Search results for "diclofenac"

The prophylactic effect of aEugenia aqueaextract against oxidative stress and inflammation associated with the development of arthritis in an adjuvan…

2018

Rheumatoid arthritis (RA) is the most common human autoimmune disease. A petroleum ether extract of Eugenia aquea (E. aquea) was analyzed by GC/MS. Antioxidant and anti-inflammatory activities were investigated in rats with adjuvant-induced arthritis (AIA). An AIA rat model received orally/daily a vehicle, diclofenac (100 mg per kg b.w.), and E. aquea extract (50 or 100 or 200 mg per kg b.w.; for 21 days). Fifty-five out of 70 compounds (97.77%) were identified: eucalyptol (34.14%), α-pinene (15.91%), l-verbenone (8.01%), camphor (7.38%) and borneol (6.74%). In an acute oral toxicity study, the E. aquea extract did not show any toxic effects in rats at 2000 mg/ kg-1. Only a high dose of the…

Drug metabolism by cultured human hepatocytes: how far are we from the in vivo reality?

2004

The investigation of metabolism is an important milestone in the course of drug development. Drug metabolism is a determinant of drug pharmacokinetics variability in human beings. Fundamental to this are phenotypic differences, as well as genotypic differences, in the expression of the enzymes involved in drug metabolism. Genotypic variability is easy to identify by means of polymerase chain reaction-based or DNA chip-based methods, whereas phenotypic variability requires direct measurement of enzyme activities in liver, or, indirectly, measurement of the rate of metabolism of a given compound in vivo. There is a great deal of phenotypic variability in human beings, only a minor part being…

2019

Tumor-derived lactic acid inhibits T and natural killer (NK) cell function and, thereby, tumor immunosurveillance. Here, we report that melanoma patients with high expression of glycolysis-related genes show a worse progression free survival upon anti-PD1 treatment. The non-steroidal anti-inflammatory drug (NSAID) diclofenac lowers lactate secretion of tumor cells and improves anti-PD1-induced T cell killing in vitro. Surprisingly, diclofenac, but not other NSAIDs, turns out to be a potent inhibitor of the lactate transporters monocarboxylate transporter 1 and 4 and diminishes lactate efflux. Notably, T cell activation, viability, and effector functions are preserved under diclofenac treatm…

Glycerosomes: Use of hydrogenated soy phosphatidylcholine mixture and its effect on vesicle features and diclofenac skin penetration.

2016

In this work, diclofenac was encapsulated, as sodium salt, in glycerosomes containing 10, 20 or 30% of glycerol in the water phase with the aim to ameliorate its topical efficacy. Taking into account previous findings, glycerosome formulation was modified, in terms of economic suitability, using a cheap and commercially available mixture of hydrogenated soy phosphatidylcholine (P90H). P90H glycerosomes were spherical and multilamellar; photon correlation spectroscopy showed that obtained vesicles were ∼131nm, slightly larger and more polydispersed than those made with dipalmitoylphosphatidylcholine (DPPC) but, surprisingly, they were able to ameliorate the local delivery of diclofenac, whic…

Rectal Diclofenac administration for prevention of post-Endoscopic Retrograde Cholangio-Pancreatography (ERCP) acute pancreatitis. Randomized prospec…

2019

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 Janu…

Relationship between rheological properties, in vitro release and in vivo equivalency of topical formulations of diclofenac.

2019

Determination of bioequivalence remains a challenge in generic topical drug development. To support pharmacokinetic studies, strategies to demonstrate microstructure sameness of the products being compared include in vitro evaluations, such as the comparison of rheological properties, droplet size and in vitro release rates. Nevertheless, defining the appropriate acceptance range to consider equivalence between test and reference formulation is complex. To shed more light into this issue, in vitro release and rheological properties were compared to in vivo bioequivalence data (systemic blood measurements within a clinical trial) after topical application of a single dose. Test and reference…

Ketorolac, diclofenac, and ketoprofen are equally safe for pain relief after major surgery

2002

Background Ketorolac is approved for the relief of postoperative pain but concerns have been raised over a possible risk of serious adverse effects and death. Two regulatory reviews in Europe on the safety of ketorolac found the data were inconclusive and lacked comparison with other non-steroidal anti-inflammatory drugs. The aim of this study was to compare the risk of serious adverse effects with ketorolac vs diclofenac or ketoprofen in adult patients after elective major surgery. Methods This prospective, randomized multicentre trial evaluated the risks of death, increased surgical site bleeding, gastrointestinal bleeding, acute renal failure, and allergic reactions, with ketorolac vs di…

Postoperative pain therapy after lumbar disc surgery.

2000

Object. This study was undertaken to determine whether a special postoperative pain administration of tramadol and diclofenac provides any benefits in patients who underwent microsurgical lumbar discectomy.  Methods. The study consisted of 60 patients undergoing microsurgical lumbar discectomy. Patients were randomly divided into two groups based on the postoperative pain management: 1) Group A (n=30): no standardized pain therapy; these patients received on demand different analgesics and at variable dosages which were selected by the neurosurgeons; 2) Group B (n=30): standardized pain therapy with specific dosages of tramadol and diclofenac in regular time intervals during the first 48 ho…

Analgesic effects of nonsteroidal anti-inflammatory drugs in cancer pain due to somatic or visceral mechanisms.

1999

The role of nonsteroidal anti-inflammatory drugs (NSAIDs) is well established in the treatment of cancer pain. This class of drugs is considered particularly effective in pain due to somatic mechanisms, although proof of this observation is lacking. To ascertain whether NSAIDs are more effective in specific nociceptive forms of cancer pain, they were administered alone or added to opioids in 32 patients with a sole pain mechanism, somatic pain due to bone metastases (17 patients) or visceral pain (15 patients), respectively. Pain intensity, mean doses of opioids used, and symptoms were recorded after starting NSAID. A significant reduction in pain intensity was found at 3, 7, and 14 days. N…

TAP Block Prior to Open Ventral Hernia Repair Improves Surgical Outcome.

2022

Abstract Background Ventral hernias commonly affect patients after major abdominal surgery. To reduce postoperative pain, the effects of the transversus abdominis plane (TAP) block, epidural analgesia and medication-only protocol have been investigated. The primary outcome was the cumulative dosage of opioids (morphine milligram equivalents MME), of acetaminophen and diclofenac for postoperative pain control on postoperative day (POD) 0, 1, and 2. Secondary outcomes were length of stay (LOS) and the pain scale rating using the numeric rating scale (NRS) on POD 0, 1, and 2. Methods The data were retrospectively extracted from the charts of the patients admitted for a surgical operation for O…