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, cardi...

Degradation reactions on diclofenac-monoglycerides (3a,b), diclofenac-(p-hydroxybenzoate)-2-monoglyceride (3c), diclofenac (1), and diclofenac lactam (4) were performed at 37 °C in isotonic buffer solutions (apparent pH range 1-8) containing varying concentrations of acetonitrile (ACN). The concentration remaining of each analyte was measured versus time. Diclofenac-monoglycerides and diclofena...

objective: to detect whether the preoperative combined administration of rectal diclofenac and paracetamol is superior to placebo or rectal diclofenac alone for pain after abdominal hysterectomy. materials and methods: ninety female patients (american society of anesthesiologists (asa) physical status i-ii), scheduled for abdominal hysterectomy were recruited to this double blind trial and were...

Pharmaceuticals form a new class of micropollutants that poses a serious threat to our aquatic environment and its organisms. Advanced technologies in waste water treatment like membrane bioreactors (MBR) have proven better elimination of organic pollutants. But still their removal capacity might be not be sufficient to remove pharmaca and their metabolites completely. Biological wastewater tre...

Diclofenac is a widely used analgesic drug that can cause serious adverse drug reactions. We used Saccharomyces cerevisiae as a model eukaryote with which to elucidate the molecular mechanisms of diclofenac toxicity and resistance. Although most yeast cells died during the initial diclofenac treatment, some survived and started growing again. Microarray analysis of the adapted cells identified ...

The amino acid residues affecting the substrate specificity of human cytochrome P450 CYP2C9 and CYP2C19 for their metabolic activities were investigated using chimeras and mutant enzymes, which were constructed by replacing the corresponding residues. Although CYP2C19 showed nearly the same tolbutamide hydroxylase activity as CYP2C9, the activities for the CYP2C19(H99I) mutant and the chimeras ...

Poor penetration of diclofenac through in vitro rat dorsal skin including subcutaneous tissue was observed. The poor penetration of diclofenac seemed to be predominIntly due to the poor permeability of the stratum corneum. Hydrogenated soya phospholipids (phospholipid) in aqueous gel form increased the penetration of diclofenac in the in vitro study, by increasing diclofenac transport through t...

The cytochrome P-450 (CYP)3A4-mediated metabolism of diclofenac is stimulated in vitro by quinidine. A similar effect is observed in incubations with monkey liver microsomes. We describe an in vivo interaction of diclofenac and quinidine that leads to enhanced clearance of diclofenac in monkeys. After a dose of diclofenac via portal vein infusion at 0.055 mg/kg/h, steady-state systemic plasma d...

Previous work demonstrates that the reactive acyl glucuronide of the nonsteroidal antiinflammatory drug diclofenac forms selective protein adducts in the liver, which may play a causal role in the pathogenesis of diclofenac-associated liver toxicity. Because glucuronide conjugates can be exported into the bile, we explored the role of diclofenac glucuronide hepatobiliary transport in the format...