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Drugs May 2015Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class with anti-inflammatory, analgesic, and antipyretic properties. Contrary to the... (Review)
Review
Diclofenac is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylacetic acid class with anti-inflammatory, analgesic, and antipyretic properties. Contrary to the action of many traditional NSAIDs, diclofenac inhibits cyclooxygenase (COX)-2 enzyme with greater potency than it does COX-1. Similar to other NSAIDs, diclofenac is associated with serious dose-dependent gastrointestinal, cardiovascular, and renal adverse effects. Since its introduction in 1973, a number of different diclofenac-containing drug products have been developed with the goal of improving efficacy, tolerability, and patient convenience. Delayed- and extended-release forms of diclofenac sodium were initially developed with the goal of improving the safety profile of diclofenac and providing convenient, once-daily dosing for the treatment of patients with chronic pain. New drug products consisting of diclofenac potassium salt were associated with faster absorption and rapid onset of pain relief. These include diclofenac potassium immediate-release tablets, diclofenac potassium liquid-filled soft gel capsules, and diclofenac potassium powder for oral solution. The advent of topical formulations of diclofenac enabled local treatment of pain and inflammation while minimizing systemic absorption of diclofenac. SoluMatrix diclofenac, consisting of submicron particles of diclofenac free acid and a proprietary combination of excipients, was developed to provide analgesic efficacy at reduced doses associated with lower systemic absorption. This review illustrates how pharmaceutical technology has been used to modify the pharmacokinetic properties of diclofenac, leading to the creation of novel drug products with improved clinical utility.
Topics: Anti-Inflammatory Agents, Non-Steroidal; Chemistry, Pharmaceutical; Cyclooxygenase Inhibitors; Delayed-Action Preparations; Diclofenac; Dose-Response Relationship, Drug; Humans; Technology, Pharmaceutical
PubMed: 25963327
DOI: 10.1007/s40265-015-0392-z -
La Clinica Terapeutica 2019Post-Endoscopic Retrograde Cholangio-Pancreatography pancreatitis (PEP) is a relevant (1-4%) complication of biliopancreatic operative endoscopy. Rectal nonsteroidal... (Randomized Controlled Trial)
Randomized Controlled Trial
INTRODUCTION
Post-Endoscopic Retrograde Cholangio-Pancreatography pancreatitis (PEP) is a relevant (1-4%) complication of biliopancreatic operative endoscopy. Rectal nonsteroidal anti-inflammatory drugs (specifically, 100 mg of diclofenac) have shown promising prophylactic activity in PEP. The aim of our prospective study is to report whether prophylactic oral versus rectal suppository versus intramuscular diclofenac versus placebo are able to reduce the incidence and the severity of ERCP-induced pancreatitis.
MATERIALS AND METHODS
In this randomized, double-blinded, prospective study, 100 patients (49 male, 51 female), similar with regard to indication for ERCP, were enrolled between January 2016 and November 2017 to undergo ERCP in the Section of General and Thoracic Surgery of University Hospital of Palermo. They were randomized into five groups, respectively 20 patients with placebo by mouth; 20 patients with 50 mg diclofenac sodium enteric-coated capsules by mouth; 20 with 100 mg rectal suppository diclofenac, 20 with 75 mg/3 ml intramuscular diclofenac sodium, 20 with 75 mg/3 ml intramuscular diclofenac sodium and 20 with 75 mg/3 ml intravenous diclofenac. All drugs were administered 30 to 90 minutes before ERCP. All clinical data were collected one day before and 2, 12 and 24 hour after ERCP.
RESULT
Data were prospectively collected and to demonstrate the preventive effect of rectal diclofenac on PEP, a two-by-two table and chi-square test with Yates correction were used: the incidence of PEP was significantly lower (p < 0.001) in the rectal diclofenac group respect to other groups and, in the same way, the incidence of post-ERCP pain was significantly lower in the rectal diclofenac group than in the other groups (p = 0.001) and patients discharge was consequently earlier (p < 0.01).
CONCLUSION
100 mg dose rectal diclofenac administered 30-60 minutes before ERCP can effectively prevent PEP.
Topics: Acute Disease; Administration, Rectal; Adult; Anti-Inflammatory Agents, Non-Steroidal; Cholangiopancreatography, Endoscopic Retrograde; Diclofenac; Double-Blind Method; Female; Humans; Male; Middle Aged; Pancreatitis; Prospective Studies; Treatment Outcome
PubMed: 31612188
DOI: 10.7417/CT.2019.2156 -
JAMA Network Open Aug 2022Renal colic is described as one of the worst types of pain, and effective analgesia in the shortest possible time is of paramount importance. (Randomized Controlled Trial)
Randomized Controlled Trial
IMPORTANCE
Renal colic is described as one of the worst types of pain, and effective analgesia in the shortest possible time is of paramount importance.
OBJECTIVES
To examine whether acupuncture, as an adjunctive therapy to analgesics, could accelerate pain relief in patients with acute renal colic.
DESIGN, SETTING, AND PARTICIPANTS
This single-center, sham-controlled, randomized clinical trial was conducted in an emergency department in China between March 2020 and September 2020. Participants with acute renal colic (visual analog scale [VAS] score ≥4) due to urolithiasis were recruited. Data were analyzed from October 2020 to January 2022.
INTERVENTIONS
After diagnosis and randomization, all patients received 50 mg/2 mL of diclofenac sodium intramuscular injection immediately followed by 30-minute acupuncture or sham acupuncture.
MAIN OUTCOMES AND MEASURES
The primary outcome was the response rate at 10 minutes after needle manipulation, which was defined as the proportion of participants whose VAS score decreased by at least 50% from baseline. Secondary outcomes included response rates at 0, 5, 15, 20, 30, 45, and 60 minutes, rescue analgesia, and adverse events.
RESULTS
A total of 115 participants were screened and 80 participants (66 men [82.5%]; mean [SD] age, 45.8 [13.8] years) were enrolled, consisting of 40 per group. The response rates at 10 minutes were 77.5% (31 of 40) and 10.0% (4 of 40) in the acupuncture and sham acupuncture groups, respectively. The between-group differences were 67.5% (95% CI, 51.5% to 83.4%; P < .001). The response rates of acupuncture were also significantly higher than sham acupuncture at 0, 5, 15, 20 and 30 minutes, whereas no significant difference was detected at 45 and 60 minutes. However, there was no difference between the 2 groups in rescue analgesia rate (difference 2.5%; 95% CI -8.8% to 13.2%; P > .99). No adverse events occurred during the trial.
CONCLUSIONS AND RELEVANCE
These findings suggest that acupuncture plus intramuscular injection of diclofenac is safe and provides fast and substantial pain relief for patients with renal colic compared with sham acupuncture in the emergency setting. However, no difference in rescue analgesia was found, possibly because of the ceiling effect caused by subsequent but robust analgesia of diclofenac. Acupuncture can be considered an optional adjunctive therapy in relieving acute renal colic.
TRIAL REGISTRATION
Chinese Clinical Trial Registry: ChiCTR1900025202.
Topics: Acupuncture Therapy; Diclofenac; Emergency Service, Hospital; Humans; Male; Middle Aged; Pain; Renal Colic; Urolithiasis
PubMed: 35943743
DOI: 10.1001/jamanetworkopen.2022.25735 -
Advanced Science (Weinheim,... Feb 2023CD73, a cell surface-bound nucleotidase, facilitates extracellular adenosine formation by hydrolyzing 5'-AMP to adenosine. Several studies have shown that CD73 plays an...
CD73, a cell surface-bound nucleotidase, facilitates extracellular adenosine formation by hydrolyzing 5'-AMP to adenosine. Several studies have shown that CD73 plays an essential role in immune escape, cell proliferation and tumor angiogenesis, making it an attractive target for cancer therapies. However, there are limited clinical benefits associated with the mainstream enzymatic inhibitors of CD73, suggesting that the mechanism underlying the role of CD73 in tumor progression is more complex than anticipated, and further investigation is necessary. In this study, CD73 is found to overexpress in the cytoplasm of pancreatic ductal adenocarcinoma (PDAC) cells and promotes metastasis in a nucleotidase-independent manner, which cannot be restrained by the CD73 monoclonal antibodies or small-molecule enzymatic inhibitors. Furthermore, CD73 promotes the metastasis of PDAC by binding to the E3 ligase TRIM21, competing with the Snail for its binding site. Additionally, a CD73 transcriptional inhibitor, diclofenac, a non-steroidal anti-inflammatory drug, is more effective than the CD73 blocking antibody for the treatment of PDAC metastasis. Diclofenac also enhances the therapeutic efficacy of gemcitabine in the spontaneous KPC (LSL-Kras , LSL-Trp53 , and Pdx-1-Cre) pancreatic cancer model. Therefore, diclofenac may be an effective anti-CD73 therapy, when used alone or in combination with gemcitabine-based chemotherapy regimen, for metastatic PDAC.
Topics: Humans; Carcinoma, Pancreatic Ductal; Diclofenac; Gemcitabine; Pancreatic Neoplasms; Nucleotidases
PubMed: 36563135
DOI: 10.1002/advs.202206335 -
International Journal of Molecular... Jan 2018Recent experiments showed a potential cardiotoxic effect of the macrolide antibiotic (tulathromycin). This study was performed to investigate whether diclofenac sodium...
Recent experiments showed a potential cardiotoxic effect of the macrolide antibiotic (tulathromycin). This study was performed to investigate whether diclofenac sodium (DFS) potentiates the cardiotoxicity of tulathromycin and increases the cardioprotective effects of lycopene against DFS and tulathromycin. Seven groups (eight per group) of adult Swiss albino mice received saline (control), tulathromycin (a single subcutaneous dose of 28 mg/kg/bw on day 14), DFS (a single oral dose of 100 mg/kg/bw on day 14), tulathromycin plus DFS, or lycopene (oral, 10 mg/kg/bw daily for 15 d) combined with tulathromycin, DFS, or both. Compared to the control group, the administration of tulathromycin or DFS (individually or in combination) caused significantly elevated ( < 0.05) serum levels of Creatine kinase-myocardial B fraction (CK-MB), lactate dehydrogenase, and cardiac-specific troponin-T and tissue levels of nitric oxide and malondialdehyde that were accompanied by significantly decreased tissue reduced glutathione content and glutathione peroxidase, superoxide dismutase, and catalase antioxidant enzyme activity. Upon histopathological and immunohistochemical examination, the mean pathology scores and the percentages of caspase-3-, Bax-, and CK-positive regions were significantly higher in the tulathromycin- and/or DFS-treated groups than in control mice. For all these parameters, the pathological changes were more significant in the tulathromycin-DFS combination group than in mice treated with either drug individually. Interestingly, co-administration of lycopene with tulathromycin and/or DFS significantly ameliorated the changes described above. In conclusion, DFS could potentiate the cardiotoxic effects of tulathromycin, whereas lycopene can serve as a cardioprotective agent against DFS and tulathromycin.
Topics: Animals; Biomarkers; Cardiotoxicity; Carotenoids; Creatine Kinase, MB Form; Diclofenac; Disaccharides; Heart; Heterocyclic Compounds; Immunohistochemistry; L-Lactate Dehydrogenase; Lipid Peroxidation; Lycopene; Male; Mice; Myocardium; Protective Agents
PubMed: 29364179
DOI: 10.3390/ijms19020344 -
International Journal of Pharmaceutics Apr 2019Oral Thin Film (OTF) is a newly emerging drug delivery system which has many benefits for patients. Although there has been some formulation of OTF products, these have...
Oral Thin Film (OTF) is a newly emerging drug delivery system which has many benefits for patients. Although there has been some formulation of OTF products, these have mainly been as confectionary or dental health products. The most significant benefit of this dosage format will only be realised once more pharmaceutical products become available. Within this paper, OTF strips containing Diclofenac Sodium were prepared using the solvent casting method and then characterised to ensure the method could conform to acceptable levels of uniformity, the mean (SD) diclofenac sodium content was 25.43 (1.39) mg, range 22.84-27.44 mg. Bioburden was tested against coliforms, yeasts and moulds and all results were confirmed to be <10 CFU/g, also similar dissolution profile when compared to a commercial product to ensure biowaiver. An acceptable level of uniformity of mass was produced. K-F titration was employed to reduce the water content of the strips and it was found to be acceptable, this represented a level of water which would not be viable for microbial growth. The technique employed here in the production of OTF resulted in high quality products and amenability to being up scaled. Furthermore, the characterisation method was also sufficient to assess the quality of the products and may be used for future analysis of OTF pharmaceuticals.
Topics: Administration, Oral; Diclofenac; Drug Contamination; Drug Delivery Systems; Drug Liberation
PubMed: 30772459
DOI: 10.1016/j.ijpharm.2019.01.064 -
Asian Journal of Surgery May 2018Despite many advances in surgery and technology, colonic anastomosis remains a challenge after colonic resection. The purpose of this study is to compare the safety of... (Comparative Study)
Comparative Study
BACKGROUND
Despite many advances in surgery and technology, colonic anastomosis remains a challenge after colonic resection. The purpose of this study is to compare the safety of using diclofenac sodium and paracetamol for analgesia in colonic anastomosis on rats.
METHODS
Wistar-Hannover rats were randomly allocated to four groups: Group 1, sham-operated group; Group 2, control group; Group 3, diclofenac sodium group; Group 4, paracetamol group. After laparotomy, the left colon was transected and a single-layer anastomosis was made with 5/0 vicryl in Groups 2, 3, and 4. Only laparotomy was performed in Group 1. After anastomosis, we administered saline to Group 2, diclofenac sodium to Group 3, and paracetamol to Group 4 for 7 days. Then, all animals were decapitated. The anastomotic region was resected, and bursting pressure was measured. Then, the specimen was sent to the laboratory for histological examination and hydroxyproline analysis.
RESULTS
Bursting pressure and hydroxyproline level were significantly higher in the paracetamol group (p<0.05). When we looked at the fibrosis levels of these groups, it was also higher in paracetamol group.
CONCLUSION
Bursting pressure, hydroxyproline levels, and fibrosis levels indicate that the perioperative use of paracetamol for analgesia when undergoing colonic anastomosis is safer than diclofenac sodium.
Topics: Acetaminophen; Anastomosis, Surgical; Anastomotic Leak; Animals; Anti-Inflammatory Agents, Non-Steroidal; Colon; Diclofenac; Pain, Postoperative; Random Allocation; Rats; Rats, Wistar; Treatment Outcome; Wound Healing
PubMed: 28190750
DOI: 10.1016/j.asjsur.2017.01.002 -
Comparison of the Effects of Piroxicam and Diclofenac Sodium as Treatments for Primary Dysmenorrhea.Medical Science Monitor : International... Jan 2019BACKGROUND NSAIDs are the most common agents used in dysmenorrhea treatment. They reduce menstrual pain by reducing uterine pressure and PGF2alpha levels in the... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND NSAIDs are the most common agents used in dysmenorrhea treatment. They reduce menstrual pain by reducing uterine pressure and PGF2alpha levels in the menstrual fluid. The aim of this study was to compare the effects of piroxicam and diclofenac sodium as treatments for primary dysmenorrhea. MATERIAL AND METHODS The study was conducted using a randomized and double-blind method. Patients with Visual Analogue Scale (VAS) scores greater than 5 were accepted into the study. The patients who were suitable for inclusion were randomized into 2 groups and received either intramuscular piroxicam or diclofenac sodium. The patients' pain levels were measured at baseline and at 15, 30, 45, and 60 min. A VAS of 10 cm, a numeric scale, a verbal scale, and additional symptoms, as well as pain relapse after 24 hours and required analgesics, were recorded. RESULTS The study included 400 patients. Overall, 200 patients (50%) were in the proxicam group, and 200 patients were in the diclofenac sodium group. The average decrease on the VAS after piroxicam or diclofenac administration was measured as 7.9±1.8 cm and 7.9±1.7 cm (median ± standard deviation), respectively. The pain-reducing efficiency of all the treatments was compared using the Mann-Whitney U test (p=0.929). Rescue medication was needed for 25 patients in the proxicam group (p=0.014). Overall, 30 patients in the proxicam group and 41 patients in the proxicam group needed analgesics again in the 24-hour period after treatment (p=0.150). CONCLUSIONS At the end of our study, it was observed that there was no difference in the results of primary dysmenorrhea treatment with 20 mg piroxicam or 75 mg diclofenac sodium.
Topics: Adult; Anti-Inflammatory Agents, Non-Steroidal; Diclofenac; Double-Blind Method; Dysmenorrhea; Emergency Medical Services; Female; Humans; Pain Measurement; Piroxicam; Young Adult
PubMed: 30612134
DOI: 10.12659/MSM.911711 -
European Review For Medical and... Nov 2023To investigate the effect of Diclofenac sodium sustained-release capsules combined with function training on functional recovery and Visual Analog Scale (VAS) score... (Randomized Controlled Trial)
Randomized Controlled Trial
OBJECTIVE
To investigate the effect of Diclofenac sodium sustained-release capsules combined with function training on functional recovery and Visual Analog Scale (VAS) score after surgery for ankle fractures.
PATIENTS AND METHODS
The study included 88 patients with ankle fractures who were surgically treated at our institution between October 2019 and October 2021. The individuals were randomized into experimental and control groups, with 44 patients in each group. Following their hospitalization, all patients had surgical therapy. After surgery, patients in the control group received conventional analgesics together with function training, whereas those in the experimental group received Diclofenac sodium sustained-release capsules along with function training. The efficacy of the post-surgical treatment in the two groups was then evaluated using functional recovery and VAS scores.
RESULTS
There was no significant difference in the VAS score between the two groups before intervention (p>0.05). After treatment, both groups experienced pain relief, with the VAS score of the experimental group being significantly lower than the control group (p<0.05). The number of patients in the experimental group who fully and partially complied with the study was 19 and 24, respectively, significantly higher than that of 15 and 20 in the control group. Only 1 patient in the experimental group was non-compliant, compared to 9 in the control group. The total compliance rate in the experimental group was 97.73%, much higher than that of 79.55% in the control group (p<0.05). Before the intervention, there was no significant difference in the range of active ankle motion between the two groups (p>0.05). After treatment, there was an improvement in the range of active motion of the ankle in patients from both groups.
CONCLUSIONS
After ankle fracture surgery, using Diclofenac sodium sustained-release capsules in conjunction with function training successfully lowers postoperative pain. It also maintains emotional stability and ensures sleep, factors which are helpful in improving patient compliance to treatment and promoting functional recovery of the ankle. The clinical value of this treatment regimen is certain, and it deserves more widespread application.
Topics: Humans; Diclofenac; Ankle Fractures; Delayed-Action Preparations; Pain, Postoperative; Analgesics; Treatment Outcome
PubMed: 38039014
DOI: 10.26355/eurrev_202311_34452 -
Urology Journal Jan 2020This study was conducted to determine the effects of tamsulosin and diclofenac sodium use on patients' pain perception after ureteral stents removal. (Comparative Study)
Comparative Study Randomized Controlled Trial
PURPOSE
This study was conducted to determine the effects of tamsulosin and diclofenac sodium use on patients' pain perception after ureteral stents removal.
MATERIALS AND METHODS
This study was a randomized control trial with double-blinded design. Eighty patients who underwent ureteral stent removal surgery at Kardinah Hospital during January to March 2017 were divided into four groups. The following medications were administered for two days, (A) placebo tid, or (B) diclofenac sodium 50 mg bid, or (C) tamsulosin 0.2 mg sid, or (D) combination of tamsulosin and diclofenac sodium. Analgesic effects were assessed with the Visual Analog Scale (VAS). Relationships among variables were assessed using one-way ANOVA and post hoc tests.
RESULTS
The surgical procedure for ureteral stent removal consisted of 48 (60%) male and 32 (40%) female. The average age of group A, B, C, and D were 51.0, 51.9, 47.6, and 47.3 years, and the average stent dwell time was 6.3 weeks. VAS values of the entire experimental group were lower than the control group on the first day until the second day after the stent removal (p < 0.05). In the experimental group, there was no difference between group B and C (p > 0.05). Group D showed better analgesic effects than group B and C (p <0.05). No severe side effects were observed.
CONCLUSION
The result shows that combination therapy of diclofenac sodium and tamsulosin is better in reducing the pain after ureteral stent removal compared to the admission of a single placebo, tamsulosin, or diclofenac sodium therapy.
Topics: Adult; Device Removal; Diclofenac; Double-Blind Method; Drug Combinations; Female; Humans; Male; Middle Aged; Pain, Postoperative; Prospective Studies; Stents; Tamsulosin; Ureter
PubMed: 31912474
DOI: 10.22037/uj.v0i0.5190