Disease relevance of Phenazone

• A randomised controlled trial of antipyrine (phenazone) in the prophylaxis of neonatal jaundice was completed in 48 women [1].
• Quantifying hepatic function in the presence of liver disease with phenazone (antipyrine) and its metabolites [2].
• An estimate is made of the sensitivity and specificity of phenazone testing for the verification of the presence of cirrhosis based on this compiled literature [2].
• This article provides a review of background information about normal plasma phenazone pharmacokinetics, urinary metabolite disposition and tabulations of reported total body clearances of the drug in the presence of cirrhosis, fatty liver, hepatitis and cholestasis in humans [2].
• Efficacy of phenazone in the treatment of acute migraine attacks: a double-blind, placebo-controlled, randomized study [3].

High impact information on Phenazone

• Whereas the elimination half-life did not change, clearance of phenazone decreased by about 50% with age in healthy women receiving phenazone without theophylline [4].
• Human over-use of analgesics containing phenacetin, antipyrene (phenazone) and caffeine has been associated with the development of both renal pelvic and bladder tumors [5].
• Compared with placebo, the phenazone treatment also resulted in a significant improvement in the associated migraine symptoms of nausea, phonophobia and photophobia [3].
• Abuse of combination analgesics containing phenacetin, phenazone and caffeine may be a risk factor for development of ureteral tumors [6].
• Thus, the two metabolites 1,5-di-methyl-1,2-dehydro-3-pyrazolone (DP) and 4-(2-methylethyl)-1,5-dimethyl-1,2-dehydro-3-pyrazolone (PDP), postulated for the degradation of phenazone and propyphenazone, were identified and detected up to the microg/L level in raw and drinking water samples from public water supply [7].

Chemical compound and disease context of Phenazone

• Rhabdomyolysis without renal failure was noted after suicidal ingestion of 29 tablets of Spalt N containing 7.25 g of acetaminophen, 7.25 g of phenazone and 1.45 g of caffeine by a 29 year-old weighing 73 kg [8].

Biological context of Phenazone

• 4. The measured pharmacokinetic parameters suggested an impaired biotransformation of phenazone in animals with obstructive cholestasis, leading to a slower drug elimination [9].
• The influence of disease on phenazone kinetics was studied before chemotherapy and the effect of anticancer drugs administration after the first cycle of chemotherapy [10].
• Effects of chronic treatment with phenazone on the hot-plate test and [3H]serotonin binding sites in pons and cortex membranes of the rat [11].
• Haem biosynthesis and hydroxylation of phenazone during lead intoxication [12].
• The LD50 of chloridazone was calculated to be for rats 800 mg/kg bw (range 552 to 1160 mg/kg bw) and for pheasants 3684 mg/kg bw (range 1768 to 7677 mg/kg bw) [13].

Anatomical context of Phenazone

• These acidic drugs also reach comparatively high concentrations in the stomach wall, kidney cortex and blood, resulting in the well-known side effects that occur with acidic compounds but not with acetaminophen and phenazone [14].
• A relationship between phenazone serum levels and the antinociceptive effect was found; acute treatment with phenazone provokes a significant decrease in serotonin binding sites both in the pons and cerebral cortex after 2, 4 and 8 h, but not after 24 h [11].
• The organochlorine herbicide chloridazon interacts with cell membranes [15].
• Cytogenetic effects of the herbicide chloridazon in cultured sheep lymphocytes [16].
• Scanning electron microscopy revealed that 0.1 mM chloridazon induced erythrocyte crenation [15].

Associations of Phenazone with other chemical compounds

• A considerably higher interindividual variability in the disposition of phenazone and theophylline was observed in the frail elderly women [4].
• After dosage with phenazone, 4,4'-dihydroxyphenazone is excreted in conjugated form by man, rabbit, guinea pig and rat [17].
• The pharmacokinetics of antipyrine (phenazone) in 3 species of non-human primate have been evaluated following its intravenous administration at a dose level of 92 mg/kg [18].
• Individual and combined effect of anthracene, cadmium, and chloridazone on growth and activity of SOD izoformes in three Scenedesmus species [19].
• Compared to results previously obtained in this model, phenazone may be preferable to acetylsalicylic acid in oral surgery, but phenazone does not compare favourably with the results obtained with paracetamol [20].

Gene context of Phenazone

• The results of the study suggest that the depression in phenazone elimination in lead intoxication is possibly due to depressed hepatic cytochrome P450 levels [21].
• Photochemical decomposition of phenazone derivatives. Part 7: Mechanism of decomposition in aqueous solutions [22].

Analytical, diagnostic and therapeutic context of Phenazone

• The mean (+/- SD) fraction of phenazone absorbed calculated from perfusion data was 51 +/- 12% (3 ml/min), 64 +/- 19% (3 ml/min), and 42 +/- 27% (6 ml/min) for the three experiments, respectively [23].
• Detection and identification of phenazone-type drugs and their microbial metabolites in ground and drinking water applying solid-phase extraction and gas chromatography with mass spectrometric detection [7].
• RESULTS: The applied chemotherapy inhibited phenazone elimination [24].
• Influence of bed rest on the pharmacokinetics of phenazone [25].
• RESULTS: The mean phenazone half-life time was significantly shorter in patients with AML (8.79 (3.01) h) than in control group (11.08 (3.61) h) (p < 0.012) [10].

References