Mesalazine pharmacokinetics and NAT2 phenotype

European Journal of Clinical Pharmacology

Volumn 65, Issue 1, 2009, Pages 47-54

  Lück, Hendrik ^a,b   Kinzig, Martina ^c   Jetter, Alexander ^a,d   Fuhr, Uwe ^a,f   Sörgel, Fritz ^c,e  

^a UNIVERSITY HOSPITAL OF COLOGNE   (Germany)

^b ITECRA Institute for Tailored Early Clinical Research and Advice GmbH and Co KG   (Germany)

^c Institute for Biomedical and Pharmaceutical Research   (Germany)

^d UNIVERSITY HOSPITAL ZURICH   (Switzerland)

^e UNIVERSITY HOSPITAL ESSEN   (Germany)

^f UNIVERSITY OF COLOGNE   (Germany)

Author keywords

Caffeine; Genetic polymorphism; Mesalazine; NAT2; Phenotyping

Indexed keywords

ARYLAMINE ACETYLTRANSFERASE; DRUG METABOLITE; MESALAZINE; N ACETYLMESALAZINE; UNCLASSIFIED DRUG;

ACETYLATOR PHENOTYPE; ADULT; AREA UNDER THE CURVE; ARTICLE; DRUG BLOOD LEVEL; DRUG URINE LEVEL; FEMALE; HUMAN; HUMAN EXPERIMENT; MALE; MAXIMUM PLASMA CONCENTRATION; NORMAL HUMAN; PHENOTYPE; PRIORITY JOURNAL; SINGLE DRUG DOSE;

ACETYLATION; ADMINISTRATION, ORAL; ADULT; ANTI-INFLAMMATORY AGENTS, NON-STEROIDAL; ARYLAMINE N-ACETYLTRANSFERASE; BIOTRANSFORMATION; CAFFEINE; EUROPEAN CONTINENTAL ANCESTRY GROUP; FEMALE; GENOTYPE; HUMANS; MALE; MESALAMINE; MODELS, BIOLOGICAL; PHENOTYPE; POLYMORPHISM, GENETIC; YOUNG ADULT;

EID: 57849137360     PISSN: 00316970     EISSN: None     Source Type: Journal    
DOI: 10.1007/s00228-008-0550-2     Document Type: Article

References (27)

1. U Klotz KE Maier 1987 Pharmacology and pharmacokinetics of 5-aminosalicylic acid Dig Dis Sci 32 12 Suppl 46S 50S
2. L Estrada-Rodgers GN Levy WW Weber 1998 Substrate selectivity of mouse N-acetyltransferases 1, 2, and 3 expressed in COS-1 cells Drug Metab Dispos 26 5 502 505
3. DW Hein MA Doll TD Rustan K Gray Y Feng RJ Ferguson 1993 Metabolic activation and deactivation of arylamine carcinogens by recombinant human NAT1 and polymorphic NAT2 acetyltransferases Carcinogenesis 14 8 1633 1638
4. KF Windmill A Gaedigk PM Hall H Samaratunga DM Grant ME McManus 2000 Localization of N-acetyltransferases NAT1 and NAT2 in human tissues Toxicol Sci 54 1 19 29
5. C Fischer K Maier E Stumpf U von Gaisberg U Klotz 1983 Disposition of 5-aminosalicylic acid, the active metabolite of sulphasalazine, in man Eur J Clin Pharmacol 25 4 511 515
6. AK Azad Khan M Nurazzaman SC Truelove 1983 The effect of the acetylator phenotype on the metabolism of sulphasalazine in man J Med Genet 20 1 30 36
7. S Bondesen J Hegnhoj F Larsen SH Hansen CP Hansen SN Rasmussen 1991 Pharmacokinetics of 5-aminosalicylic acid in man following administration of intravenous bolus and per os slow-release formulation Dig Dis Sci 36 12 1735 1740
8. H Allgayer NO Ahnfelt W Kruis U Klotz K Frank-Holmberg HN Soderberg 1989 Colonic N-acetylation of 5-aminosalicylic acid in inflammatory bowel disease Gastroenterology 97 1 38 41
9. E Ricart WR Taylor EV Loftus D O'Kane RM Weinshilboum WJ Tremaine 2002 N-acetyltransferase 1 and 2 genotypes do not predict response or toxicity to treatment with mesalamine and sulfasalazine in patients with ulcerative colitis Am J Gastroenterol 97 7 1763 1768
10. M Hausmann G Paul K Menzel R Brunner-Ploss W Falk J Scholmerich 2008 NAT1 genotypes do not predict response to mesalamine in patients with ulcerative colitis Z Gastroenterol 46 3 259 265
11. A Jetter M Kinzig-Schippers M Illauer R Hermann K Erb J Borlak 2004 Phenotyping of N-acetyltransferase type 2 by caffeine from uncontrolled dietary exposure Eur J Clin Pharmacol 60 1 17 21
12. M Kinzig-Schippers D Tomalik-Scharte A Jetter B Scheidel V Jakob M Rodamer 2005 Should we use N-acetyltransferase type 2 genotyping to personalize isoniazid doses? Antimicrob Agents Chemother 49 5 1733 1738
13. S Garte L Gaspari AK Alexandrie C Ambrosone H Autrup JL Autrup 2001 Metabolic gene polymorphism frequencies in control populations Cancer Epidemiol Biomarkers Prev 10 12 1239 1248
14. A Jetter M Kinzig-Schippers M Illauer D Tomalik-Scharte F Sörgel U Fuhr 2004 When should urine samples for NAT2 phenotyping with caffeine be collected? Clin Pharmacol Ther 75 2 P69
15. U Fuhr A Jetter J Kirchheiner 2007 Appropriate phenotyping procedures for drug metabolizing enzymes and transporters in humans and their simultaneous use in the "cocktail" approach Clin Pharmacol Ther 81 2 270 283
16. U Fuhr KL Rost R Engelhardt M Sachs D Liermann C Belloc 1996 Evaluation of caffeine as a test drug for CYP1A2, NAT2 and CYP2E1 phenotyping in man by in vivo versus in vitro correlations Pharmacogenetics 6 2 159 176
17. D Hickman J Pope SD Patil G Fakis V Smelt LA Stanley 1998 Expression of arylamine N-acetyltransferase in human intestine Gut 42 3 402 409
18. WJ Sandborn SB Hanauer 2003 Systematic review: the pharmacokinetic profiles of oral mesalazine formulations and mesalazine pro-drugs used in the management of ulcerative colitis Aliment Pharmacol Ther 17 1 29 42
19. JG Hardy WJ Harvey RA Sparrow GB Marshall KP Steed M Macarios 1993 Localization of drug release sites from an oral sustained-release formulation of 5-ASA (Pentasa) in the gastrointestinal tract using gamma scintigraphy J Clin Pharmacol 33 8 712 718
20. A Ireland JD Priddle DP Jewell 1990 Acetylation of 5-aminosalicylic acid by isolated human colonic epithelial cells Clin Sci (Lond) 78 1 105 111
21. SS Mahid DW Colliver NP Crawford BD Martini MA Doll DW Hein 2007 Characterization of N-acetyltransferase 1 and 2 polymorphisms and haplotype analysis for inflammatory bowel disease and sporadic colorectal carcinoma BMC Med Genet 8 28
22. C Delomenie S Fouix S Longuemaux N Brahimi C Bizet B Picard 2001 Identification and functional characterization of arylamine N-acetyltransferases in eubacteria: evidence for highly selective acetylation of 5-aminosalicylic acid J Bacteriol 183 11 3417 3427
23. RA van Hogezand HM Kennis A van Schaik JP Koopman PA van Hees JH van Tongeren 1992 Bacterial acetylation of 5-aminosalicylic acid in faecal suspensions cultured under aerobic and anaerobic conditions Eur J Clin Pharmacol 43 2 189 192
24. JM Walraven JO Trent DW Hein 2008 Structure-function analyses of single nucleotide polymorphisms in human N-acetyltransferase 1 Drug Metab Rev 40 1 169 184
25. C Bruhn J Brockmoller I Cascorbi I Roots HH Borchert 1999 Correlation between genotype and phenotype of the human arylamine N-acetyltransferase type 1 (NAT1) Biochem Pharmacol 58 11 1759 1764
26. K Dilger D Trenk M Rossle M Cap A Zahringer V Wacheck 2007 A clinical trial on absorption and N-acetylation of oral and rectal mesalazine Eur J Clin Invest 37 7 558 565
27. AF Muller PE Stevens AS McIntyre H Ellison RF Logan 2005 Experience of 5-aminosalicylate nephrotoxicity in the United Kingdom Aliment Pharmacol Ther 21 10 1217 1224