Use Of Diclofenac Sodium Research Articles

Diclofenac sodium effectively inhibits the biofilm formation of Staphylococcus epidermidis.

Staphylococcus epidermidis is an opportunistic pathogen commonly implicated in medical device-related infections. Its propensity to form biofilms not only leads to chronic infections but also exacerbates the issue of antibiotic resistance, necessitating high-dose antimicrobial treatments. In this study, we explored the use of diclofenac sodium, a non-steroidal anti-inflammatory drug, as an anti-biofilm agent against S. epidermidis. In this study, crystal violet staining and confocal laser scanning microscope analysis showed that diclofenac sodium, at subinhibitory concentration (0.4 mM), significantly inhibited biofilm formation in both methicillin-susceptible and methicillin-resistant S. epidermidis isolates. MTT assays demonstrated that 0.4 mM diclofenac sodium reduced the metabolic activity of biofilms by 25.21-49.01% compared to untreated controls. Additionally, the treatment of diclofenac sodium resulted in a significant decrease (56.01-65.67%) in initial bacterial adhesion, a crucial early phase of biofilm development. Notably, diclofenac sodium decreased the production of polysaccharide intercellular adhesin (PIA), a key component of the S. epidermidis biofilm matrix, in a dose-dependent manner. Real-time quantitative PCR analysis revealed that diclofenac sodium treatment downregulated biofilm-associated genes icaA, fnbA, and sigB and upregulated negative regulatory genes icaR and luxS, providing potential mechanistic insights. These findings indicate that diclofenac sodium inhibits S. epidermidis biofilm formation by affecting initial bacterial adhesion and the PIA synthesis. This underscores the potential of diclofenac sodium as a supplementary antimicrobial agent in combating staphylococcal biofilm-associated infections.

Effect ratio of stearic acid and oleic acid on characteristics of diclofenac sodium nanostructured lipid carrier

Background: Osteoarthritis treatment generally involves using a Non-steroidal Anti-inflammatory Drug (NSAID), and the most common is Diclofenac sodium. The oral use of diclofenac sodium presents some adverse effects on the gastrointestinal tract. Trans-dermal diclofenac sodium's biological efficacy can be affected by factors including its log P value of 1.13. Nanostructured Lipid Carrier (NLC) may solve these concerns. Objective: This study examined how stearic and oleic acid concentrations customise diclofenac sodium NLC's physicochemical properties. Method: High shear homogenisation was used to compare stearic acid and oleic acid at 6:4, 7:3, and 8:2. Furthermore, the physicochemical properties of diclofenac sodium NLC were assessed, such as organoleptic, particle size and poly-dispersity index, pH, viscosity, zeta potential, entrapment efficiency, profiles of FTIR and DSC. Result: This study found that particle size ranged from 333.60 ± 144.29 to 791.77 ± 85.57, and entrapment efficiency was 89.38 ± 3.69 to 76.96 ± 3.29. Increasing the content of oleic acid as a liquid lipid reduces particle size and improves diclofenac sodium NLC entrapment. According to One-Way ANOVA, the dependent variable was not significantly affected by any independent variables (p-value > 0.05) except for particle size and entrapment efficiency. Conclusion: Stearic acid-oleic acid concentration ratios affect diclofenac sodium NLC's physicochemical properties.

Effects of non-steroidal anti-inflammatory agents on systemic hemostasis during the most acute period of cold injury in rats

Non-steroidal anti-inflammatory drugs (NSAIDs) have recently been considered promising agents for the prevention and treatment of cold injuries. The results of previous studies demonstrate a distinct frigoprotective effect of diclofenac sodium and etoricoxib.
 The aim of the study: to assess the impact of diclofenac sodium and etoricoxib, as the most effective frigoprotectors among NSAIDs, on coagulation indicators during the most acute phase of cold injuries using an acute model of general cooling in rats.
 Materials and Methods: The experiment was carried out using 41 outbreed male rats weighing 310±10 g. Cold injury was induced by acute general cooling (exposure to –18 °C for 2 hours). Diclofenac sodium (7 mg/kg) and etoricoxib (5 mg/kg) were administered intragastrically 30 minutes before the onset of cold exposure. Rectal temperature was measured before and after cold exposure. Immediately after exposure, plasma was used to determine prothrombin time (PT), thrombin time (TT), activated partial thromboplastin time (APTT), fibrinogen levels, and in blood serum – the residual amount of prothrombin, thrombin, fibrinogen, as well as D-dimer using species-specific immunoenzymatic analysis kits.
 Results: Etoricoxib and especially diclofenac sodium significantly reduced the degree of hypothermia (rectal temperature decreased by 1.3 % and 1.9 %, respectively, compared to a 5.4 % decrease in the control group, p < 0.05). In the acute phase of cold injury in the untreated control group, there was a significant increase in D-dimer (by 2.7 times) and fibrinogen content (by 1.9 times) in blood serum, alongside a 21.7 % increase in thrombin time, indicating a heightened risk of thrombus formation and DIC syndrome development. The other coagulation indicators did not show significant changes. Both diclofenac sodium and etoricoxib significantly reduced elevated D-dimer and serum fibrinogen, normalizing thrombin time and indicating an antithrombotic effect. There was no significant difference in the effect of both NSAIDs on blood coagulation status.
 Conclusions: The acute phase of cold injury demonstrates a dangerous shift in blood coagulation towards thrombus formation and DIC syndrome development. Prophylactic use of diclofenac sodium and, to a lesser extent, etoricoxib displays an anti-hypothermic effect, reducing the risk of thrombosis and DIC syndrome. This proves the expediency of using these NSAIDs for acute cold injury

Efficacy of Palashgudavarti and Diclofenac Sodium Suppository in the management of Acute fissure in ano

Introduction: Parikartika is most common ano-rectal disorder. The text of parikartika is mentioned in Samhitas. In this disease there are symptoms such as bleeding per rectum, hard stools, burning sensation around anal region. In this trial, group A (n=30) included Palashadigudavarti, whereas group B included Diclofenac sodium suppository for administration over Parikartika (acute anal fissures). Gandharva haritaki choorna acts as laxative and helps to relieve constipation and sitz bath was given to both group as conservative management.. Materials and method: Literary aspect of the study was collected from classical Ayurvedic and contemporary text and updated with recent medical journals, previous research work done on same topic. Observation and results: Assessment was done by the parameters such as pain, bleeding and itching as Subjective and healing as Objective Parameter. Results were obtained by statistical analysis. Discussion: In this research work Palash, Goghrita and Beewax as suppository base was used in the form of varti application (advanced anal Suppository) for managing Anal fissure. There is need of ayurvedic suppository easily available in market which will relieves anorectal symptoms instantly, because repeated use of diclofenac sodium have side effect to the body. In the present case series, it proved to be significant in managing Fissure in ano, it reduced pain, itching, bleeding and promoted healing. Conclusion: In the treatment of Parikartika, Palashadigudavarti was more effective than Diclofenac sodium suppository
 Keywords: Parikartika, fissure in ano, Palashadigudavarti, Diclofenac Sodium Suppository.

The debut of Schamberg disease (a clinical case)

A group of pigmented purpuric dermatoses includes a list of skin diseases characterized by multiple petechial hemorrhages, purpura, and increased skin pigmentation (yellow, brown, or red patchy). Schamberg disease is the most common representative of this group with a benign, chronic and recurrent course of idiopathic origin. The lesions are often asymptomatic or associated with mild pruritus, usually occurring on the lower extremities. The diagnosis is not a dilemma, as it is made based on clinical examinations and identification of the classical rash morphology, but is also emphasizing the role of a wide range of specialists in the evaluation and treatment of this pathological condition. The aim of the study. To analyze a clinical case of the debut of Schamberg disease. Results. Considering the sporadic nature and rarity of the disease, the clinical case of Schamberg disease diagnosed in a 53-year-old man who visited a pediatrician concerning his child’s illness is presented. The probable cause of the disease debut was a complex trigger effect (a long-term use of diclofenac sodium, drinking alcohol on the eve). Conclusions. The report is aimed at drawing attention to Schamberg disease (Schamberg purpura) as a diagnostic and therapeutic challenge not only for general practitioners, internal medicine specialists but also for dermatologists, phlebologists, hematologists in particular.

Mandarin peel ethanolic extract attenuates diclofenac sodium induced hepatorenal toxicity in rats by mitigating oxidative stress and inflammation

Nonsteroidal anti-inflammatory drugs (NSAIDs) constitute approximately one-third of the global pharmaceutical market and are the first drugs of choice when treating fever and pain. Furthermore, among NSAIDs, the use of diclofenac sodium (DS) is preferred as it is a strong inhibitor of cyclooxygenase enzyme. However, despite its strong efficacy, DS is known for its potential to cause hepatorenal damage. Currently, to mitigate the adverse effects of certain drugs, medically effective agricultural products are often preferred as they are inexpensive, effective and safe. One such agricultural product—mandarin—is noteworthy for its high phenolic contents. The purpose of the present study was to assess the efficacy of mandarin peel ethanolic extract (MPEE) in protecting against hepatorenal damage induced by DS. Four groups (six/group) of adult male albino rats received oral administration of physiological saline (control group), DS (10 mg/kg body weight), MPEE (200 mg/kg body weight), and DS + MPEE for 7 days. Rats in the DS group showed increased serum levels of ALT, AST, ALP, BUN, CRE, and UA. Furthermore, the hepatic and renal tissue levels of MDA, TNF-α and IL-1β increased, whereas those of GSH, SOD, GP-x and IL-10 decreased (p < 0.05). Investigation of MPEE in terms of its effects on biochemical, oxidative and inflammatory parameters, it exerted protective and healing effects. Therefore, MPEE can be used to ameliorate DS-induced hepatorenal damage.

Room-temperature synthesis of ionic covalent organic frameworks for efficient removal of diclofenac sodium from aqueous solution

The excessive use of diclofenac sodium (DCF) has led to environmental and food safety problems. Effective removal of DCF in aqueous environment is of great significance. Ionic covalent organic frameworks (iCOFs) are effective adsorbents for the removal of pollutants due to their unique structure and properties, but conventional synthesis of iCOFs is limited by high temperature and long reaction time. Herein, we report a room-temperature strategy to synthesize iCOFs in 24 h for the first time. The room-temperature synthesized ionic COF (RT-iCOF) shows better crystallinity, lager uptake capacity and faster kinetics than those synthesized at high temperature with long reaction time. The adsorption kinetics, isotherms and thermodynamics, the effects of ionic strength, pH, humic acid, and reusability of RT-iCOF for DCF were studied in detail. The prepared RT-iCOF gave the maximum adsorption capacity of 857.5 mg g−1, featuring the highest uptake capacity for DCF so far. The adsorption of DCF on the RT-iCOF are driven by ion exchange, π-π interactions, electrostatic and hydrogen bonds interaction. The adsorption efficiency of RT-iCOF for DCF was still above 90% after 5 regeneration cycles. This work also promotes the facile synthesis and application of iCOFs for the removal of pollutants.

ADVERSE EFFECTS OF DICLOFENAC SODIUM ON KIDNEYS IN ADULT VOLUNTEERS

The use of diclofenac sodium is a major concern in terms of renal function, patients were not given attention despite the clinical importance. This study aims to evaluate the prescribed doses (50mg/day) of diclofenac sodium by doctors for patients in the orthopedic unit.This study was conducted on 36 volunteers, male and female, who were randomly selected from the orthopedic out-patient department and were divided into two groups (two treatments). The first group (18 volunteers) received diclofenac sodium 50 mg and the second group did not receive any medicine (control). The age of volunteers in this study ranged between 20 years to 59 years, both male and female, from September 2020 to September 2021.The main indicators to detect toxic effects of diclofenac sodium on kidney function were urea, uric acid, and creatinine. The urea level in this study was 27mg/dL in the first group and 25mg/dL in the control. Uric acid was 4.12mg/dL in the first treatment and 4.04mg/dL in control and Creatinine level was 0.55mg/dL and control treatment was 0.48mg/dL .All these values collected from the study are within the normal range and cause no pathological or renal disorder.

Ефективність декскетопрофену трометамолу при лікуванні післяопераційного болю

Актуальність. Питання лікування післяопераційного болю залишаються предметом активного обговорення і великої кількості медичних публікацій. Мета дослідження: оцінити ефективність застосування декскетопрофену трометамолу при лікуванні післяопераційного больового синдрому у хворих, які перенесли оперативне втручання на органах черевної порожнини. Матеріали і методи. Обстежено 40 хворих, яких було прооперовано з приводу патології органів черевної порожнини. Залежно від характеру післяопераційного знеболювання (застосування диклофенаку натрію або декскетопрофену трометамолу) хворі були розподілені на 2 групи. Результати. При лікуванні післяопераційного больового синдрому диклофенаком натрію упродовж перших двох діб після операції зберігався помірний больовий синдром, що потребувало додаткового знеболювання наркотичними анальгетиками у 80–90 % хворих (дворазово — в 1-шу добу, одноразово — в 2-гу добу). Післяопераційний біль супроводжувався симпатикотонією, гіперглікемією, вазоспазмом і тахікардією. Формувався відносно гіпердинамічний тип кровообігу. Активація симпатичної ланки вегетативної нервової системи сприяла збільшенню системного транспорту і споживання кисню. Застосування декскетопрофену трометамолу при лікуванні післяопераційного больового синдрому було ефективним і дозволяло якісно обмежити розвиток післяопераційної гіпералгезії. Висновки. Традиційне використання диклофенаку натрію для лікування болю після планового оперативного втручання в абдомінальній хірургії зберігає помірний больовий синдром, що у 80–90 % хворих вимагає неодноразового додаткового введення наркотичних анальгетиків протягом перших двох діб. При застосуванні декскетопрофену трометамолу больовий синдром зменшується до легкого вже з 1-ї доби після операції, що у 40–60 % пацієнтів вимагає тільки одноразового додаткового знеболювання, сприяє нормалізації судинного тонусу і серцевого ритму, транспорту і споживання кисню при відносній парасимпатикотонії.

EVALUATION OF THE THERAPEUTIC EFFECT OF THE COMBINED USE OF CRYOPRESERVED PLACENTA EXTRACT AND DICLOFENAC SODIUM IN EXPERIMENTAL RHEUMATOID ARTHRITIS BY HEMATOLOGICAL PARAMETERS

Relevance. Cryopreserved placenta extract (CPE) increase the resistance of the mucous membrane of the gastrointestinal tract to the damaging effects of nonsteroidal anti-inflammatory drugs. Preventive administration of CPE can reduce the ulcerogenic effect of meloxicam, ibuprofen, diclofenac sodium (DS) and others. There is evidence of CPE's own anti-inflammatory activity, which can be successfully combined with the pharmacological properties of nonsteroidal anti-inflammatory drugs, while improving their safety profile.&#x0D; Objective: to characterize the therapeutic activity of the combined use of CPE and DS according to hematological parameters in the model of experimental rheumatoid arthritis (RA).&#x0D; Materials and methods. Studies were performed on 28 nonlinear laboratory rats. The rats were divided into 4 groups: I (n = 7) – intact rats; II (n = 7) – rats with experimental RA; ІІІ (n = 7) – rats with experimental RA, treated with DN; IV (n = 7) – rats with experimental RA, treated with DN and CPE. Adjuvant arthritis was modeled by subplantar administration of complete Freund's adjuvant. Treatment was performed from 14 to 28 days. CPE was administered on days 14, 17, 20, 23 and 26, and DS – daily. Blood tests were performed on day 28 of the experiment.&#x0D; Results. The combined use of CPE and DS is accompanied by a more pronounced leveling of inflammatory signs by hematological parameters – erythrocyte clotting rate decreased by 72.2% (p&lt;0.001), and the number of leukocytes decreased by 54.81% (p&lt;0.001) relative to rats with adjuvant arthritis without treatment. There was a leveling of signs of anemia of chronic inflammation – the level of hemoglobin and erythrocytes increased (p&lt;0,001) by 17.6% and 36.8%, respectively, relative to rats with adjuvant arthritis without treatment.&#x0D; Conclusions. The combined use of CPE and DS is superior in therapeutic activity to monotherapy with this nonsteroidal anti-inflammatory drug of experimental rheumatoid arthritis.

Characteristics of the mechanisms of anti-inflammatory action of cryopreserved placenta extract and diclofenac sodium by their threaded administration

Introduction. Inflammation is a complex multicomponent adaptive pathological process based on three enzymatic pathways of arachidonic acid metabolism: cyclooxygenase, lipoxygenase and epoxygenase. Nonsteroidal anti-inflammatory drugs are the most numerous and most widely used group of drugs used in the pharmacocorrection of inflammatory processes of various etiologies.&#x0D; Purpose of the study. The aim is to characterize the effect of cryopreserved placenta extract on the anti-inflammatory activity of diclofenac sodium with their threaded administration in a model of zymosan-induced inflammation.&#x0D; Materials and methods. In vivo experimental studies were performed on 28 nonlinear laboratory male rats weighing 200–220 g. Acute exudative inflammation was reproduced by subplantar administration of rat limb 0,1 ml of 2,0% zymosan suspension. The anti-exudative effect was assessed by the magnitude of limb edema, which was assessed using an aqueous plethysmometer.&#x0D; Results and discussion. The study showed that subplantar administration of 2,0% suspension of zymosan led to a statistically significant (p &lt; 0,05) increase in the volume of the damaged limb after 30 minutes. by 28,1 ± 5,4% relative to baseline and was 2,01 ± 0,06 ml. The most pronounced and almost comparable anti-inflammatory activity was observed against the background of the use of cryopreserved placenta extract and the combined use of diclofenac sodium and cryopreserved placenta extract. Thus, for 60 min the antiinflammatory activity was (p &lt; 0,05) 46,5% and 53,2%, respectively.&#x0D; Conclusions. It is established that one of the leading mechanisms of anti-inflammatory activity of cryopreserved placenta extract is the inhibition of the lipoxygenase pathway of arachidonic acid metabolism. This was indicated by statistically significant (p &lt; 0,05) suppression of zymosaninduced inflammation in rats by 78,8% and 74,8% by 120 and 180 min, respectively.

EFFECT OF CRYOPRESERVED PLACENTA EXTRACT ON SOME BIOCHEMICAL INDICES OF THERAPEUTIC EFFICIENCY AND TOXICITY OF DICLOFENAC SODIUM IN ADJUVANT-INDUCED EXPERIMENTAL ARTHRITIS

Non-steroidal anti-inflammatory drugs are among the top requested ones in the clinic of internal medicine. However, these drugs are associated with a wide range of adverse reactions involving a number of organs and systems, in particular the gastrointestinal tract, cardiovascular system and kidneys. The aim of the study is to characterize the effect of the combined use of cryopreserved placenta extract and diclofenac sodium on the prooxidant-oxidative system, the activity of inflammatory, destructive and cytolytic processes, as well as protein and lipid metabolism in rats with experimental rheumatoid arthritis. Results. The administration of diclofenac sodium and cryopreserved placenta extract to rats with adjuvant arthritis normalized the level of active products of thiobarbituric acid and hence was indicative of the neutralization of an arthritis-induced oxidative stress. A statistically significant (p=0.01) increase of in a superoxide dismutase activity (by 30.6% relative as compared with rats of the control group) has also been established. An increase in the anti-inflammatory properties of diclofenac sodium in the combined use of diclofenac sodium with a cryopreserved placenta extract has been found out. The level of C-reactive protein decreased (p&lt;0.001) by 61.1% as compared with the untreated rats, and the level of seromucoid has been significantly (p&lt;0.01) decreased by 17.1% as compared with the rats of the monotherapy group treated with the studied NSAIDs. It was shown that alanine aminotransferase and aspartate levels were significantly lower (by 38.9%, p&lt;0.01 and by 37.9%, p&lt;0.01, respectively) as compared with those of the animals that had been administrated with diclofenac sodium. Their indices were by 16.7% (p=0.02) and 17.2% (p&lt;0.001) lower than the indices of the control group rats with untreated adjuvant arthritis. The established changes of aminotransferases levels indicate the ability of a cryopreserved placenta extract to level not only an arthritis-induced cytolytic syndrome, but also a diclofenac-induced one. The combined use of cryopreserved placenta extract and diclofenac sodium was accompanied by the normalization of the total lipids level and phospholipids in the blood serum of rats against the background of experimental rheumatoid arthritis. Thus, the content of phospholipids in the lipid pool statistically significantly (p=0.02) increased by 22.6% as compared with the indices of the animals with adjuvant arthritis without treatment. Conclusion. The study showed that the combined use of diclofenac sodium and cryopreserved placenta extract leads to the restoration of the balance of the prooxidant-antioxidant system that is more pronounced than monotherapy with diclofenac sodium. A decrease in the activity of inflammatory, destructive and cytolytic processes, as well as the restoration of lipid metabolism in the rats with experimental rheumatoid arthritis, has also been observed.

ANALGESIC EFFICACY OF TRAMADOL/ ACETAMINOPHEN COMBINATION WITH DICLOFENAC SODIUM IN MODERATE TO SEVERE LOW BACK PAIN

This prospective randomized cohort study was conducted in two parallel groups to compare the analgesic effects in conventional use of oral Diclofenac tablet, 50 mg tablet three times daily or 75 mg tablet twice daily (DIC group) with oral combination of Tramadol 37.5 mg and Acetaminophen (Paracetamol) 325 mg (T-APAP group) one tablet twice daily. The number of patients n= 150 in each group. Study data of total 300 patients of age 20 - 60 years, with moderate to severe Low back pain (LBP) was collected from the public and two private setup OPDs in Karachi, Pakistan. Patient demographic data of gender, age, BMI and socioeconomic status were collected. Numeric Pain Rating Scale (NPRS) was used to measure pain intensity and overall pain intensity at the baseline 0, 1st, 2nd, 3rd and 4th week of the treatment. The results indicated that the incidence of Low back pain (LBP) is highest 41.0 % (n = 123) in 30-39 years age group. According to Body Mass Index (BMI) classification most of the patients 63.6 % (n = 191) patients are overweight. In socioeconomic classification 47.3 % (n = 142) are from lower socioeconomic status. The duration of perceived pain was found to be shorter with 58.6 % (n = 88) recovery within one week of the treatment in the T-APAP Group, compared to 35.3 % (n = 53) recovery in DIC group (p&lt; 0.05). Oral combination of Tramadol plus Paracetamol is found to be more effective than the use of oral Diclofenac alone. 79.4 % Overall Pain Relief with 5.8 scores of Overall Pain Relief (p&lt; 0.05) were observed in the T-APAP Group. It is concluded that the oral combination of Tramadol 37.5 mg and Acetaminophen (Paracetamol) 325 mg is more effective analgesic than oral use of Diclofenac sodium alone in moderate to severe LBP.

The effects of different doses of diclofenac sodium on newborn rat hippocampus exposed during the third trimester

The main aim of the present study was to examine the neurotoxic effects of prenatal exposure to varying doses of diclofenac sodium (DS) on the rat hippocampus. Twenty-eight Wistar albino adult female rats weighing 280-300 g were initially used for pregnancy. When vaginal plaques were seen in female rats, it was accepted as the 0th day of pregnancy. Female rats were divided into five main groups; pure control, saline, low dose DS (3.6 mg/kg), moderate dose DS (9 mg/kg), and high dose DS (18 mg/kg). They were exposed to these treatments during their gestation. After birth, all newborn male rats were euthanized by overdose anesthesia on the 7th postnatal day. Histological and stereological techniques were used for analyzing tissue samples. The stereological analyses in this study showed that the number of neurons in the hippocampus may be reduced due to the use of DS. Histological investigation of the drug-treated groups showed significant cell loss compared to the control. Darkly stained nuclei of the neurons in the high dose group compared to the other groups were also obvious. When the results are evaluated, it can be concluded that the use of diclofenac sodium during pregnancy may have teratogenic effects on the development of the nervous system.

Analysis of clinical efficacy and safety of intravenous use of diclofenac for the prevention of postoperative pain: current status and strategic aspect

The aim of the work is to analyze and systematize the literature data regarding the current state and strategic aspect of intravenous use of diclofenac for the prevention of postoperative pain, namely clinical efficacy and safety.Materials and methods. Studies were conducted using databases on the Internet: PubMed; Food and Drug Administration, European Medicines Agency. It has used retrospective, logical, research methods, content analysis.Results. Conducted clinical data analysis indicates that diclofenac sodium, when administered intravenously, has an opioid-saving effect, is effective in patients experiencing acute postoperative pain, or as part of a multimodal analgesic strategy to achieve perioperative pain control. This increases the possibility of relief of pain and promotes accelerated rehabilitation after surgery, reduces the need for opiates. The incidence of side effects with intravenous diclofenac was similar to that seen with other treatments. New opportunities of the strategic aspect of intravenous use of diclofenac is related to the use of Dyloject, Hospira Inc., USA, which has improved solubility, shorter administration time than infusion. The incidence of thrombophlebitis on treatment with Dyloject was less pronounced compared to Voltarol.Conclusions. Thus, the experience of clinical intravenous use of diclofenac sodium for the prevention of postoperative pain has confirmed its efficacy, favorable safety profile and the ability to reduce the need for opiates. The promising strategic aspect is the creation of domestic diclofenac sodium preparations for intravenous administration, which have improved solubility, shorter administration time than infusions and have no additional safety risk

A Facile One-Pot Synthesis of 3-Methylbenzisoxazoles via a Key Intermediate of ortho-Ethoxyvinyl Nitroaryls by Domino Rearrangement and Their Anti- Inflammatory Activity.

Recently, there has been a lot of scientific interest in exploring the syntheses of oxygen and nitrogen-containing heterocyclic compounds due to their pharmacological activities. In addition, benzisoxazoles play a very important role in organic synthesis as key intermediates. In this paper, we focused on developing a novel synthetic route for biologically active arylisoxazoles under normal conditions, and simplified it to get high purities and yields, and also reported their anti-inflammatory activities. An efficient and simple method has been explored for the synthesis of novel 3-methyl arylisoxazoles from o-nitroaryl halides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via Domino rearrangement in one pot synthesis. We synthesized novel 3-methylarylisoxazoles from o-nitroarylhalides via o-ethoxyvinylnitroaryls, using dihydrated stannous chloride (SnCl2.2H2O) in MeOH / EtOAc (1:1) via domino rearrangement. In this reduction, nitro group and ethoxy vinyl group change to the functional acyl ketones, followed by hetero cyclization. Here, the reaction proceeds without the isolation of intermediates like 2-acylnitroarenes and 2- acylanilines. All the synthesized compounds were completely characterized by the NMR and mass spectra. The compounds were also explored for their anti-inflammatory activity by carrageenan-induced inflammation in the albino rats (150-200 g) of either sex used in this entire study with the use of Diclofenac sodium as the standard drug. The initial evaluations identified leading targets with good to moderate anti-inflammatory activity. A simple, one-pot and convenient method has been explored for the synthesis of novel 3- methylarylisoxazoles with high purity and reaction yields. All the compounds 3a, 3c, 3d, 3f, 3g and 3h exhibited 51-64% anti-inflammatory activities.

THE EFFECT OF SILODOSIN AND SODIUM DICLOFENAC TO REDUCE PAIN AFTER DJ STENT REMOVAL IN SOETOMO HOSPITAL: DOUBLE-BLINDED RANDOMIZED-CONTROLLED TRIAL

Objective: To analyze, measure, compare, prove, and evaluate effectiveness of silodosin, diclofenac sodium, and the combination of both drugs in pain management after stent removal. Materials &amp; Methods: Thirty-three patients were divided into three groups. Group I was given diclofenac Sodium 50 mg, group II was given silodosin 8 mg and group III was given the combination of diclofenac sodium 50 mg and silodosin 8 mg. The Wong Baker Pain Scale (WBPS) was assessed serially: two hours before the DJ stent removal, during DJ stent removal, and after the DJ stent removal (2 hours and 24 hours after). The data was analyzed by ANOVA and Kruskal-Wallis test. Results: In this study, 33 patients who underwent DJ stent removal were obtained. Wong Baker was presented in median (min-max) form. The WBPS study in each group did not differ statistically significant. Lowest WBPS during DJ stent removal was found in group III. Group III was better and statistically significant in reducing pain compared to group I and group II (p&lt;0.05). WBPS two hours after removal in each group decreased and group III was better and statistically significant in reducing pain compared to group II, whereas group III compared to group I had an equivalent effectiveness. While the WBPS 24 hours after removal had the same value and did not differ significantly. No side effects or adverse events were found in the use of diclofenac sodium, silodosin, and their combinations. Conclusion: Single oral dose of diclofenac sodium combined with silodosin is effective to reduce pain after DJ stent removal.

Assessment of the Effect of 3% Diclofenac Sodium on Photodamaged Skin by Means of Reflectance Confocal Microscopy.

Treatment of actinic keratosis with 3% diclofenac sodium w/w in hyaluronic acid is associated with a concomitant improvement in signs of photodamaged skin. However this effect has not yet been examined in depth. Twenty patients with actinic keratosis and signs of photodamaged skin were studied. They received treatment with diclofenac sodium w/w in hyaluronic acid for 2 months. Clinical and reflectance confocal microscopy assessment on signs of photodamaged skin were performed. Regarding reflectance confocal microscopy, the most common descriptors were: irregular honeycomb pattern in 18/20 patients (90%), mottled pigmentation in 17/20 (85%), coarse collagen structures in all patients, and huddled collagen and curled bright structures in 16/20 (77.8%). After treatment, significant improvement in clinical parameters: irregular pigmentation and coarseness, and confocal parameters: irregular honeycomb pattern and mottled pigmentation, were noted. Reflectance confocal microscopy is a useful tool in monitoring changes in photodamaged skin after treatment. The use of diclofenac sodium w/w in hyaluronic acid is associated with an improvement in some clinical and reflectance confocal microscopy parameters of photodamaged skin.

Effect of certain non-steroidal anti-inflammatory drugs on the paraoxonase 2 (PON2) in human monocytic cell line U937

The paraoxonase gene family in humans consists of three members as PON1, PON2 and PON3. PON2 can be expressed in several tissues; however, it is not released from the cells in those tissues. PON2 is also expressed in macrophages. Firstly, the commonly used NSAIDs diclofenac sodium and tenoxicam were applied on U937 cell line, the in vitro human monocyte cell line. Than PON2 specific Lactonase activity and paraoxonase family specific arylesterase were determined. Use of Diclofenac sodium in 0.845 mM dose during 6–12 h of incubation and Tenoxicam in 0.74 mM dose during 6 h of incubation resulted in a significant decline in the lactonase activity. Diclofenac sodium didn’t make any change in the arylesterase activity. On the other hand, tenoxicam decreased arylesterase activity during the use of 12 h, in 0.74 mM and 1.48 mM dose.

Effects of photobiomodulation therapy and topical non-steroidal anti-inflammatory drug on skeletal muscle injury induced by contusion in rats-part 1: morphological and functional aspects.

Musculoskeletal injuries are very frequent and are responsible for causing pain and impairment of muscle function, as well as significant functional limitations. In the acute phase, the most prescribed treatment is with non-steroidal anti-inflammatory drugs (NSAIDs), despite their questionable effectiveness. However, the use of photobiomodulation therapy (PBMT) in musculoskeletal disorders has been increasing in the last few years, and this therapy appears to be an interesting alternative to the traditional drugs. The objective of the present study was to evaluate and compare the effects of PBMT, with different application doses, and topical NSAIDs, under morphological and functional parameters, during an acute inflammatory process triggered by a controlled model of musculoskeletal injury induced via contusion in rats. Muscle injury was induced by means of a single trauma to the animals' anterior tibialis muscle. After 1h, the rats were treated with PBMT (830nm; continuous mode, with a power output of 100mW; 3.57W/cm2; 1J-35.7J/cm2, 3J-107.1J/cm2, and 9J-321.4J/cm2; 10, 30, and 90s) or diclofenac sodium for topical use (1g). Morphological analysis (histology) and functional analysis (muscle work) were performed, 6, 12, and 24h after induction of the injury. PBMT, with all doses tested, improved morphological changes caused by trauma; however, the 9J (321.4J/cm2) dose was the most effective in organizing muscle fibers and cell nuclei. On the other hand, the use of diclofenac sodium produced only a slight improvement in morphological changes. Moreover, we observed a statistically significant increase of muscle work in the PBMT 3J (107.1J/cm2) group in relation to the injury group and the diclofenac group (p<0.05). The results of the present study indicate that PBMT, with a dose of 3J (107.1J/cm2), is more effective than the other doses of PBMT tested and NSAIDs for topical use as a means to improve morphological and functional alterations due to muscle injury from contusion.