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Cocaine and cocaethylene binding to human milk
1Department of Pathology, University of California, San Diego, USA.
American Journal of Clinical Pathology
|October 8, 1998
Summary
Cocaine and cocaethylene bind to human milk proteins like albumin, potentially increasing their transfer to nursing infants. This milk binding may affect drug levels and infant exposure.
Area of Science:
- Pharmacology
- Biochemistry
- Toxicology
Background:
- Cocaine and its metabolite, cocaethylene, are known substances of abuse.
- Maternal drug use during lactation poses risks to nursing infants.
- Understanding drug binding to human milk is crucial for assessing infant exposure.
Purpose of the Study:
- To investigate the binding characteristics of cocaine and cocaethylene to human milk.
- To quantify the binding affinity and capacity of milk components for these drugs.
- To evaluate the potential implications of milk binding on drug transfer to infants.
Main Methods:
- Equilibrium dialysis was employed at 4°C to study drug-milk interactions.
- Binding constants (Ka) and binding site concentrations (B0) were determined for both drugs.
- Potential binding components, such as albumin and lipids, were considered.
Main Results:
- Both cocaine and cocaethylene exhibited low-affinity, high-capacity binding to human milk.
- Albumin was identified as a likely primary binder, with additional weaker binding possibly due to lipids.
- Up to 55% of cocaine and 61% of cocaethylene were bound to milk components.
Conclusions:
- The significant binding of cocaine and cocaethylene to human milk suggests substantial partitioning into breast milk.
- The lower pH of milk compared to serum may further facilitate the mammary secretion of these basic drugs.
- These findings highlight potential risks for nursing infants due to enhanced drug transfer and exposure.