PubMed · 9876805
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J Gallo. 1998. Brodifacoum.. https://pubmed.ncbi.nlm.nih.gov/9876805/
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The binding of drugs to human serum albumin determines the drug distribution through the systemic circulation and its pharmacological effects on the organism. Then, with the aim of obtaining information concerning the drug structural features which favour their binding on seroalbumin we have studied the seroalbumin binding to the heterocyclic drugs such as warfarin, propylthiouracil and cromoglycate and to similar compounds such as 4-hydroxy-coumarin, 3-acetylcoumarin, coumarin, benzylthiouracil, propyluracil, thiouracil, chromone and chromanol. These compounds were competitively displaced by warfarin at their primary binding sites on seroalbumin. The comparative analysis of the binding data showed that heterocyclic compounds such as benzopyranes (coumarins and chromanol) and benzyl pyrimidines with 4-hydroxyl groups bind specifically in the warfarin binding site. Then, 4-hydroxyl-bencene heterocycles will displace other ligands from the subdomain IIA of the seroalbumin molecule. Therefore, we can predict that the administration concomitant of warfarin, cromoglycate, propylthiouracil and analogous heterocyclic drugs involves the displacement of the drug without 4-hydroxyl and benzyl groups, increasing their free fraction in serum and the amount of active drug.
Cerium complexes of Umbellipherone, Mendiaxon, Warfarin, Coumachlor, and Niffcoumar have been synthesized by reaction of the ligands with cerium nitrate in a stoichiometric ratio of 1:2. The formation of the complexes has been proved on the basis of elemental analysis, conductivities, IR spectroscopy, and 1H-NMR spectroscopy. The molecules of the ligands were optimized by means of the semiempirical quantum mechanical method PM3 to the energetically most stable conformers. All the ligands were characterized by molecular and submolecular electronic indices and the putative donor centers are proposed. It is concluded that the lactone- and the keto-carbonyl groups of Warfarin, Coumachlor, and Niffcoumar are bonded to the metal ion as bidentate ligands. The other two coumarins are bonded as monodentate ligands. Conductivity measurements show the non-electrolytic nature of the complexes. Cytotoxic screening by MTT assay was carried out. The cerium complexes were found to be more active than the inorganic salts.
OBJECTIVE: To determine whether routine follow-up coagulation studies are useful in children with accidental exposures to rodenticides containing superwarfarin compounds. DESIGN: Retrospective review of poison center charts involving pediatric superwarfarin exposures occurring in two 2-year periods. SETTING: An American Association of Poison Control Centers-certified regional poison control center with an annual call volume of 55 000 calls per year from a 2-state area with a combined population of 4 million people. OUTCOME MEASURES: Prothrombin times and/or international normalized ratios and reported clinical signs of excessive anticoagulation after exposure. RESULTS: Of 542 children in 4 years of data collection, follow-up prothrombin times and/or international normalized ratios measurements did not detect any significant coagulation abnormalities. No child developed bleeding complications. No child required or received antidotal treatment with vitamin K. CONCLUSION: Normal preschool-aged children with unintentional acute exposures to superwarfarin rodenticides do not require any routine follow-up laboratory studies and do not require any medical intervention.