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Rapid and Sustained Oral Theophyllinen Loading: An Alternative to Intravenous Aminophylline Therapy

Rapid and Sustained Oral Theophyllinen Loading: An Alternative to Intravenous Aminophylline Therapy Abstract • We evaluated an oral theophylline loading-dose procedure that was designed to rapidly achieve and sustain theophylline serum concentrations of approximately 10 to 12 μg/mL. Ten healthy adults were given an oral loading dose of approximately 6 mg/kg of aminophylline, (Aminophyllin®) (ie, 4.8 mg/kg of theophylline). Two hours later, each subject was given approximately 6 mg/kg of a sustained-release theophylline tablet (Theo-Dur®). Serum samples were collected at 1/2, 1, 2, 3, 6, 9, and 12 hours, then assayed for theophylline concentration. The mean theophylline concentration (±SD) one hour after the initial loading dose was 10.5±2.3 μg/mL. Subsequent theophylline concentrations demonstrated minimal fluctuation, with means ranging from 10.7 ± 1.6 to 13.6 ± 2.8 μg/mL. Four of the subjects reported headache; none vomited or experienced severe nausea. We conclude that this method of oral theophylline loading can be effective in achieving prompt and sustained therapeutic theophylline levels without significant side effects and that this may provide a valuable therapeutic alternative in those asthmatic patients who do not clearly require intravenous aminophylline therapy. (Arch Intern Med 1983;143:794-796) References 1. Weinberger M, Hendeles L, Bighley L: The relation of product formulation to absorption of oral theophylline. N Engl J Med 1978;299: 852-857.Crossref 2. Powell JR, Thiercelin JF, Vozeh S, et al: The influence of cigarette smoking and sex on theophylline disposition. Am Rev Respir Dis 1977;116: 17-23. 3. Hendeles L, Weinberger M, Johnson G: Monitoring serum theophylline levels. Clin Pharamcokinet 1978;3:294-312.Crossref 4. IV dosage guidelines for theophylline products. FDA Drug Bull 1980;10:4-6. 5. Rubenstein KE: Homogeneous enzyme immunoassay today. Scand J Immunol Suppl 1978;8:53-62.Crossref 6. EMIT-aad Theophylline Assay Product Information . Palo Alto, Calif, Syva Corp, 1977. 7. Kwok F, Kradjan WA: Comparative bioavailability of two uncoated aminophylline tablets. Am J Hosp Pharm 1980;37:1618-1620. 8. Upton RA, Sansom L, Guentert TW, et al: Evaluation of the absorption from 15 commercial theophylline products indicating deficiencies in currently applied bioavailability data. J Pharmacokinet Biopharm 1980;8: 229-242.Crossref 9. Kelly HW, Murphy S: Serum theophylline levels in asthmatic children receiving sustained-release theophylline tablets. Am J Hosp Pharm 1979; 10:1698-1701. 10. Spangler DL, Kalof DD, Bloom FL, et al: Theophylline bioavailability following oral administration of six sustained-release preparations. Ann Allergy 1978;40:6-11. 11. Domson JF, Hein EW, Sheen A, et al: Comparison of Theolair SR and Theo-Dur tablets. Ann Allergy 1979;43:220-222. 12. Kelly HW, Murphy S: Efficacy of a 12-hour sustained-release preparation in maintaining therapeutic serum theophylline levels in asthmatic children. Pediatrics 1980;66:97-102. 13. Hein EW, Domson JF, Sheen A, et al: Simultaneous use of rapidly absorbed and sustained-release theophylline preparations in children. Ann Allergy 1979;43:217-219. 14. Powell JR, Vozeh S, Hopewell P, et al: Theophylline disposition in acutely ill hospitalized patients. Am Rev Resp Dis 1978;118:229-238. 15. Jusko WJ, Gardner MJ, Mangione A, et al: Factors affecting theophylline clearances: Age, tobacco, marijuana, cirrhosis, congestive heart failure, obesity, oral contraceptives, benzodiazepines, barbituates, and ethanol. J Pharm Sci 1979;68:1358-1366.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Internal Medicine American Medical Association

Rapid and Sustained Oral Theophyllinen Loading: An Alternative to Intravenous Aminophylline Therapy

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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.1983.00350040184027
Publisher site
See Article on Publisher Site

Abstract

Abstract • We evaluated an oral theophylline loading-dose procedure that was designed to rapidly achieve and sustain theophylline serum concentrations of approximately 10 to 12 μg/mL. Ten healthy adults were given an oral loading dose of approximately 6 mg/kg of aminophylline, (Aminophyllin®) (ie, 4.8 mg/kg of theophylline). Two hours later, each subject was given approximately 6 mg/kg of a sustained-release theophylline tablet (Theo-Dur®). Serum samples were collected at 1/2, 1, 2, 3, 6, 9, and 12 hours, then assayed for theophylline concentration. The mean theophylline concentration (±SD) one hour after the initial loading dose was 10.5±2.3 μg/mL. Subsequent theophylline concentrations demonstrated minimal fluctuation, with means ranging from 10.7 ± 1.6 to 13.6 ± 2.8 μg/mL. Four of the subjects reported headache; none vomited or experienced severe nausea. We conclude that this method of oral theophylline loading can be effective in achieving prompt and sustained therapeutic theophylline levels without significant side effects and that this may provide a valuable therapeutic alternative in those asthmatic patients who do not clearly require intravenous aminophylline therapy. (Arch Intern Med 1983;143:794-796) References 1. Weinberger M, Hendeles L, Bighley L: The relation of product formulation to absorption of oral theophylline. N Engl J Med 1978;299: 852-857.Crossref 2. Powell JR, Thiercelin JF, Vozeh S, et al: The influence of cigarette smoking and sex on theophylline disposition. Am Rev Respir Dis 1977;116: 17-23. 3. Hendeles L, Weinberger M, Johnson G: Monitoring serum theophylline levels. Clin Pharamcokinet 1978;3:294-312.Crossref 4. IV dosage guidelines for theophylline products. FDA Drug Bull 1980;10:4-6. 5. Rubenstein KE: Homogeneous enzyme immunoassay today. Scand J Immunol Suppl 1978;8:53-62.Crossref 6. EMIT-aad Theophylline Assay Product Information . Palo Alto, Calif, Syva Corp, 1977. 7. Kwok F, Kradjan WA: Comparative bioavailability of two uncoated aminophylline tablets. Am J Hosp Pharm 1980;37:1618-1620. 8. Upton RA, Sansom L, Guentert TW, et al: Evaluation of the absorption from 15 commercial theophylline products indicating deficiencies in currently applied bioavailability data. J Pharmacokinet Biopharm 1980;8: 229-242.Crossref 9. Kelly HW, Murphy S: Serum theophylline levels in asthmatic children receiving sustained-release theophylline tablets. Am J Hosp Pharm 1979; 10:1698-1701. 10. Spangler DL, Kalof DD, Bloom FL, et al: Theophylline bioavailability following oral administration of six sustained-release preparations. Ann Allergy 1978;40:6-11. 11. Domson JF, Hein EW, Sheen A, et al: Comparison of Theolair SR and Theo-Dur tablets. Ann Allergy 1979;43:220-222. 12. Kelly HW, Murphy S: Efficacy of a 12-hour sustained-release preparation in maintaining therapeutic serum theophylline levels in asthmatic children. Pediatrics 1980;66:97-102. 13. Hein EW, Domson JF, Sheen A, et al: Simultaneous use of rapidly absorbed and sustained-release theophylline preparations in children. Ann Allergy 1979;43:217-219. 14. Powell JR, Vozeh S, Hopewell P, et al: Theophylline disposition in acutely ill hospitalized patients. Am Rev Resp Dis 1978;118:229-238. 15. Jusko WJ, Gardner MJ, Mangione A, et al: Factors affecting theophylline clearances: Age, tobacco, marijuana, cirrhosis, congestive heart failure, obesity, oral contraceptives, benzodiazepines, barbituates, and ethanol. J Pharm Sci 1979;68:1358-1366.Crossref

Journal

Archives of Internal MedicineAmerican Medical Association

Published: Apr 1, 1983

References