Disease relevance of SU 21524

• Although the risk of fulminant hepatitis is very low, we recommend that, in patients taking pirprofen for more than 2 mo and complaining of asthenia, nausea, or vomiting, serum aminotransferase levels should be measured and administration of the drug should be interrupted as soon as an increased level is noted [1].
• A total of 55 patients with primary dysmenorrhea who had shown a favorable response to a preliminary treatment cycle with placebo were admitted to a double-blind study on placebo versus antiprostaglandin agents (naproxen and pirprofen) [2].
• This study establishes the usefulness of pirprofen in the treatment of acute migraine [3].
• Working ability was well preserved with pirprofen, especially among patients with common migraine, and this treatment was ranked highest by the patients [3].
• At the dose of 100 mg/kg body weight for 1, 3, and 5 days, pirprofen was unable to induce its own glucuronidation [4].

High impact information on SU 21524

• We studied hepatic MTP activity, the lipoproteins present in the ER lumen, and hepatic lipoprotein secretion 4 hours after administration of a single dose of amineptine (1 mmol/kg), amiodarone (1 mmol/kg), doxycycline (0.25 mmol/kg), tetracycline (0.25 mmol/kg), tianeptine (0.5 mmol/kg), or pirprofen (2 mmol/kg) in mice [5].
• Pirprofen and aspirin in the treatment of rheumatoid arthritis [6].
• There were no statistically significant differences in efficacy between pirprofen and aspirin, as evidenced by patient opinion, observer opinion, grip strength, walking time, number of tender joints, number of swollen joints, or erythrocyte sedimentation rate [6].
• Audiologic evaluation revealed 3 pirprofen-treated patients and 5 aspirin-treated patients in whom sensorineural hearing loss progressed during therapy and required either discontinuation or reduction of drug dosage [6].
• Orally administered pirprofen is rapidly and almost completely absorbed from the gastrointestinal tract, resulting in maximum plasma levels in 1 to 2 hr [7].

Chemical compound and disease context of SU 21524

• Placebo-controlled double-blind trial of pirprofen and an ergotamine tartrate compound in migraine attacks [3].
• The study confirmed the usefulness of both pirprofen and piroxicam in a short-term treatment of decompensated osteoarthritis of weight-bearing joints associated with night pain [8].

Biological context of SU 21524

• A specific binding site for pirprofen on the HSA was found to be site II, benzodiazepine site, using fluorescence probes and drug markers [9].
• The assay was found suitable for the study of the pharmacokinetics of pirprofen enantiomers in the rat [10].
• The kinetics of the degradation of pirprofen to its pyrrole derivative were investigated [11].
• Selective high-performance liquid chromatographic methods for the simultaneous determination of pirprofen and five of its metabolites either in plasma or in urine before and after chemical hydrolysis were developed [12].
• No significant changes were produced in these measures and in vitro studies showed no displacement of glibenclamide by pirprofen from plasma protein binding [13].

Anatomical context of SU 21524

• We describe a high-performance liquid chromatographic method, using electrochemical detection, for the determination of pirprofen in cerebrospinal fluid (CSF), plasma, and synovial fluid (SF) [14].
• Analysis of pirprofen in cerebrospinal fluid, plasma, and synovial fluid by high-performance liquid chromatography with electrochemical detection [14].
• Gastric mucosa lesions were observed in 90% of pirprofen-treated patients and in 60% of those on naproxen (P = 0.03) [15].
• Central nervous system effects and tinnitus were reported by more patients in the aspirin group than in either of the pirprofen groups [16].
• Glucuronidation of 2-arylpropionic acids pirprofen, flurbiprofen, and ibuprofen by liver microsomes [4].

Associations of SU 21524 with other chemical compounds

• In a double-blind, between-patient trial, a new cyclo-oxygenase inhibitor, pirprofen (800 mg/day), was compared with indomethacin (100 mg/day) and placebo in 56 patients undergoing cataract extraction [17].
• The susceptibility of established Trypanosoma brucei (8/18 strain) infection in mice and rabbits to low doses of diminazene (Berenil) in combination therapy with non-steroidal anti-inflammatory drugs (NSAIDs) has been evaluated using piroxicam (Feldene) and pirprofen (Rengasil) as examples of the NSAID [18].
• The direct effects on the cartilage articular surface of three anti-inflammatory drugs (Diclofenac, Pirprofen and acetyl-salicylic acid) and of a polysulfated glycosaminoglycan (Arteparon), were studied using an in vitro system in which BALB-c mouse femoral heads were incubated with the drugs [19].
• Experimental spinal cord trauma was performed intraoperatively in 132 rabbits (Allen's method modified by Faden et al.). Only 77 animals were administered drugs (glucocorticoids, antioxidants and anti-inflammatory nonsteroids): Prednisolon, Fluocinolon-N-spray, Epurox, Ketazone, Rheopyrin and Rengasil [20].
• Inhibition of prostaglandin synthase by pirprofen. Studies with sheep seminal vesicle enzyme [21].

Gene context of SU 21524

• These experimental results suggest that a reduction of the accumulation and activation of inflammatory cells in tissues may represent another way, together with cyclooxygenase inhibition, by which pirprofen realizes its antiinflammatory activity in vivo [22].

Analytical, diagnostic and therapeutic context of SU 21524

• A high-performance liquid chromatographic (HPLC) method was developed to determine the (+)- and (-)-enantiomers of pirprofen, an anti-inflammatory drug [23].
• Determination of the (+)- and (-)-enantiomers of pirprofen in human plasma by high-performance liquid chromatography [23].
• Thirty-two patients with JRA were enrolled in a 4-wk open-labeled, non-controlled multicentre trial of pirprofen [24].
• Determination of pirprofen in biological material by gas-liquid chromatography with nitrogen-specific and electron-capture detection [11].
• Pirprofen was well absorbed by man, rhesus monkey, rat, and mouse after oral administration of a solution of 14C-labeled compound [25].

References