Differential effects of hepatic cirrhosis on the plasma protein binding of drugs.
The binding of sulfisoxazole (sulfafurazole-INN) (100 micrograms/ml), diazepam (3 micrograms/ml) and digitoxin (0.025 micrograms/ml) has been studied in plasma from normal volunteers and from patients with hepatic cirrhosis. The free fraction of sulfisoxazole and diazepam in plasma was increased in these patients (22.9 +/- 3.0% and 6.5 +/- 0.7%) vs 6.6 +/- 0.6% and 3.1 +/- 0.2% in normal subjects, respectively), but binding of digitoxin did not greatly change (13.7 +/- 3.95% vs 13.9 +/- 2.27% in the control group). The increase in the free fraction of sulfisoxazole and diazepam correlated well with decreased serum albumin levels; but a change in albumin affinity, perhaps due to increased bilirubin levels, should also to be taken in consideration to explain this decreased drug binding in hepatic cirrhosis.
D001798:Blood Proteins / Q000378:metabolism*; D003975:Diazepam / Q000097:blood; D004074:Digitoxin / Q000097:blood; D005260:Female; D006801:Humans; D008103:Liver Cirrhosis / Q000378:metabolism*; D008297:Male; D004364:Pharmaceutical Preparations / Q000097:blood*; D011485:Protein Binding; D012709:Serum Albumin / Q000378:metabolism; D013444:Sulfisoxazole / Q000097:blood
D001798:Blood Proteins; D004364:Pharmaceutical Preparations; D012709:Serum Albumin; D013444:Sulfisoxazole; D004074:Digitoxin; D003975:Diazepam