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Phenylbutazone and Sulfinpyrazone Interaction With Oral Anticoagulant Phenprocoumon

Phenylbutazone and Sulfinpyrazone Interaction With Oral Anticoagulant Phenprocoumon Abstract • To compare the marked hypoprothrombinemic augmentation in man of racemic warfarin sodium by the pyrazolons phenylbutazone and sulfinpyrazone with that of the coumarin anticoagulant phenprocoumon, these interactions were studied prospectively in six normal subjects. Large single doses of racemic phenprocoumon, 0.6 mg/kg orally, were administered with and without daily phenylbutazone, 300 mg, or sulfinpyrazone, 400 mg, beginning three days before phenprocoumon and continuing for 14 days. Daily blood samples were drawn for phenprocoumon content and one-stage prothrombin time. Phenylbutazone markedly increased both the phenprocoumon concentrations and prothrombin times, whereas sulfinpyrazone did not. (Arch Intern Med 1982;142:1634-1637) References 1. O'Reilly RA, Trager WF, Motley CH, et al: Stereoselective interaction of phenylbutazone with 12C-/13C-warfarin pseudoracemates in man. J Clin Invest 1980;65:746-752.Crossref 2. O'Reilly RA: Stereoselective interaction of sulfinpyrazone with racemic warfarin and its separated enantiomorphs in man. Circulation 1982;65:202-207.Crossref 3. Eisen MJ: Combined effect of sodium warfarin and phenylbutazone. JAMA 1964;189:64-65.Crossref 4. Bailey RR, Reddy J: Potentiation of warfarin action by sulphinpyrazone. Lancet 1980;1:254.Crossref 5. Seiler K, Duckert F: Properties of 3-(1-phenyl-propyl)-4-oxycoumarin (Marcoumar) in the plasma when tested in normal cases and under the influence of drugs. Thromb Diath Haemorrh 1968;19:389-396. 6. Michot F, Holt NF, Fontanilles F: Über die Beeinflussung der gerinnungshemmenden Wirkung von Acenocoumarol durch Sulfinpyrazon. Schweiz Med Wochenschr 1981;111:255-260. 7. Schmidt W, Jähnchen E: Interaction of phenylbutazone with racemic phenprocoumon and its enantiomers in rats. J Pharmacokinet Biopharm 1979;7:643-663.Crossref 8. Diamond S: Information and Error: An Introduction to Statistical Analysis . New York, Basic Books Inc, 1959, p 104. 9. O'Reilly RA: Interaction of sodium warfarin and disulfiram (Antabuse) in man. Ann Intern Med 1973;78:73-76.Crossref 10. O'Reilly RA, Goulart DA: Comparative interaction of sulfinpyrazone and phenylbutazone with racemic warfarin: Alteration in vivo of free fraction of plasma warfarin. J Pharmacol Exp Ther 1981;219:691-694. 11. Yacobi A, Lai C-M, Levy G: Comparative pharmacokinetics of coumarin anticoagulants XLV: Pharmacokinetic and pharmacodynamic studies of acute interaction between warfarin and phenylbutazone in rats. J Pharm Sci 1980;69:14-20.Crossref 12. Wheeler C, Trager WF, Porter WR: Stereochemical aspects of the metabolism of phenprocoumon in rat liver microsomes. Biochem Pharmacol 1981;30:1785-1790.Crossref 13. Jähnchen E, Meinertz T, Gilfrich HJ: Interaction of allopurinol with phenprocoumon in man. Klin Wochenschr 1977;55:759-761.Crossref 14. Self TH, Evans WE, Ferguson T: Drug enhancement of warfarin activity. Lancet 1975;2:557-558.Crossref 15. Zimmermann R, Ehlers W, Walter E, et al: The effect of bezafibrate on the fibrinolytic enzyme system and the drug interaction with racemic phenprocoumon. Atherosclerosis 1978;29:477-485.Crossref 16. O'Reilly RA, Sahud MA, Robinson AJ: Studies on the interaction of warfarin and clofibrate in man. Thromb Diath Haemorrh 1972;27:309-318. 17. Heni N, Lehnhardt G, Glogner P: Eliminationskinetik von Phenprocoumon (Marcumar) bei Leberzirrhose und nach Vorbehandlung mit Phenobarbital. Int J Clin Pharmacol Ther Toxicol 1976;13:253-261. 18. Schmidt W, Trenk D, Jähnchen E: Effect of induction and inhibition of drug metabolism on pharmacokinetics and anticoagulant activity of the enantiomers of phenprocoumon in rats. Pharmacology 1980;21:313-322.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Internal Medicine American Medical Association

Phenylbutazone and Sulfinpyrazone Interaction With Oral Anticoagulant Phenprocoumon

Archives of Internal Medicine , Volume 142 (9) – Sep 1, 1982

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Publisher
American Medical Association
Copyright
Copyright © 1982 American Medical Association. All Rights Reserved.
ISSN
0003-9926
eISSN
1538-3679
DOI
10.1001/archinte.1982.00340220048010
Publisher site
See Article on Publisher Site

Abstract

Abstract • To compare the marked hypoprothrombinemic augmentation in man of racemic warfarin sodium by the pyrazolons phenylbutazone and sulfinpyrazone with that of the coumarin anticoagulant phenprocoumon, these interactions were studied prospectively in six normal subjects. Large single doses of racemic phenprocoumon, 0.6 mg/kg orally, were administered with and without daily phenylbutazone, 300 mg, or sulfinpyrazone, 400 mg, beginning three days before phenprocoumon and continuing for 14 days. Daily blood samples were drawn for phenprocoumon content and one-stage prothrombin time. Phenylbutazone markedly increased both the phenprocoumon concentrations and prothrombin times, whereas sulfinpyrazone did not. (Arch Intern Med 1982;142:1634-1637) References 1. O'Reilly RA, Trager WF, Motley CH, et al: Stereoselective interaction of phenylbutazone with 12C-/13C-warfarin pseudoracemates in man. J Clin Invest 1980;65:746-752.Crossref 2. O'Reilly RA: Stereoselective interaction of sulfinpyrazone with racemic warfarin and its separated enantiomorphs in man. Circulation 1982;65:202-207.Crossref 3. Eisen MJ: Combined effect of sodium warfarin and phenylbutazone. JAMA 1964;189:64-65.Crossref 4. Bailey RR, Reddy J: Potentiation of warfarin action by sulphinpyrazone. Lancet 1980;1:254.Crossref 5. Seiler K, Duckert F: Properties of 3-(1-phenyl-propyl)-4-oxycoumarin (Marcoumar) in the plasma when tested in normal cases and under the influence of drugs. Thromb Diath Haemorrh 1968;19:389-396. 6. Michot F, Holt NF, Fontanilles F: Über die Beeinflussung der gerinnungshemmenden Wirkung von Acenocoumarol durch Sulfinpyrazon. Schweiz Med Wochenschr 1981;111:255-260. 7. Schmidt W, Jähnchen E: Interaction of phenylbutazone with racemic phenprocoumon and its enantiomers in rats. J Pharmacokinet Biopharm 1979;7:643-663.Crossref 8. Diamond S: Information and Error: An Introduction to Statistical Analysis . New York, Basic Books Inc, 1959, p 104. 9. O'Reilly RA: Interaction of sodium warfarin and disulfiram (Antabuse) in man. Ann Intern Med 1973;78:73-76.Crossref 10. O'Reilly RA, Goulart DA: Comparative interaction of sulfinpyrazone and phenylbutazone with racemic warfarin: Alteration in vivo of free fraction of plasma warfarin. J Pharmacol Exp Ther 1981;219:691-694. 11. Yacobi A, Lai C-M, Levy G: Comparative pharmacokinetics of coumarin anticoagulants XLV: Pharmacokinetic and pharmacodynamic studies of acute interaction between warfarin and phenylbutazone in rats. J Pharm Sci 1980;69:14-20.Crossref 12. Wheeler C, Trager WF, Porter WR: Stereochemical aspects of the metabolism of phenprocoumon in rat liver microsomes. Biochem Pharmacol 1981;30:1785-1790.Crossref 13. Jähnchen E, Meinertz T, Gilfrich HJ: Interaction of allopurinol with phenprocoumon in man. Klin Wochenschr 1977;55:759-761.Crossref 14. Self TH, Evans WE, Ferguson T: Drug enhancement of warfarin activity. Lancet 1975;2:557-558.Crossref 15. Zimmermann R, Ehlers W, Walter E, et al: The effect of bezafibrate on the fibrinolytic enzyme system and the drug interaction with racemic phenprocoumon. Atherosclerosis 1978;29:477-485.Crossref 16. O'Reilly RA, Sahud MA, Robinson AJ: Studies on the interaction of warfarin and clofibrate in man. Thromb Diath Haemorrh 1972;27:309-318. 17. Heni N, Lehnhardt G, Glogner P: Eliminationskinetik von Phenprocoumon (Marcumar) bei Leberzirrhose und nach Vorbehandlung mit Phenobarbital. Int J Clin Pharmacol Ther Toxicol 1976;13:253-261. 18. Schmidt W, Trenk D, Jähnchen E: Effect of induction and inhibition of drug metabolism on pharmacokinetics and anticoagulant activity of the enantiomers of phenprocoumon in rats. Pharmacology 1980;21:313-322.Crossref

Journal

Archives of Internal MedicineAmerican Medical Association

Published: Sep 1, 1982

References