Estudio comparativo de una asociación de diclofenac, betametasona y vitamina b12 (blokium b12®) con diclofenac (sin asociar) en el tratamiento de patología dolorosa de columna con compromiso neural / COMPARATIVE STUDY OF AN ASSOCIATION OF DICLOFENAC, BETAMETASONE AND VITAMIN B12 (BLOKIUM B12®) WITH DICLOFENAC (WITHOUT ASSOCIATION) IN THE TREATMENT OF PAINFUL SPINE PATHOLOGY WITH NEURAL COMMITMENT

El dolor lumbar bajo y el dolor cervical con o sin irradiación son causas muy comunes de consulta a los médicos generalistas en los países desarrollados. La discopatía aguda y el dolor por estenosis del canal espinal son los diagnósticos más frecuentes. La postura tradicional ha sido la de administrar antiinflamatorios no esteroideos (AINES) para estas lumbalgias o cervicalgias agudas. Cuando existe irradiación neural por compresión radicular es usual asociar al AINE un corticoide a baja dosis, así como un antineurítico, para lograr un mejor resultado. Con el objeto de documentar la utilidad de esta práctica habitual, efectuamos en 142 pacientes ambulatorios un estudio multicéntrico randomizado que compara la efectividad y la tolerancia de una asociación a dosis fija de diclofenac, betametasona y cianocobalamina administrada por vía oral versus la administración de diclofenac como monofármaco en el tratamiento de la patología dolorosa de la columna lumbar y cervical asociada a compresión neural. La asociación demostró ser más eficaz en controlar el dolor y mejorar la funcionalidad de los pacientes que la administración de diclofenac en forma aislada y se asoció a escasos efectos colaterales, principalmente digestivos

Low back pain and neck pain with or without radiation are very common causes of consultation with general practitioners in developed countries. Acute discopathy and pain due to spinal canal stenosis are the most frequent diagnoses. The traditional approach has been to administer non-steroidal antiinflammatory drugs (NSAIDs) for these acute low back or cervical pain. When there is neural radiation due to root compression, it is usual to associate a low-dose corticosteroid with the NSAID, as well as an antineuritic, to achieve a better result. In order to document the usefulness of this routine practice, we conducted a randomized multicenter study in 142 outpatients that compared the effectiveness and tolerance of a fixed-dose combination of diclofenac, betamethasone, and cyanocobalamin administered orally versus the administration of diclofenac as Monopharmaceutical in the treatment of painful pathology of the lumbar and cervical spine associated with neural compression. The association proved to be more effective in controlling pain and improving the functionality of patients than the administration of diclofenac in isolation and was associated with few side effects, mainly digestive

Systemic absortion and adverse effects of topical ocular use of ketorolac tromethamine and sodium diclofenac in New Zealand rabbits for 90 days / Absorção sistêmica e efeitos adversos do uso tópico ocular por 90 dias de cetorolaco de trometamina e diclofenacode sódio em coelhos da raça Nova Zelândia

The effect of the systemic absorption of 0.1% diclofenac sodium (DS) eyedrop was compared to that of 0.5% ketorolac tromethamine (KT) in female New Zealand white rabbits treated on both eyes three times a day for 90 days. The rabbits were divided in three groups of six animals (n= 18): KT group, DS group, and control (Co) group, in which saline (0.9% NaCl) solution was instilled. Water and food consumption were measured daily, clinical examination was performed weekly, and blood samples were collected every 30 days for laboratory examination. The plasma was analyzed for the presence of KT and DS by solid-phase extraction (SPE) associated with mass spectrometry (MS). Systemic absorption of these drugs was confirmed by SPE-MS, allowing their separation and identification in the plasma. At the end of the treatment, the animals were euthanized and necropsied, and no macroscopic or microscopic changes were found. This observation confirmed the laboratory results, which were within normal reference standards for the species. According to the results obtained, it can be concluded that treatment with eyedrops containing KT and DS for 90 days in healthy rabbits does not cause adverse systemic effects.(AU)

Comparou-se o efeito da absorção sistêmica do colírio de diclofenaco de sódio 0,1% (DS) em relação ao de cetorolaco de trometamina 0,5% (CT) em coelhas da raça Nova Zelândia, tratadas nos dois olhos, três vezes ao dia, por 90 dias. As coelhas foram separadas em três grupos de seis animais (n=18): grupo CT, grupo DS e grupo controle (Co), no qual foi instilada solução fisiológica (NaCl 0,9%). Os consumos de água e ração foram mensurados diariamente, os exames clínicos foram realizados semanalmente e o sangue foi coletado a cada 30 dias para realização de exames laboratoriais. O plasma foi analisado para detectar a presença de CT e DS por extração em fase sólida (SPE) associada à espectrometria de massas (MS). A absorção sistêmica desses fármacos foi confirmada por SPE-MS, permitindo sua separação e identificação no plasma. Ao final do tratamento, os animais foram eutanasiados e necropsiados, e não foram encontradas alterações macroscópicas ou microscópicas. Essa observação confirmou os resultados laboratoriais, que estavam dentro dos padrões de referência para a espécie. De acordo com os resultados obtidos, pode-se concluir que o tratamento com colírio contendo KT e DS, por 90 dias, em coelhos saudáveis, não causa efeitos adversos sistêmicos.(AU)

A study on the toxic effect of different doses of diclofenac sodium on the development of the kidney in the postnatal period / Estudio sobre el efecto tóxico de diferentes dosis de diclofenaco sódico en el desarrollo del riñón en el período postnatal

The toxic effects of different doses of diclofenac sodium (DS) on the kidney on the postnatal period (0-7 days) by morphometrical and immunohistochemical methods were investigated. For this purpose, 15 female adult wistar albino rats were used and divided into 5 main groups. Group Ia served as normal control, physiologic group Ib received normal saline, group II received low dose (3.9 mg/kg), group III received medium dose (9 mg/kg) and group IV received high dose (18 mg/kg). Male offspring's from 0-7 days after birth were used in this study. On the 8th day of postnatal life, all animals were anesthetized. Then, the kidney samples were analyzed. Haematoxylin and eosin staining showed degeneration and necrosis, apparent atrophy of the glomeruli, mononuclear cell infiltration, congested vessels, increased fibrous tissue and distortion of the proximal convoluted tubules with interruption of the brush margin of the DS treated group. Increased level of Caspase-3 and upregulation of TNF-α with different doses of DS. In light of our findings, DS may lead to adverse effects that are dose-dependent in the prenatal subjected kidney to this drug.

Se investigaron los efectos tóxicos de diferentes dosis de diclofenaco sódico (DS) en el riñón de ratas, durante su período postnatal (0-7 días), por métodos morfométricos e inmunohistoquímicos. Para este propósito, se utilizaron 20 crías macho, de ratas Wistar albinas, y se dividieron en 5 grupos principales. El grupo Ia sirvió como control normal, el grupo fisiológico Ib recibió solución salina normal, el grupo II recibió una dosis baja de DS (3,9 mg/kg), el grupo III recibió una dosis media de DS (9 mg/kg) y el grupo IV recibió una dosis alta de DS (18 mg/kg). Se administraron los medicamentos de 0 a 7 días después del nacimiento de las ratas. En el octavo día de vida postnatal, todos los animales fueron sacrificados. Luego, se analizaron las muestras de riñón. Mediante hematoxilina-eosina se evidenció degeneración y necrosis, aparente atrofia de los glomérulos, infiltración de células mononucleares, vasos congestionados, aumento del tejido fibroso y distorsión de los túbulos contorneados proximales, con interrupción del margen en cepillo del grupo tratado con DS. Se detectó un aumento del nivel de caspasa-3 y regulación al alza de TNF-α con diferentes dosis de DS. A la luz de nuestros hallazgos, la DS puede provocar efectos adversos en el riñón, que dependen de la dosis de este medicamento administrada en el período posnatal.

The effects of bioadhesive hyaluronic acid gel versus diclofenac after surgical removal of impacted wisdom teeth

Surgical extraction of impacted lower wisdom teeth is a frequent minor intraoral surgical process. It is regularly linked with aching and postoperative consequences as pain and swelling. The aim of this study is to evaluate the efficacy of two methods in reducing swelling and pain subsequent to the removal of impacted wisdom teeth. This randomized study incorporated 20 patients with impacted wisdom teeth of different surgical complexity. Topical hyaluronic acid gel 2g/2ml with aloe vera (Kin®Care) was given to the patients to be applied to the surgical area three times a day, or diclofenac sodium tablet 50mg (Voltaren®) to be taken every eight hours, for one week. Swelling was estimated using a strip gauge technique, and pain with a visual analogue scale. Evaluations were made on day one of surgical treatment and on 72hrs and one week later. Statistically no significant differences were identified regarding the swelling and pain values between the two treatment groups on the third and seventh day after surgery. Hyaluronic acid gel was as efficient as diclofenac tablets in reducing the two parameters. The use of hyaluronic acid may be advantageous in medically compromised patient such as those with hypertension, chronic asthma, gastric ulcers or in those with any contraindications to using non-steroidal anti-inflammatory drugs, or in pregnant patients to reduce pain and swelling subsequent to impacted wisdom teeth surgery.

Comparative study on the efficacy of non-steroidal, steroid and non-use of anti-inflammatory in the treatment of acute epidemic conjunctivitis

Abstract Purpose To evaluate the effects of prednisolone against sodium diclofenac both with ciprofloxacin compared to artificial tears on the symptoms and signs of acute viral conjunctivitis. Methods Study included 37 patients diagnosed with acute conjunctivitis and distributed by three groups: A (1% prednisolone acetate + ciprofloxacin (0.3%); B (Sodium diclofenac (0.1%) + ciprofloxacin (0.3%) and C (artificial tears + ciprofloxacin (0.3%). Patients received medication 6/6 hours daily. Signs and symptoms (e.g. lacrimation, burning, photophobia, etc.) were scored at baseline and on the first, third, fifth and seventh days and in the end of treatment using a standardized questionnaire and slit lamp anterior segment examination. Results All three groups demonstrated an improvement in the signs and symptoms of conjunctivitis in their follow-up visits. There was no significant difference in symptom and sign scores between Group A and B and B and C in the study visits ( p >0.05). However, the comparison between groups A and C showed a clinical trend (p=0.05) on third evaluation suggesting better clinical action using the corticosteroids. Conclusion The prednisolone acetate was not superior to the use of sodium diclofenac or artificial tears in relieving the signs and symptoms of viral conjunctivitis.

Anti-inflammatory and antinociceptive effects of phonophoresis in animal models: a randomized experimental study

The aim of this study was to evaluate the therapeutic effects of ultrasound (US)-mediated phonophoresis alone or in association with diclofenac diethylammonium (DCF) administered topically in animal models of inflammation. A pre-clinical, prospective, and randomized experimental study of quantitative and qualitative nature was carried out. Phonophoresis was performed using a therapeutic ultrasound apparatus in two distinct models of acute inflammation. Edema was induced by an intraplantar injection of carrageenan and measured by plethysmography. The Hargreaves test was used to evaluate the antinociceptive activity and investigate the action of phonophoresis on tumor necrosis factor (TNF)-α production. A histological analysis with hematoxylin-eosin was used to evaluate tissue repair, and the expression of COX-2 was determined by immunohistochemical analysis. At the peak of inflammatory activity (3 h), treatment with US, US+DCF, and DCF significantly reduced edema formation compared to the control group. Treatment with US+DCF was more effective than treatment with US alone at both analyzed times. In the analysis of the antinociceptive activity, the treatments significantly increased the latency time in response to the thermal stimulus. Histopathological analysis revealed a reduction of the inflammatory infiltrates and immunohistochemistry demonstrated that the association was effective in reducing COX-2 expression compared to the control group. The association of DCF with US produced anti-inflammatory and antinociceptive effects in rat models of inflammation, which may be associated with inhibition of COX-2 and TNF-α production.

Intrasound therapy: an effective alternative to sodium diclofenac phonophoresis in the management of mechanical chronic cervical spine pain

The efficacy of Sodium Diclofenac Phonophoresis (SDP) as an effective adjunct in the management of inflammation and pain has been established though its application entails complicated choices of treatment parameters. Intrasound Therapy (IST), acclaimed for its simplicity of operation has been reported to promote healing though no studies have been done on its effect in Chronic cervical spine pain (CCSP). The aim of this study was to determine if IST could be an effective therapeutic option to SDP as an adjunct in the management of CCSP. Forty seven (47) participants with CCSP that had definite diagnoses were randomly assigned into 3 groups. All participants had exercises and massage while in addition, group 1 had SDP and group 2 IST for 10 minutes each. Participants were treated for 40 minutes twice a week for 4 weeks and were evaluated for pain, Quality of life (QoL), disability and range of motion (ROM) of the cervical spine. Paired sample t-test was used to compare the outcome parameters in each group and data presented as Mean ± SEM with significance at p<0.05. IST and SDP significantly (p˂0.05) improved the clinical parametres compared with the control group and there were no significant (p ˃0.05) differences in clinical outcome between the IST and SDP groups. IST was as effective as SDP and considering its relative simplicity of operation could be an alternative therapeutic adjunct in the management of chronic cervical pain

Efficacy of lumiracoxib versus diclofenac sodium in pain control following extraction of impacted lower third molar / Eficacia de lumiracoxib frente a diclofenaco de sodio en el control del dolor después de la extracción de un tercer molar inferior impactado

The aim of this paper was to compare the efficacy of two different anti-inflammatory agents, Diclofenac (Deltaflogin®) and Lumiracoxib (Prexige®) in the control of postoperative pain that results from surgical removal of impacted lower third molars. Twenty adult patients from the Oral and Maxillofacial Surgery Division of the Araraquara Dentistry School, UNESP who presented bilateral impacted lower third molars were included in the study. Removal of the impacted teeth was performed in each side in different operative moments in a split mouth design for the study. The anti-inflammatory drugs evaluated were randomly administered on the first and second surgical procedures. The pain level was recorded using an analogical visual scale at 6, 24, 48 and 72 hours after surgical intervention. Both lumiracoxib 400 mg and diclofenac 100 mg are efficient for acute pain control after surgical removal of impacted lower third molars. However, lumiracoxib offered better pain control.

El objetivo de este trabajo fue comparar la eficacia de dos agentes antiinflamatorios distintos, Diclofenaco (Deltaflogin®) y Lumiracoxib (Prexige®) en el control del dolor postoperatorio resultante de la extracción quirúrgica de terceros molares inferiores impactados. Fueron incluídos, veinte pacientes adultos de la División de Cirugía Oral y Maxilofacial de la Escuela de Odontología de Araraquara, UNESP que presentaron terceros molares inferiores impactados. La extracción de los dientes impactados se realizó en distintos tiempos operatorios a cada lado en un diseño de estudio de boca dividida. Los antinflamatorios evaluados fueron administrados de forma aleatoria en el primer y segundo procedimento quirúrgico. El nivel de dolor se registró utilizando una escala visual análoga a las 6, 24, 48 y 72 horas después de la intervención. Ambos; lumiracoxib 400 mg y diclofenaco 100 mg son eficientes para el control del dolor agudo, después de la extracción quirúrgica de terceros molares inferiores impactados. Sin embargo, lumiracoxib ofreció mejor control del dolor.

Osseointegration of titanium implants anodized with and without fluoride in the electrolyte: a study in rats / Osteo-integración de implantes de titanio anodizado con y sin agregado de fluoruro en el electrolito: estudio en la rata

Based on the hypothesis that fluoride acts as a bone anabolic agent, the aim of this study was to measure in rats the osseointegration of implants (grade II titanium wire, 1 mm diameter, 4 mm long) submitted to anodic oxidation in 2 M phosphoric acid solution (control implants) or b) in 2 M phosphoric acid solution plus 0.2 M NaF (F-modified implants). Chemical composition of the implants surface was assessed by energy-dispersive X-ray spectroscopy. The surface of F-modified implants contained a 2.57% fluorine in weight. Adult male Sprague Dawley rats (300-350 g body weight) received two implants (in the femur and in the tibia, close to the knee) in each hind limb. Control and F-modified implants were inserted in the left and right hind limbs, respectively. Three weeks after surgery, the animals were sacrificed. The undecalcified bones were embedded in methylmetacrylate. Sections were obtained to measure two histomorphometric magnitudes: bone-toimplant contact (BIC) and bone volume in a defined volume of tissue around the implant (BV/TV). BIC was significantly increased on F-modified implants with respect to their controls (57.2%±3.3%, vs. 47.9±3.4, p<0.05). BV/TV did not differ significantly between F-modified and control implants (24.5±2.2% vs. 22.9±1.4, p=0.30). Profiles of the average gray pixel levels of pseudo3D images showed a greater roughness of F-modified implants respect to their controls (p<0.05). The relative contributions of surface roughness and its fluorine content to the osseointegration process requires further research. (AU)

Con la hipótesis de que el ión fluoruro actúa como anabólico sobre las células óseas, el objetivo de este trabajo fue determinar el grado de osteo-integración (en la rata) de implantes (alambre de titanio II, 1 mm de diámetro, 4 mm de largo) anodizados en solución de ácido fosfórico 2 M + NaF 0,2 M (implantes-F) comparados con implantes controles, anodizados en solución de ácido fosfórico 2 M. La composición química de la superficie de los implantes fue evaluada mediante el espectro de dispersión de rayos X producidos durante la observación en el microscopio electrónico de barrido. La superficie de los implantes-F contiene 2.57% de flúor. Ratas macho Sprague-Dawley recibieron dos implantes (en el fémur y en tibia, próximos a la rodilla). Los implantes-F y controles se insertaron en las patas izquierda y derecha respectivamente. En los cortes de hueso sin decalcificación previa se midió el contacto hueso-implante (BIC) y volumen óseo en un volumen definido de tejido (BV/TV). BIC fue significativamente mayor con los Implantes-F respecto de los controles (57,2±3,3% vs. 47,9±3,4, p<0,05). BV/TV no exhibió diferencias significativas entre implantes-F y controles (24,5±2,2% vs. 22,9±1,4, p=0,30). Los perfiles de los niveles de grises de los imágenes pseudo3D de las superficies de los implantes pusieron en evidencia la mayor rugosidad de los implantes-F respecto de los controles (p<0,05). Las contribuciones relativas de la rugosidad y del flúor en el proceso de osteo-integración requieren investigación adicional. (AU)

Efecto analgésico y sobre la neuroconducta de la interacción entre tramadol y diclofenaco en dosis escalonada en ratones / Analgesic and neurobehavioral effect of the interaction between Tramadol and Diclofenac in escalated doses in mice

Determinar el efecto sobre el dolor y el sistema nervioso de la interacción entre tramadol y diclofenaco, en dosis escalonadas. Materiales y métodos. Se utilizaron 60 ratones albinos, distribuidos en diez grupos; cuatro grupos fueron de interacción y recibieron VO tramadol 10 mg/Kg y diclofenaco en dosis escalonada (10, 15, 20 y 25 mg/Kg). Seis grupos recibieron VO tramadol, 10 mg/Kg; diclofenaco, 10 mg/Kg; diazepam, 25 mg/Kg; cafeína, 25 mg/Kg y agua destilada, 0,1 mL/10 g; este último grupo no recibió medicamentos. Las sustancias se administraron una hora antes de la inducción del dolor. Se emplearon la prueba de contorsiones abdominales, para evaluar el dolor, y la prueba de Irwin, para el sistema nervioso. Se evaluaron el porcentaje de inhibición de contorsiones abdominales, porcentaje de prolongación del periodo de latencia, número de contorsiones abdominales y período de latencia. Se aplicaron las pruebas ANOVA de una cola, Tukey y correlación de Pearson. Para la prueba de Irwin se aplicó la prueba de Fisher. Resultados. Los porcentajes de inhibición de las contorsiones abdominales fueron de 55,1%; 89,9%; 74,5% y 94,5% en los grupos de interacción 2, 4, 7 y 10, respectivamente, frente a 31,6% (tramadol), 19,4% (diclofenaco) y 4,8% (control). El período de latencia fue de 609,7; 891,2; 860,5 y 1100 segundos en los grupos de interacción 2, 4, 7 y 10, respectivamente, frente a 479,7 (tramadol), 281,8 (diclofenaco) y 475,7 segundos (control). La prueba de ANOVA demostró diferencias significativas (p < 0,05; IC 95%) con relación al porcentaje de inhibición de contorsiones y el periodo de latencia. La prueba de Irwin evidenció piloerección, sedación, aumento de la respiración, incoordinación motora y cola de Straub. Conclusiones. Se comprobó el efecto analgésico sinérgico de la coadministración de tramadol en dosis fija y diclofenaco en dosis escalonada...

Determine the effect on pain and nervous system of the interaction between tramadol and diclofenac, in escalating doses. Materials and methods. 60 albino mice, divided into ten groups were used; four groups were for interaction and they received tramadol VO 10 mg/Kg and diclofenac in staggered doses (10, 15, 20 and 25 mg/Kg). Six groups received tramadol 10 mg/Kg; diclofenac 10 mg/Kg; diazepam, 25 mg/ Kg; caffeine, 25 mg/Kg and distilled water, 0.1 mL/10 g; this last group received no medication. The substances were administered one hour before pain induction. Writhing test assessed the effect on pain and Irwin test evaluated the nervous system. The statistical validation of the writhing inhibition percentage, latency percentage, number of writhes and latency was performed using ANOVA one tail, Tukey and Pearson correlation. For Irwin test, Fisher's test was applied. Results. The percentage of writhing inhibition were 55.1%, 89.9%, 74.5% and 94.5% by interaction groups 2, 4, 7 and 10, respectively, versus 31.6% (tramadol), 19.4% (diclofenac) and 4.8% (control). The latency period was 609.7; 891.2; 860.5 and 1100 seconds by interaction groups 2, 4, 7 and 10, respectively, versus 479.7 (tramadol), 281.8 (diclofenac) and 475.7 seconds (control). ANOVA showed significant differences (p < 0.05; CI 95%) relative to the percent inhibition of contortions and the latency period. Irwin test showed piloerection, sedation, increased respiration, motor incoordination and Straub tail. Conclusions. Synergistic analgesic effect of co-administration of fixed dose tramadol and diclofenac dose escalation was found...

Novel approach of aceclofenac fast dissolving tablet

Fast disintegrating tablets [FDTs] have received ever increasing demand during the last decade, and the field has become a hastily growing area in the pharmaceutical industry. Upon introduction into the mouth, these tablets dissolve or disintegrate in the mouth in the absence of additional water for easy administration of active pharmaceutical ingredients. Aceclofenac, an NSAID, has been recommended orally for the treatment of bone and connective tissue disorder and thus the formulation of the same resulted in development of several FDT technologies. The present aim is to formulate a tablet which disintegrate and dissolve rapidly and give its rapid onset of action: analgesic, antipyretic and anti-inflammatory action. Besides, the conventional tablets also show poor patient compliance an attempt had been made to formulate for FDT of aceclofenac by using various super disintegrants like sodium starch glycolate, croscarmellose sodium and crosspovidone [polyplasdone XL] and PEG 6000 followed by novel technique. The tablets were evaluated for friability, hardness, weight variation, disintegration time, wetting time, in vitro dissolution studies and drug content studies. It was concluded that the batch which was prepared by using combination of crosspovidone and sodium starch glycolate as a super disintegrant shows excellent disintegration time, enhance dissolution rate, taste masking and hence lead to improve efficacy and bioavailability of drug

Quality evaluation and in vitro interaction studies between levofloxacin 250mg and diclofenac sodium 50mg tablets

Fluoroquinolones are broad-spectrum antibiotics, work against Gram-positive and Gram-negative bacteria and are a clinically proven option for many resistant infections. Among fluoroquinolones Levofloxacin works best against acute sinusitis, inflammation of the lower airways, acute exacerbation of chronic bronchitis, community acquired pneumonia, complicated urinary tract infection including Pyelonephritis, chronic bacterial prostatitis and skin and soft tissue infection. Levofloxacin is a frequently prescribed antibacterial agent with Diclofenac Sodium for pain management in infectious conditions. The objective of the present work is to evaluate the level of interaction between Levofloxacin and Diclofenac Sodium. In this work market available brands of both drugs were also evaluated for quality. The physiochemical parameters like weight variation, thickness variation, and mechanical strength were determined. Similarly the percentage drug release and content uniformity test were also analyzed; the tested quality attributes were found within the recommended pharmacopeia ranges except brand L6 that had high drug content 124.629 +/- 3.614 while brand L[4] and L[5] were not found similar in pH 1.2. When subjected to model dependent analysis Levofloxacin showed compliance with [first order, Higuchi, Hixson Crowell and Weibull] at pH [1.2, 4.5 and 6.8]. However Diclofenac Sodium showed adherence with [first order, Hixson Crowell and Weibull] at pH [1.2, 4.5 and 6.8] but following Higuchi at pH 1.2 and 4.5 only. The interaction studies were also performed spectrophotometrically and simultaneous equation was used to estimate the percentage availability of both the drugs at pH 4.5, 6.8, FaSSGF and FaSSIF. The studies showed that the percent availability of Levofloxacin was increased significantly in FaSSIF i.e. 129.173 +/- 0.323 at 45 minutes in the presence of Diclofenac Sodium

Oral udenafil and aceclofenac for the prevention of post-endoscopic retrograde cholangiopancreatography pancreatitis in high-risk patients: a randomized multicenter study

BACKGROUND/AIMS: Acute pancreatitis is a common complication of endoscopic retrograde cholangiopancreatography (ERCP). Combination therapy w ith ora l udenafil and aceclofenac may reduce the occurrence of post-ERCP pancreatitis by targeting different pathophysiological mechanisms. We investigated whether combining udenafil and aceclofenac reduced the rates of post-ERCP pancreatitis. METHODS: A prospective, randomized, double-blind, placebo-controlled, multicenter study was conducted in four academic medical centers. Between January 2012 and June 2013, a total of 216 patients who underwent ERCP were analyzed for the occurrence of post-ERCP pancreatitis. Patients were determined to be at high risk for pancreatitis based on validated patient and procedure-related risk factors. RESULTS: Demographic features, indications for ERCP, and therapeutic procedures were similar in each group. There were no significant differences in the rate (15.8% [17/107] vs. 16.5% [18/109], p = 0.901) and severity of post-ERCP pancreatitis between the udenafil/aceclofenac and placebo groups. One patient in each group developed severe pancreatitis. Multivariate analyses indicated that suspected dysfunction of the sphincter of Oddi and endoscopic papillary balloon dilation without sphincterotomy were associated with post-ERCP pancreatitis. CONCLUSIONS: Combination therapy with udenafil and aceclofenac is not effective for the prevention of post-ERCP pancreatitis.

The Toxicity of Nonsteroidal Anti-inflammatory Eye Drops against Human Corneal Epithelial Cells in Vitro

This study investigated the toxicity of commercial non-steroid anti-inflammatory drug (NSAID) eye solutions against corneal epithelial cells in vitro. The biologic effects of 1/100-, 1/50-, and 1/10-diluted bromfenac sodium, pranoprofen, diclofenac sodium, and the fluorometholone on corneal epithelial cells were evaluated after 1-, 4-, 12-, and 24-hr of exposure compared to corneal epithelial cell treated with balanced salt solution as control. Cellular metabolic activity, cellular damage, and morphology were assessed. Corneal epithelial cell migration was quantified by the scratch-wound assay. Compared to bromfenac and pranoprofen, the cellular metabolic activity of diclofenac and fluorometholone significantly decreased after 12-hr exposure, which was maintained for 24-hr compared to control. Especially, at 1/10-diluted eye solution for 24-hr exposure, the LDH titers of fluorometholone and diclofenac sodium markedly increased more than those of bromfenac and pranoprofen. In diclofenac sodium, the Na+ concentration was lower and amount of preservatives was higher than other NSAIDs eye solutions tested. However, the K+ and Cl- concentration, pH, and osmolarity were similar for all NSAIDs eye solutions. Bromfenac and pranoprofen significantly promoted cell migration, and restored wound gap after 48-hr exposure, compared with that of diclofenac or fluorometholone. At 1/50-diluted eye solution for 48-hr exposure, the corneal epithelial cellular morphology of diclofenac and fluorometholone induced more damage than that of bromfenac or pranoprofen. Overall, the corneal epithelial cells in bromfenac and pranoprofen NSAID eye solutions are less damaged compared to those in diclofenac, included fluorometholone as steroid eye solution.

A randomized, double blind comparison of pethidine and ketoprofen as adjuvants for lignocaine in intravenous regional anaesthesia / Estudo comparativo, randômico e duplo-cego de petidina e cetoprofeno como adjuvantes de lidocaína em anestesia regional intravenosa / Estudio comparativo, aleatorizado y doble ciego, de la petidina y del ketoprofeno como adyuvantes de la lidocaína en la anestesia regional intravenosa

BACKGROUND AND OBJECTIVES: A review of all the adjuncts for intravenous regional anaesthesia concluded that there is good evidence to recommend NonSteroidal Anti-Inflammatory agents and pethidine in the dose of 30 mg dose as adjuncts to intravenous regional anaesthesia. But there are no studies to compare pethidine of 30 mg dose to any of the NonSteroidal Anti-Inflammatory agents. METHODS: In a prospective, randomized, double blind study, 45 patients were given intravenous regional anaesthesia with either lignocaine alone or lignocaine with pethidine 30 mg or lignocaine with ketprofen 100 mg. Fentanyl was used as rescue analgesic during surgery. For the first 6 h of postoperative period analgesia was provided by fentanyl injection and between 6 and 24 h analgesia was provided by diclofenac tablets. Visual analogue scores for pain and consumption of fentanyl and diclofenac were compared. RESULTS: The block was inadequate for one case each in lignocaine group and pethidine group, so general anaesthesia was provided. Time for the first dose of fentanyl required for postoperative analgesia was significantly more in pethidine and ketoprofen groups compared to lignocaine group (156.7 ± 148.8 and 153.0 ± 106.0 vs. 52.1 ± 52.4 min respectively). Total fentanyl consumption in first 6 h of postoperative period was less in pethidine and ketoprofen groups compared to lignocaine group (37.5 ± 29.0 mcg, 38.3 ± 20.8 mcg vs. 64.2 ± 27.2 mcg respectively). Consumption of diclofenac tablets was 2.4 ± 0.7, 2.5 ± 0.5 and 2.0 ± 0.7 in the control, pethidine and ketoprofen group respectively, which was statistically not significant. Side effects were not significantly different between the groups. CONCLUSION: Both pethidine and ketoprofen are equally effective in providing postoperative analgesia up to 6 h, without significant difference in the side effects and none of the adjuncts provide significant ...

JUSTIFICATIVA E OBJETIVOS: uma revisão de todos os adjuvantes para anestesia regional intravenosa concluiu que há boas evidências para recomendar os agentes anti-inflamatórios não esteroides e petidina em dose de 30 mg como adjuvantes para anestesia regional intravenosa. Porém, não há estudos que comparem petidina (30 mg) com quaisquer dos agentes anti-inflamatórios não esteroides. MÉTODOS: em um estudo prospectivo, randômico e duplo-cego, 45 pacientes receberam anestesia regional intravenosa com apenas lidocaína ou lidocaína com petidina (30 mg) ou lidocaína com cetoprofeno (100 mg). Fentanil foi usado como analgésico de resgate durante a cirurgia. Durante as seis primeiras horas de pós-operatório, analgesia foi fornecida via injeção de fentanil e, entre seis e 24 horas, analgesia foi fornecida via comprimidos de diclofenaco. Os escores visuais analógicos para dor e do consumo de fentanil e diclofenaco foram comparados. RESULTADOS: o bloqueio foi inadequado para um caso tanto do grupo lidocaína quanto do grupo petidina; portanto, anestesia geral foi administrada. O tempo para a primeira dose necessária de fentanil para analgesia pós-operatória foi significativamente maior nos grupos petidina e cetoprofeno em comparação com o grupo lidocaína (156,7 ± 148,8 e 153,0 ± 106,0 vs. 52,1 ± 52,4 minutos, respectivamente). O consumo total de fentanil nas primeiras seis horas de pós-operatório foi menor nos grupos petidina e cetoprofeno em comparação com o grupo lidocaína (37,5 ± 29,0 mcg, 38,3 ± 20,8 mcg vs. 64,2 ± 27,2 mcg, respectivamente). O consumo de comprimidos de diclofenaco foi de 2,4 ± 0,7, 2,5 ± 0,5 e 2,0 ± 0,7 no grupo controle, petidina e cetoprofeno, respectivamente, o que não foi estatisticamente significante. ...

JUSTIFICACIÓN Y OBJETIVOS: una revisión sobre todos los adyuvantes para la anestesia regional intravenosa concluyó que hay buenas evidencias para recomendar los agentes antiinflamatorios no esteroideos y la petidina en dosis de 30 mg como adyuvantes para la anestesia regional intravenosa. Sin embargo, no hay estudios comparando la petidina (30 mg) con cualesquiera de los agentes antiinflamatorios no-esteroideos. MÉTODOS: en un estudio prospectivo, aleatorizado y doble ciego, 45 pacientes recibieron anestesia regional intravenosa con solamente lidocaína o lidocaína con petidina (30 mg) o lidocaína con ketoprofeno (100 mg). El fentanilo fue usado como analgésico de rescate durante la cirugía. Durante las 6 primeras horas del postoperatorio, la analgesia fue suministrada vía inyección de fentanilo y entre 6 y 24 h, la analgesia fue suministrada vía comprimidos de diclofenaco. Se compararon las puntuaciones visuales analógicas para el dolor y el consumo de fentanilo y diclofenaco. RESULTADOS: el bloqueo fue inadecuado para un caso tanto del grupo lidocaína como del grupo petidina; por tanto, se administró anestesia general. El tiempo para la primera dosis necesaria de fentanilo para analgesia postoperatoria fue significativamente mayor en los grupos petidina y ketoprofeno en comparación con el grupo lidocaína (156,7 ± 148,8 y 153,0 ± 106,0 vs. 52,1 ± 52,4 min, respectivamente). El consumo total de fentanilo en las primeras 6 h del postoperatorio fue menor en los grupos petidina y ketoprofeno en comparación con el grupo lidocaína (37,5 ± 29,0 mcg; 38,3 ± 20,8 mcg vs. 64,2 ± 27,2 mcg, respectivamente). El consumo de comprimidos de diclofenaco fue de 2,4 ± 0,7; 2,5 ± 0,5; y 2 ± 0,7 en el grupo control, petidina y ketoprofeno, respectivamente, lo que no fue estadísticamente significativo. Los ...

Comparative study of actinic keratosis treatment with 3% diclofenac sodium and 5% 5-fluorouracil / Estudo comparativo do tratamento de ceratoses actinicas com diclofenaco sodico 3% e 5-fluorouracil 5%

BACKGROUND: Actinic keratosis is a frequent lesion which occurs in sunlight exposed areas. Diclofenac sodium and 5-Fluorouracil are effective, non-invasive and easy-to-apply topical treatment options. OBJECTIVES: To assess and compare the effectiveness of 3% diclofenac sodium associated with 2.5% hyaluronic acid and of 5% 5-Fluorouracil for the treatment of actinic keratosis, as well as the patient's degree of satisfaction and tolerability. METHODS: 28 patients with a clinical diagnosis of actinic keratosis were randomized to receive diclofenac sodium or 5-Fluorouracil and were clinically assessed before and after treatment as well as 8 weeks after the end of treatment. Modified versions of the Investigator and Patient Global Improvement Scores were used. RESULTS: The average number of lesions in the diclofenac sodium group before and after treatment was 13.6 and 6.6 (p<0,001), respectively, while it was 17.4 and 3.15 (p<0.001) in the 5-Fluorouracil group. There was a significant reduction in the number of lesions in the 5-Fluorouracil group in relation to the diclofenac sodium group (p<0.001). To the non-blinded physician, there was a higher satisfactory therapeutic response in the 5-Fluorouracil group (p<0.001); to the blinded physician, there was a higher satisfactory response in this same group, although not statistically significant (p=0.09). There was a high degree of satisfaction in both groups (73% in the diclofenac sodium group and 77% in the 5-Fluorouracil group; p=0.827). Regarding adverse effects, the diclofenac sodium group presented a higher degree of satisfaction (93.3% vs 38.4%; p=0.008). Erythema, edema, crusts and itching were significantly higher in the 5-Fluorouracil group. CONCLUSION: We concluded that 5-Fluorouracil was more effective; however, it showed lower tolerability than diclofenac sodium. .

FUNDAMENTOS: Ceratose actínica é uma lesão frequente que ocorre em áreas de exposição solar. Diclofenaco sódico e 5-Fluorouracil são opções de tratamento tópico efetivo, não invasivo e de fácil aplicação. OBJETIVOS: Avaliar e comparar a efetividade do diclofenaco sódico 3% associado ao ácido hialurônico 2,5% e do 5-fluorouracil 5% no tratamento de ceratose actínica, assim como a tolerabilidade e o grau de satisfação do paciente. MÉTODOS: 28 pacientes com diagnóstico clínico de ceratoses actínicas foram randomizados para receber diclofenaco sódico ou 5-fluorouracil e foram avaliados clinicamente antes, ao término e após 8 semanas do tratamento. Utilizou-se o Escore de Melhora Global do Investigador e do Paciente, ambos modificados. RESULTADOS: A média de lesões no grupo do diclofenaco sódico antes e depois do tratamento foi de 13,6 e 6,6 (p<0,001) e no grupo do 5-fluorouracil foi de 17,4 e 3,15 (p<0,001). Houve uma diminuição significativa no número de lesões no grupo do 5-fluorouracil em relação ao grupo do diclofenaco sódico (p<0,001). Para o médico não cegado houve uma resposta terapêutica satisfatoriamente maior no grupo do 5-fluorouracil (p<0,001); para o cegado, houve uma maior resposta nesse mesmo grupo, porém não significativa (p=0,09). Houve alta satisfação com o tratamento em ambos os grupos (73% no diclofenaco sódico e 77% no 5-fluorouracil; p=0,827). Já em relação aos efeitos adversos, o grupo do diclofenaco sódico apresentou taxa de satisfação maior (93,3% vs 38,4%; p=0,008). Eritema, edema, crostas e prurido foram significativamente maiores no tratamento com 5-fluorouracil. CONCLUSÕES: Concluímos que o 5-fluorouracil foi mais efetivo, ...

Comparative analysis of preemptive analgesic effect of dexamethasone and diclofenac following third molar surgery

The objective of the study was to compare the analgesic effectiveness of dexamethasone and diclofenac sodium administered preemptively after surgical removal of third molars. Forty-four ASA (American Society of Anesthesiologists) I patients (19 men, 35 women; 16–28 years old) randomly and double-blindly received diclofenac sodium (50 mg) or dexamethasone (8 mg) or placebo 1 h before surgery. Intensity of pain, measured with a visual analog scale (VAS), was the variable studied at different postoperative times (1 h, 2 h, 3 h, 6 h, 8 h, 12 h, 48 h, 4 d and 7 d). The total amount of rescue medication (TARM) ingested (paracetamol) was another variable of the study. The Kruskal-Wallis statistical test was used. A p value of < .05 was adopted to reject the null hypothesis. The dexamethasone group showed lower pain intensity (p < .05) than the diclofenac sodium and placebo groups (p < .05). No difference in TARM was observed among the groups (p < .05). Preemptively administered, dexamethasone was effective in controlling postoperative pain.

Development and implication of methodology for aceclofenac in pure and pharmaceutical formulations by microwave assisted spectrophotometry

A simple, fast and cost effective method for determination of Aceclofenac in pure and tablet formulations has been developed and validated. The method is based on formation of stable blue coloured complex [lambda[max] = 740nm] of Aceclofenac with ammonium molybdate in presence of sulfuric acid under microwave irradiation for 5min. Peak shift in FT-IR spectra also indicated the formation of complex. Measurement of absorbance was carried out at lambda[max] = 740nm. The reaction obeys Beer's law over the concentration range of 50-250 micro g/ml of Aceclofenac. The RSD [intra-day and inter-day precision] for the drug is not greater than 0.95% and recoveries were found to be in range of 99.01-99.99%. The proposed method can be used successfully for routine analysis of Aceclofenac in pure and tablet formulations

Concentração plasmática de diclofenaco sódico em cães, submetidos à fonoforese / Plasma concentration of diclofenac sodium in dogs submitted to diclofenac phonophoresis

Com o objetivo de avaliar a concentração plasmática de diclofenaco sódico (DS) emulgel em cães com ou sem o uso de fonoforese e de verificar se a fonoforese induz à maior absorção desse fármaco, foram utilizados cinco cães, e todos eles passaram por oito grupos distintos. Um grupo recebeu, via oral, um comprimido de DS, 40mg, por animal, e sete grupos receberam aplicação transdérmica de diclofenaco sódico emulgel por ultrassom. Pela via transdérmica, a área de aplicação era de 20cm². A frequência do ultrassom foi de 1MHz, modo contínuo, com intensidade de 0,4Wcm-2. Colheram-se amostras de sangue antes de se executarem os protocolos - tempo zero -, após uma hora - tempo 1 - e após quatro horas da aplicação - tempo 2 - em todos os grupos, e realizou-se análise das amostras por cromatografia líquida de alta eficiência. Houve diferença (P<0,05) apenas nas amostras no tempo 1 do grupo que recebeu dose oral de DS em relação às outras amostras. Não foi possível verificar concentração plasmática de diclofenaco sódico com aplicação tópica em cães submetidos ou não à fonoforese, apenas quantificou-se o diclofenaco sódico pela administração via oral. A facilitação da penetração transdérmica pelo ultrassom não foi verificada sob o protocolo especificado nesta pesquisa.

The aim of this study was to evaluate the plasma concentration of diclofenac sodium (DS) in dogs submitted to diclofenaco phonophoresis and to evaluate if phonophoresis induces greater absorption of this drug in dogs. Five dogs were used in eight different groups at different times: One group received oral administration of 40mg of DS per dog and seven groups received topical application of emulgel DS. The topical application area was 20cm². A continuous ultrasound frequency of 1MHz and intensity of 0.4W cm-2 was used. Blood collections were performed before the treatment (T0), and 1h (T1) and 4h (T2) after ultrasound application for all groups. DS concentrations in plasma were measured by high performance liquid choramatohraphy (HPLC). There was significant increase of DS plasma concentration only at T1 in the oral administration group. It was not possible to detect any concentration of DS in the plasma of dogs after topical application of DS, even after DS phonophoresis. The facilitation of transdermal penetration by ultrasound has not been verified under the protocol specified in this research.