Disease relevance of Napanol

• Overview of efficacy of fenbufen in rheumatoid arthritis and osteoarthritis [1].
• Elevations of alkaline phosphatase and serum glutamic oxaloacetic transaminase levels, occurred occasionally with eosinophilia, particularly during the first four weeks of therapy with fenbufen [2].
• Single 800-mg doses of fenbufen were safely administered to 10 healthy subjects and to 16 patients with varying degrees of renal insufficiency [3].
• Fenbufen: a review of its pharmacological properties and therapeutic use in rheumatic diseases and acute pain [4].
• Compound 6l also showed potent in vivo antibacterial activity against Gram-positive and Gram-negative bacteria, and did not cause convulsions in mice with the concomitant administration of fenbufen [5].

High impact information on Napanol

• Long-term trials provided important information as to the relative effectiveness and tolerance of fenbufen in the management of patients with rheumatoid arthritis and osteoarthritis [1].
• The effects of fenbufen (1,000 mg a day), indomethacin (150 mg a day), naproxen (750 mg a day), and placebo on gastric mucosa were determined by endoscopy and recorded photographically [6].
• The results revealed that the effects of fenbufen on gastric mucosa were significantly (p less than or equal to 0.05) less than those of either naproxen or indomethacin and not statistically different from those observed with placebo [6].
• Mechanistic studies indicate that fenbufen has no intrinsic effect on cyclooxygenase activity, whereas its major metabolite, biphenylacetic acid, is a potent inhibitor of prostaglandin synthesis [7].
• Kinetics of single doses of fenbufen in patients with renal insufficiency [3].

Chemical compound and disease context of Napanol

• At a daily dosage of 600mg, fenbufen is comparable with aspirin 3.6g or indomethacin 75mg in osteoarthritis [4].
• One hundred analogs of fenbufen were prepared and tested using the carrageenan, polyarthritis, and UV erythema anti-inflammatory tests and the 2-phenyl-1,4-benzoquinone writhing and inflamed paw pressure analgesic tests [8].
• A single-blind cross-over comparison of fenbufen 600 mg nocte and piroxicam 20 mg nocte in osteoarthritis [9].
• The objective of the study was to compare efficacy and safety of Fenbufen and Aspirin in osteoarthritis [10].

Biological context of Napanol

• In contrast to the quinolones, which only increased the amplitudes of electrically evoked potentials, fenbufen induced spontaneous firing in the pyramidal cell layer without stimulation in addition to its dose-dependent effects on the amplitudes of the evoked potentials [11].
• Fenbufen, a new anti-inflammatory analgesic: synthesis and structure-activity relationships of analogs [8].
• 5. LPS treatment induced similar losses in body weight and muscle protein in both control and fenbufen groups, despite a 50% lower food intake in the LPS plus fenbufen group compared with the LPS-only group [12].
• Plasma concentration-time curves, pharmacokinetic parameters and serum protein binding of fenbufen and felbinac were not affected by the coadministration with ofloxacin [13].
• Pharmacokinetics of fenbufen in man [14].

Anatomical context of Napanol

• Assessment of the effects of combination therapy with ciprofloxacin and fenbufen on the central nervous systems of healthy volunteers by quantitative electroencephalography [15].
• These data indicate that 3T3-L1 adipocytes can synthesize fenbufen-containing lipids and release them into the medium on hormonal stimulation [16].
• Effect of fenbufen on the penetration of quinolone antibiotics into cerebrospinal fluid. Comparative study with 5 quinolones [17].
• The storage of xenobiotic compounds as glycerolipids and their subsequent mobilization was studied using fenbufen and differentiated 3T3-L1 cells in culture [16].
• Effect of the anti-inflammatory agent fenbufen on the quinolone-induced inhibition of gamma-aminobutyric acid binding to rat brain membranes in vitro [18].

Associations of Napanol with other chemical compounds

• When ciprofloxacin was administered in combination with fenbufen, none of the EEG parameters or VAS ratings measured were significantly different from those measured when the drugs were administered alone [15].
• When oleic acid was used in place of fenbufen, the majority of the radioactivity released in a chase experiment was the non-esterified acid (over 90%) and neither mono- nor di-acylglycerol was detected [16].
• The effects of fenbufen on the serum concentrations and penetration into the brain and CSF of sparfloxacin (AT-4140), a new quinolone antibacterial agent, were investigated in rats [19].
• Simultaneous determination of ofloxacin, fenbufen and felbinac in rat plasma by high-performance liquid chromatography [20].
• A six-month parallel group comparison of fenbufen and naproxen in the treatment of rheumatoid arthritis [21].

Gene context of Napanol

• The overall experience with fenbufen in 60 US and 37 foreign clinical trials is summarized in this report with respect to the following: therapeutic efficacy and safety in rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, analgesia and gout [22].
• Therefore, the convulsive action induced by quinolones and fenbufen does not seem to involve the function change of NMDA receptor [23].
• Fenbufen is currently marketed in Brazil, Columbia, Costa Rica, Dominican Republic, Ecuador, El Salvador, Great Britain, Greece, Guatemala, Honduras, Ireland, Italy, Japan, South Korea, Mexico, Nicaragua, Panama, Peru, Philippines, Rhodesia, Spain, South Africa, Switzerland, Trinidad and FR Germany [22].
• Tolmetin (100 mg/kg) and fenbufen (50 mg/kg) increased carnitine acetyltransferase (CAT) and fatty acyl-coenzyme A oxidizing system (FAOS) activities, which participate in hepatic lipid metabolism [24].

Analytical, diagnostic and therapeutic context of Napanol

• No cases of drug-related jaundice have been reported either in clinical trials or from countries where fenbufen is marketed [2].
• 1. Interaction of quinolone antibiotics and the anti-inflammatory agent fenbufen with the gamma-aminobutyric acid-A (GABAA) receptor-chloride channel complex in pyramidal neurons freshly dissociated from the hippocampal CA1 region of the rats was investigated in whole-cell mode, using the patch-clamp technique under voltage-clamp conditions [25].
• High-performance liquid chromatography assay for fenbufen and two serum metabolites [26].
• In a randomized, double-blind crossover study patients received 75 mg of indomethacin daily or 600 mg of fenbufen daily for six weeks and then were treated with the alternate regimen for a similar period [27].
• Improved dissolution behavior of fenbufen by spherical crystallization [28].

References