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Protein binding characteristics of bumetanide
P C Walker1, N S Berry, D J Edwards
1Department of Pharmacy Practice, Wayne State University College of Pharmacy, Detroit, Mich.
Developmental Pharmacology and Therapeutics
|January 1, 1989
Summary
Bumetanide highly binds to plasma proteins in adults and infants, with two binding sites identified. Binding capacity exceeds therapeutic levels across all studied populations.
Area of Science:
- Pharmacokinetics
- Biochemistry
- Neonatal Medicine
Background:
- Bumetanide is a potent loop diuretic.
- Understanding drug binding to plasma proteins is crucial for pharmacokinetics.
- Variations in protein binding can affect drug efficacy and safety, especially in neonates.
Purpose of the Study:
- To determine the association constants (k) and binding capacities (np) of bumetanide in different populations.
- To compare bumetanide protein binding in adults, healthy term infants, and critically ill neonates.
Main Methods:
- Ultrafiltration technique was employed.
- Pooled venous blood from adults, cord blood from healthy infants, and blood from critically ill neonates were analyzed.
- Bumetanide binding to plasma proteins was quantified.
Main Results:
- Bumetanide exhibited high plasma protein binding (approximately 97%) across all groups.
- Two classes of binding sites were identified: high-affinity/low-capacity and low-affinity/high-capacity.
- Binding capacities were similar in all populations and exceeded the presumed therapeutic concentration of bumetanide.
Conclusions:
- Bumetanide's high protein binding is consistent across adult, infant, and neonatal populations.
- The identified binding sites and capacities suggest ample binding availability for bumetanide.
- These findings have implications for bumetanide dosing and therapeutic monitoring in diverse patient groups, particularly neonates.