Protein binding characteristics of bumetanide.
The association constants (k) and binding capacities (np) of bumetanide were determined in pooled venous blood obtained from adults, venous cord blood of healthy full-term infants, and critically ill neonates using ultrafiltration. Bumetanide was highly bound to plasma proteins (approximately 97%) in all three populations studied. Two classes of binding sites were identified, a high-affinity, low-capacity site with k and np in the order of 10(3) M-1 and 10(-3) M, respectively, and a low-affinity, high-capacity site with k and np in the order of 10(2) M-1 and 10(-2) M, respectively. Binding capacities were similar between the three groups studied and were larger than the 'presumed' therapeutic concentration following intravenous administration of the drug, which is on the order of 10(-6) M (less than or equal to 0.5 microgram/ml).
Walker
P C
PC
Department of Pharmacy Practice, Wayne State University College of Pharmacy, Detroit, Mich.
Berry
N S
NS
Edwards
D J
DJ
D000328:Adult; D000367:Age Factors; D001663:Bilirubin / Q000097:blood; D001798:Blood Proteins / Q000378:metabolism*; D002034:Bumetanide / Q000378:metabolism*; D004232:Diuretics / Q000378:metabolism*; D005312:Fetal Blood / Q000378:metabolism; D006801:Humans; D007231:Infant, Newborn; D007232:Infant, Newborn, Diseases / Q000097:blood / Q000378:metabolism*; D011485:Protein Binding; D012709:Serum Albumin / Q000032:analysis
D001798:Blood Proteins; D004232:Diuretics; D012709:Serum Albumin; D002034:Bumetanide; D001663:Bilirubin