The binding of acetaminophen, lidocaine, and valproic acid to human milk

The binding of acetaminophen, lidocaine, and valproic acid to pooled normal mature human milk was studied in vitro by using equilibrium dialysis. Scatchard analysis revealed high-affinity, low-capacity binding for acetaminophen (Ka [affinity constant of association], 1.47 x 10(4) L/mol; Bo [concentr...

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Bibliographic Details
Published in:American journal of clinical pathology 2004-05, Vol.121 (5), p.754-757
Main Authors: BAILEY, David N, BRIGGS, John R
Format: Article
Language:English
Subjects:
Acetaminophen - metabolism
Analgesics, Non-Narcotic - metabolism
Anesthetics, Local - metabolism
Anticonvulsants - metabolism
Biological and medical sciences
Female
General aspects
Humans
Lidocaine - metabolism
Medical sciences
Milk, Human - metabolism
Tumors
Valproic Acid - metabolism
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Summary:The binding of acetaminophen, lidocaine, and valproic acid to pooled normal mature human milk was studied in vitro by using equilibrium dialysis. Scatchard analysis revealed high-affinity, low-capacity binding for acetaminophen (Ka [affinity constant of association], 1.47 x 10(4) L/mol; Bo [concentration of binding sites], 9.01 x 10(-4) mol/L) and some minimal, nonspecific binding. Binding ranged up to 85%. For lidocaine, low-affinity, high-capacity binding was noted (Ka, 1.42 x 10(2) L/mol; Bo, 1.69 x 10(-2) mol/L). Binding ranged up to 72%. For valproic acid, only minimal, nonspecific binding was noted at low drug concentrations with binding ranging up to 64%. The binding of these drugs to milk might enhance their excretion and subsequent ingestion by infants who are breast-fed. In addition, the low pH of the milk (6.24) may cause "ion trapping" of acetaminophen (pKa, 9.5) and lidocaine (pKa, 7.9).
ISSN:0002-9173
1943-7722
DOI:10.1309/A7M2FN2TYE6A8UFX