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Influence of Chronic Obstructive Lung Disease on the Disposition of an Acidic Drug (Sulfamethazine)

Influence of Chronic Obstructive Lung Disease on the Disposition of an Acidic Drug (Sulfamethazine) Abstract • The influence of chronic respiratory failure (CRF) on the pharmacokinetics of an acidic drug has been studied in 11 patients and in eight normal volunteers who received 10 mg/kg of oral sulfamethazine. Blood and urine samples were collected for 24 and 48 hours, respectively. No differences were observed in the rate of sulfamethazine absorption, but bioavailability was decreased when compared with control subjects. Sulfamethazine volume of distribution (Vd) was larger in patients than in control subjects. These differences in Vd may be secondary to an increase in sulfamethazine unbound fraction. No differences were observed in sulfamethazine elimination. It is concluded that in patients with CRF sulfamethazine bioavailability decreases, and Vd increases secondary to a decrease in binding. Despite the fact that plasma concentrations of the test drug will be decreased, the administration of higher doses may not be advisable. (Arch Intern Med 1983;143:233-236) References 1. Rowland M, Tozer TN: Clinical Pharmacokinetics: Concepts and Applications . Philadelphia, Lea & Febiger, 1980. 2. Odar-Cederlöf I, Borga O: Kinetics of diphenylhydantoin in uremic patients: Consequences of decreased plasma protein binding. Eur J Clin Pharmacol 1974;7:31-37.Crossref 3. Gugler R, Shoeman DW, Huffman DH, et al: Pharmacokinetics of drugs in patients with the nephrotic syndrome. J Clin Invest 1975;55:1182-1189.Crossref 4. Yacobi A, Udall JA, Levy G: Serum protein binding as a determinant of warfarin body clearance and anticoagulant effect. Clin Pharmacol Ther 1976;19:552-558. 5. Klotz U, Antonin KH, Bieck PR: Pharmacokinetics and plasma binding of diazepam in man, dog, rabbit, guinea pig and rat. Pharmacol Exp Ther 1976;199:67-73. 6. Williams RL, Blaschke TR, Meffin PJ, et al: Influence of acute viral hepatitis on disposition and plasma binding of tolbutamide. Clin Pharmacol Ther 1977;21:301-309. 7. Löscher W: Serum protein binding and pharmacokinetics of valproate in man, dog, rat and mouse. J Pharmacol Exp Ther 1978;204:255-261. 8. Pérez-Mateo M, Erill S: Protein binding of salicylate and quinidine in plasma from patients with renal failure, chronic liver disease and chronic respiratory insufficience. Eur J Clin Pharmacol 1977;11:225-231.Crossref 9. Resar RK, Walson PD, Fritz WL, et al: Kinetics of theophylline: Variability and effect of arterial pH in chronic obstructive lung disease. Chest 1979;76:11-16.Crossref 10. Bratton AP, Marshall E: New coupling component for sulfonamides determination. J Biol Chem 1939;128:537-550. 11. Du Souich P, McLean AJ, Lalka D, et al: Sulfadiazine handling in the rabbit: II. Mechanisms of nonlinear kinetics of elimination. J Pharmacol Exp Ther 1978;207:228-235. 12. Du Souich P, Lalka D, Slaughter R, et al: Mechanisms of nonlinear disposition kinetics of sulfamethazine. Clin Pharmacol Ther 1979;25:172-183. 13. Metzler CM: NONLIN: A Computer Program for Parameter Estimation in Nonlinear Situations: Technical Report No 7292/69/7292/005 . Kalamazoo, Mich, Upjohn Co, 1969. 14. Gibaldi M, Perrier D: One-compartment model , in Swarbrick J (ed): Pharmacokinetics . New York, Marcel Dekker Inc, 1975, pp 1-43. 15. Du Souich P, McLean AJ, Stoeckel K, et al: Screening methods using sulfamethazine for determining acetylator phenotype. Clin Pharmacol Ther 1979;26:757-765. 16. Du Souich P, Erill S: Metabolism of procainamide in patients with chronic heart failure, chronic respiratory failure and chronic renal failure. Eur J Clin Pharmacol 1978;14:21-27.Crossref 17. Reidenberg MM, Affrime M: Influence of disease on binding of drugs to plasma proteins. Ann NY Acad Sci 1973;226:115-126.Crossref 18. Ehrnebo M, Agurell S, Jailing B, et al: Age differences in drug binding by plasma proteins: Studies on human foetuses, neonates and adults. Eur J Clin Pharmacol 1971;3:189-193.Crossref 19. Vallner JJ, Speir WA, Kolbeck RC, et al: Effect of pH on the binding of theophylline to serum proteins. Am Rev Respir Dis 1979;120:83-86. 20. Agnihotri SN, Clark RA, Cooper S, et al: Chronic pulmonary disease and antipyrine disposition. Br J Clin Pharmacol 1970;5:275-277.Crossref 21. Sotaniemi E, Arvela P, Huhti E, et al: Half-life of tolbutamide in patients with chronic respiratory failure. Eur J Clin Pharmacol 1971;4:29-31.Crossref 22. Boston Collaborative Drug Surveillance Program: Boston University Medical Center: Diphenylhydantoin side effects and serum albumin levels. Clin Pharmacol Ther 1973;14:529-532. 23. Reidenberg MM, Odar-Cederlof I, Von Bahr C, et al: Protein binding of diphenylhydantoin and desmethylimipramine in plasma from patients with poor renal function. N Engl J Med 1971;285:264-267.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Internal Medicine American Medical Association

Influence of Chronic Obstructive Lung Disease on the Disposition of an Acidic Drug (Sulfamethazine)

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Publisher
American Medical Association
Copyright
Copyright © 1983 American Medical Association. All Rights Reserved.
ISSN
0003-9926
eISSN
1538-3679
DOI
10.1001/archinte.1983.00350020051011
Publisher site
See Article on Publisher Site

Abstract

Abstract • The influence of chronic respiratory failure (CRF) on the pharmacokinetics of an acidic drug has been studied in 11 patients and in eight normal volunteers who received 10 mg/kg of oral sulfamethazine. Blood and urine samples were collected for 24 and 48 hours, respectively. No differences were observed in the rate of sulfamethazine absorption, but bioavailability was decreased when compared with control subjects. Sulfamethazine volume of distribution (Vd) was larger in patients than in control subjects. These differences in Vd may be secondary to an increase in sulfamethazine unbound fraction. No differences were observed in sulfamethazine elimination. It is concluded that in patients with CRF sulfamethazine bioavailability decreases, and Vd increases secondary to a decrease in binding. Despite the fact that plasma concentrations of the test drug will be decreased, the administration of higher doses may not be advisable. (Arch Intern Med 1983;143:233-236) References 1. Rowland M, Tozer TN: Clinical Pharmacokinetics: Concepts and Applications . Philadelphia, Lea & Febiger, 1980. 2. Odar-Cederlöf I, Borga O: Kinetics of diphenylhydantoin in uremic patients: Consequences of decreased plasma protein binding. Eur J Clin Pharmacol 1974;7:31-37.Crossref 3. Gugler R, Shoeman DW, Huffman DH, et al: Pharmacokinetics of drugs in patients with the nephrotic syndrome. J Clin Invest 1975;55:1182-1189.Crossref 4. Yacobi A, Udall JA, Levy G: Serum protein binding as a determinant of warfarin body clearance and anticoagulant effect. Clin Pharmacol Ther 1976;19:552-558. 5. Klotz U, Antonin KH, Bieck PR: Pharmacokinetics and plasma binding of diazepam in man, dog, rabbit, guinea pig and rat. Pharmacol Exp Ther 1976;199:67-73. 6. Williams RL, Blaschke TR, Meffin PJ, et al: Influence of acute viral hepatitis on disposition and plasma binding of tolbutamide. Clin Pharmacol Ther 1977;21:301-309. 7. Löscher W: Serum protein binding and pharmacokinetics of valproate in man, dog, rat and mouse. J Pharmacol Exp Ther 1978;204:255-261. 8. Pérez-Mateo M, Erill S: Protein binding of salicylate and quinidine in plasma from patients with renal failure, chronic liver disease and chronic respiratory insufficience. Eur J Clin Pharmacol 1977;11:225-231.Crossref 9. Resar RK, Walson PD, Fritz WL, et al: Kinetics of theophylline: Variability and effect of arterial pH in chronic obstructive lung disease. Chest 1979;76:11-16.Crossref 10. Bratton AP, Marshall E: New coupling component for sulfonamides determination. J Biol Chem 1939;128:537-550. 11. Du Souich P, McLean AJ, Lalka D, et al: Sulfadiazine handling in the rabbit: II. Mechanisms of nonlinear kinetics of elimination. J Pharmacol Exp Ther 1978;207:228-235. 12. Du Souich P, Lalka D, Slaughter R, et al: Mechanisms of nonlinear disposition kinetics of sulfamethazine. Clin Pharmacol Ther 1979;25:172-183. 13. Metzler CM: NONLIN: A Computer Program for Parameter Estimation in Nonlinear Situations: Technical Report No 7292/69/7292/005 . Kalamazoo, Mich, Upjohn Co, 1969. 14. Gibaldi M, Perrier D: One-compartment model , in Swarbrick J (ed): Pharmacokinetics . New York, Marcel Dekker Inc, 1975, pp 1-43. 15. Du Souich P, McLean AJ, Stoeckel K, et al: Screening methods using sulfamethazine for determining acetylator phenotype. Clin Pharmacol Ther 1979;26:757-765. 16. Du Souich P, Erill S: Metabolism of procainamide in patients with chronic heart failure, chronic respiratory failure and chronic renal failure. Eur J Clin Pharmacol 1978;14:21-27.Crossref 17. Reidenberg MM, Affrime M: Influence of disease on binding of drugs to plasma proteins. Ann NY Acad Sci 1973;226:115-126.Crossref 18. Ehrnebo M, Agurell S, Jailing B, et al: Age differences in drug binding by plasma proteins: Studies on human foetuses, neonates and adults. Eur J Clin Pharmacol 1971;3:189-193.Crossref 19. Vallner JJ, Speir WA, Kolbeck RC, et al: Effect of pH on the binding of theophylline to serum proteins. Am Rev Respir Dis 1979;120:83-86. 20. Agnihotri SN, Clark RA, Cooper S, et al: Chronic pulmonary disease and antipyrine disposition. Br J Clin Pharmacol 1970;5:275-277.Crossref 21. Sotaniemi E, Arvela P, Huhti E, et al: Half-life of tolbutamide in patients with chronic respiratory failure. Eur J Clin Pharmacol 1971;4:29-31.Crossref 22. Boston Collaborative Drug Surveillance Program: Boston University Medical Center: Diphenylhydantoin side effects and serum albumin levels. Clin Pharmacol Ther 1973;14:529-532. 23. Reidenberg MM, Odar-Cederlof I, Von Bahr C, et al: Protein binding of diphenylhydantoin and desmethylimipramine in plasma from patients with poor renal function. N Engl J Med 1971;285:264-267.Crossref

Journal

Archives of Internal MedicineAmerican Medical Association

Published: Feb 1, 1983

References