BACKGROUND: Clinical trial evidence is limited to identify better topical non-steroidal anti-inflammatory drugs (NSAIDs) for treating knee osteoarthritis (OA). We aimed to compare the clinical efficacy and safety of flurbiprofen cataplasms (FPC) with loxoprofen sodium cataplasms (LSC) in treating patients with knee OA. METHODS: This is an open-label, non-inferiority randomized controlled trial conducted at Peking University Shougang Hospital. Overall, 250 patients with knee OA admitted from October 2021 to April 2022 were randomly assigned to FPC and LSC treatment groups in a 1:1 ratio. Both medications were administered to patients for 28 days. The primary outcome was the change of pain measured by visual analog scale (VAS) score from baseline to day 28 (range, 0-10 points; higher score indicates worse pain; non-inferiority margin: 1 point; superiority margin: 0 point). There were four secondary outcomes, including the extent of pain relief, the change trends of VAS scores, joint function scores measured by the Western Ontario and McMaster University Osteoarthritis Index (WOMAC), and adverse events. RESULTS: Among 250 randomized patients (One patient without complete baseline record in the flurbiprofen cataplasms was excluded; age, 62.8 ± 10.5 years; 61.4% [153/249] women), 234 (93.6%) finally completed the trial. In the intention-to-treat analysis, the decline of the VAS score for the 24-h most intense pain in the FPC group was non-inferior, and also superior to that in the LSC group (differences and 95% confidence interval, 0.414 (0.147-0.681); P <0.001 for non-inferiority; P = 0.001 for superiority). Similar results were observed of the VAS scores for the current pain and pain during exercise. WOMAC scores were also lower in the FPC group at week 4 (12.50 [8.00-22.50] vs . 16.00 [11.00-27.00], P = 0.010), mainly driven by the dimension of daily activity difficulty. In addition, the FPC group experienced a significantly lower incidence of adverse events (5.6% [7/124] vs . 33.6% [42/125], P <0.001), including irritation, rash and pain of the skin, and sticky hair uncovering pain. CONCLUSIONS This study suggested that FPC is superior to LSC for treating patients with knee OA in pain relief, joint function improvement, and safety profile.
Humans ; Female ; Middle Aged ; Aged ; Osteoarthritis, Knee/drug therapy* ; Flurbiprofen/therapeutic use* ; Anti-Inflammatory Agents, Non-Steroidal/therapeutic use* ; Pain/drug therapy* ; Treatment Outcome ; Double-Blind Method

Objective To observe the changes of brain function in patients with trigeminal neuralgia after administration of flurbiprofen axetil by using the resting-state functional magnetic resonance imaging(fMRI)and based on the amplitude of low-frequency fluctuation(ALFF). Methods Resting fMRI data of 20 patients with trigeminal neuralgia before and after treatment with flurbiprofen axetil were collected by 1.5T magnetic resonance imaging system.The resting fMRI data were pretreated by Statistical Parametric Mapping and DPABI(a toolbox for Data Processing and Analysis for Brain Imaging)software,and the difference of low-frequency oscillation amplitude of brain spontaneous activity before and after treatment with flurbiprofen axetil was analyzed by ALFF. Results The Visual Analogue Scale of pain intensity after flurbiprofen axetil injection was significantly lower than that before administration,and the pain relieved significantly(P=0.000).The ALFF values of right dorsolateral prefrontal lobe,bilateral medial prefrontal lobe,and right middle cingulate gyrus in patients treated with flurbiprofen axetil at rest were significantly lower than those before administration(P=0.000). Conclusions The analgesic effect of flurbiprofen axetil is exerted on the central system.This agent can inhibit the abnormal brain function caused by chronic pain stimulation and thus reduce pain.However,the specific mechanism needs further investigations.
Brain ; drug effects ; Brain Mapping ; Flurbiprofen ; analogs & derivatives ; pharmacology ; Humans ; Magnetic Resonance Imaging ; Trigeminal Neuralgia ; drug therapy

BACKGROUNDThe effect of selective and non-selective cyclooxygenase (COX) inhibitors on tendon healing was variable. The purpose of the study was to evaluate the influence of non-selective COX inhibitor, ibuprofen and flurbiprofen axetil and selective COX-2 inhibitor, celecoxib on the tendon healing process in a rabbit model.

METHODSNinety-six New Zealand rabbits were used as rotator cuff repair models. After surgery, they were divided randomly into four groups: ibuprofen (10 mg·kg-1·d-1), celecoxib (8 mg·kg-1·d-1), flurbiprofen axetil (2 mg·kg-1·d-1), and control group (blank group). All drugs were provided for 7 days. Rabbits in each group were sacrificed at 3, 6, and 12 weeks after tendon repair. Tendon biomechanical load failure tests were performed. The percentage of type I collagen on the bone tendon insertion was calculated by Picric acid Sirius red staining and image analysis. All data were compared among the four groups at the same time point. All data in each group were also compared across the different time points. Qualitative histological evaluation of the bone tendon insertion was also performed among groups.

RESULTSThe load to failure increased significantly with time in each group. There were significantly lower failure loads in the celecoxib group than in the control group at 3 weeks (0.533 vs. 0.700, P = 0.002), 6 weeks (0.607 vs. 0.763, P = 0.01), and 12 weeks (0.660 vs. 0.803, P = 0.002), and significantly lower percentage of type I collagen at 3 weeks (11.5% vs. 27.6%, P = 0.001), 6 weeks (40.5% vs. 66.3%, P = 0.005), and 12 weeks (59.5% vs. 86.3%, P = 0.001). Flurbiprofen axetil showed significant differences at 3 weeks (failure load: 0.600 vs. 0.700, P = 0.024; percentage of type I collagen: 15.6% vs. 27.6%, P = 0.001), but no significant differences at 6 and 12 weeks comparing with control group, whereas the ibuprofen groups did not show any significant difference at each time point.

CONCLUSIONSNonsteroidal anti-inflammatory drugs can delay tendon healing in the early stage after rotator cuff repair. Compared with nonselective COX inhibitors, selective COX-2 inhibitors significantly impact tendon healing.

Animals ; Anti-Inflammatory Agents, Non-Steroidal ; pharmacology ; Biomechanical Phenomena ; Celecoxib ; pharmacology ; Cyclooxygenase 2 Inhibitors ; pharmacology ; Flurbiprofen ; pharmacology ; Ibuprofen ; pharmacology ; Male ; Rabbits ; Rotator Cuff ; drug effects ; pathology ; Tendon Injuries ; drug therapy ; Wound Healing ; drug effects

Animals ; Brain Ischemia ; drug therapy ; Cyclooxygenase Inhibitors ; pharmacology ; Flurbiprofen ; analogs & derivatives ; Male ; Neuroprotective Agents ; pharmacology ; PPAR gamma ; physiology

To study the in situ intestinal absorption kinetics of flrubiprofen in rats, the absorption of flurbiprofen in small intestine (duodenum, jejunum and ileum) and colon of rats was investigated using in situ single-pass perfusion method and the drug content was measured by HPLC. The effects of drug concentration on the intestinal absorption were investigated. The K(a) and P(app) values of flurbiprofen in the small intestine and colon had no significant difference (P > 0.05). Drug concentration (4.0, 10.0 and 16.0 mg x L(-1)) had no significant influence on the K(a) values (P > 0.05). However, when concentration was 4.0 mg x L(-1) and 10.0 mg x L(-1), significant effect on the P(app) values (P < 0.05) was found, but significant effect on the P(app) values was not shown between 10.0 mg x L(-1) and 16.0 mg x L(-1) (P > 0.05). The K(a) and P(app) values of flurbiprofen on the perfusion flow rate had significant difference (P < 0.05). Flurbiprofen could be absorbed at all segments of the intestine in rats and had no special absorption window. The absorption of flurbiprofen complies with the facilitated diffusion in the general intestinal segments, and accompany with the cytopsistransport mechanism probably. The perfusion flow rate had significant effect on the K(a) and P(app).
Analgesics ; administration & dosage ; pharmacokinetics ; Animals ; Anti-Inflammatory Agents, Non-Steroidal ; administration & dosage ; pharmacokinetics ; Colon ; metabolism ; Dose-Response Relationship, Drug ; Duodenum ; metabolism ; Female ; Flurbiprofen ; administration & dosage ; pharmacokinetics ; Ileum ; metabolism ; Intestinal Absorption ; Jejunum ; metabolism ; Male ; Perfusion ; Rats ; Rats, Sprague-Dawley

Adolescent ; Adult ; Analgesics ; administration & dosage ; Anesthetics, Intravenous ; administration & dosage ; Flurbiprofen ; administration & dosage ; Humans ; Hypnotics and Sedatives ; administration & dosage ; Midazolam ; administration & dosage ; Middle Aged ; Molar, Third ; Pain Measurement ; Pain, Postoperative ; prevention & control ; Patient Satisfaction ; Preoperative Care ; Prospective Studies ; Tooth Extraction ; Young Adult

Two dogs were presented with melena, vomiting and depression after accidental swallowing of candy form of Strepsils (flurbiprofen), which is one of non-steroidal anti-inflammatory drugs used in human medicine for controlling a sore throat. These dogs had common signs of anemia induced by gastrointestinal ulceration and hemorrhage with azotemia and leukocytosis. The dogs were treated with blood transfusion, fluid therapy, proton-pump inhibitor, antiemetics, mucus protectant and antibiotic. Although most of clinical signs of two dogs were resolved, azotemic problem with evidence of renal injury have remained.
Anemia ; Animals ; Antiemetics ; Azotemia ; Blood Transfusion ; Candy ; Deglutition ; Depression ; Dogs* ; Fluid Therapy ; Flurbiprofen* ; Hemorrhage ; Humans ; Leukocytosis ; Lidocaine ; Melena ; Mucus ; Pharyngitis ; Ulcer ; Vomiting ; Wounds and Injuries

BACKGROUNDOur previous papers indicate that flurbiprofen axetil (FA), a cyclooxygenase inhibitor, is a promising therapeutic strategy for cerebral ischemia in rats. This study aimed to investigate whether FA could promote a neuroprotective effect by activation of peroxisome proliferator-activated receptor-γ (PPAR-γ) after focal cerebral ischemia in rats.

METHODSTotally 48 male Sprague-Dawley (SD) rats were randomly assigned into six groups (n = 8 in each group): animals in group ischemia/reperfusion (I/R) only received 120-minute transient middle cerebral artery occlusion (tMCAO); animals in group I/R + FA were administered FA (10 mg/kg) by caudal vein just after 120-minute tMCAO; animals in group I/R + FA + GW9662 were administered GW9662 (a PPAR-γ inhibitor, 1 mg/kg) intraperitoneally 30 minutes before cerebral ischemia onset and FA (10 mg/kg) by caudal vein just after 120-minute tMCAO; animals in group I/R + GW9662 were administered GW9662 (1 mg/kg) intraperitoneally 30 minutes before cerebral ischemia onset; animals in group I/R + DMSO were administered 3% DMSO (vehicle of GW9662, 1 ml/kg) intraperitoneally 30 minutes before cerebral ischemia onset; animals in sham group experienced the identical surgery apart from the insertion of the nylon filament. The neurologic deficit score (NDS) were performed at 72 hours after reperfusion, and then mean brain infarct volume percentage (MBIVP) was determined with 2,3,5-triphenyltetrazolium chloride (TTC) 10 g/L staining.

RESULTSNDS was significantly increased in group I/R + FA (12.0 (10.0 - 15.0)), group I/R + FA + GW9662 (10.0 (8.0 - 12.0)), and in group I/R + FA + DMSO (12.0 (9.0 - 14.0)) at 72 hours after reperfusion compared with those in group I/R (7.5 (6.0 - 10.0)). NDS was conspicuously different between group I/R + FA (12.0 (10.0 - 15.0)) and group I/R + FA + GW9662 (10.0 (8.0 - 12.0)). MBIVP in group I/R ((45.82 - 8.83)%) was significantly greater than that in group I/R + FA ((23.52 - 9.90)%), group I/R + FA + GW9662 ((33.17 - 7.15)%); MBIVP in group I/R + FA ((23.52 - 9.90)%) was significantly smaller than that in group I/R + FA + GW9662 ((33.17 - 7.15)%).

CONCLUSIONSFA confers the neuroprotective effect on tMCAO in rats and the selective PPAR-γ antagonist GW9662 attenuates the effect of FA. FA could promote a neuroprotective effect by, or in part, activation of PPAR-γ after focal cerebral ischemia in rats.

Animals ; Brain Ischemia ; drug therapy ; Cyclooxygenase Inhibitors ; pharmacology ; Flurbiprofen ; analogs & derivatives ; pharmacology ; Male ; Neuroprotective Agents ; pharmacology ; PPAR gamma ; physiology ; Rats ; Rats, Sprague-Dawley

BACKGROUNDSystemic non-steroidal anti-inflammatory drugs have been evaluated for their possible preemptive analgesic effects. The efficacy of flurbiprofen axetil for preemptive analgesia in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach needs further investigation. The aim of this study was to research the preemptive analgesic effects of flurbiprofen axetil in thoracic surgery, and the influence of preoperative administration on postoperative respiratory function.

METHODSThis randomized, double-blind, controlled trial enrolled 60 patients undergoing radical resection of esophageal carcinoma via the left thoracic approach. Anesthesia management was standardized. Each patient was randomly assigned to receive either 100 mg flurbiprofen axetil intravenously 15 minutes before incision (PA group) or intravenous normal saline as a control (C group). Postoperative analgesia was with sufentanil delivered by patient-controlled analgesia pump. Postoperative sufentanil consumption, visual analog scale pain scores, plasma levels of interleukin-8, and oxygenation index were measured.

RESULTSCompared with the preoperative baseline, postoperative patients in the PA group had no obvious increase in pain scores (P > 0.05), but patients in the C group had significantly increased pain scores (P < 0.05). Pain scores in the C group were significantly higher at 24 hours postoperatively than preoperatively. Intergroup comparisons showed lower visual analog scale scores at 2 - 24 hours postoperatively in the PA group than the C group (P < 0.05). Sufentanil consumption and plasma interleukin-8 levels at 2 and 12 hours postoperatively were significantly lower in the PA group than the C group (P < 0.05). The oxygenation index at 2 and 12 hours postoperatively was significantly higher in the PA group than the C group (P < 0.05).

CONCLUSIONSIntravenous flurbiprofen axetil appears to have a preemptive analgesic effect in patients undergoing radical resection of esophageal carcinoma via the left thoracic approach, and appears to contribute to recovery of respiratory function and to reduction of the postoperative inflammatory reaction.

Analgesia, Patient-Controlled ; methods ; Double-Blind Method ; Esophageal Neoplasms ; surgery ; Flurbiprofen ; analogs & derivatives ; therapeutic use ; Humans

Alzheimer's disease is increasingly common in elderly population with a large socioeconomic burden. Current available drugs for Alzheimer's disease are acetylcholinesterase inhibitors and N-methyl-D-aspartate receptor antagonist. Much effort is directed towards not just symptomatic treatments but disease-modifying treatments. Several drugs with differing targets and mechanisms of action are under development for the treatment of Alzheimer's disease. Phase III trials of dimebon, Ginkgo biloba, non-steroidal anti-inflammatory drugs, phenserine, statins, semagacestat, tarenflurbil, tramiprosate, valproate, xaliproden have been completed without demonstrating adequate efficacy. Encouraging results would be expected from ongoing phase III trials of bapineuzumab and solanezumab. The clinical trials for the disease-modifying treatment of Alzheimer's disease have resulted in both promise and disappointment.
Aged ; Alanine ; Alzheimer Disease ; Antibodies, Monoclonal, Humanized ; Azepines ; Cholinesterase Inhibitors ; Flurbiprofen ; Ginkgo biloba ; Humans ; Indoles ; N-Methylaspartate ; Naphthalenes ; Physostigmine ; Pyridines ; Taurine ; Valproic Acid