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Braz. J. Pharm. Sci. (Online) ; 59: e201178, 2023. tab, graf
Article in English | LILACS | ID: biblio-1439535


Abstract Diclofenac sodium (DF) is a non-steroidal anti-inflammatory drug (NSAID) that possesses antipyretic, analgesic, antinociceptive and anti-inflammatory activities. Like other NSAIDs, DF is known to be associated with renal, cardiovascular, and gastrointestinal complications. The present study was carried out to evaluate the adverse effects of DF in vivo in wistar albino rats and to assess if oral administration of the organic osmolyte betaine mitigates the adverse effect of DF. Eighteen male Wistar rats were divided into three groups, one group of animals was fed orally with 20 mg/kg of DF once/day, and the other group received a combination of 20 mg/kg of DF and 30 mg/kg of betaine, once/day. Apart from the hematological and biochemical parameters, histopathological changes in the liver, lungs, brain, heart and kidney were also investigated. Histopathological alterations that were found in the liver, kidney, and lungs of DF-treated animals were found to be minimal or absent in DF + betaine-treated animals, as compared to untreated control. The results showed that betaine mitigates the adverse effects associated with DF treatment.

Animals , Male , Rats , Betaine/agonists , Diclofenac/adverse effects , Pharmaceutical Preparations/administration & dosage
Braz. J. Pharm. Sci. (Online) ; 58: e18655, 2022. tab, graf
Article in English | LILACS | ID: biblio-1364423


Abstract Periodontitis is an oral disease associated with inflammation and pain with swollen and bleeding gums. In the present study, dental pastes containing NSAIDs, namely, diclofenac sodium and nimesulide (1 % w/w) were prepared to treat periodontitis. Dental pastes of diclofenac sodium and nimesulide (1 % w/w) were prepared with/without mucoadhesive hydrocolloid polymers such as sodium carboxy methyl cellulose (NaCMC), hydroxyl ethyl cellulose (HEC) and methyl cellulose (MC) by conventional trituration method. The pH, drug content, viscosity, tube spreadability and tube extrudability of these prepared dental pastes were measured. These dental pastes of diclofenac sodium and nimesulide (1 % w/w) were characterized by FTIR analyses for drug-excipient compatibility. The in vitro drug releases from these dental pastes in 6.4 pH phosphate buffer solution displayed sustained release over longer period and the drug release rate was found to be decreased when the concentration of mucoadhesive polymer was increased. These dental pastes displayed good adhesion to the oral mucosa revealing more retention time in mouth when tested for ex vivo mucoadhesion using bovine cheek pouch. The stability study results reveal that the DC3 and NC3 dental paste formulations were found stable enough over a longer period in different storage conditions. The present study revealed that the prepared mucoadhesive dental pastes of diclofenac sodium and nimesulide (1 % w/w) had good adhesion with the oral mucosa to maintain consistent release of drugs over prolonged time.

Toothpastes/analysis , Pharmaceutical Preparations , Anti-Inflammatory Agents, Non-Steroidal/analysis , Mouth , Mouth Mucosa/abnormalities , Periodontitis , In Vitro Techniques/methods , Diclofenac/adverse effects , Disease/classification , Spectroscopy, Fourier Transform Infrared , Drug Liberation , Gingiva/abnormalities , Inflammation/complications
Arq. bras. med. vet. zootec. (Online) ; 71(6): 1865-1872, Nov.-Dec. 2019. tab, graf, ilus
Article in English | LILACS, VETINDEX | ID: biblio-1055154


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)

Animals , Rabbits , Ophthalmic Solutions/adverse effects , Diclofenac/administration & dosage , Diclofenac/adverse effects , Ketorolac Tromethamine/administration & dosage , Ketorolac Tromethamine/adverse effects , Absorption, Physiological/drug effects
Braz. J. Pharm. Sci. (Online) ; 55: e18022, 2019. tab, graf
Article in English | LILACS | ID: biblio-1039067


Eugenol has been employed for decades as a condiment, an antimycotic, an antibacterial, an antiviral, and an antioxidant, and it is one of the natural analgesics most frequently utilized for pain and inflammation. Our objective was to determine the analgesic/anti-inflammatory effect of eugenol compared with diclofenac, naproxen, and tramadol using the formalin test. The formalin method was used in 6- to 10-week-old Wistar rats (weighing 250 g each) divided into six groups: saline (0.9%); formalin (5%); diclofenac (250 µg/kg); naproxen (400 µg/kg); tramadol (500 µg/kg), and eugenol (1,400 µg/kg), in the intraplantar part of the hind-end trunk of the rats, with n = 5 per group. Eugenol diminished 44.4% of nociceptive behavior in phase 1 and 48% in phase 2 (p ≤0.05 vs formalin). Eugenol was shown to be 1.14 times more effective than diclofenac, but 1.62 and 1.75 times less effective than naproxen and tramadol, respectively, in phase 1 and 1.45 times less effective than diclofenac and naproxen and 1.66 less effective than tramadol in phase 2 (p ≤0.05). These data suggest that eugenol possesses moderate activity in the acute pain phase and greater activity in inflammatory-type pain, and both effects are comparable to those produced by diclofenac and are less than the effects produced by naproxen and tramadol in the formalin test

Animals , Male , Rats , Eugenol/adverse effects , Anti-Inflammatory Agents, Non-Steroidal/analysis , Diclofenac/adverse effects , Tramadol/adverse effects , Pain Measurement/methods , Naproxen/adverse effects
Braz. J. Pharm. Sci. (Online) ; 55: e17240, 2019. tab, graf
Article in English | LILACS | ID: biblio-1019531


Iguratimod (IGU, also known as T-614), a novel disease modifying antirheumatic drug intended to cure patients with rheumatoid arthritis (RA). The purpose of this study is to evaluate the effect of IGU on the pharmacokinetics of CYP2C9 probe drug diclofenac and its metabolite 4′-hydroxy diclofenac in vivo and in vitro. In in vivo experiments, 24 rats were randomly assigned to three groups consisting of the control group (Normal saline), low dose IGU group (10 mg/kg) and high dose IGU group (30 mg/kg). Blood samples were collected from orbital sinuses vein before 1 hour and serial times of giving diclofenac (15 mg/kg) to all the rats. Plasma concentration of diclofenac and its metabolite 4´-hydroxy diclofenac were assayed by high performance liquid chromatography. Pharmacokinetic parameters were assessed by Winnonlin 6.4 pharmacokinetic software. Moreover, in vitro studies were performed in recombinant human CYP2C9 yeast cell system. IGU at low dose showed no significant differences in the pharmacokinetic parameters of diclofenac and 4-hydroxy diclofenac in vivo when compared with control group (p>0.005). However, at the high dose of IGU, the pharmacokinetic parameters of 4´-hydroxy metabolite of diclofenac increase in half-life (T1/2) and mean area under the curve (AUC0→24), while a decrease in mean clearance (CL, mL/h/kg) and volume of distribution Vz (mL/kg). In addition, in in vitro study, high doses of IGU reduces the metabolism rate of diclofenac. IGU at high dose significantly increase the pharmacokinetics parameters of 4´-hydroxy diclofenac in rats. Additionally, it also showed the potent inhibitory effect on diclofenac metabolism in recombinant human CYP2C9 yeast cells.

Animals , Male , Female , Rats , Diclofenac/adverse effects , Cytochrome P-450 CYP2C9 , Cytochrome P-450 CYP2C9/pharmacokinetics , Anti-Inflammatory Agents/adverse effects , Arthritis, Rheumatoid/classification , In Vitro Techniques
Rev. cient. Esc. Univ. Cienc. Salud ; 5(1): 41-49, ene.-jun. 2018. tab
Article in Spanish | LILACS | ID: biblio-979935


Diclofenaco es un fármaco de variado uso por su libre venta en todos los países. Es un derivado de fenil-acético con propiedades analgésicas, antiinflamatorias y antipiréti-cas, debido a su mecánismo de acción: inhi-bición de las ciclooxigenasas con mediana selectividad hacia la ciclooxigenasa. Su principal indicación es para dolor de leve a moderado. El tiempo de uso del diclofenaco dependerá de la forma y objetivo de aplica-ción; los efectos adversos están estrecha-mente relacionados con el tiempo de uso y la idiosincrasia de cada persona. Algunas de las consecuencias destacables se manifies-tan en el sistema gastrointestinal, hematoló-gico, hepático, cardiaco, renal, sistema nervioso central y piel. El uso prescrito del diclofenaco, es de 3 - 5 días y se relaciona con la inducción de dispepsia, esofagitis, náuseas, vómitos, cefaleas e hipercoagula-bilidad, mientras que el uso crónico, alrede-dor de 90 días, puede inducir el desarrollo de hipertensión arterial, accidente cerebro vascular, infarto agudo al miocardio, hepati-tis fulminante, hemorragias gástricas, úlce-ras pépticas, fallo renal agudo, entre otras. El síndrome de Steven-Johnson y la necró-lisis epidérmica tóxica, son reacciones de hipersensibilidad relacionados con el tiempo de uso de este fármaco. Entre otros efectos del diclofenaco encontramos el bloqueo de los canales de sodio, calcio y potasio depen-dientes de voltaje, mecanismo por el cual causa analgesia sin la inhibición de la forma ción de prostaglandinas...(AU)

Humans , Diclofenac/adverse effects , Stroke/complications , Arterial Pressure/drug effects , Drug Misuse/adverse effects
Gut and Liver ; : 371-379, 2014.
Article in English | WPRIM | ID: wpr-175285


BACKGROUND/AIMS: The use of proton pump inhibitors or misoprostol is known to prevent the gastrointestinal complications of nonsteroidal anti-inflammatory drugs (NSAIDs). Rebamipide is known to increase the mucosal generation of prostaglandins and to eliminate free oxygen radicals, thus enhancing the protective function of the gastric mucosa. However, it is unknown whether rebamipide plays a role in preventing NSAID-induced gastropathy. The aim of this study was to determine the effectiveness of rebamipide compared to misoprostol in preventing NSAID-induced gastrointestinal complications in patients requiring continuous NSAID treatment. METHODS: We studied 479 patients who required continuous NSAID treatment. The patients were randomly assigned to groups that received 100 mg of rebamipide three times per day or 200 microg of misoprostol three times per day for 12 weeks. The primary endpoint of the analysis was the occurrence rate of gastric ulcers, as determined by endoscopy after 12 weeks of therapy. RESULTS: Of the 479 patients in the study, 242 received rebamipide, and 237 received misoprostol. Ultimately, 44 patients (18.6%) withdrew from the misoprostol group and 25 patients (10.3%) withdrew from the rebamipide group. There was a significant difference in withdrawal rate between the two groups (p=0.0103). The per protocol analysis set was not valid because of the dropout rate of the misoprostol group; thus, the intention to treat (ITT) analysis set is the main set for the efficacy analysis in this study. After 12 weeks, the occurrence rate of gastric ulcers was similar in the rebamipide and misoprostol groups (20.3% vs 21.9%, p=0.6497) according to ITT analysis. In addition, the therapeutic failure rate was similar in the rebamipide and misoprostol groups (13.6% vs 13.1%, p=0.8580). The total severity score of the gastrointestinal symptoms was significantly lower in the rebamipide group than in the misoprostol group (p=0.0002). The amount of antacid used was significantly lower in the rebamipide group than in the misoprostol group (p=0.0258). CONCLUSIONS: Rebamipide can prevent gastric ulcers when used with NSAIDs and can decrease the gastrointestinal symptoms associated with NSAID administration. When the possibility of poor compliance and the potential adverse effects of misoprostol are considered, rebamipide appears to be a clinically effective and safe alternative.

Adult , Aged , Humans , Middle Aged , Alanine/administration & dosage , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Anti-Ulcer Agents/administration & dosage , Arthritis/drug therapy , Butanones/adverse effects , Diclofenac/adverse effects , Double-Blind Method , Drug Administration Schedule , Gastric Mucosa , Misoprostol/administration & dosage , Quinolones/administration & dosage , Stomach Ulcer/chemically induced , Thiazines/adverse effects , Thiazoles/adverse effects , Treatment Outcome
An. bras. dermatol ; 88(5): 732-738, out. 2013. tab, graf
Article in English | LILACS | ID: lil-689729


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, ...

Aged , Aged, 80 and over , Female , Humans , Male , Middle Aged , Dermatologic Agents/administration & dosage , Diclofenac/administration & dosage , Fluorouracil/administration & dosage , Keratosis, Actinic/drug therapy , Administration, Cutaneous , Chi-Square Distribution , Dermatologic Agents/adverse effects , Diclofenac/adverse effects , Fluorouracil/adverse effects , Patient Satisfaction , Time Factors , Treatment Outcome
Rev. bras. anestesiol ; 63(5): 426-428, set.-out. 2013.
Article in Portuguese | LILACS | ID: lil-691379


A Síndrome de Kounis (SK) corresponde ao aparecimento simultâneo de síndromes coronárias agudas (SCA) com reações alérgicas ou de hipersensibilidade. Na literatura têm sido reportados vários casos associados a fármacos, picadas de inseto, alimentos, exposições ambientais e doenças médicas. Essa síndrome é encontrada na prática médica diária mais frequentemente do que antecipada. Por isso, o desconhecimento dessa síndrome poderá contribuir para a falha no diagnóstico. Apresentamos um caso clínico de Síndrome de Kounis secundária à ingestão de diclofenaco.

Kounis Syndrome (KS) is the contemporary occurrence of Acute Coronary Syndromes (ACS) with an allergic or hypersensitivity reaction. This syndrome has been reported in association with a variety of drugs, food, insect stings, environmental exposures and medical conditions. Cases of KS seem to be more often encountered in everyday clinical practice than anticipated. It is believed that the lack of awareness of this association may lead to underreporting. We report a case of KS secondary to diclofenac intake.

El Síndrome de Kounis (SK) es el surgimiento simultáneo de síndromes coronarios agudos (SCA) con reacciones alérgicas o de hipersensibilidad. En la literatura han sido reportados varios casos asociados con fármacos, picadas de insecto, alimentos, exposiciones ambientales y enfermedades médicas. Ese síndrome se encuentra en la práctica médica diaria con más frecuencia de lo que se cree. Por eso, su descubrimiento podrá contribuir a la mejoría en los fallos de diagnóstico. Presentamos un caso clínico del Síndrome de Kounis secundario a la ingestión de diclofenaco.

Humans , Male , Middle Aged , Diclofenac/adverse effects , Acute Coronary Syndrome/complications , Kounis Syndrome/etiology , Cardiac Catheterization/instrumentation , Electrocardiography/instrumentation
Acta cir. bras ; 27(2): 131-136, Feb. 2012. ilus, graf
Article in English | LILACS | ID: lil-614531


PURPOSE: To study diclofenac sodium induced histological and mechanical alterations and their prevention with Imipenem in rat intestine. METHODS: Male Wistar rats (n=240) were randomly assigned to four experimental groups: GI: n=60 treated with 0.9 percent saline IM; GII: n=60 treated with 6mg/kg body weight diclofenac sodium IM for four days; GIII: n=60 treated with 30mg/kg body weight Imipenem IM for four days, and GIV n=60 treated with diclofenac sodium plus Imipenem at the above doses IM for 4 days. Each group was further divided into 4 subgroups of 15 rats each and sacrificed at 4, 7, 14, and 21 days of follow-up, respectively. Abdominal cavity macroscopy and histology, and small bowel breaking strength were analyzed at each sacrifice moment. RESULTS: There were no histological or mechanical alterations in normal control rats throughout the study. Ulcerated lesions in intestinal mucosa were observed and breaking strength decreased in all diclofenac sodium treated rats. Ulcerated lesions in intestinal mucosa were prevented by Imipenem in all rats. CONCLUSION: Diclofenac sodium induced ulcerated lesions in rat intestinal mucosa can be prevented by Imipenem treatment.

OBJETIVO: Avaliar as alterações histológicas e biomecânicas do diclofenaco de sódio na mucosa intestinal do rato e a associação com o uso de Imipenem. MÉTODOS: Foram estudados 240 ratos Wistar distribuídos aleatoriamente em quatro grupos experimentais: GI: 60 ratos tratados com injeção IM de soro fisiológico 0,9 por cento; GII: 60 ratos tratados com injeção IM de diclofenaco de sódio na dose de 6mg/kg de peso por 4 dias; GIII: 60 ratos tratados com injeção IM de Imipenem na dose de 30 mg/kg de peso por 4 dias; GIV: 60 ratos tratados com injeção IM de soro fisiológico e diclofenaco de sódio nas doses acima. Em cada grupo os animais foram posteriormente divididos em 4 momentos de 15 animais em cada um para sacrifício, respectivamente, no 4º, 7º, 14º e 21º dias após o início do tratamento. As alterações da cavidade abdominal, assim como as características histológicas e de força de ruptura do intestino delgado foram analisadas em cada momento, em cada grupo. RESULTADOS: Não foram encontradas alterações histológicas e biomecânicas nos animais do Grupo I nesse estudo. Lesões ulceradas na mucosa do intestino delgado foram observadas nos animais tratados com diclofenaco de sódio, assim como diminuição da força de ruptura. As lesões ulceradas encontradas foram prevenidas pelo uso de Imipenem. CONCLUSÃO: O diclofenaco de sódio induz lesões ulceradas na mucosa intestinal do rato que podem ser prevenidas pelo uso de Imipenem.

Animals , Male , Rats , Anti-Bacterial Agents/pharmacology , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Diclofenac/adverse effects , Imipenem/pharmacology , Intestinal Diseases/prevention & control , Intestinal Mucosa/drug effects , Ulcer/prevention & control , Intestinal Diseases/chemically induced , Intestine, Small/drug effects , Random Allocation , Rats, Wistar , Time Factors , Ulcer/chemically induced
São Paulo med. j ; 129(5): 335-345, 2011. ilus, tab
Article in English | LILACS | ID: lil-604794


CONTEXT AND OBJECTIVE: Lumiracoxib is an anti-inflammatory drug that has been used to treat acute dental pain, mainly in postsurgical settings, in which the greatest levels of pain and discomfort are experienced during the first 24 hours. This study aimed to assess the efficacy and safety of lumiracoxib for treating acute postsurgical dental pain. DESIGN AND SETTING: Systematic review developed at the Brazilian Cochrane Centre, Universidade Federal de São Paulo. METHODS: An electronic search was conducted in the PubMed, Cochrane Library, Lilacs (Literatura Latino-Americana e do Caribe em Ciências da Saúde), SciELO (Scientific Electronic Library Online) and Embase databases. A manual search was also performed. Only randomized controlled trials were included, and these were selected and assessed by two researchers with regard to the risk of bias. RESULTS: Three clinical trials with 921 participants were included. Lumiracoxib 400 mg produced onset of analgesia in a shorter time than shown by lumiracoxib 100 mg, celecoxib 200 mg and ibuprofen 400 mg. There was no difference between lumiracoxib 400 mg and rofecoxib 50 mg. In two studies, the mean time taken to attain onset of analgesia for the placebo was not estimated because the number of participants who reached onset was too small. CONCLUSION: There is evidence with a moderate risk of bias that recommends the use of lumiracoxib for acute postoperative dental pain. However, the adverse effects are not completely known. Given that lumiracoxib is currently available in only three countries, further studies are likely to be rare and discouraged.

CONTEXTO E OBJETIVO: O lumiracoxibe é um anti-inflamatório que tem sido utilizado no tratamento de dor dental aguda, principalmente no cenário pós-cirúrgico, no qual níveis mais elevados de dor e desconforto são sentidos durante as primeiras 24 horas. Este estudo teve por objetivo avaliar a eficácia e a segurança do lumiracoxibe no tratamento da dor dental aguda e pós-operatória. TIPO DE ESTUDO E LOCAL: Revisão sistemática desenvolvida no Centro Cochrane do Brasil, Universidade Federal de São Paulo. MÉTODOS: Foi realizada busca eletrônica nas bases de dados PubMed, Cochrane Library, Lilacs (Literatura Latino-Americana e do Caribe em Ciências da Saúde), SciELO (Scientific Electronic Library Online) e Embase. Também foi realizada busca manual. Apenas ensaios clínicos randomizados foram incluídos e foram selecionados e avaliados por dois pesquisadores quanto ao risco de viés. RESULTADOS: Foram incluídos três ensaios clínicos com 921 participantes. O lumiracoxibe 400 mg mostrou menor tempo de início de analgesia que o lumiracoxibe 100 mg, celecoxibe 200 mg e ibuprofeno de 400 mg. Não houve diferença entre lumiracoxibe 400 mg e rofecoxibe 50 mg. Em dois estudos o tempo médio de início de analgesia para o placebo não foi estimado, pois o número de participantes que a alcançou foi pequeno. CONCLUSÃO: Há evidências, com moderado risco de viés, que recomendam o uso de lumiracoxibe para a dor dental aguda e pós-operatória. No entanto, os efeitos adversos não são completamente conhecidos. Considerando que o lumiracoxibe está disponível em apenas três países, provavelmente a realização de pesquisas futuras será rara e desestimulada.

Humans , /therapeutic use , Diclofenac/analogs & derivatives , Pain, Postoperative/drug therapy , Toothache/drug therapy , Acute Pain/drug therapy , Anti-Inflammatory Agents/adverse effects , Anti-Inflammatory Agents/therapeutic use , /adverse effects , Diclofenac/adverse effects , Diclofenac/therapeutic use , Randomized Controlled Trials as Topic , Risk Assessment
Article in Portuguese | LILACS, BBO | ID: lil-663256


Objetivo: Avaliar a ação do medicamento homeopático Arnica montana 6 cH comparada ao Diclofenaco Sódico 50mg no controle do edema após remoção de terceiros molares inclusos. Métodos: O trabalho tratou-se de uma pesquisa experimental, cruzada, randomizada, duplo-cega, realizada em 30 alunos voluntários do curso de Odontologia da Universidade Federal de Sergipe, com presença de dentes inclusos em bilaterais, perfazendo um total de 120 dentes, com indicação da mesma técnica cirúrgica exodôntica. Os grupos foram divididos em Grupo A: os que usaram a Arnica Montana 6cH e Grupo D: os que usaram Diclofenaco de Sódio 50mg. Para a mensuração do edema, foi utilizada uma fita métrica com a qual foram tomadas três medidas como referência: 1) canto de olho ao tragus (CO-T); 2) canto de olho ao ângulo da mandíbula (CO-AM); 3) comissura labial ao tragus (CL-T). Estas foram realizadas quatro vezes sendo a primeira logo após o fim do procedimento cirúrgico, e as demais após 24h, 48h e 72h da cirurgia. O teste de Shapiro-Wilk foi usado para verificação da distribuição normal das variáveis. Nas variáveis que apresentaram dados paramétricos foi usado o teste de comparação de Student. Os dados foram considerados estatisticamente significantes quando p menor que 0,05. Resultados: No período de 48h pós-cirurgia, o edema foi mais marcante para ambos os grupos nos segmentos CO-AM e CL-T. Após 72h ocorreu uma regressão do edema para ambas as medicações testadas. O segmento que menos apresentou edema foi o CO-T para as duas medicações. O teste de Student mostrou que as medicações se equivalem na efetividade anti-edematosa (p maior que 0,05). Conclusão: O medicamento homeopático Arnica montana 6 cH possui eficácia no controle do edema pós-extração de terceiros molares inclusos. A Arnica montana 6cH quando comparada ao Diclofenaco de Sódio 50mg se mostrou equivalente no controle do edema pós-cirúrgico.

Objective: To evaluate the Arnica montana 6 cH homeopathic efficacy compared to 50mg Diclofenac Sodium in the control of edema after removal of third molars. Methods: This work was an experimental, cross, randomized, double-blind study held on 30 volunteers student from the Dental School at the Sergipe Federal University, with the presence of impacted teeth on both sides, making a total of 120 teeth, indicating the same surgical technique. The groups were divided as follows: GROUP A: those who used the Arnica Montana 6cH and GROUP D: those who used 50mg Diclofenac Sodium. For edema measurement, we used a measure tape with which three measures were taken as reference: 1) eye corner to the tragus (EC-T); 2) eye corner to the jaw angle (EC-JA); 3) labial commissure to the tragus (LC-T). These were four times the first being shortly after the end of surgery and the remaining after 24h, 48h and 72h the end of surgery. Shapiro-Wilk test was used to verify the normal distribution of the studied variables. For normal distribution, Student test was used. The data were considered statistically significant when p less than 0.05. Results: In 48h post-surgery, the edema was notable for both groups in the segments EC-JA and LC-T. After 72h there was decrease of the edema for both drugs tested. The segment EC-T showed less edema for two medications. Student test showed that medications were similar anti-edematous efficacy (p greater than 0.05). Conclusions: The homeopathic remedy Arnica montana 6 cH has efficacy in controlling post-extraction edema of third molars. The Arnica montana 6cH compared to 50mg Diclofenac Sodium was equivalent to control postoperative edema.

Humans , Diclofenac/adverse effects , Arnica/adverse effects , Students, Dental , Surgical Procedures, Operative , Surgery, Oral , Radiography, Panoramic/instrumentation , Molar
Braz. j. vet. res. anim. sci ; 47(2): 118-126, 2010. tab
Article in Portuguese | LILACS | ID: lil-559362


O presente trabalho avaliou os parâmetros hematológicos e bioquímicos do uso de diclofenaco de sódio, meloxicam e firocoxibe em ratos Wistar. Os ratos foram distribuídos em grupos: G1 (controle), G2 (diclofenaco de sódio: 15 mg/kg), G3 (meloxicam: 2,0 mg/ kg), G4 (meloxicam: 10,0 mg/ kg), G5 (firocoxibe: 5,0 mg/ kg) e G6 (firocoxibe: 25,0 mg/ kg). Os fármacos foram administrados por via intragástrica (gavage) a cada 24 horas, durante cinco dias e avaliados em três momentos: M1 (48 horas após o início do tratamento), M2 (96 horas após o início do tratamento) e M3 (72 horas após o término do tratamento). Em cada momento de cada grupo, foram avaliados de cinco a sete animais e realizados os exames laboratoriais. Não foram observadas alterações significativas nos parâmetros bioquímicos e hematológicos com o uso de meloxicam e firocoxibe. O diclofenaco de sódio produziu alterações no eritrograma (redução de hemácias, hematócrito e na taxa de hemoglobina) durante o tratamento e não alterou a contagem das plaquetas e leucometria, com exceção dos basófilos. Não produziu alterações nas atividades de AST, FA, GGT, ureia, creatinina, sódio e potássio. Entretanto, causou diminuições das proteínas plasmática e total sérica, albumina e globulina. Conclui-se que o diclofenaco de sódio não produz grandes alterações no hemograma e exames bioquímicos, enquanto que, o meloxicame o firocoxibe não produzem alterações e efeitos deletérios dose-dependentes nestes exames laboratoriais.

This work has evaluated the hematological and biochemical profile by the use of sodium diclofenac, meloxicam and firocoxib in Wistar rats. The rats were distributed in groups: G1 (control), G2 (diclofenac sodium: 15 mg/kg), G3 (meloxicam: 2.0 mg/ kg), G4 (meloxicam: 10.0 mg/ kg), G5 (firocoxib: 5.0 mg/ kg) e G6 (firocoxib: 25.0 mg/ kg). The drugs were administered intragastrically (gavage) once a day, during five days and evaluated in three moments: M1 (48 hours after the beginning of the treatment), M2 (96 hours after the beginning of the treatment) and M3 (72 hours after the ending of the treatment). In each moment of each group, five to seven animals were evaluated and laboratory exams were performed. There were no significant changes observed in the biochemical and hematological parameters by the use of meloxicam and firocoxib. One of the effects of the sodium diclofenac was eritrogram variation as hematocrit, erythrocytes, hemoglobin decrease during the treatment. In addition, the platelets and total white blood cells counts did not change except for basophil. There was no changes in AST, ALP, GGT, urea, creatinine, sodium, potassium values. However, the values of protein, globulin and albumin decreased. It was concluded that diclofenac sodium does not provide large variations in the hemogram and biochemical profile than the meloxicam and firocoxib do not provide delletery effects in laboratories tests.

Animals , Diclofenac/adverse effects , Rats, Wistar/blood , Hematologic Tests/veterinary
IPMJ-Iraqi Postgraduate Medical Journal. 2010; 9 (3): 306-310
in English | IMEMR | ID: emr-129092


Non steroidal anti-inflammatory drugs [NSAIDs] are used to treat musculoskeletal disorders, inflammation and to control pain. Virtually all [NSAIDs] are capable of producing liver injury ranging from mild reversible elevation of liver enzymes to severe hepatic failure. To estimate the hepatic risk associated with the use of some NSAIDs. 80 osteoarthritis patients were on diclofenac acid [voltarin] tablets 75 mg, 60 of them were female and 20 were male, laboratory estimateion of serum alkaline aminotransferase [ALT], serum aspartate aminotransferase [AST], serum alkaline phosphatase activity and total serum bilirubin [TSB] were done. For comparison age and sex matched 96 apparently healthy persons serve as controls. 27 [33.75%] of the diclofenac treated patients had some impairment of liver function tests, 66.6% of the liver injury found in patients aged more than 50 years and 88.8% had occurred in females. Hepatocelluar injury characterizes most USAIDs induced hepatotoxicity. The frequency of drug induced liver injury [DILI] in diclofenac treated patients is about 33.75%. DILI is more common in females and old age

Humans , Male , Female , Osteoarthritis/drug therapy , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Diclofenac/adverse effects , Alanine Transaminase/blood , Aspartate Aminotransferases/blood , Alkaline Phosphatase/blood , Bilirubin/blood , Liver Function Tests
Rev. chil. dermatol ; 26(4): 396-398, 2010. ilus
Article in Spanish | LILACS | ID: lil-721801


La Dermatosis IgA lineal es una enfermedad vesiculoampollar subepidérmica autoinmune caracterizada por anticuerpos IgA en la unión dermoepidérmica. Es una enfermedad poco frecuente, siendo la mayoría de los casos idiopáticos, pero con reporte de casos por medicamentos, infecciones virales, enfermedades autoinmunes y tumores malignos. Se presentará un caso clínico de Dermatosis IgA lineal causada por Diclofenaco.

Linear IgA dermatosis is an autoimmune subepidermal vesiculobullous disease characterized by IgA antibodies at the dermo-epidermal junction. It is an uncommon disease, with most cases idiopathic, but with case reports caused by drug, viral infections, autoimmune diseases and malignant tumors. A clinical case of Linear IgA dermatosis caused by diclofenac is presented.

Humans , Adult , Female , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Linear IgA Bullous Dermatosis/chemically induced , Linear IgA Bullous Dermatosis/drug therapy , Diclofenac/adverse effects , Autoimmune Diseases , Linear IgA Bullous Dermatosis/pathology , Fluorescent Antibody Technique, Direct
Oman Medical Journal. 2008; 23 (2): 118-119
in English | IMEMR | ID: emr-89319
Arq. bras. med. vet. zootec ; 59(4): 837-843, ago. 2007. tab
Article in Portuguese | LILACS | ID: lil-462174


Avaliou-se a inibição da produção do fator de necrose tumoral alfa (TNF-alfa) devido ao pré-tratamento com antiinflamatório esteroidal (dexametasona) e não esteroidal (diclofenaco sódico) em eqüinos com endotoxemia induzida experimentalmente. Foram utilizados 15 cavalos machos não castrados, distribuídos em três grupos de cinco animais: controle (C), diclofenaco sódico (DS) e dexametasona (DM). A endotoxemia subletal foi induzida pela infusão intravenosa (IV) de 0,1mg/kg/pv de lipopolissacarídeo (LPS) de Escherichia coli 055:B5, administrado em 250ml de solução estéril de cloreto de sódio a 0,9 por cento, durante 15min. Os cavalos do grupo-controle foram tratados com solução de cloreto de sódio a 9 por cento IV. Nos animais do grupo DS, administraram-se, por via oral, 2,2mg/kg de diclofenaco sódico e, nos do grupo DM, 1,1mg/kg de dexametasona IV, respectivamente, 60 e 30min antes da infusão da endotoxina. Mensurou-se, por meio de ensaio de toxicidade com células da linhagem L929, a concentração de TNF-alfa no soro e no líquido peritoneal às 0, 1», 3 e 6 horas após injeção do LPS. No grupo-controle, observou-se aumento significativo de TNF-alfa sérico, em relação ao valor basal e aos grupos DS e DM, 1,15 horas após a indução da endotoxemia. No líquido peritoneal, as concentrações observadas estavam abaixo daquelas da curva padrão de TNF-alfa, não havendo diferença entre os grupos (P>0,05)

The inhibition of tumor necrosis factor alpha (TNF-alpha) production due to pre-treatment with steroidal (dexamethazone) and non-steroidal (sodium diclofenac) anti-inflammatories was studied in horses under experimentally induced endotoxemy. Fifteen stallions were allotted into three groups of five animals each: control (C), sodium diclofenac (SD) and dexamethazone (DM). Sublethal endotoxemy was induced with 0.1mg/kg/bw Escherichia coli 055:B5 lipopolysaccharide (LPS), IV, administrated in 250ml of 0.9 percent sterile sodium chloride, during 15 minutes. Control group horses received 9 percent sodium chloride, IV. SD group animals were orally administrated 2.2mg/kg sodium diclofenac and DM horses received 1.1mg/kg dexamethazone, IV, 30 and 60 minutes before endotoxin infusion, respectively. TNF-alpha concentration was measured in serum and peritoneal fluid by toxicity assay using L929 lineage cells at 0, 1», 3 and 6 hours after LPS injection. Ninety minutes after endotoxemy induction, it was verified a significant increase of serum TNF-a concentration in horses from control group in relation to the basal values as well as results of horses from SD and DM groups. In peritoneal fluid, the measured concentrations were lower than those from TNF-a standard curve and difference among the groups was not verified (P>0.05)

Animals , Male , Anti-Inflammatory Agents , Cytokines/analysis , Dexamethasone/administration & dosage , Dexamethasone/adverse effects , Diclofenac/adverse effects , Endotoxemia/chemically induced , Escherichia coli/pathogenicity , Tumor Necrosis Factor-alpha/adverse effects , Horses
Rev. ciênc. farm. básica apl ; 28(1): 67-75, 2007. tab
Article in Portuguese | LILACS | ID: lil-485203


O estudo teve como objetivo descrever o padrão de uso de antiinflamatórios não-esteróides (AINE) por pacientes encaminhados para endoscopia digestiva alta no Hospital das Clínicas/UFMG, Belo Horizonte/MG. Trata-se de um estudo transversal de uma amostra de 533 pacientes com idade igual ou superior a 17 anos, com endoscopia previamente marcada. Os dados foram coletados por meio de questionário padronizado. As variáveis estudadas foram relativas aos antiinflamatórios não-esteróidese ao seu modo de uso. Cerca de 34% dos entrevistados relatou uso de AINE no período de um mês anterior à endoscopia. Os AINE mais utilizados foram o ácido acetilsalicílico e o diclofenaco e o uso caracterizou-se, principalmente, pela forma esporádica e por período inferior a sete dias. Entre os AINE que foram utilizados por período prolongado, foram mais frequentes o uso em dose diária elevada e o uso de mais de uma especialidade. Evidenciou-se um cenário de utilização inadequada destes medicamentos entre os pacientes estudados, caracterizado pelo uso de especialidades desaconselhadas, uso de AINE em indicações inadequadas, uso de associações medicamentos as questionáveis e uso desnecessário de especialidades dispendiosas em detrimento daquelas seguras e mais acessíveis. Os resultados apontam para a necessidade de estudos adicionais, a fim de maior aprofundamento no conhecimento dessa questão no Brasil.

The objective of this study was to describe the pattern of use of nonsteroidal anti-inflammatory drugs (NSAIDs) among patients referred for upper endoscopy at the Teaching Hospital of the Federal University of Minas Gerais, Belo Horizonte, Brazil. This cross-sectional survey included 533 patients, aged 17 or older, whose endoscopies had been previously scheduled. A standardized questionnaire was used to collect the data, which related to the nonsteroidal anti-inflammatory drugs taken and the way in which they were used. Almost 34% of the interviewed subjects reported having taken NSAIDs during the month prior to the endoscopy. The NSAIDs used most were acetylsalicylic acid and diclofenac and their pattern of use was characterized, in the main, by sporadic use over a period of less than seven days. Among the NSAIDs taken for long periods of time (> 30 dias), a commonly observed pattern was high daily doses and more than one kind of drug. The general picture that emerged was of inappropriate use of these medicines among the studied patients, typically the use of non-recommended types of drug, inappropriate use of NSAIDs for certain conditions, use of questionable drug combinations and the unnecessary use of expensive drugs despite the availability of safer and cheaper alternatives. The results point to the need to carry out more research, to improve our understanding of this question in Brazil.

Humans , Male , Female , Adolescent , Adult , Middle Aged , Anti-Inflammatory Agents, Non-Steroidal , Aspirin/administration & dosage , Aspirin/adverse effects , Aspirin/pharmacology , Aspirin/therapeutic use , Diclofenac/administration & dosage , Diclofenac/adverse effects , Diclofenac/pharmacology , Diclofenac/therapeutic use , Endoscopy, Digestive System/adverse effects , Hospitals, University
Clinics ; 61(5): 409-416, Oct. 2006. tab
Article in English | LILACS | ID: lil-436765


BACKGROUND: Nonsteroidal anti-inflammatory drugs are widely used in Brazil in spite of the known risks associated with their use, but investigation of their side effects conducted in this country has been far from sufficient. This study investigates the use of NSAIDs among patients undergoing upper endoscopy in the Hospital das Clínicas of the Federal University of Minas Gerais and the association of this use with the endoscopic diagnosis of gastric erosions, gastric erosions with hematin pigmentation, and gastric ulcer. METHODS: The cross-sectional methodological approach was used; 533 patients aged 17 or older were interviewed, between June and December, 2000. Data were submitted to bivariate and multivariate analyses. RESULTS: More than two thirds of the interviewed population reported the use of nonsteroidal anti-inflammatory drugs in a period of 1 month before the upper endoscopy. The most used nonsteroidal anti-inflammatory drugs were acetylsalicylic acid and diclofenac. An association was clearly shown between the use of these drugs and the occurrence of the studied lesions, with the latter attaining significance. There was also a significant association between nonsteroidal anti-inflammatory drugs use for a period greater than 15 days and the occurrence of the gastric lesions, with a higher odds ratio than for the other comparisons. CONCLUSIONS: The results suggest that nonsteroidal anti-inflammatory drugs have a significant association with the occurrence of the gastric lesions and point to the need of further study of this issue in Brazil.

INTRODUÇÃO: No Brasil são bastante evidentes os riscos associados ao uso de medicamentos. No entanto, tal questão não é devidamente privilegiada no campo da investigação científica. O presente estudo se refere ao uso de antiinflamatórios não-esteróides, fármacos amplamente utilizados no país. O objetivo foi investigar o uso de antiinflamatórios não-esteróides entre pacientes submetidos à endoscopia digestiva alta no Hospital das Clínicas da Universidade Federal de Minas Gerais e sua associação com a ocorrência de erosões gástricas, erosões gástricas com pigmento de hematina e úlcera gástrica. MÉTODOS: Estudo transversal em que 533 pacientes com idade igual ou superior a 17 anos foram entrevistados no período de junho a dezembro de 2000. Os dados foram submetidos às análises bivariada e multivariada. RESULTADOS: Mais de dois terços da população entrevistada relatou o uso de antiinflamatórios não-esteróides no período de um mês anterior à endoscopia digestiva alta. Os antiinflamatórios mais utilizados foram o ácido acetilsalicílico e o diclofenaco. Evidenciou-se uma associação positiva e significativa entre o uso desses fármacos e a ocorrência das lesões em questão. Ao se avaliar a associação entre o uso de antiinflamatórios não-esteróides por um período superior a 15 dias e a ocorrência das lesões gástricas, esta foi positiva e significativa, apresentado odds ratio superiores àqueles apresentados para as associações anteriores. CONCLUSÕES: Os resultados sugerem que os antiinflamatórios não-esteróides têm uma associação significativa com a ocorrência de lesões gástricas e apontam para a necessidade de aprofundamento no estudo desta questão no Brasil.

Humans , Middle Aged , Anti-Inflammatory Agents, Non-Steroidal/adverse effects , Drug Utilization/statistics & numerical data , Duodenal Ulcer/chemically induced , Endoscopy, Gastrointestinal , Gastric Mucosa/injuries , Stomach Ulcer/chemically induced , Anti-Inflammatory Agents, Non-Steroidal/administration & dosage , Aspirin/administration & dosage , Aspirin/adverse effects , Brazil/epidemiology , Diclofenac/administration & dosage , Diclofenac/adverse effects , Duodenal Ulcer/epidemiology , Epidemiologic Methods , Gastric Mucosa/drug effects , Hemin/chemistry , Hospitals, University/statistics & numerical data , Socioeconomic Factors , Stomach Ulcer/epidemiology
Rev. ciênc. farm. básica apl ; 26(3): 189-193, 2005.
Article in Portuguese | LILACS | ID: lil-458678


Mostrou-se que o pré-tratamento com as vitaminas tiamina[B1], piridoxina[B6] e cianocobalamina [B12], isoladas ou administradas conjuntamente, não inibiu o edema de pata produzido pela carragenina em ratos, nem as contorções abdominais produzidas pelo ácido acético em camundongos.Por outro lado, o diclofenaco [25 ou 50mg/kg] ou talidomida [45mg/kg] inibiram o edema de pata em ratos, e a associação das três vitaminas à estas drogas, mas não as vitaminas administradas isoladamente, potencializou os efeitos do diclofenaco [25 ou 50mg/kg] no tempo de quatro horas e a talidomida [45mg/kg], nos tempos de duas, três e quatro horas após a carragenina.As contorções abdominais em camundongos foram inibidas pelas doses de 25 ou 50mg/ kg de diclofenaco.A associação das três vitaminas ou apenas da cianocobalamina, potencializou as duas doses do diclofenaco utilizadas.As contorções abdominais foram inibidas também pela talidomida [45mg/kg] e a associação das três vitaminas, ou cada uma das vitaminas administradas isoladamente, foram capazes de potencializar os efeitos da talidomida.É provável que a diferença no mecanismo de ação destas drogas seja responsável por esta diferença dos efeitos das vitaminas.O presente estudo preconiza o uso de antiinflamatórios, combinados com as vitaminas tiamina[B1], piridoxina[B6] e cianocobalamina [B12], em doenças crônicas, diminuindo assim a dose destas drogas e seus efeitos colaterais

Animals , Diclofenac/adverse effects , Diclofenac/therapeutic use , Pyridoxine/adverse effects , Thalidomide/adverse effects , Thalidomide/therapeutic use , Thiamine/adverse effects , /adverse effects , Anti-Inflammatory Agents , Chronic Disease/therapy