Abstract
The kinetic disposition of piroxicam, under evaluation in man as a new anti-inflammatory drug, was studied in human volunteers given a single oral dose after both overnight fasting and food. Total absorption was uninfluenced by food intake, although the data indicate that food causes some delay in attainment of peak serum levels. The halflife of drug in plasma in the fasting subjects (37.5±2.4hr) was similar in both the fasting state and after food, suggesting that once-daily dosing may be appropriate for maintaining therapeutic plasma levels. Mean pharmacokinetic parameters for both studies in the fasting state and after meals are volume of distribution divided by availability, 0.140 or 0.136 liter/kg; total plasma clearance divided by availability, 2.68 or 3.12 ml/hr/kg. Approximately 10% of a single dose of piroxicam was eliminated in the urine within 8 days after oral drug administration. Renal clearance of the drug (0.28±0.10 ml/hr/kg) was 10.4% or less of plasma clearance, suggesting that piroxicam is extensively metabolized. In this study one subject showed a reduction in white blood count on the sixteenth day after a 60-mg dose; however, hematology values evaluated in both intraand intersubject comparisons did not show any other differences in the present study.
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E. H. Wiseman, Y.-H. Cheng, and J. G. Lombardino. Piroxicam, a novel antiinflammatory agent.Arzneim. Forsch. 26:1300–1303 (1976).
M. Weintraub, R. F. Jacox, C. D. Angevine, and E. C. Atwater. Piroxicam (CP 16171) in rheumatoid arthritis: A controlled clinical trial with novel assessment techniques.J. Rheumatol. 4:393–404 (1977).
E. H. Wiseman. Review of preclinical studies with piroxicam: Pharmacology, toxicology and pharmacokinetics. Piroxicam Symposium, XIV International Congress of Rheumatology, San Francisco, Calif., June 26–July 1, 1977, abst., p. 219.
P. Nuotio and P. MÄkisara. Pharmacokinetic and clinical study of piroxicam. Piroxicam Symposium, XIV International Congress of Rheumatology, San Francisco, Calif., June 26–July 1, 1977, abst., p. 221.
R. N. Brodgen, R. M. Pinder, T. M. Speight, and G. S. Avery. Fenoprofen: A review of its pharmacological properties and therapeutic efficacy in rheumatic diseases.Drugs 13:241–265 (1977).
D. J. Greenblatt and J. Koch-Weser. Clinical pharmacokinetics (second of two parts).New Engl. J. Med. 293:964–970 (1975).
M. Gibaldi and G. Levy. Pharmacokinetics in clinical practice.J. Am. Med. Assoc. 235:1864–1867 (1976).
J. Koch-Weser. Bioavailability of drugs (first of two parts).New Engl. J. Med. 291:233–237 (1974).
D. L. Azarnoff and D. H. Huffman. Therapeutic implications of bioavailability.Ann. Rev. Pharmacol. Toxicol. 16:53–66 (1976).
R. G. Wiegand and P. G. Sanders. Calculation of kinetic constants from blood levels of drugs.J. Pharmacol. Exp. Ther. 146:271–275 (1964).
W. J. Dixon.BMD Biomedical Computer Programs, University of California Press, Berkeley, 1968.
R. Gugler, W. Herold, and H. J. Dengler. Pharmacokinetics of pindolol in man.Eur. J. Clin. Pharmacol. 7:17–24 (1974).
M. L. Selley, J. Glass, E. J. Triggs, and J. Thomas. Pharmacokinetic studies of tolmetin in man.Clin. Pharmacol. Ther. 17:599–605 (1975).
E. S. Vesell. Relationship between drug distribution and therapeutic effects in man.Ann. Rev. Pharmacol. 14:249–270 (1974).
J. G. Wagner, J. I. Northam, C. D. Aiway, and O. S. Carpenter. Blood levels of drug at the equilibrium state after multiple dosing.Nature 207:1301–1302 (1965).
G. E. Ehrlich. Guidelines for anti-inflammatory drug research.J. Clin. Pharmacol. 17:697–703 (1977).
G. E. Schumacher. Keeping bioavailability in perspective.Am. J. Hosp. Pharm. 30:150–154 (1973).
P. G. Welling. Influence of food and diet on gastrointestinal drug absorption: A review.J. Pharmacokin. Biopharm. 5:291–334 (1977).
L. F. Prescott. Antiinflammatory analgesics and drugs used in the treatment of rheumatoid arthritis and gout. In M. N. G. Dukes (ed.),Meyler's Side Effects of Drugs, North-Holland, Amsterdam, Vol. 8, 1975, pp. 207–240.
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This work was supported in part by a grant from Japan Rheumatoid Foundation (JRP).
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Ishizaki, T., Nomura, T. & Abe, T. Pharmacokinetics of piroxicam, a new nonsteroidal anti-inflammatory agent, under fasting and postprandial states in man. Journal of Pharmacokinetics and Biopharmaceutics 7, 369–381 (1979). https://doi.org/10.1007/BF01062535
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DOI: https://doi.org/10.1007/BF01062535