Disposition and metabolism of rifapentine, a rifamycin antibiotic, in mice, rats, and monkeys

Drug Metabolism and Disposition

Volumn 26, Issue 8, 1998, Pages 725-731

  Emary, W Bart ^a   Toren, Paul C ^b   Mathews, Brad ^b   Huh, Kay ^b  

^a SANOFI   (France)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

25 DEACETYLRIFAPENTINE; 3 FORMYL 25 DESACETYLRIFAPENTINE; 3 FORMYLRIFAPENTINE; ANTIBIOTIC AGENT; CARBON 14; DRUG METABOLITE; RIFAMYCIN DERIVATIVE; RIFAPENTINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BILIARY EXCRETION; CONTROLLED STUDY; DRUG BILE LEVEL; DRUG DISPOSITION; DRUG ELIMINATION; DRUG FECES LEVEL; DRUG METABOLISM; DRUG STRUCTURE; DRUG TISSUE LEVEL; DRUG TRANSFORMATION; DRUG URINE LEVEL; INTRAVENOUS DRUG ADMINISTRATION; MALE; MONKEY; MOUSE; NONHUMAN; ORAL DRUG ADMINISTRATION; PRIORITY JOURNAL; RADIOACTIVITY; RAT; SPECIES DIFFERENCE;

ANIMALS; ANTITUBERCULAR AGENTS; BILE; BIOTRANSFORMATION; CARBON RADIOISOTOPES; CHROMATOGRAPHY, HIGH PRESSURE LIQUID; FECES; MACACA FASCICULARIS; MALE; MASS SPECTROMETRY; MICE; RATS; RATS, WISTAR; RIFAMPIN; SPECIES SPECIFICITY; TISSUE DISTRIBUTION;

ANIMALIA; MYCOBACTERIUM; MYCOBACTERIUM AVIUM; MYCOBACTERIUM AVIUM COMPLEX; MYCOBACTERIUM TUBERCULOSIS;

EID: 0031843565     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (15)

1. Arioli V, Berti M, Carniti G, Randist E, Rossi E and Scotti R (1981) Antibacterial activity of DL 473, a new semisynthetic rifamycin derivative. J Antibiot 34:1026-1032.
2. Assandri A, Cristina T and More L (1978) Physiological disposition of a series of rifamycins in rat: a comparative study. J Antibiot 31:894-901.
3. Assandri A, Ratti B and Cristina T (1984) Pharmacokinetics of rifapentine, a new long lasting rifamycin, in the rat, the mouse and the rabbit. J Antibiot 37:1066-1075.
4. 14C-rifabutin in animals and man. J Antimicrob Chemother 26:813-822.
5. 14C-rifabulin in rats. Antimicrob Agents Chemother 35:1391-1396.
6. Birmingham AT, Coleman AJ, Orme ML, Park BK, Pearson NJ, Short AH and Southgate PJ (1978) Antibacterial activity in serum and urine following oral administration in man of DL473 (a cyclopentyl derivative of rifampicin). Br J Clin Pharmacol 6:455P-456P.
7. Buniva G, Sassella D and Frigo GM (1983) Pharmacokinetics of rifapentine in man. Proc Int Congr Chemother 111:29-33.
8. Dickinson JM and Mitchison DA (1987) In vitro properties of rifapentine (MDL473) relevant to its use in intermittent chemotherapy of tuberculosis. Tubercle 68:113-119.
9. Heifets LB, Lindholm-Levy PJ and Flory MA (1990) Bactericidal activity in vitro of various rifamycins against M. avium and M. tuberculosis. Am Rev Respir Dis 141:626-630.
10. Koudriakova T, Iatsimirskaia E, Tulebaev S, Spetie D, Utkin I, Mullet D, Thompson T, Vouros P and Gerber N (1996) In vivo disposition of the antitubercular drug rifabutin in rats. J Pharmacol Exp Ther 279:1300-1309.
11. Pattyn SR (1987) Rifabutin and rifapentine compared with rifampin against Hycobacterium leprae in mice. Antimicrob Agents Chemother 31:134.
12. Truffot-Pernot C, Gosset J, Bismuth R and LeCoeur H (1983) The activity of intermittent rifampicin and cyclopentyl rifampicin (or DL473) on experimental tuberculosis in the mouse. Rev Franc Malad Respir 11:875-882.
13. Utkin I, Koudriakova T, Thompson T, Cottrell C, Iatsimirskaia E, Barry J, Vouros P and Gerber N (1997) Isolation and identification of major urinary metabolites of rifabutin in rats and humans. Drug Metab Dispos 25:963-969.
14. Weber A, Opheim KE, Smith AL and Wong K (1983) High-pressure liquid chromatographic quantitation of rifampin and its two major metabolites in urine and serum. Rev Infect Dis 5(Suppl. 3):S433-439.
15. Yates MD and Collins CH (1982) Comparison of the sensitivity of mycobacteria to the cyclopentyl rifamycin DL473 and rifamycin. J Antimicrob Chemother 10:147-150.