Disease relevance of Bucolom

• Induction of kernicterus by bucolome in rats [1].
• To determine whether bucolome (5-n-butyl-1-cyclohexyl-2,4,6-trioxoperhydropyrimidine), a nonsteroidal anti-inflammatory agent, can reverse diuretic resistance of furosemide in patients with nephrotic syndrome, we examined the inhibitory effect of bucolome on the protein binding of furosemide in serum and urine [2].
• No sedation or drowsiness was observed in the infants given bucolome, and though the drug caused some vomiting, weight gains were unaffected [3].

High impact information on Bucolom

• When kernicterus was induced in jaundiced rats by an injection of bucolome, the NSE level in cerebrospinal fluid was elevated up to more than 30-fold the control, together with a significantly higher level of alpha gamma form in blood plasma are helpful in detecting neuronal damage in the central nervous system [4].
• Even at higher urine levels of furosemide, the inhibitory effect of bucolome on the protein binding of furosemide in UPA remains constant, and changes in pH at weakly acidic pH levels (pH 5.5-6.5) did not alter the inhibitory effect of bucolome [2].
• In contrast, bucolome elicited no appreciable changes in the plasma unbound (S)-warfarin concentration versus the international normalized ratio relationship [5].
• In vitro studies with recombinant human cytochrome P-450 2C9 and liver microsomes showed that bucolome was a potent mixed-type inhibitor for (S)-warfarin 7-hydroxylation, with K(i) of 8.2 and 20.2 microM, respectively [5].
• This combination increases the anticoagulant effect, which is most likely due to the interaction of bucolome with the pharmacokinetics (PK) or pharmacodynamics (PD) of warfarin [6].

Biological context of Bucolom

• Plasma volume as determined by 131I-labelled albumin dilution was not decreased in bucolome treated rats [7].

Associations of Bucolom with other chemical compounds

• In in vitro study, bucolome displaced bilirubin from human albumin strongly [8].
• The effects of bucolome (BC, 1-cyclohexyl-5-n-butyl-2,4,6-trioxoperhydropyrimidine, a non-steroid antiinflammatory agent), a potent choleretic, on the maximal biliary excretion rates (Tm) of sulfobromophthalein (BSP) and indocyanine green (ICG) were investigated in rats [9].
• BSP-binding capacity of the Yprotein was increased by phenobarbital, phetharbital and bucolome, and decreased by one of the N-phenylbarbiturates [10].

Analytical, diagnostic and therapeutic context of Bucolom

• Fifty preterm babies were randomly assigned to a group given oral bucolome (30 mg/kg per day for 5 days) and a control group [3].
• When the biliary radioactivity was examined by thin layer chromatography, it was found that the excretion of free colchicine was significantly increased in bucolome treated rats which accounted for the observed increase in the biliary excretion of radioactivity in bucolome treated rats [11].

References