroidal anti-inflammatory drug commonly used in avian species. In this study, the pharmacokinetic parameters for meloxicam were determined following single intravenous (i.v.), intramuscular (i.m.) and oral (p.o.) administrations of the drug (1 mg/kg·b.w.) in adult African grey parrots (Psittacus erithacus; n = 6). Serial plasma samples were collected and meloxicam concentrations were determined using a validated high-performance liquid chromatography assay. A noncompartmental pharmacokinetic analysis was performed...
September 6, 2016: Journal of Veterinary Pharmacology and Therapeutics
Mohamed M Katary, Chelsey Pye, Ahmed A Elmarakby
The pro-inflammatory cyclooxygenase (COX)-derived prostaglandins and the anti-inflammatory cytochrome P450 epoxygenase-derived epoxyeicosatrienoic acids (EETs) play an important role in the regulation of renal injury. The current study examined whether COX inhibition augments the reno-protective effects of increased EETs levels via inhibiting EETs degradation by soluble epoxide hydrolase (sEH) in diabetic rats. Streptozotocin (50mg/kg, i.v) was used to induce diabetes in male Sprague Dawley rats. Rats were then divided into 5 groups (n=6-8); control non diabetic, diabetic, diabetic treated with the sEH inhibitor trans-4-[4-(3-adamantan-1-yl-ureido)-cyclohexyloxy]-benzoic acid (t-AUCB), diabetic treated with the COX inhibitor meloxicam and diabetic treated with meloxicam plus t-AUCB for 2 months...
September 2, 2016: Prostaglandins & Other Lipid Mediators
Yuuichi Sakurai, Madoka Shiino, Sayako Horii, Hiroyuki Okamoto, Koki Nakamura, Akira Nishimura, Yukikuni Sakata
BACKGROUND: Gastroprotective agents are recommended for patients receiving low-dose aspirin (LDA) or nonsteroidal anti-inflammatory drugs (NSAIDs). Vonoprazan is a potassium-competitive acid blocker recently approved for the prevention of peptic ulcer recurrence in patients receiving LDA or NSAIDs. METHODS: This phase 2, open-label, single-center study in healthy Japanese males evaluated drug-drug interactions between vonoprazan 40 mg and LDA (100 mg) or NSAIDs [loxoprofen sodium (60 mg), diclofenac sodium (25 mg), or meloxicam (10 mg)] and vice versa...
August 31, 2016: Clinical Drug Investigation
Kathleen Yin, Jennifer R Deuis, Richard J Lewis, Irina Vetter
Burn injury is a cause of significant mortality and morbidity worldwide and is frequently associated with severe and long-lasting pain that remains difficult to manage throughout recovery. We characterised a mouse model of burn-induced pain using pharmacological and transcriptomic approaches. Mechanical allodynia elicited by burn injury was partially reversed by meloxicam (5 mg/kg), gabapentin (100 mg/kg) and oxycodone (3 and 10 mg/kg), while thermal allodynia and gait abnormalities were only significantly improved by amitriptyline (3 mg/kg) and oxycodone (10 mg/kg)...
2016: Molecular Pain
E van de Water, M Oosterlinck, M Dumoulin, N M Korthagen, P R van Weeren, J van den Broek, H Everts, F Pille, D A van Doorn
BACKGROUND: Nutraceuticals are often used in the management of equine osteoarthritis, but scientific evidence of their efficacy is lacking. OBJECTIVES: To study the preventive effects of two new nutraceuticals after the experimental induction of synovitis in comparison with positive and negative control treatments. STUDY DESIGN: Blinded, controlled, randomised experiment. METHODS: Twenty-four healthy Standardbred horses were randomly allocated to supplement AT (multi-ingredient, 28 days), supplement HP (collagen hydrolysate, 60 days), meloxicam (4 days) or placebo (60 days)...
August 24, 2016: Equine Veterinary Journal
Vivian Leung, Emily Zhang, Daniel Sj Pang
Rodent grimace scales have been recently validated for pain assessment, allowing evaluation of facial expressions associated with pain. The standard scoring method is retrospective, limiting its application beyond pain research. This study aimed to assess if real-time application of the Rat Grimace Scale (RGS) could reliably and accurately assess pain in rats when compared to the standard method. Thirty-two male and female Sprague-Dawley rats were block randomized into three treatment groups: buprenorphine (0...
2016: Scientific Reports
Chrystalleni Hadjicharalambous, Vasileia Ismini Alexaki, Kalliopi Alpantaki, Maria Chatzinikolaidou
OBJECTIVES: Non-steroidal anti-inflammatory drugs (NSAIDs), used in the treatment of musculoskeletal pathologies, have been associated with impaired bone healing, possibly through inhibition of osteogenic differentiation. The adipose tissue (AT) is regarded as an attractive source of stromal cells for autologous cell transplantation in the bone. The effects of NSAIDs on human AT-derived stromal cells (hADSCs) are unknown. METHODS: We examined the effect of several NSAIDs including meloxicam, parecoxib, lornoxicam, diclofenac and paracetamol on the proliferation of hADSCs by means of the PrestoBlue(®) viability assay, and the osteogenic differentiation capacity of hADSCs by means of the alkaline phosphatase (ALP) activity, calcium deposition by alizarin red staining and osteogenic gene expression by semi-quantitative PCR...
August 14, 2016: Journal of Pharmacy and Pharmacology
Jiahong Gang, Yiqun Mi, Huamin Wang
OBJECTIVE: To compare the clinical efficacy on knee osteoarthritis (KOA) at the early and middle stage between electroacupuncture (EA) and meloxicam. METHODS: Ninety patients of KOA at the early and middle stage were randomized into an EA group and a meloxicam group, 45 cases in each one. In the EA group, EA was applied to Dubi (ST 35), Neixiyan (EX-LE 4), Liangqiu (ST 34), Heding (EX-LE 2), Xuehai (SP 10), Yan- glingquan (GB 34) and Zusanli (ST 36); the needles were retained for 20 min and EA was applied once every two days...
May 2016: Zhongguo Zhen Jiu, Chinese Acupuncture & Moxibustion
Amy L Miller, Gemma L Kitson, Benjamin Skalkoyannis, Paul A Flecknell, Matthew C Leach
Mice used in biomedical research should have pain reduced to an absolute minimum through refinement of procedures or by the provision of appropriate analgesia. Vasectomy is a common and potentially painful surgical procedure carried out on male mice to facilitate the production of genetically modified mice. The aim of our study was to determine if 0.05 mg/kg buprenorphine would ameliorate pain associated changes following abdominal vasectomy and to determine if the mouse grimace scale is an appropriate tool for the assessment of pain in this model...
August 2016: Applied Animal Behaviour Science
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