Biomaterial Database

Elevated free fatty acid concentrations in lipemic sera reduce protein binding of valproic acid significantly more than phenytoin. 1997

A Dasgupta, and M J Crossey

Department of Pathology, University of New Mexico School of Medicine, Albuquerque 87106, USA.

Higher concentrations of free valproic acid and phenytoin have been reported in patients with uremia and liver disease. Free fatty acids also displace valproic acid and phenytoin. This is a study of the magnitude of displacement of valproic acid and phenytoin from protein binding by free fatty acid in lipemic sera. Higher concentrations of free fatty acids in lipemic sera affected protein binding of valproic acid significantly more than that of phenytoin. Supplementing normal sera with free fatty acids also increased the free concentrations of both valproic acid and phenytoin as expected, but the observed effect was several times higher in magnitude with valproic acid. There was an increased free fraction of valproic acid in patients who received valproic acid and had hypertriglyceridemia. In a patient with uremia, there was also a significant increase in free valproic acid concentration after routine hemodialysis caused by an increase in free fatty acid concentration secondary to hemodialysis. Increased protein binding of valproic acid in sera was observed after treatment with activated charcoal because charcoal can remove free fatty acid. Because higher free fatty acid concentration significantly affects protein binding of valproic acid, careful monitoring of free valproic acid in patients with lipid disorder may be beneficial.

UI	MeSH Term	Description	Entries
D006949	Hyperlipidemias	Conditions with excess LIPIDS in the blood.	Hyperlipemia,Hyperlipidemia,Lipemia,Lipidemia,Hyperlipemias,Lipemias,Lipidemias
D010672	Phenytoin	An anticonvulsant that is used to treat a wide variety of seizures. It is also an anti-arrhythmic and a muscle relaxant. The mechanism of therapeutic action is not clear, although several cellular actions have been described including effects on ion channels, active transport, and general membrane stabilization. The mechanism of its muscle relaxant effect appears to involve a reduction in the sensitivity of muscle spindles to stretch. Phenytoin has been proposed for several other therapeutic uses, but its use has been limited by its many adverse effects and interactions with other drugs.	Diphenylhydantoin,Fenitoin,Phenhydan,5,5-Diphenylhydantoin,5,5-diphenylimidazolidine-2,4-dione,Antisacer,Difenin,Dihydan,Dilantin,Epamin,Epanutin,Hydantol,Phenytoin Sodium,Sodium Diphenylhydantoinate,Diphenylhydantoinate, Sodium
D011485	Protein Binding	The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.	Plasma Protein Binding Capacity,Binding, Protein
D001798	Blood Proteins	Proteins that are present in blood serum, including SERUM ALBUMIN; BLOOD COAGULATION FACTORS; and many other types of proteins.	Blood Protein,Plasma Protein,Plasma Proteins,Serum Protein,Serum Proteins,Protein, Blood,Protein, Plasma,Protein, Serum,Proteins, Blood,Proteins, Plasma,Proteins, Serum
D002606	Charcoal	An amorphous form of carbon prepared from the incomplete combustion of animal or vegetable matter, e.g., wood. The activated form of charcoal is used in the treatment of poisoning. (Grant & Hackh's Chemical Dictionary, 5th ed)	Activated Charcoal,Actidose,Actidose-Aqua,Adsorba,Carbomix,Charbon,CharcoAid,CharcoCaps,Charcodote,Formocarbine,Insta-Char,Kohle-Compretten,Kohle-Hevert,Kohle-Pulvis,Kohle-Tabletten Boxo-Pharm,Liqui-Char,Norit,Ultracarbon,Charcoal, Activated
D003404	Creatinine		Creatinine Sulfate Salt,Krebiozen,Salt, Creatinine Sulfate,Sulfate Salt, Creatinine
D005230	Fatty Acids, Nonesterified	FATTY ACIDS found in the plasma that are complexed with SERUM ALBUMIN for transport. These fatty acids are not in glycerol ester form.	Fatty Acids, Free,Free Fatty Acid,Free Fatty Acids,NEFA,Acid, Free Fatty,Acids, Free Fatty,Acids, Nonesterified Fatty,Fatty Acid, Free,Nonesterified Fatty Acids
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001663	Bilirubin	A bile pigment that is a degradation product of HEME.	Bilirubin IX alpha,Bilirubin, (15E)-Isomer,Bilirubin, (4E)-Isomer,Bilirubin, (4E,15E)-Isomer,Bilirubin, Calcium Salt,Bilirubin, Disodium Salt,Bilirubin, Monosodium Salt,Calcium Bilirubinate,Hematoidin,delta-Bilirubin,Bilirubinate, Calcium,Calcium Salt Bilirubin,Disodium Salt Bilirubin,Monosodium Salt Bilirubin,Salt Bilirubin, Calcium,delta Bilirubin
D014280	Triglycerides	An ester formed from GLYCEROL and three fatty acid groups.	Triacylglycerol,Triacylglycerols,Triglyceride