Influence of concentration-dependent protein binding on serum concentrations and urinary excretion of disopyramide and its metabolite following oral administration
✍ Scribed by David B. Haughey; John J. Lima
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- English
- Weight
- 494 KB
- Volume
- 4
- Category
- Article
- ISSN
- 0142-2782
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✦ Synopsis
Abstract
Concentrations of disopyramide (D) and mono‐N‐dealkyldisopyramide (MND) were measured in serum and urine following administration of 100, 150, 200, and 300 mg D to four volunteers. The free fraction of D in serum was drug concentration‐dependent in all four subjects following the administration of the four doses. Areas under the free (unbound) D serum concentration‐time curves (AUC) were linearly related to dose following 100–200 mg D. AUC values were 30–60 per cent higher than expected in two subjects following 300 mg D due to an apparent dose‐dependent decrease in D renal tubular secretion. Renal clearance of free D averaged 10·91h^−1^. The renal clearance of MND averaged 10·31h^−1^. The urinary excretion of MND was proportional to disopyramide dose.