Migración de neutrófilos en larvas de pez cebra expuestos a extractos de sofrito de tomate / Neutrophils migration in zebrafish larvae exposed to tomato sofrito extracts

Este trabajo se fundamenta en la evaluación de la actividad antiinflamatoria de extractos de sofrito de tomate, así como de compuestos estándares de la dieta mediterránea, usando un modelo experimental optimizado basado en larvas de pez cebra. La migración de neutrófilos en larvas de pez cebra de 96 horas post fertilización se indujo mediante una lesión y se potenció añadiéndole lipopolisacárido, dicha migración se visualizó y cuantificó mediante análisis de imagen. El efecto antiinflamatorio del extracto de tomate y de los compuestos utilizados fue correlacionado porcentualmente por la disminución de la migración de los neutrófilos. Los resultados muestran que el extracto de tomate presentó una reducción en la migración de neutrófilos de 40 % respecto al grupo control. Por otra parte, el ácido clorogénico y la cianidina presentes en el sofrito de tomate utilizados como estándares presentaron una disminución de la migración de neutrófilos de un 66,7 % y 62,5 % respectivamente. Estos porcentajes son comparables a los resultados observados en ensayos con drogas antiinflamatorias como la indometacina y piroxicam. Los resultados muestran que el extracto de sofrito de tomate presenta posible actividad antinflamatoria demostrada por la reducción de la migración de neutrófilos, además el modelo se mostró sensible y válido para ser aplicado en matrices alimentarias complejas(AU)

The main of this study was to evaluate the anti-inflammatory activity of tomato sofrito extracts, as well as standard compounds present in the Mediterranean diet, using an optimized experimental model based on zebrafish larvae. Neutrophil migration in zebrafish larvae 96 hours post fertilization was induced by a cut in the caudal fin and enhanced by adding lipopolysaccharide and was visualized and quantified by image analysis. The anti-inflammatory effect of tomato extract and the compounds used was correlated by the percentage decrease in the migration of neutrophils. The results showed that, tomato extract showed a reduction in neutrophil migration of 40% compared to the control group. Moreover, chlorogenic acid and cyanidin present in tomato sofrito sauce showed a decrease in neutrophil migration of 66.7% and 62.5% respectively. These percentages are comparable to the results observed in trials with anti-inflammatory drugs such as indomethacin and piroxicam. The results show that tomato sofrito extract has possible anti-inflammatory activity demonstrated by the reduction of neutrophil migration, furthermore the model was sensitive and valid to be applied in complex food matrices(AU)

Preemptive use of piroxicam on tooth sensitivity caused by in-office bleaching: a randomized clinical trial

Abstract This clinical trial evaluated the effect of preemptive use of the non-steroidal anti-inflammatory drug piroxicam in a single dose 30 min prior to in-office bleaching on the prevention of tooth sensitivity (TS) reported by patients. Fifty patients were submitted to two sessions of in-office tooth bleaching with 35% hydrogen peroxide used for 2 sessions, each consisting of a single 45-min application, with an interval of 7 days between session. Thirty minutes prior to the procedure, the patient randomly received a single dose of piroxicam (200 mg) or placebo in a double-blind, randomized, crossover design. The TS was evaluated using verbal rate (VRS) and visual analog (VAS) scales during the bleaching procedure and at 24 h after each session. The color changes were assessed by the Vita Bleachedguide scale 1 week after each bleaching session. Risk of TS was calculated from the VRS and analyzed by the McNemar test, while the level of TS was analyzed by the Mann-Whitney test. For the VAS, t-tests were used to compare data from the treatments at each assessment time. Data regarding color changes were subjected to Wilcoxon and Mann-Whitney tests (α=0.05). The preemptive administration of piroxicam did not affect the risk and level of TS compared to placebo, irrespective of the assessment time. The treatment sequence did not affect bleaching effectiveness. In conclusion, the administration of a single dose of piroxicam prior to in-office tooth bleaching was unable to significantly reduce the risk and level of TS.

Resumo Este ensaio clínico avaliou o efeito do uso preemptivo do anti-inflamatório não-esteroidal piroxicam em dose única 30 minutos antes do clareamento de consultório na prevenção de sensibilidade dentária (SD) relatada pelos pacientes. Cinquenta pacientes foram submetidos a duas sessões de clareamento dental em consultório com peróxido de hidrogênio a 35% por 2 sessões, consistindo de aplicação única de 45 minutos, com um intervalo de 7 dias entres as sessões. Trinta minutos antes do procedimento, o paciente recebia aleatoriamente dose única de piroxicam (200 mg) ou do placebo em um desenho duplo-cego, randomizado e cruzado. A SD foi avaliada usando a escalas de gradação verbal (EGV) e visual analógica (EVA) durante o procedimento clareador e 24h após o procedimento. As mudanças de cor foram avaliadas usando a escala Vita Bleachedguide uma semana após cada sessão de clareamento. O risco de SD foi calculado a partir de EGV a analisado pelo teste de McNemar, enquanto o nível de SD foi analisada pelo teste de Mann-Whitney. Para EVA, testes T foram usados para comparar dados dos tratamentos em cada tempo de avaliação. Dados de mudança de cor foram submetidos aos testes de Wilcoxon e Mann-Whitney (α=0.05). A administração preemptiva de piroxicam não afetou o risco e nível de SD quando comparado ao placebo, independentemente do tempo de avaliação. A sequencia de tratamento não afetou a efetividade do clareamento. Como conclusão, a administração de dose única de piroxicam previamente ao clareamento dental de consultório não foi efetiva em reduzir significantemente o risco e nível de SD.

Ultrasonographic assessment of transitional cell carcinoma of the urinary bladder in dogs: a perspective of tumor size change

Study purposes were to evaluate ultrasonographic characteristics of transitional cell carcinoma (TCC) and quantitate bladder tumor size in dogs. Heterogeneous mass, wall involvement, and broad-based attachment were significantly associated with TCC, but not prominently the trigone region. Mass size evaluation revealed a significant correlation between progressive disease (PD) in TCC patients with piroxicam therapy. Largest diameter of target lesion/body weight (cm/kg) ratio showed a high mean value in PD. A value > 0.3 was associated with PD with 83% sensitivity and 66% specificity. The results suggest that ultrasonography can provide evidence for diagnosing and predicting a prognosis for TCC.

Comparison of tramadol and lornoxicam in intravenous regional anesthesia: a randomized controlled trial / Comparação de tramadol e lornoxicam em anestesia regional por via intravenosa, um estudo randomizado e controlado

BACKGROUND AND OBJECTIVES: Tourniquet pain is one of the major obstacles for intravenous regional anesthesia. We aimed to compare tramadol and lornoxicam used in intravenous regional anesthesia as regards their effects on the quality of anesthesia, tourniquet pain and postoperative pain as well. METHODS: After the ethics committee approval 51 patients of ASA physical status I-II aged 18-65 years were enrolled. The patients were divided into three groups. Group P (n = 17) received 3 mg/kg 0.5% prilocaine; group PT (n = 17) 3 mg/kg 0.5% prilocaine + 2 mL (100 mg) tramadol and group PL (n = 17) 3 mg/kg 0.5% prilocaine + 2 mL (8 mg) lornoxicam for intravenous regional anesthesia. Sensory and motor block onset and recovery times were noted, as well as tourniquet pains and postoperative analgesic consumptions. RESULTS: Sensory block onset times in the groups PT and PL were shorter, whereas the corresponding recovery times were longer than those in the group P. Motor block onset times in the groups PT and PL were shorter than that in the group P, whereas recovery time in the group PL was longer than those in the groups P and PT. Tourniquet pain onset time was shortest in the group P and longest in the group PL. There was no difference regarding tourniquet pain among the groups. Group PL displayed the lowest analgesic consumption postoperatively. CONCLUSION: Adding tramadol and lornoxicam to prilocaine for intravenous regional anesthesia produces favorable effects on sensory and motor blockade. Postoperative analgesic consumption can be decreased by adding tramadol and lornoxicam to prilocaine in intravenous regional anesthesia.

JUSTIFICATIVA E OBJETIVOS: A dor relacionada ao torniquete é um dos maiores obstáculos para a anestesia regional intravenosa (ARIV). Nosso objetivo foi comparar tramadol e lornoxicam usados em ARIV em relação aos seus efeitos sobre a qualidade da anestesia, dor relacionada ao torniquete e dor no pós-operatório. MÉTODOS: Após a aprovação do Comitê de Ética, 51 pacientes com estado físico ASA I-II entre 18-65 anos foram inscritos. Os pacientes foram divididos em três grupos. Grupo P (n = 17) recebeu 3 mg/kg de prilocaína a 0,5%; Grupo PT (n = 17) 3 mg/kg de prilocaína a 0,5% + 2 mL (100 mg) de tramadol e Grupo PL (n = 17) de 3 mg/kg de prilocaína a 0,5% + 2 mL (8 mg) de lornoxicam para ARIV. O início do bloqueio sensorial e motor e os tempos de recuperação foram registrados, bem como a dor relacionada ao torniquete e o consumo de analgésico no pós-operatório. RESULTADOS: Os tempos de início do bloqueio sensorial foram mais curtos nos grupos PT e PL, enquanto que os tempos de recuperação correspondentes foram mais longos do que os do Grupo P. Os tempos de início do bloqueio motor nos grupos PT e PL foram menores do que no Grupo P, enquanto que o tempo de recuperação do grupo PL foi maior do que os dos grupos P e PT. O tempo para início da dor relacionada ao torniquete foi menor no Grupo P e maior no Grupo PL. Não houve diferença em relação à dor relacionada ao torniquete entre os grupos. O Grupo PL apresentou o menor consumo de analgésicos no pós-operatório. CONCLUSÃO: A adição de tramadol e lornoxicam à prilocaína para ARIV produz efeitos favoráveis sobre o bloqueio sensorial e motor. O consumo de analgésicos no pós-operatório pode ser reduzido com a adição de tramadol e lornoxicam à prilocaína em ARIV.

Effective method for the detection of piroxicam in human plasma using HPLC

Abstract Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used by the general population to alleviate inflammation and pain after oral surgeries. Piroxicam is among the most commonly used NSAIDs and excels in controlling pain, swelling, trismus and other common symptoms of inflammation. This study aimed to evaluate different concentrations of piroxicam and its major metabolite, 5'-hydroxypiroxicam, in human plasma samples over time using high performance liquid chromatography (HPLC) after liquid-liquid extraction. Briefly, 10 volunteers participated in this study after approval by the Ethics Committee of Bauru School of Dentistry, Universidade de São Paulo - USP, Brazil. Volunteers received a single dose oral of piroxicam (20 mg) and had blood collected at various times following an established protocol. The methodology of liquid-liquid extraction was effective for determining concentrations of piroxicam in plasma using HPLC in 10 out of 10 volunteers while 5'-hydroxypiroxicam was only detected in 2 out of 10 volunteers.

Comparison of the effectivity of oral and intra-articular administration of tenoxicam in patients with knee osteoarthritis / Comparação da eficácia de tenoxicam administrado por via oral e intra-articular a pacientes com osteoartrite de joelhos

ABSTRACTBACKGROUND AND OBJECTIVES:Tenoxicam is widely used in osteoarthritis treatment and we aimedto compare the effectivity of oral and intra-articular administration of tenoxicam in osteoarthri-tis treatment.METHODS: This study was performed between 2011 and 2012 by retrospectively analyzing andcomparing the findings of 60 patients who were clinically and radiologically diagnosed with kneedegenerative osteoarthritis in Bünyan state hospital pain policlinic. 60 patients included in thestudy were divided into two groups. The first group (tenoxicam IA, n = 30) included patientfindings of those subjected to intra-articular injection of 20 mg tenoxicam to the knee oncea week for three weeks and the second group (oral tenoxicam, n = 30) included patients whowere administered 20 mg oral tenoxicam once a day for three weeks. All patients were clini-cally evaluated pre-treatment and in the 1st week, 1st month and 3rd month post-treatmentaccording to specified criteria.RESULTS AND CONCLUSIONS: Twenty two of 60 patients included in the study were male and 38were female. In both groups significant improvements were detected in all of the observedparameters: visual analog scale, Western Ontario McMaster Osteoarthritis Index (pain, physicalactivity, knee stiffness) and Lequesne index scores and in the evaluations performed in 1st week,1st month and 3rd month with respect to pre-treatment values. Besides, a better complianceto treatment and gastrointestinal system tolerability in tenoxicam IA group was also observed.Intra-articular tenoxicam administration could be thought as an alternative treatment methodin patients with knee osteoarthritis who cannot use oral tenoxicam especially due to systemicgastrointestinal system side effects and those who have difficulties in adapting to treatment.

RESUMOJUSTIFICATIVA E OBJETIVOS: Tenoxicam é amplamente usado no tratamento da osteoartrite (OA)e o nosso objetivo foi comparar a eficácia de tenoxicam administrado por via oral (VO) e intra-articular (IA) no tratamento da OA.MÉTODOS: Este estudo foi conduzido entre 2011 e 2012 por meio de análise retrospectiva ecomparação dos resultados de 60 pacientes que foram clínica e radiologicamente diagnosticadoscom OA degenerativa de joelhos na Policlínica de Tratamento da Dor do Hospital Estadual deBünyan. Os 60 pacientes incluídos no estudo foram alocados em dois grupos. O primeiro grupo(tenoxicam IA, n = 30) incluiu resultados de pacientes submetidos à injeção nos joelhos porvia IA de 20 mg de tenoxicam uma vez por semana durante três semanas e o segundo grupo(tenoxicam VO, n = 30) incluiu pacientes que receberam 20 mg de tenoxicam por VO uma vezpor dia durante três semanas. Todos os pacientes foram avaliados clinicamente na fase basalpré-tratamento e em uma semana, um mês e três meses pós-tratamento, de acordo com oscritérios especificados.RESULTADOS E CONCLUSÕES: Dos 60 pacientes, 22 eram do sexo masculino e 38 do sexo feminino.Em ambos os grupos, melhorias significativas foram detectadas em todos os parâmetros da escalavisual analógica, do índice Western Ontario and MacMaster (Womac --- dor, atividade física erigidez dos joelhos) e do índice de Lequesne nas avaliações feitas em uma semana, um mês etrês meses e comparadas aos valores basais. Além disso, uma melhor adesão ao tratamento etolerabilidade ao sistema gastrointestinal no grupo tenoxicam IA também foram observadas. Aadministração de tenoxicam IA pode ser considerada como um método opcional de tratamentoem pacientes com OA de joelhos que não podem usar tenoxicam por VO, especialmente porcausa dos efeitos colaterais sobre o sistema gastrintestinal, e naqueles com dificuldades de adaptação ao tratamento.

Comparison of different postoperative paın managements in patients submitted to transperitoneal laparoscopic renal and adrenal surgery

ABSTRACTPurpose:We compared the effects of local levobupivacaine infiltration, intravenous paracetamol, intravenous lornoxicam treatments on postoperative analgesia in patients submitted to transperitoneal laparoscopic renal and adrenal surgery.Materials and Methods:Sixty adult patients 26 and 70 years who underwent laparoscopic renal and adrenal surgery were randomized into three groups with 20 patients each: Group 1 received local 20mL of levobupivacaine 0.25% infiltration to the trocar incisions before skin closure. In group 2, 1g paracetamol was given to the patients intravenously 30 minutes before extubation and 5g paracetamol was given intravenoulsy in the 24 postoperative period. In group 3, 8mg lornoxicam i.v. was given 30 minutes before extubation and 8mg lornoxicam i.v. was given in the 24 postoperative period. In the postoperative period, pain scores, cumulative tramadol, and additional pethidine consumption were evaluated.Results:Postoperative pain scores significantly reduced in each group (p < 0.05). Although pain levels of the groups were not significantly different at 1, 2, 4, 8, 12 and 24 hours postoperatively, cumulative tramadol consumptions were higher in group 1 than the others. (Group 1 = 370.6 ± 121.6mg, Group 2: 220.9 ± 92.5mg, Group 3 = 240.7 ± 100.4mg.) (p < 0.005). The average dose of pethidine administered was significantly lower in groups 2 and 3 compared with group 1 (Group 1: 145mg, Group 2: 100mg, Group 3: 100mg) (p = 0.024).Conclusions:Levobupivacaine treated group required significantly more intravenous tramadol when compared with paracetamol and lornoxicam groups in patients submitted to transperitoneal laparoscopic renal and adrenal surgery.

Evaluation of protein undernourishment on the condylar process of the Wistar rat mandible correlation with insulin receptor expression

The mandible condylar process cartilage (CP) of Wistar rats is a secondary cartilage and acts as a mandibular growth site. This phenomenon depends on adequate proteins intake and hormone actions, including insulin. Objectives The present study evaluated the morphological aspects and the expression of the insulin receptor (IR) in the cartilage of the condylar process (CP) of rats subjected to protein undernourishment. Material and Methods The nourished group received a 20% casein diet, while the undernourished group (U) received a 5% casein diet. The re-nourished groups, R and RR, were used to assess the effects of re-nutrition during puberty and adulthood, respectively. CPs were processed and stained with picro-sirius red, safranin-O and azocarmine. Scanning electron microscopy and immunohistochemistry were also performed. Results The area of the CP cartilage and the number of cells in the chondroblastic layer decreased in the U group, as did the thickness of the CP layer in the joint and hypertrophic layer. Renourishment during the pubertal stage, but not during the adult phase, restored these parameters. The cell number was restored when re-nutrition occurred in the pubertal stage, but not in the adult phase. The extracellular matrix also decreased in the U group, but was restored by re-nutrition during the pubertal stage and further increased in the adult phase. IR expression was observed in all CPs, being higher in the chondroblastic and hypertrophic cartilage layers. The lowest expression was found in the U and RR groups. Conclusions Protein malnutrition altered the cellularity, the area, and the fibrous cartilage complex, as well as the expression of the IRs. .

Cirurgia reconstrutiva com retalho cutâneo de avanço como técnica alternativa para tratamento de carcinoma de células escamosas em cães: relato de caso / Reconstructive surgery with skin flap advance as alternative technique for treating squamous cell carcinoma in dog: case report

O carcinoma de células escamosas (CCE) é uma das neoplasias mais frequentemente observadas no trato genital de cães. O tratamento de eleição para o CCE é a exérese com ampla margem cirúrgica (1 a 3 cm), porém quando a região prepucial está comprometida, se torna difícil obter margem adequada, tanto pela anatomia da região quanto pelas características agressivas dessa neoplasia. A penectomia com uretrostomia pré-escrotal seria a técnica mais indicada nesses casos, entretanto, complicações pós-cirúrgicas podem reduzir a qualidade e a expectativa de vida do animal. O objetivo deste relato foi demonstrar uma técnica cirúrgica conservativa, com base em plásticas reconstrutivas com retalhos cutâneos, como tratamento para CCE em prepúcio e região inguinal, associada ao uso do piroxicam como terapia adjuvante. O animal não apresentou recidiva do tumor ou complicações secundárias ao tratamento até a última avaliação, um ano após o término do tratamento.

Squamous cell carcinoma (SCC) is one of the most frequently neoplasms observed in genital tract in dogs. The treatment of choice for the CCE is the excision with wide surgical margin (1-3 cm), but when the foreskin region is committed becomes difficult to obtain adequate margin, due both the anatomy of the region and the aggressive characteristics of this neoplasm. The penectomy with pre-scrotal urethrostomy would be the most suitable technique in such cases, however, postoperative complications may reduce the quality and expectancy of life. The objective of this report was to present a conservative surgical technique, based on reconstructive plastic with skin flap as a treatment for SCC in prepuce and inguinal region, associated with the use of piroxicam as adjuvant therapy. The dog was evaluated during one year after the end of treatment and haven't showed any tumor recurrence or secondary complications to treatment.

Formulation and evaluation of mini-tablets-filled-pulsincap delivery of lornoxicam in the chronotherapeutic treatment of rheumatoid arthritis

In this present research work, we have designed a pulsincap formulation comprising mini-tablets, which to the best of our knowledge this combination has not been reported yet. We successfully combined the advantages of minitablets technology to meet the optimized requirements of our pulsincap formulation. Our main aim was to target lornoxicam to treat rheumatoid arthritis as per the chronotherapeutic pattern of the disease. Directly compressing method was used to prepare mini-tablets. The drug, polymers and combine mixtures of drug and polymers was evaluated for preformulation testing. Prepared mini-tablets were also evaluated for physicochemical, dissolution and stability studies. From FTIR and DSC evaluation, we found no interaction between the drug and polymers used. For mini-tablets, all the physico-chemical parameters were in limit. The mini-tablets of lornoxicam were filled into an insoluble body of capsule, and its opening was sealed by plugging it with a polymer. The complete capsule body after sealing with a cap was given enteric coating. Different polymers in various concentrations were used as a plug, to identify the most suitable which gives a complete lag time of 5 hours when combined with 5% CAP coating. HPMC-K100M in 30% and sodium alginate in 40% concentrations were identified as the most suitable plugs. Our optimized pulsincap formulations releases lornoxicam after a lag time of 5 hrs and maximum portion of the drug will be released in the early morning hours. It was also found to be stable for a period of 6 months as per ICH guidelines

Lornoxicam versus tramadol for post-operative pain relief in patients undergoing ENT procedures

Pain following ear-nose and throat surgery is one of the most important complaints for which, several drugs are used. This prospective, randomized, double-blind controlled trial was designed to compare the analgesic effect of tramadol versus lornoxicam for post-operative pain relief in patients undergoing ENT surgical procedures. One hundred and twenty patients of ASA class I-II, who had undergone elective ENT surgical procedures under general anesthesia, were assigned in a randomized manner into three equal groups. Group L received lornoxicam8 mg IV, Group T received tramadol 1 mg/kg IV and Group C received IV saline after induction of anesthesia before the start of the surgery. Post-operative pain was assessed using the visual analogue scale [VAS] and sedation level was evaluated during stay in the post-anesthesia care unit with a four-point sedation scale. Intraoperative blood loss was estimated using the Five-Point Scale. Adverse events in the first 24 h post-operative were recorded. The VAS pain scores were significantly higher in Group C as compared with those in Groups L and T at 30 min and 1, 2, 4and 6 h post-operatively, with no significant difference between Group L and Group T. The amount of morphine consumption post-operatively was significantly lower in Group L [5.2 +/- 2.5 mg] and Group T [5.0 +/- 2.0 mg] as compared with that in Group C [7.4 +/- 2.3 mg] [P = 0.001]. The time for the first analgesic requirement was significantly less in Group L [92.62 +/- 24.23 min] and Group T [88 +/- 21.43 min] as compared with that in Group C [42.82 +/- 25.61 min], with no significant difference between the other two groups. Estimated intraoperative blood loss score by the surgeons showed no significant difference between the three groups. The most frequent side-effects in the three groups were nausea and vomiting, and their incidence was significantly higher in the placebo group as compared with the other two groups. Tramadol 1 mg/kg was comparable to lornoxicam 8 mg for post-operative pain relief in patients undergoing ENT surgical procedures; both drugs helped to reduce the post-operative opioid requirement and consequently minimized the related adverse effects of the opioids

Concentration of Non-Steroidal Anti-Inflammatory Drugs in the Pelvic Floor Muscles: An Experimental Comparative Rat Model

PURPOSE: The aim of this study is to explore non-steroid anti-inflammation drugs (NSAIDs) potency for pelvic floor muscle pain by measuring local concentration in a rat model. MATERIALS AND METHODS: We used nine NSAIDs, including nabumetone, naproxen, ibuprofen, meloxicam, piroxicam, diclofenac potassium, etodolac, indomethacin, and sulindac, and 9 groups of female Wister rats. Each group of rats was fed with one kind of NSAID (2 mg/mL) for three consecutive days. Thereafter, one mL of blood and one gram of pelvic floor muscle were taken to measure drug pharmacokinetics, including partition coefficient, lipophilicity, elimination of half-life (T1/2) and muscle/plasma converting ratio (Css, muscle/Css, plasma). RESULTS: Diclofenac potassium had the lowest T1/2 and the highest mean Css, muscle/Css, plasma (1.9 hours and 0.85+/-0.53, respectively). The mean Css, muscle/Css, plasma of sulindac, naproxen and ibuprofen were lower than other experimental NSAIDs. CONCLUSION: Diclofenac potassium had the highest disposition in pelvic floor muscle in a rat model. The finding implies that diclofenac potassium might be the choice for pain relief in pelvic muscle.

Comparison of Piroxicam Pharmacokinetics and Anti-Inflammatory Effect in Rats after Intra-Articular and Intramuscular Administration

This study evaluated the pharmacokinetic profile and therapeutic efficacy of piroxicam (PX), a long acting non-steroidal anti-inflammatory drug for the treatment of arthritis, following intra-articular (IA) injection in comparison to the pharmacokinetic profile and therapeutic efficacy of PX after intramuscular (IM) injection. In the pharmacokinetic study in rats, systemic exposure and pharmacokinetic parameters of PX after a single IA dose were compared with systemic exposure and pharmacokinetic parameters of PX after administration of the same dose IM (0.6 mg/kg). The anti-inflammatory and analgesic effects of IA PX were evaluated simultaneously in a monoiodoacetate-induced osteoarthritis rat model. The plasma PX concentration rapidly rose following IA injection, and it was comparable to the plasma PX concentration following IM injection, suggesting the rapid efflux of the drug molecule from the joint cavity. However, in the efficacy study, the IA PX administration significantly reduced the knee swelling by reducing the level of prostaglandin E2 in the joint, compared to that following administration of IA vehicle and after administration of the IM PX dose. In addition, we found that the anti-inflammatory and anti-nociceptive efficacies of IA PX were synergistically increased upon co-treatment with hyaluronic acid (HA), a potent agent for the treatment of osteoarthritis, at the weight ratio of 1:1 or 1:2, and these effects were more pronounced than those following administration of HA or PX alone. In conclusion, this study demonstrated the efficacy of the IA use of PX alone and/or in combination with HA in osteoarthritis.

Comparação de lornoxicam e fentanil adicionados à lidocaína em anestesia regional intravenosa / Comparison of lornoxicam and fentanyl when added to lidocaine in intravenous regional anesthesia / Comparación de lornoxicam y fentanilo adicionados a la lidocaína en la anestesia regional intravenosa

JUSTIFICATIVA E OBJETIVO: Comparar os efeitos analgésicos nos períodos intra e pós-operatório de lornoxicam e fentanil adicionados à lidocaína para anestesia regional intravenosa (ARIV) em um grupo de pacientes submetidos à cirurgia de mão. MÉTODOS: Estudo randômico, duplo-cego e controlado. Foram incluídos e randomizados 45 pacientes em três grupos: o Grupo I recebeu 3 mg.kg-1 de lidocaína a 2% (40 mL); o Grupo II recebeu 3 mg.kg-1 de lidocaína (38 mL) + 2 mL de lornoxicam; o Grupo III recebeu 3 mg.kg-1 de lidocaína (38 mL) + 2 mL de fentanil. O desfecho primário avaliado foi o tempo até a primeira necessidade de analgésicos no pós-operatório. RESULTADOS: Lornoxicam adicionado à lidocaína em ARIV aumentou o tempo de recuperação do bloqueio sensorial sem aumentar os efeitos colaterais, e o tempo até a primeira necessidade de analgésicos no pós-operatório em comparação com lidocaína sozinha (p < 0,001, p < 0,001, respectivamente) e fentanil adicionado à lidocaína (p < 0,001, p < 0,001, respectivamente). Além disso, também descobrimos que fentanil diminuiu a dor ocasionada pelo torniquete (p < 0,01) em comparação com lidocaína, mas mostrou efeito analgésico similar ao de lornoxicam (p > 0,05), embora os escores da escala visual analógica (EVA) relacionados à dor ocasionada pelo torniquete tenham sido menores no grupo fentanil. Lornoxicam adicionado à lidocaína em ARIV não foi superior à lidocaína sozinha para diminuir a dor ocasionada pelo torniquete. CONCLUSÃO: A adição de fentanil à lidocaína em ARIV parece ser superior à lidocaína sozinha e ao lornoxicam adicionado à lidocaína para diminuir a dor ocasionada pelo torniquete, apesar de aumentar os efeitos secundários. No entanto, lornoxicam não aumentou os efeitos secundários e proporcionou analgesia nos períodos tanto intraoperatório quanto pós-operatório. Portanto, lornoxicam pode ser mais adequado para o uso clínico.

BACKGROUND AND OBJECTIVES: In this study, our goal was to compare intraoperative and postoperative analgesic effects of lornoxicam and fentanyl when added to lidocaine Intravenous Regional Anesthesia (IVRA) in a group of outpatients who underwent hand surgery. METHODS: This is a double blind randomized study. A total of 45 patients were included, randomized into three groups. Patients in Group I (L) received 3 mg.kg-1 of 2% lidocaine 40 mL; patients in Group II (LL) received 3 mg.kg-1 lidocaine 38 mL + 2 mL lornoxicam; patients in Group III (LF) received 3 mg.kg-1 lidocaine 38 mL + 2 mL fentanyl. Our primary outcome was first analgesic requirement time at postoperative period. RESULTS: Lornoxicam added to lidocaine IVRA increased the sensory block recovery time without increasing side effects and increased first analgesic requirement time at the postoperative period when compared to lidocaine IVRA (p < 0.001, p < 0.001 respectively) and fentanyl added to lidocaine IVRA (p < 0.001, p < 0.001 respectively). In addition, we also found that fentanyl decreased tourniquet pain (p < 0.01) when compared to lidocaine but showed similar analgesic effect with lornoxicam (p > 0.05) although VAS scores related to tourniquet pain were lower in fentanyl group. Lornoxicam added to lidocaine IVRA was not superior to lidocaine IVRA in decreasing tourniquet pain. CONCLUSIONS: Addition of fentanyl to lidocaine IVRA seems to be superior to lidocaine IVRA and lornoxicam added to lidocaine IVRA groups in decreasing tourniquet pain at the expense of increasing side effects. However, lornoxicam did not increase side effects while providing intraoperative and postoperative analgesia. Therefore, lornoxicam could be more appropriate for clinical use.

JUSTIFICATIVA Y OBJETIVO: Comparar los efectos analgésicos en los períodos intra y postoperatorio del lornoxicam y del fentanilo adicionados a la lidocaína para la anestesia regional intravenosa (ARIV), en un grupo de pacientes sometidos a la cirugía de mano. MÉTODOS: Estudio aleatorio, doble ciego y controlado. Fueron incluidos y aleatorizados por el equipo de investigación 45 pacientes en tres grupos: el Grupo I recibió 3 mg.kg-1 de lidocaína al 2% (40 mL); el Grupo II recibió 3 mg.kg-1 de lidocaína (38 mL) + 2 mL de lornoxicam; el Grupo III recibió 3 mg.kg-1 de lidocaína (38 mL) + 2 mL de fentanilo. El resultado primario evaluado fue el tiempo hasta la primera necesidad de analgésicos en el postoperatorio. RESULTADOS: El Lornoxicam adicionado a la lidocaína en ARIV aumentó el tiempo de recuperación del bloqueo sensorial, sin aumentar los efectos colaterales y el tiempo hasta la primera necesidad de analgésicos en el postoperatorio en comparación con la lidocaína sola (p < 0,001, p < 0,001, respectivamente) y el fentanilo adicionado a la lidocaína (p < 0,001, p < 0,001, respectivamente). Además de eso, también descubrimos que el fentanilo redujo el dolor ocasionado por el torniquete (p < 0,01) en comparación con la lidocaína, pero mostró un efecto analgésico parecido con el del lornoxicam (p > 0,05), aunque las puntuaciones de la escala visual analógica (EVA) relacionadas con el efecto ocasionado por el torniquete, hayan sido menores en el grupo fentanilo. El Lornoxicam adicionado a la lidocaína en ARIV no fue superior a la lidocaína sola para reducir el dolor ocasionado por el torniquete. CONCLUSIÓN: Podemos decir que la adición del fentanilo a la lidocaína en ARIV parece ser superior a la lidocaína sola y al lornoxicam adicionado a la lidocaína para disminuir el dolor ocasionado por el torniquete, a pesar de aumentar los efectos secundarios. Sin embargo, el lornoxicam no aumentó los efectos secundarios, proporcionando una analgesia en los períodos tanto intraoperatorio como postoperatorio. Por tanto, el lornoxicam puede ser más adecuado para el uso clínico.

Clinical study of analgesic effect of lornoxicam in nasal packing / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To explore the pain control effect of lornoxicam on patients after nasal packing.@*METHOD@#A total of 56 patients undergoing nasal packing between January 2011 and August 2011 were randomly divided into the treatment group and control group. (1) Treatment group: routinely given lornoxicam for injection 8 mg(2 ml), intravenous injection, twice a day; (2) CONTROL GROUP: given saline 2 ml, intravenous injection, twice a day, other treatments are the same with the treatment group. Visual analog scale was used to record the painful severity of nose and head at 3, 6, 12, 24 and 48 h,and record the sleep quality score at 24 and 48 h.@*RESULT@#The pain in nose and head and night sleeping in treatment group were all significantly better than that in control group.@*CONCLUSION@#The analgesic effect of lornoxicam in nasal packing is good, with no evident adverse reactions.

A Randomized, Open Label, 2-Way Crossover Study to Assess the Pharmacokinetic Characteristics and Skin Irritation of Murupe(R) Patch Compared with Trast(R) Patch in Healthy Volunteers

BACKGROUND: A piroxicam patch has been widely used to treat musculoskeletal pain. The aim of this study was to assess the pharmacokinetic (PK) characteristics and skin irritation of Murupe(R) patch (piroxicam 96 mg) compared with Trast(R) patch (piroxicam 96 mg) in healthy volunteers. METHODS: A randomized, open-label, 2-way crossover study was conducted in 12 healthy Korean male subjects. They were allocated to one of the two treatment sequences of RT and TR (R, reference drug, Trast(R) patch; T, test drug, Murupe(R) patch). Each patch was applied to the subject once during 48 hours. Serial blood samples were collected up to 72 hours after removing the patch and plasma concentrations were determined by high performance liquid chromatography. Safety was monitored and the skin irritation potential was assessed. RESULTS: The plasma concentration-time profile during 48 hours showed an exponential increase in both of two patch products. Mean C(max) and AUC(last) values were not statistically different between two patch groups. Mean AUC[0-48h] was lower in Murupe(R) patch group than that in Trast(R) patch group; 806.4 and 1196.5 ng.h/mL. However, the mean AUC[48-120h] value tended to be higher in Murupe(R) patch group, implying more delayed excretion than in Trast(R) patch group; 2724.7 ng.h/mL and 1989.2 ng.h/mL. The overall results of skin irritation potential test showed no clinically significant differences between two patch groups. CONCLUSION: Mean Cmax and AUC(last) values in Murupe(R) patch group were comparable to those in Trast(R) patch group. Murupe(R) patch was safe and well tolerated in healthy male subjects.

Quantitation of meloxicam in the plasma of koalas (Phascolarctos cinereus) by improved high performance liquid chromatography

An improved method to determine meloxicam (MEL) concentrations in koala plasma using reversed phase high performance liquid chromatography equipped with a photo diode array detector was developed and validated. A plasma sample clean-up step was carried out with hydrophilic-lipophilic copolymer solid phase extraction cartridges. MEL was separated from an endogenous interference using an isocratic mobile phase [acetonitrile and 50 mM potassium phosphate buffer (pH 2.15), 45:55 (v:v)] on a Nova-Pak C18 4-microm (300 x 3.9 mm) column. Retention times for MEL and piroxicam were 8.03 and 5.56 min, respectively. Peak area ratios of MEL to the internal standard (IS) were used for regression analysis of the calibration curve, which was linear from 10 to 1,000 ng/mL (r2 > 0.9998). Average absolute recovery rates were 91% and 96% for MEL and the IS, respectively. This method had sufficient sensitivity (lower quantitation limit of 10 ng/mL), precision, accuracy, and selectivity for routine analysis of MEL in koala plasma using 250-microL sample volumes. Our technique clearly resolved the MEL peak from the complex koala plasma matrix and accurately measured MEL concentrations in small plasma volumes.

Quantitation of meloxicam in the plasma of koalas (Phascolarctos cinereus) by improved high performance liquid chromatography

An improved method to determine meloxicam (MEL) concentrations in koala plasma using reversed phase high performance liquid chromatography equipped with a photo diode array detector was developed and validated. A plasma sample clean-up step was carried out with hydrophilic-lipophilic copolymer solid phase extraction cartridges. MEL was separated from an endogenous interference using an isocratic mobile phase [acetonitrile and 50 mM potassium phosphate buffer (pH 2.15), 45:55 (v:v)] on a Nova-Pak C18 4-microm (300 x 3.9 mm) column. Retention times for MEL and piroxicam were 8.03 and 5.56 min, respectively. Peak area ratios of MEL to the internal standard (IS) were used for regression analysis of the calibration curve, which was linear from 10 to 1,000 ng/mL (r2 > 0.9998). Average absolute recovery rates were 91% and 96% for MEL and the IS, respectively. This method had sufficient sensitivity (lower quantitation limit of 10 ng/mL), precision, accuracy, and selectivity for routine analysis of MEL in koala plasma using 250-microL sample volumes. Our technique clearly resolved the MEL peak from the complex koala plasma matrix and accurately measured MEL concentrations in small plasma volumes.

Comparison efficacy of topical piroxicam gel and lidocaine with intravenous pethidine in reducing pain during Eswl

ESWL is a non-invasive method of breaking stones, using acoustic shock waves. Shock waves cause temporary deep visceral pain and discomfort in entry; therefore, administration of sedatives is necessary. The purpose of this study was to compare the effect of topical lidocaine and piroxicam gel with intravenous pethidine in reducing pain during ESWL. This clinical trial study was performed on 159 patients who referred to Ayatollah Kashani Hospital in Shahrkord for ESWL in 2009. Patients were randomly divided into three-groups. For the first group, intravenous pethidine [0.5 mg/kg alone] was administered. The second group received topical piroxicam, and the third group received topical lidocaine in the area of flank for half an hour before ESWL. During the operation, those patients who had unbearable pain, received another 0.5 mg/kg of pethidine. Data was collected using MC Gill questionnaires and analyzed using the SPSS software, using parametric, nonparametric methods and Dunn's Multiple Comparisons tests. The mean of pain scores in the first group [pethidine] was 6.2 +/- 6.9 while these scores were 3.2 +/- 2 .7 and 3.9 +/- 3.1 for the second [piroxicam gel] and third group [lidocaine gel] respectively. The differences in the mean score of pain was significant in the pethidine group compared to the other groups [P <0.05]. The average pethidin consumption were 24 +/- 16 mg for the first group [pethidine], 10 +/- 13 mg for the second group [piroxicam gel], and 5 +/- 9 mg for the third group [lidocaine gel]. The mean difference was significant in pethidine treated group in comparison with other two groups [P < 0.05]. The use of topical piroxicam or lidocaine reduces pain in patients after ESWL It also reduces the need for sedative drugs