Clarithromycin is absorbed by an intestinal uptake mechanism that is sensitive to major inhibition by rifampicin: Results of a short-term drug interaction study in foals

Drug Metabolism and Disposition

Volumn 40, Issue 3, 2012, Pages 522-528

  Peters, Jette ^a   Eggers, Karen ^b   Oswald, Stefan ^a   Block, Wiebke ^b   Luẗjohann, Dieter ^c   Lam̈mer, Marc ^b   Venner, Monica ^b   Siegmund, Werner ^a  

^a UNIVERSITY OF GREIFSWALD   (Germany)

^b Lewitz Stud ^*  (Germany)

^c UNIVERSITY OF BONN   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

11 HYDROXYCLARITHROMYCIN; CLARITHROMYCIN; DRUG METABOLITE; OATP1A2 PROTEIN; OATP1B1 PROTEIN; OATP1B3 PROTEIN; OATP2B1 PROTEIN; ORGANIC ANION TRANSPORTER; RIFAMPICIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; BRONCHOALVEOLAR LAVAGE CELL; CONTROLLED STUDY; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG UPTAKE; EPITHELIAL LINING FLUID; EPITHELIUM; FEMALE; FOAL; HUMAN; HUMAN CELL; IC 50; IN VITRO STUDY; KIDNEY CELL; LUNG ALVEOLUS CELL; MALE; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; PRIORITY JOURNAL; TIME TO MAXIMUM PLASMA CONCENTRATION;

ANIMALS; CLARITHROMYCIN; DRUG INTERACTIONS; FEMALE; HEK293 CELLS; HORSES; HUMANS; INTESTINAL ABSORPTION; INTESTINES; LUNG; MALE; ORGANIC ANION TRANSPORTERS; RESPIRATORY MUCOSA; RIFAMPIN; TRANSFECTION; UP-REGULATION;

EID: 84857407899     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.042267     Document Type: Article

References (37)

1. Acocella G (1978) Clinical pharmacokinetics of rifampicin. Clin Pharmacokinet 3:108-127.
2. Burrows GE, MacAllister CG, Ewing P, Stair E, and Burrows SL (1992) Rifampin disposition in the horse: effects of repeated dosage of rifampin or phenylbutazone. J Vet Pharmacol Ther 15:305-308.
3. Diczfalusy U, Kanebratt KP, Bredberg E, Andersson TB, Böttiger Y, and Bertilsson L (2009) 4β-Hydroxycholesterol as an endogenous marker for CYP3A4/5 activity: stability and half-life of elimination after induction with rifampicin. Br J Clin Pharmacol 67:38-43.
4. Ferrero JL, Bopp BA, Marsh KC, Quigley SC, Johnson MJ, Anderson DJ, Lamm JE, Tolman KG, Sanders SW, and Cavanaugh JH (1990) Metabolism and disposition of clarithromycin in man. Drug Metab Dispos 18:441-446. (Pubitemid 20220966)
5. Garver E, Hugger ED, Shearn SP, Rao A, Dawson PA, Davis CB, and Han C (2008) Involvement of intestinal uptake transporters in the absorption of azithromycin and clarithromycin in the rat. Drug Metab Dispos 36:2492-2498.
6. Geick A, Eichelbaum M, and Burk O (2001) Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J Biol Chem 276:14581-14587.
7. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM,et al. (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
8. Giguère S, Jacks S, Roberts GD, Hernandez J, Long MT, and Ellis C (2004) Retrospective comparison of azithromycin, clarithromycin, and erythromycin for the treatment of foals with Rhodococcus equi pneumonia. J Vet Intern Med 18:568-573. (Pubitemid 39107551)
9. Jacks S, Giguère S, Gronwall PR, Brown MP, and Merritt KA (2001) Pharmacokinetics of azithromycin and concentration in body fluids and bronchoalveolar cells in foals. Am J Vet Res 62:1870-1875. (Pubitemid 33130532)
10. Jacks SS, Giguère S, and Nguyen A (2003) In vitro susceptibilities of Rhodococcus equi and other common equine pathogens to azithromycin, clarithromycin, and 20 other antimicrobials. Antimicrob Agents Chemother 47:1742-1745. (Pubitemid 36548565)
11. Kanebratt KP, Diczfalusy U, Bäckström T, Sparve E, Bredberg E, Böttiger Y, Andersson TB, and Bertilsson L (2008) Cytochrome P450 induction by rifampicin in healthy subjects: determination using the Karolinska cocktail and the endogenous CYP3A4 marker 4β-hydroxycholesterol. Clin Pharmacol Ther 84:589-594.
12. Kast HR, Goodwin B, Tarr PT, Jones SA, Anisfeld AM, Stoltz CM, Tontonoz P, Kliewer S, Willson TM, and Edwards PA (2002) Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor. J Biol Chem 277:2908-2915. (Pubitemid 34953324)
13. Lan T, Rao A, Haywood J, Davis CB, Han C, Garver E, and Dawson PA (2009) Interaction of macrolide antibiotics with intestinally expressed human and rat organic anion-transporting polypeptides. Drug Metab Dispos 37:2375-2382.
14. Leonhardt M, Keiser M, Oswald S, Kühn J, Jia J, Grube M, Kroemer HK, Siegmund W, and Weitschies W (2010) Hepatic uptake of the magnetic resonance imaging contrast agent Gd-EOB-DTPA: role of human organic anion transporters. Drug Metab Dispos 38:1024-1028.
15. Luo G, Cunningham M, Kim S, Burn T, Lin J, Sinz M, Hamilton G, Rizzo C, Jolley S, Gilbert D,et al. (2002) CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes. Drug Metab Dispos 30:795-804. (Pubitemid 34671092)
16. Mandery K, Bujok K, Schmidt I, Keiser M, Siegmund W, Balk B, König J, Fromm MF, and Glaeser H (2010) Influence of the flavonoids apigenin, kaempferol, and quercetin on the function of organic anion transporting polypeptides 1A2 and 2B1. Biochem Pharmacol 80:1746-1753.
17. Meyer zu Schwabedissen HE, Tirona RG, Yip CS, Ho RH, and Kim RB (2008) Interplay between the nuclear receptor pregnane X receptor and the uptake transporter organic anion transporter polypeptide 1A2 selectively enhances estrogen effects in breast cancer. Cancer Res 68:9338-9347.
18. MunićV, KelnerićZ,Mikac L, and ErakovićHaber V (2010) Differences in assessment of macrolide interaction with human MDR1 (ABCB1, P-gp) using rhodamine-123 efflux, ATPase activity and cellular accumulation assays. Eur J Pharm Sci 41:86-95.
19. Oswald S, Giessmann T, Luetjohann D, Wegner D, Rosskopf D, Weitschies W, and Siegmund W (2006) Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, an inhibitor of multidrug transport proteins. Clin Pharmacol Ther 80:477-485. (Pubitemid 44767877)
20. Oswald S, Peters J, Venner M, and SiegmundW(2011) LC-MS/MS method for the simultaneous determination of clarithromycin, rifampicin and their main metabolites in horse plasma, epithelial lining fluid and broncho-alveolar cells. J Pharm Biomed Anal 55:194-201.
21. Peters J, Block W, Oswald S, Freyer J, Grube M, Kroemer HK, Lämmer M, Lütjohann D, Venner M, and Siegmund W (2011) Oral absorption of clarithromycin is nearly abolished by chronic comedication of rifampicin in foals. Drug Metab Dispos 39:1643-1649.
22. Rennard SI, Basset G, Lecossier D, O'Donnell KM, Pinkston P, Martin PG, and Crystal RG (1986) Estimation of volume of epithelial lining fluid recovered by lavage using urea as marker of dilution. J Appl Physiol 60:532-538. (Pubitemid 16019939)
23. Seithel A, Eberl S, Singer K, Auge D, Heinkele G, Wolf NB, Dörje F, Fromm MF, and König J (2007) The influence of macrolide antibiotics on the uptake of organic anions and drugs mediated by OATP1B1 and OATP1B3. Drug Metab Dispos 35:779-786. (Pubitemid 46641549)
24. Suzuki A, Iida I, Hirota M, Akimoto M, Higuchi S, Suwa T, Tani M, Ishizaki T, and Chiba K (2003) CYP isoforms involved in the metabolism of clarithromycin in vitro: comparison between the identification from disappearance rate and that from formation rate of metabolites. Drug Metab Pharmacokinet 18:104-113.
25. Taki H, Ogawa K, Nakagawa T, Kashima K, Tarumi O, Saitou Y, Yamada N, Tano M, and Nikai T (2007) [Clinical analysis of drug interaction between rifampicin and clarithromycin which are used for treating pulmonary Mycobacterium avium complex infection]. Kekkaku 82:641-646.
26. Tomalik-Scharte D, Lütjohann D, Doroshyenko O, Frank D, Jetter A, and Fuhr U (2009) Plasma 4β-hydroxycholesterol: an endogenous CYP3A metric? Clin Pharmacol Ther 86:147-153.
27. Torii M, Takiguchi Y, Izumi M, Fukushima T, and Yokota M (2002) Carbapenem antibiotics inhibit valproic acid transport in Caco-2 cell monolayers. Int J Pharm 233:253-256. (Pubitemid 34230437)
28. Tydén E, Bjornstrom H, Tjälve H, and Larsson P (2010) Expression and localization of BCRP, MRP1 and MRP2 in intestines, liver and kidney in horse. J Vet Pharmacol Ther 33:332-340.
29. Tydén E, Olsén L, Tallkvist J, Larsson P, and Tjälve H (2004) CYP3A in horse intestines. Toxicol Appl Pharmacol 201:112-119.
30. Tydén E, Tallkvist J, Tjälve H, and Larsson P (2009) P-glycoprotein in intestines, liver, kidney and lymphocytes in horse. J Vet Pharmacol Ther 32:167-176.
31. Urquhart BL, Tirona RG, and Kim RB (2007) Nuclear receptors and the regulation of drugmetabolizing enzymes and drug transporters: implications for interindividual variability in response to drugs. J Clin Pharmacol 47:566-578.
32. van der Deen M, de Vries EG, Timens W, Scheper RJ, Timmer-Bosscha H, and Postma DS (2005) ATP-binding cassette (ABC) transporters in normal and pathological lung. Respir Res 6:59.
33. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, and Fattinger K (2002) Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 36:164-172. (Pubitemid 34700774)
34. Wallace RJ Jr, Brown BA, Griffith DE, Girard W, and Tanaka K (1995) Reduced serum levels of clarithromycin in patients treated with multidrug regimens including rifampin or rifabutin for Mycobacterium avium-M. intracellulare infection. J Infect Dis 171:747-750.
35. Yang Z and Rodrigues AD (2010) Does the long plasma half-life of 4β-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric? J Clin Pharmacol 50:1330-1338.
36. Zhou C, Assem M, Tay JC, Watkins PB, Blumberg B, Schuetz EG, and Thummel KE (2006) Steroid and xenobiotic receptor and vitamin D receptor crosstalk mediates CYP24 expression and drug-induced osteomalacia. J Clin Invest 116:1703-1712.
37. Ziglam HM, Baldwin DR, Daniels I, Andrew JM, and Finch RG (2002) Rifampicin concentrations in bronchial mucosa, epithelial lining fluid, alveolar macrophages and serum following a single 600 mg oral dose in patients undergoing fibre-optic bronchoscopy. J Antimicrob Chemother 50:1011-1015. (Pubitemid 36032825)