Home LiteratureArticle Details
PMID: 6508979 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.

British journal of clinical pharmacology ·Vol. 18 ·No. 5 ·1984-11-00 ·Pages 701-6

Teunissen MW, Bakker W, Meerburg-Van der Torren JE, Breimer DD

Abstract

The influence of an 8-day therapy with rifampicin (600 mg daily) was studied on antipyrine plasma clearance and metabolite formation in seven patients with tuberculosis (age 18-79 years), who were also treated with isoniazid and pyrazinamide. After rifampicin treatment the elimination half-life of antipyrine had decreased in all patients from 12.9 +/- 5.0 to 8.8 +/- 2.0 h (P less than 0.05). Antipyrine clearance had increased from 2.2 +/- 0.9 to 2.9 +/- 0.7 l/h (P less than 0.05), while no change in apparent volume of distribution was observed. The increase in antipyrine clearance was primarily due to a selective increase in the rate of formation of norantipyrine by 80% from 6.9 +/- 3.4 to 12.4 +/- 3.4 ml/min. Rifampicin seems to induce preferentially the cytochrome P-450 (iso-) enzyme(s) involved in the demethylation of antipyrine to norantipyrine. Other pathways of antipyrine metabolism were hardly affected. This provides further evidence for the involvement of different iso-enzymes of the cytochrome P-450 system in antipyrine metabolism in man.

MeSH Terms
Adolescent Adult Aged Antipyrine/metabolism Female Half-Life Humans Male Metabolic Clearance Rate/drug effects Middle Aged Rifampin/pharmacology Tuberculosis, Pulmonary/metabolism
Chemicals
Antipyrine Rifampin
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Teunissen M W
Bakker W
Meerburg-Van der Torren J E
Breimer D D
References (29)
29 references, click to expand
  1. Pharmacological implications of microsomal enzyme induction.
    Pharmacol Rev. 1967 Sep;19(3):317-66 PMID: 4383307
  2. Automated high-performance liquid chromatographic determination of antipyrine and its main metabolites in plasma, saliva and urine, including 4,4'-dihydroxyantipyrine.
    J Chromatogr. 1983 Dec 9;278(2):367-78 PMID: 6668316
  3. [The simultaneous use of rifampicin and other antitubercular agents with oral contraceptives].
    Prax Pneumol. 1971 May;25(5):255-62 PMID: 5556355
  4. Antipyrine metabolism in man: influence of age, alcohol, caffeine, and smoking.
    Clin Pharmacol Ther. 1975 Oct;18(4):425-32 PMID: 1164824
  5. Influence of dietary protein and carbohydrate on antipyrine and theophylline metabolism in man.
    Clin Pharmacol Ther. 1976 Dec;20(6):643-53 PMID: 991535
  6. Influence of rifampicin on drug metabolism: differences between hexobarbital and antipyrine.
    Clin Pharmacol Ther. 1977 Apr;21(4):470-81 PMID: 849678
  7. Induction of hepatic microsomal enzymes after brief administration of rifampicin in man.
    Gastroenterology. 1977 May;72(5 Pt 1):924-6 PMID: 849823
  8. Pharmacokinetic interactions with rifampicin.
    Clin Pharmacokinet. 1977 Jan-Feb;2(1):61-70 PMID: 140033
  9. Genetic and environmental factors affecting drug disposition in man.
    Clin Pharmacol Ther. 1977 Nov;22(5 Pt 2):659-79 PMID: 334437
  10. Measurement of urinary 6-beta-hydroxycortisol excretion as an in vivo parameter in the clinical assessment of the microsomal enzyme-inducing capacity of antipyrine, phenobarbitone and rifampicin.
    Eur J Clin Pharmacol. 1979 Mar 26;15(2):139-45 PMID: 35353
  11. Assay of antipyrine and its primary metabolites in plasma, saliva and urine by high-performance liquid chromatography and some preliminary results in man.
    Pharmacology. 1979;18(4):210-23 PMID: 461498
  12. Influence of cigarette smoking on drug metabolism in man.
    Drug Metab Rev. 1979;9(2):221-36 PMID: 385272
  13. Blood levels of rifampicin, desacetylrifampicin and isoniazid during combined therapy.
    J Antimicrob Chemother. 1979 Jul;5(4):447-54 PMID: 489492
  14. Studies on the different metabolic pathways of antipyrine in rats: influence of phenobarbital and 3-methylcholanthrene treatment.
    Xenobiotica. 1979 Nov;9(11):695-702 PMID: 119355
  15. Rifampicin and vitamin D metabolism.
    Clin Pharmacol Ther. 1980 Jun;27(6):810-4 PMID: 7379450
  16. Effect of isoniazid on vitamin D metabolism and hepatic monooxygenase activity.
    Clin Pharmacol Ther. 1981 Sep;30(3):363-7 PMID: 7273600
  17. Differential effects of enzyme induction on antipyrine metabolite formation.
    Br J Clin Pharmacol. 1982 Mar;13(3):379-86 PMID: 7059438
  18. Effect of rifampicin on metoprolol and antipyrine kinetics.
    Br J Clin Pharmacol. 1982 Mar;13(3):387-91 PMID: 7059439
  19. Induction of hexobarbital and antipyrine metabolism by rifampicin treatment in the pig.
    Drug Metab Dispos. 1981 Nov-Dec;9(6):541-4 PMID: 6120813
  20. 3-Hydroxymethyl antipyrine excretion in urine after an oral dose of antipyrine. A reconsideration of previously published data and synthesis of a pure reference substance.
    Pharmacology. 1982;24(3):181-4 PMID: 7071130
  21. Comparison of the in vivo and in vitro rates of formation of the three main oxidative metabolites of antipyrine in man.
    Br J Clin Pharmacol. 1981 Dec;12(6):771-7 PMID: 7340879
  22. Differential induction of antipyrine metabolism by rifampicin.
    Eur J Clin Pharmacol. 1981;21(2):155-60 PMID: 7341283
  23. Studies of the different metabolic pathways of antipyrine in man. Oral versus i.v. administration and the influence of urinary collection time.
    Eur J Clin Pharmacol. 1982;21(5):433-41 PMID: 7075648
  24. Influence of sex and oral contraceptive steroids on antipyrine metabolite formation.
    Clin Pharmacol Ther. 1982 Aug;32(2):240-6 PMID: 7094512
  25. Effect of rifampicin and isoniazid on vitamin D metabolism.
    Clin Pharmacol Ther. 1982 Oct;32(4):525-30 PMID: 7116768
  26. The metabolism of fenclofenac in the horse.
    Xenobiotica. 1983 Apr;13(4):233-40 PMID: 6624138
  27. Interindividual variations in drug disposition. Clinical implications and methods of investigation.
    Clin Pharmacokinet. 1983 Sep-Oct;8(5):371-7 PMID: 6627809
  28. Correlation between the in vivo metabolism of hexobarbital and antipyrine in rats.
    J Pharmacol Exp Ther. 1983 Nov;227(2):459-65 PMID: 6631725
  29. Metabolism of drugs. LXX. Further study on antipyrine metabolism.
    Chem Pharm Bull (Tokyo). 1971 Jan;19(1):41-5 PMID: 5544367
Article Info
Journal
British journal of clinical pharmacology
Abbr.
Br J Clin Pharmacol
ISSN
0306-5251
DOI
10.1111/j.1365-2125.1984.tb02532.x
Published
1984-11-00
Pages
701-6
Language
English
Region
England
NLM ID
7503323
PMCID
PMC1463547
Subset
IM
External Links
PubMed source DOI: 10.1111/j.1365-2125.1984.tb02532.x PMC Full Text View journal details
Analysis Services
Analysis Services

Contact

No. 2 Wenbo Road, Zhangqiu District, Jinan, Shandong

Qilu Normal University · Genelibs Bioinformatics Lab

750 Shunhua Rd, Jinan

2F, Bldg F, University Science Park

Tel: 0531-88819269

WeChat Official Account

Follow our WeChat subscription account for real-time updates and the latest in medical and biological research.


Business Email

E-mail: product@genelibs.com

Copyright © 2026.Genelibs Jinan Honghui Biotechnology Co., Ltd. 鲁ICP备20007159号-2