Plasma protein binding of carbamazepine

Hooper W.D., Dubetz D.K., Bochner F., Cotter L.M., Smith G.A., Eadie M.J. and Tyrer J.H. (1975) Plasma protein binding of carbamazepine. Clinical Pharmacology and Therapeutics, 17 4: 433-440.

Author Hooper W.D.
Dubetz D.K.
Bochner F.
Cotter L.M.
Smith G.A.
Eadie M.J.
Tyrer J.H.
Title Plasma protein binding of carbamazepine
Journal name Clinical Pharmacology and Therapeutics   Check publisher's open access policy
ISSN 0009-9236
Publication date 1975-01-01
Sub-type Article (original research)
Volume 17
Issue 4
Start page 433
End page 440
Total pages 8
Subject 3004 Pharmacology
2736 Pharmacology (medical)
Abstract The binding of carbamazepine to the proteins of human plasma has been studied using ultrafiltration techniques. In vitro studies at 37° C showed the relation between concentration of unbound drug and total drug to be linear through the range of total concentration of 5 to 50 μg/ml. The per cent unbound drug increased slightly as concentration increased. There was little difference between the extent of binding at 4° C and 20° C, but more carbamazepine was unbound at 37° C. Under in vitro conditions, 6 other anticonvulsants, and aspirin, were tested individually, each at high therapeutic or toxic concentration, and shown not to displace carbamazepine from plasma proteins to a significant degree. The extent of binding of carbamazepine in vivo was determined in a total of 54 plasma samples collected from treated patients; 26.9 ± SD 9.4% of the drug was unbound. In blood samples from 23 of these patients, the red cell concentration of carbamazepine averaged 38.3 ± SD 17.9% of the plasma concentration. The effects of hepatic and renal diseases on the carbamazepine binding capacity of plasma proteins were assessed by comparing the binding capacity of plasma from diseased persons with that from normal subjects. There was no significant difference in binding capacity between plasma from patients with renal disease and that from normal subjects. However, the plasma from patients with hepatic disease bound a slightly lower percentage of carbamazepine than did normal plasma (p < 0.05). This alteration did not correlate with changes in any of 15 biochemical parameters measured in these patients. The clinical significance of these results is discussed.
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import - Archived
 
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