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Triazolam protein binding and correlation with alpha‐1 acid glycoprotein concentration
Author(s) -
Kroboth Patricia D,
Smith Randall B,
Sorkin Michael I,
Silver Marcia R,
Rault Raymond,
Garry Michael,
Juhl Randy P
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.191
Subject(s) - triazolam , chemistry , orosomucoid , albumin , hypnotic , chromatography , plasma concentration , clinical pharmacology , plasma protein binding , dialysis , serum albumin , pharmacology , endocrinology , medicine , glycoprotein , biochemistry , benzodiazepine , receptor
On two occasions separated by a minimum of 1 wk, plasma was obtained from 12 patients (aged 18 to 73 yr) on dialysis after an overnight fast. Samples were assayed for albumin and α 1 ‐acid glycoprotein (AGP) concentrations. 14 C‐Triazolam was added to each sample to a final concentration of 5 ng/ml. Protein binding was determined by equilibrium dialysis. Unbound triazolam ranged from 6.4% to 15.4% (X̄ = 10.0%). AGP concentrations ranged from 71.8 to 205.1 mg% (X̄ = 123.4 mg%). Triazolam binding ratio (bound/unbound concentration) correlated with AGP concentration (r 2 = 0.69) but not with albumin concentration, age, or sex. This correlation was verified by adding AGP in varying amounts to control plasma. Clinical Pharmacology and Therapeutics (1984) 36, 379–383; doi: 10.1038/clpt.1984.191