Rifampicin bioavailability: A review of its pharmacology and the chemotherapeutic necessity for ensuring optimal absorption

International Journal of Tuberculosis and Lung Disease

Volumn 3, Issue 11 SUPPL. 3, 1999, Pages

  Ellard, G A ^a   Fourie, P B ^b  

^a ST GEORGE'S UNIVERSITY OF LONDON   (United Kingdom)

^b SOUTH AFRICAN MEDICAL RESEARCH COUNCIL   (South Africa)

Author keywords

Bioavailability; Combined formulations; Pharmacology; Rifampicin; Tuberculosis

Indexed keywords

ETHAMBUTOL; ISONIAZID; PYRAZINAMIDE; RIFAMPICIN; TUBERCULOSTATIC AGENT;

CONFERENCE PAPER; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DETERMINATION; DRUG EXCRETION; DRUG METABOLISM; HUMAN; PRIORITY JOURNAL; URINARY EXCRETION;

ABSORPTION; ANTIBIOTICS, ANTITUBERCULAR; ANTITUBERCULAR AGENTS; BIOLOGICAL AVAILABILITY; DRUG COMBINATIONS; HUMANS; RIFAMPIN; TUBERCULOSIS;

EID: 0032737204     PISSN: 10273719     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Conference Paper

References (121)

1. World Health Organization. Treatment of tuberculosis: guidelines for national programmes. 2nd ed. Geneva: WHO, 1997.
2. International Union Against Tuberculosis and Lung Disease/ World Health Organization. The promise and reality of fixed-dose combinations with rifampicin. Tubercle Lung Dis 1994; 75: 180-181.
3. Canetti G, Le Lirzin M, Porven G, Rist N, Grumbach F. Some comparative aspects of rifampicin and isoniazid. Tubercle 1968; 49: 367-376.
4. East African/British Medical Research Councils. Controlled clinical trial of four short-course (6-month) regimens of chemotherapy for treatment of pulmonary tuberculosis. Third Report. Lancet 1974; ii: 237-240.
5. Fox W, Mitchison D A. Short-course chemotherapy for pulmonary tuberculosis. Am Rev Respir Dis 1975; 111: 325-353.
6. Grosset J. The sterilizing value of rifampicin and pyrazinamide in experimental short course chemotherapy. Tubercle 1978; 59: 287-297.
7. Mitchison D A. Basic mechanisms of chemotherapy. Chest 1979; 76S: 771S-781S.
8. Dutt A K, Stead W W. Chemotherapy of tuberculosis for the 1980s. Clin Chest Med 1980; 1: 243-252.
9. Grosset J. Bacteriologic basis of short-course chemotherapy for tuberculosis. Clin Chest Med 1980; 1: 231-241.
10. Dickinson J M, Mitchison D A. Experimental models to explain the high sterilizing activity of rifampin in the chemotherapy of tuberculosis. Am Rev Respir Dis 1981; 123: 367-371.
11. Girling D J. The chemotherapy of tuberculosis. In: Ratledge C, Stanford J L, Grange J M, eds. Biology of the mycobacteria. Vol 3. Clinical aspects of mycobacterial disease. London/ New York: Academic Press 1989: pp 285-323.
12. Donald P R, Sirgel F A, Botha F J, et al. The early bactericidal activity of isoniazid relared ro irs dose size in pulmonary tuberculosis. Am J Respir Crit Care Med 1997; 156: 895-900.
13. East and Central African/British Medical Research Council. Controlled clinical trial of 4 short-course regimens of chemotherapy (three 6-month and one 8-month) for pulmonary tuberculosis. Tubercle 1983; 64: 153-166.
14. Singapore Tuberculosis Service/British Medical Research Council. Long-term follow-up of a clinical trial of six-month and four-month regimens of chemotherapy in the treatment of pulmonary tuberculosis. Am Rev Respir Dis 1986; 133: 779-793.
15. Singapore Tuberculosis Service/British Medical Research Council. Clinical trial of three 6-month regimens of chemotherapy given intermittently in the continuation phase in the treatment of pulmonary tuberculosis. Am RevRespir Dis 1985; 132: 374-378.
16. Girling D J. Adverse reactions to rifampicin in antituberculosis regimens. J Antimicrob Chemother 1977; 3: 115-132.
17. Girling D J. The hepatic toxicity of antituberculosis regimens containing Isoniazid, rifampicin and pyrazinamide. Tubercle 1978; 59: 13-32.
18. Girling D J, Hitze K L. Adverse reactions to rifampicin. Bull World Health Organ 1979; 57: 45-49.
19. Grosset J, Leventis S. Adverse effects of rifampin. Rev Infect Dis 1983; 5 (Suppl 3): S440-S446.
20. Acocella G, Pagani V, Marchetti M, Baroni G C, Nicolis F B. Kinetic studies on rifampicin: 1. Serum concentration analysis in subjects treated with different oral doses over a period of two weeks. Chemotherapy 1971; 16: 356-370.
21. Acocella G, Lamarina A, Nicolis F B, Pagani V, Segre G. Kinetic studies on rifampicin. II Multicompartmental analysis of the serum, urine and bile concentrations in subjects treated for one week. Eur J Clin Pharmacol 1972; 5: 111-115.
22. Acocella G, Mattiussi R, Segre G. Multicompartmental analysis of serum, urine and bile concentrations of rifampicin and desacetyl-rifampicin in subjects treated for one week. Pharmacol Res 1978; 10: 271-288.
23. Acocella G, Bonollo L, Garimoldi M, Mainardi M, Tenconi T, Nicolis F B. Kinetics of rifampicin and isoniazid administered alone and in combination to normal subjects and patients with liver disease. Gut 1972; 13: 47-53.
24. Nitti V, Delli-Veneri F, Ninni A, Meola G. Rifampicin blood serum levels and half-life during prolonged administration in tuberculous patients. Chemotherapy 1972; 17: 121-129.
25. Boman G. Serum concentration and half-life of rifampicin after simultaneous oral administration of aminosalicylic acid or isoniazid. Eur J Clin Pharmacol 1974; 7: 217-225.
26. Buniva G, Pagani V, Carozzi A. Bioavailability of rifampicin capsules. Int J Clin Pharmacol Therapy Toxicol 1983; 21: 404-409.
27. Dans P E, McGehee R F, Wilcox C, Finland M. Rifampin: antibacterial activity in vitro and absorption and excretion in normal men. Am J Med Sci 1970; 259: 120-132.
28. Siegler D I, Bryant M, Burley D M, Citron M, Standen S M. Effect of meals on rifampicin absorption. Lancet 1974; ii: 197-198.
29. Boman G, Hanngren A, Malmborg A S, Borga O, Sjöqvist F. Drug interaction. Decreased serum concentrations of rifampicin when given with PAS. Lancet 1971; 1: 800.
30. Boman G, Malmborg A S. Rifampicin in plasma and pleural fluid after single oral doses. Eur J Clin Pharmacol 1974; 7: 51-58.
31. Virtanen S, Tala E. Serum concentration of rifampicin after oral administration. Clin Pharmacol Therap 1974; 16: 817-820.
32. Dickinson M, Aber V R, Allen B W, Ellard G A, Mitchison D A. Assay of rifampicin in serum. J Clin Path 1974; 27: 457-462.
33. Immanuel C, Jayasankar K, Narayana A S L, Sarma G R. Self-induction of rifampicin metabolism in man. Indian J Med Res 1985; 82: 381-387.
34. Ellard G A, Ellard D R, Allen B W, et al. The bioavailability of isoniazid, rifampin, and pyrazinamide in two commercially available combined formulations designed for use in the short-course treatment of tuberculosis. Am Rev Respir Dis 1986; 133: 1076-1080.
35. Gurumurthy P, Sarma G R, Jayasankar K, et al. Single-dose pharmacokinetics of isoniazid and rifampicin in patients with chronic renal failure. Indian J Tuberc 1992; 39: 221-228.
36. Goucher C R, Peters J H, Gordon G R, et al. Chemical and bacteriological assays of rifampin, rifampin-quinone and desacetylrifampin. 12th US-Japan Joint Conference on Leprosy, Boston MA, Sept 27-29, 1977: pp 47-59.
37. Peters J H, Gordon G R, Murray J F, et al. Measurement of rifampin in plasma: Chemical vs bacteriologic assay. Proc West Pharmacol Soc 1977; 20: 211-215.
38. Gurumurthy P, Rahman F, Narayan A S L, Sarma G R. Salivary levels of isoniazid and rifampicin in tuberculous patients. Tubercle 1990; 71: 29-33.
39. Männistö P. Absorption of rifampin from various preparations and pharmaceutic forms. Clin Pharmacol Ther 1977; 21: 370-374.
40. Kenny M T, Strates B. Metabolism and pharmacokinetics of the antibiotic rifampin. Drug Metab Rev 1981; 12: 159-218.
41. Gallo G G, Radaelli P. Rifampicin. In: Florey K, ed. Analytical profiles of drug substances. Vol 5. New York: Academic Press 1976; 5: 467-513.
42. Burkhardt K R, Nel E E. Monitoring regularity of drug intake in tuberculosis patients by means of simple urine tests. South African Med J 1980; 57: 981-985.
43. Jeanes C W L, Jessamine A G, Eidus L. Treatment of chronic drug-resistant pulmonary tuberculosis with rifampin and ethambutol. Can Med Assoc J 1972; 106: 884-888.
44. Eidus L, Harnanansingh A M T. Simple procedures for checking rifampin in urine. Am Rev Respir Dis 1969; 100: 738-739.
45. Ishii M, Agata H. Determination of rifampicin and its main metabolite in human plasma. J Chromatogr 1988; 426: 412-416.
46. Ratti B, Roosina-Parenti R, Toselli A, Zerrili L F. Quantitative assay of rifampicin and its metabolite 25 desacetyl-rifampicin in human plasma by reversed phase high-performance liquid chromatography. J Chromatogr 1981; 225: 526-531.
47. Boman G, Lundgren P, Stjernström G. Mechanism of the inhibitory effect of PAS granules on the absorption of rifampicin: adsorption of rifampicin by an excipient, bentonite. Eur J Clin Pharmacol 1975; 8: 293-299.
48. Sunahara S, Nakagawa H. Metabolic study and controlled clinical trials of rifampin. Chest 1972; 61: 526-532.
49. Maggi N, Furesz S, Pallanza R, Pelliza G. Rifampicin desacetylation in the human organism. Arzneimittelforschung 1969; 19: 651-654.
50. Koup J R, Williams-Warren , Weber A, Smith A L. Pharmacokinetics of rifampin in children. I. Multiple dose intravenous infusion. Ther Drug Monit 1986; 8: 11-16.
51. Acocella G, Conti R, Luisetti M, Pozzi E, Grassi C. Pharmacokinetic studies of antituberculosis regimens in humans. 1. Absorption and metabolism of the compounds used in the initial intensive phase of the short-course regimens: Single administration study. Am Rev Respir Dis 1985; 132: 510-515.
52. Acocella G, Nonis A, Gialdroni-Grassi G, Grassi C. Comparative bioavailability of isoniazid, rifampin, and pyrazinamide administered in free combination and in a fixed triple formulation designed for daily use in antituberculosis chemotherapy. I. Single-dose study. Am Rev Respir Dis 1988; 138: 882-885.
53. Chouchane N, Barre J, Toumi A, Tillement J P, Benakis A. Bioequivalence study of two pharmaceutical forms of rifampicin capsules in man. Eur J Drug Metabol Pharmacokinet 1995; 20: 315-320.
54. Advenir C, Gobert C, Houin G, Bidet D, Richelet S, Tillement J P. Pharmacokinetic studies of rifampicin in the elderly. Ther Drug Monit 1983; 5: 61-65.
55. Lecaillon J B, Febvre N, Metayer J P, Souppart C. Quantitative assay of rifampicin and three of its metabolites in human plasma, urine and saliva by high-performance liquid chromatography. J Chromatogr 1978; 145: 319-324.
56. Archer G L, Armstrong B C, Kline B J. Rifampin blood and tissue levels in patients undergoing cardiac valve surgery. Antimicrobial Agents Chemother 1982; 21: 800-803.
57. Guillaumont M, Leclercq M, Frobert Y, Guise B, Harf R. Determination of rifampicin, desacetylrifampicin, isoniazid and acetylisoniazid by high performance liquid chromatography: application to human serum extracts, polymorphonucleocytes and alveolar macrophages. J Chromatogr 1982; 232: 369-376.
58. Weber A, Opheim K E, Smith A L, Wong K. High-pressure liquid chromatographic quantitation of rifampin and its two major metabolites in urine and serum. Rev Infect Dis 1983; 5 (Suppl 3): S433-S439.
59. Holdiness M R. Chromatographic analysis of antituberculosis drugs in biological samples. J Chromatogr 1985; 340: 321-359.
60. Woo J, Humphries M, Chan K, O'Mahony G, Teoh R. Cerebrospinal fluid and serum levels of pyrazinamide and rifampicin in patients with tuberculous meningitis. Curr Therap Res 1987; 42: 235-242.
61. Woo J, Wong C L, Teoh R, Chan K. Liquid chromatographic assay for the simultaneous determination of pyrazinamide and rifampicin in serum samples from patients with tuberculous meningitis. J Chromatogr 1987; 420: 73-80.
62. Jenner P J. The determination of antimycobacterial drugs in body fluids by high-performance liquid chromatography. In: Reeves D S, Ullmann U, eds. High performance liquid chromatography in medical microbiology. Stuttgart/New York: Gustav Fischer Verlag 1988: pp 153-164.
63. Lee H S, Shin H C, Han S S, Roh J K. High-performance liquid chromatographic determination of rifapentine in serum using column switching. J Chromatogr 1992; 574: 175-178.
64. Nau R, Prange W H, Menck S, Kolenda H, Visser K, Seydel J K. Penetration of rifampicin into the cerebrospinal fluid of adults with uninflamed meninges. J Antimicrob Chemother 1992; 29: 719-724.
65. Swart K J, Papgis M. Automated high-performance liquid chromatographic method for the determination of rifampicin in plasma. J Chromatogr 1992; 593: 21-24.
66. Zent C, Smith P. Study of the effect of concomitant food on the bioavailability of rifampicin, isoniazid and pyrazinamide. Tubercle Lung Dis 1995; 76: 109-113.
67. Smith P J, van Dyk J, Fredericks A. Determination of rifampicin, isoniazid and pyrazinamide by high performance liquid chromatography after their simultaneous extraction from plasma. Int J Tuberc Lung Dis 1999; 3 (Suppl 3): S325-S328.
68. Le Guellec C, Gaudet M L, Lamanetre S, Breteau M. Stability of rifampicin in plasma. Consequences for therapeutic monitoring and pharmacokinetic studies. Therap Drug Monitor 1997; 19: 669-674.
69. Binda G, Domenichini E, Gottardi A, et al. Rifampicin, a general review. Arzneinmittelforschung 1971; 21: 1908-1977.
70. Nitti V. Antituberculosis activity of rifampicin. Chest 1972; 61: 589-598.
71. Acocella G. Clinical pharmacokinetics of rifampicin. Clin Pharmacokinet 1978; 3: 108-127.
72. Holdiness M R. Clinical pharmacokinetics of the antituberculosis drugs. Clin Pharmacokin 1984; 9: 511-544.
73. Dollery C. Rifampicin. In: Dollery C, ed. Therapeutic drugs. Edinburgh: Churchill Livingstone 1991: pp R23-R29.
74. Pelloquin C A. Antituberculosis drugs: pharmacokinetics. In Heifets L B, ed. Drug susceptibility in the chemotherapy of mycobacterial infections. Florida: CRC Press 1991: pp 13-57.
75. Ellard G A. Assuring the quality of drugs used for the treatment and control of leprosy. Lepr Rev 1992; 63: 305-316.
76. Furesz S. Rifampicin: Chemical and biological properties of rifampicin. Antibiotica et Chemotherapia 1970; 16: 316-351.
77. Furesz S, Scotti R, Pallanza R, Mapelli E. Rifampicin: a new rifamycin. Arzneimittelforschung 1967; 17: 534-537.
78. Curci G, Bergamini N, Delli Veneri F, Ninni A, Nitti V. Half-life of rifampicin after repeated administration of different doses in humans. Chemotherapy 1972; 17: 373-381.
79. Dickinson J M, Mitchison D A, Lee S K, et al. Serum rifampicein concentration related to dose size and to the incidence of the 'flu' syndrome during intermittent rifampicin administration. J Antimicrob Chemother 1977; 3: 445-452.
80. Brechbühler S, Flueher H, Riess W, Theobald W. The renal elimination of rifampicin as a function of the oral dose. A convenient way to assess relative bioavailability. Arzneimittelforschung 1978; 28: 480-483.
81. Hong Kong Treatment Services/British Medical Research Council. A controlled clinical trial of small daily doses of rifampiein in the prevention of adverse reactions to the drug in a once-weekly regimen of chemotherapy. Clin Allergy 1974; 4: 1-12.
82. Acocella G. A metabolic and kinetic study of the association rifampicin-isoniazid. Respiration 1971; 28 (Suppl): 1-6.
83. Acocella G, Nonis A, Perna G, Patane E, Gialdroni-Grassi G, Grassi C. Comparative bioavailability of isoniazid, rifampin, and pyrazinamide administered in free combination and in a fixed triple formulation designed for daily use in antituberculosis chemotherapy. II. Two-month, daily administation study. Am Rev Respir Dis. 1988; 138: 886-890.
84. Nakagawa H, Sunahara S. Rifampicin-glucuronide in human urine. 1973. In: Dickinson J M, ed. Reports on rifampicin presented at the 22nd International Tuberculosis Conference. Published for Lepetit by Excerpta Medica, Tokyo. 1973: pp 90-94.
85. Nakagawa H, Umene Z, Sunahara S. Increased desacetyl-rifampicin and adverse reactions. Bull Int Union Tuberc 1979; 54: 171-172.
86. Keberle H. Physico-chemical factors of drugs affecting absorption, distribution and excretion. Acta Pharmacologica et Toxicologica 1971; 29: 30-47.
87. Acocella G, Bonollo L, Mainardi M, Margaroli P, Tenconi L T. Serum and urine concentrations of rifampicin administered by intravenous infusion in man. Arzneimittelforschung 1977; 27: 1221-1226.
88. Nitti V, Virgilio R, Patricolo M R, Iuliano A. Pharmacokinetic study of intravenous rifampicin. Chemotherapy 1977; 23: 1-6.
89. Koup J R, Williams-Warren J, Viswanathan C T, Weber A, Smith A L. Pharmacokinetics of rifampin in children. II. Oral bioavailability. Ther Drug Monitor 1986; 8: 17-22.
90. Israili Z H, Rogers C M, El-Attar H. Pharmacokinetics of antituberculosis drugs in patients. J Clin Pharmacol 1987; 27: 78-83.
91. Ellard G A. The chemotherapy of tuberculosis for patients with renal impairment. Nephron 1993; 64: 169-181.
92. Garnham J C, Taylor T, Turner P, Chasseaud L F. Serum concentrations and bioavailability of rifampicin and isoniazid in combination. Br J Clin Pharmacol 1976; 3: 897-902.
93. Boman G. Protein binding of rifampicin - a review. Scand J Respir Dis 1973; 84 (Suppl): 40-43.
94. Boman G, Ringberger V A. Binding of rifampicin by human plasma proteins. Eur J Clin Pharmacol 1974; 7: 369-373.
95. Cavenaghi R. Rifampicin raw material characteristics and their effect on bioavailability. Bull Int Union Tuberc Lung Dis 1989; 64: 36-37.
96. Zwolska Z, Niemirowska-Mikulska H, Augustynowicz-Kopec E, et al. Bioavailability of rifampicin, isoniazid and pyrazinamide from fixed-dose combination capsules. Int J Tuberc Lung Dis 1998; 2: 824-830.
97. Fox W. Compliance of patients and physicians: experience and lessons from tuberculosis-I. Br Med J 1983; 287: 33-35.
98. Fox W. Compliance of patients and physicians experience and lessons from tuberculosis-II. Br Med J 1983; 287: 101-105.
99. Hong Kong Chest Service/British Medical Research Council. Acceptability, compliance, and adverse reactions when isoniazid, rifampin, and pyrazinamide are given as a combined formulation or separately during three-times-weekly antituberculosis chemotherapy. Am Rev Respir Dis 1989; 140: 1618-1622.
100. Hong Kong Chest Service/British Medical Research Council. Controlled trial of 2,4, and 6 months of pyrazinamide in 6-month, three-times-weekly regimens for smear-positive pulmonary tuberculosis, including an assessment of a combined preparation of isoniazid, rifampin, and pyrazinamide. Results at 30 months. Am Rev Respir Dis 1991; 143: 700-706.
101. Singapore Tuberculosis Service/British Medical Research Council. Assessment of a daily combined preparation of isoniazid, rifampin, and pyrazinamide in a controlled trial of three 6-month regimens for smear-positive pulmonary tuberculosis. Am Rev Respir Dis 1991; 143: 707-712.
102. Fox W. Tuberculosis in India, past, present and future. Indian J Tuberc 1990; 37: 175-213.
103. Fox W. Drug combinations and the bioavailability of rifampicin. Tubercle 1990; 71: 241-245.
104. Pelizza G, Nebuloni M, Ferrari P, Gallo G G. Polymorphism of rifampicin. II Farmaco (Edizione Scientifica) 1977; 32: 471-481.
105. Acocella G. Human bioavailability studies. Bull Int Union Tuberc Lung Dis 1989; 64: 38-40.
106. Aspesi F. Dissolution testing. Bull Int Union Tuberc Lung Dis 1989; 64: 37-38.
107. Schall R, Muller F O, Duursema L, et al. Relative bioavailability of rifampicin, isoniazid and ethambutol from a combination tablet vs concomitant administration of a capsule containing rifampicin and a tablet containing isoniazid and ethambutol. Arzneimittelforschung 1995; 45: 1236-1239.
108. Gelber R, Jacobsen P, Levy L. A study of the availability of six commercial formulations of isoniazid. Clin Pharmacol Therap 1969; 10: 841-848.
109. Anonymous. Editorial. Multi-drug formulations. Indian J Tuberc 1988; 35: 161-162.
110. Girling D J. Discussion. Satellite symposium on quality control of antituberculosis drugs. Bull Int Union Tuberc Lung Dis 1989; 64: 40-41.
111. Grumbach F. Experimental 'in vivo' studies of new antituberculosis drugs: capreomycin, ethambutol, rifampicin. Tubercle 1969; 50 (Suppl): 12-21.
112. Long M W, Snider D E, Farer L S. US Public Health Service Cooperative Trial of three rifampicin-isoniazid regimens in treatment of pulmonary tuberculosis. Am Rev Respir Dis 1979; 119: 879-894.
113. Jindani A, Aber V R, Edwards E A, Mitchison D A. The early bactericidal activity of drugs in patients with pulmonary tuberculosis. Am Rev Respir Dis 1980; 121: 939-949.
114. Chan S L, Yew W W, Ma D, et al. The early bactericidal activity of rifabutin measured by sputum viable counts in Hong Kong patients with pulmonary tuberculosis. Tubercle Lung Dis 1992; 73: 33-38.
115. Sirgel F A, Botha F J H, Parkin D P, et al. The early bactericidal activity of rifabutin in patients with pulmonary tuberculosis measured by sputum viable counts: a new method of drug assessment. J Antimicrob Chemother 1993; 32: 867-875.
116. Schuirmann D J. A comparison of the two one-sided tests procedure and the power approach for assessing the equivalence of average bioavailability. J Pharmacokin Biopharm 1987; 15: 657-680.
117. Hauschke D, Steinijans V W, Diletti E. A distribution-free procedure for the statistical analysis of bioequivalence studies. Int J Clin Pharmacol Ther Tox 1990; 28: 72-78.
118. World Health Organization. Multisource (generic) pharmaceutical products: guidelines on registration requirements to establish interchangeability. WHO Technical Report Series, No. 863. Annex 9. Geneva: WHO, 1996.
119. Fourie P B. Proposed minimum registration requirements for fixed-dose combination anti-tuberculosis drugs. Int J Tuberc Lung Dis 1999; 3 (Suppl 3): S362-S367.
120. Quality assurance: protocol for assessing the rifampicin bioavailability of combined formulations in healthy volunteers. Int J Tuberc Lung Dis 1999; 3 (Suppl 3): S284-S285.
121. Ellard G A. The evaluation of rifampicin bioavailabilities of fixed-dose combinations of anti-tuberculosis drugs: procedures for ensuring laboratory proficiency. Int J Tuberc Lung Dis 1999; 3 (Suppl 3): S322-S324.