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  • alpha1-acid glycoprotein  (2)
  • NONMEM
  • 1985-1989  (2)
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  • 1
    ISSN: 1432-1041
    Keywords: carbamazepine ; epilepsy ; carbamazepine-10,11 epoxide ; alpha1-acid glycoprotein ; serum protein binding ; children
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The relationship between the serum protein binding of carbamazepine (CBZ) and carbamazepine-10,11 epoxide (CBZ-E) and the concentration of α1-acid glycoprotein (AAG) and albumin (HSA) was examined in 39 CBZ-treated epileptic children aged 4 months to 12 years. A significant inverse correlation was found between the free fraction of both compounds and serum AAG, even though changes in AAG concentration explained only part of the variation in binding. No correlation was found between the free fraction of CBZ and CBZ-E and HSA, probably due to the small intersubject variation in HSA concentration. In vitro experiments showed that both CBZ and CBZ-E were bound to HSA and to a lesser extent to AAG. At equivalent HSA concentrations, the binding of CBZ and its metabolite increased proportionately with increasing AAG concentration within the range occurring clinically.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: carbamazepine ; serum protein binding ; alpha1-acid glycoprotein ; albumin
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The protein binding of carbamazepine (CBZ) in vitro was assessed in sera from 47 patients with various diseases known to alterα 1-acid glycoprotein (AAG) concentration and from 20 drug-free normal control subjects. In the patient group, AAG and albumin (HSA) concentrations ranged from 6 to 74 µmol/l and from 377 to 652 µmol/l, respectively; in the controls, protein concentrations were less variable, ranging from 11 to 26 µmol/l for AAG and from 623 to 754 µmol/l for HSA. In both the patient and the combined patient and control groups, free CBZ fractions were inversely correlated with the serum AAG concentration (r=−0.62). No significant relationship could be found between the free CBZ fraction and the serum HSA concentration. The free CBZ fraction was moderately but significantly decreased in patients with AAG levels above 26 µmol/l (the highest value found in controls) as compared either to patients with a normal AAG concentration or to control subjects (19±5% vs 23±4% and 23±2%), despite the finding of a higher HSA concentration in the control group. The data confirm AAG as an important determinant of interindividual variability in serum CBZ binding.
    Type of Medium: Electronic Resource
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