Disease relevance of Phenylprenazone

• Safety and efficacy of feprazone for long-term treatment of rheumatoid arthritis and osteoarthritis [1].
• Fixed drug eruptions with feprazone are linked to HLA-B22 [2].
• Contact dermatitis from feprazone [3].
• Renal failure complicating feprazone treatment [4].
• Thrombocytopenia and haemolytic anaemia due to feprazone [5].

High impact information on Phenylprenazone

• Two studies are reported; a double-blind cross-over trial of feprazone 600 mg daily and aspirin 3.6 g daily in the treatment of rheumatoid arthritis, and an uncontrolled open study of gastrointestinal tolerance in twenty rheumatoid arthritis patients with known intolerance to other drugs [6].
• A strong correlation was found between B22 antigen and feprazone-induced FDE [7].
• Feprazone: absence of hemolytic effects in glucose-6-phosphate dehydrogenase-deficient subjects [8].
• Eleven normal subjects were treated with feprazone and their erythrocytes were incubated in their own sera (containing active feprazone metabolites) and [1-14C]-glucose [8].
• Long-term safety and efficacy of feprazone (4-prenyl-1,2-diphenyl-3,5-pyrazolidinedione), an antirheumatic drug that is well tolerated in the gastrointestinal tract, were assessed in a noncontrolled multicenter trial [1].

Biological context of Phenylprenazone

• 1. The pharmacokinetics of feprazone were studied in nine healthy volunteers and 10 elderly patients [9].
• 4. When 4'-hydroxyfeprazone was administered as a single oral dose to a human volunteer the plasma elimination half-life of the metabolite was 18 h, but after administration of feprazone the half-life of 4'-hydroxyfeprazone was 45 +/- 29 h (10 subjects), indicating the slow hydroxylation of feprazone and the slow excretion of 4'-hydroxyfeprazone [10].
• A 31-year-old woman with three pemphigus-prone antigens in her HLA haplotype (B7, DR4, DQw7) developed the disease soon after taking a pyrazolone derivative, viz. feprazone [11].
• 3. These results show no impairment of the elimination of feprazone in RA or RI patients; Vd and Cl are greater than in healthy young volunteers or elderly subjects, the AUC values are lower, but t1/2 values are similar in all groups [12].
• A monitored-release study of methrazone in general practice [13].

Associations of Phenylprenazone with other chemical compounds

• Feprazone, a non-steroidal anti-inflammatory drug, was compared with indomethacin in a double-blind cross-over trial in 24 patients with ankylosing spondylitis, over eight weeks [14].
• A short-term double-bind cross-over trial of prenazone 600 mg daily and phenylbutazone 300 mg daily was carried out in twenty out-patients with rheumatoid arthritis [15].
• A double-blind cross-over trial of Prenazone 600 mg and Aspirin 4 g daily was carried out on 20 patients suffering with rheumatoid arthritis [16].

Gene context of Phenylprenazone

• A trial of feprazone in ankylosing spondylitis [14].
• Chemical characterization of decomposition products of pyrazolidinedione-3,5 derivatives. Part 2: Chemical transformations of 4-prenyl-1,2-diphenyl-3,5-pyrazolidinedione (prenazone) and its main decomposition product N,N'-diphenylhydrazide-2-carboxy-5-methyl-4-hexenoic acid in sulphuric acid concentrated [17].

Analytical, diagnostic and therapeutic context of Phenylprenazone

• Rectal administration of feprazone in healthy volunteers [18].
• The disposition of feprazone and its hydroxylated metabolite in human volunteers [10].
• In our newly developed HPLC method, using feprazone as an internal standard, extreme care is taken to avoid degradation of the compounds during the extraction procedure [19].
• The blood levels and excretion of radioactivity administered as 14C- or 3H-4-prenyl-1,2-diphenyl-3,5-pyrazolidinedione (DA 2370) have been studied after oral administration to dogs and man [20].
• The use of thermography in the evaluation of the anti-inflammatory activity of feprazone on rheumatoid arthritis [21].

References