caa a22 4500 477058337 CHVBK 20180405111353.0 cr unu---uuuuu 170330e19960201xx s 000 0 eng 10.1007/BF00203784 doi (NATIONALLICENCE)springer-10.1007/BF00203784 Inhibition of human thiopurine methyltransferase by furosemide, bendroflumethiazide and trichlormethiazide [Elektronische Daten] [R. Lysaa, T. Giverhaug, H. Libæk Wold, J. Aarbakke] Results: Incubation in vitro of human recombinant and erythrocyte (RBC) thiopurine methyl transferase (TPMT) with furosemide, bendroflumethiazide and trichlormethiazide demonstrated inhibition of both enzyme preparations, with IC50 values of 170 μM, 360 μM and 1 mM, respectively. Kinetic studies revealed that the inhibition was mixed or non-competitive with regard both to the thiopurine substrate 6-mercaptopurine (6-MP) and the methyl donor S-adenosyl-L-methionine. Conclusion: Since S-methylation is a major pathway in the metabolism of thiopurines, our data point to the possibility of a clinically significant diuretic-thiopurine interaction in patients treated simultaneously with these drugs. Springer-Verlag, 1996 Thiopurine methyltransferase nationallicence diuretics nationallicence furosemide nationallicence bendroflumethiazide nationallicence trichlormethiazide nationallicence Lysaa R. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut Giverhaug T. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut Libæk Wold H. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut Aarbakke J. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut European Journal of Clinical Pharmacology Springer-Verlag 49/5(1996-02-01), 393-396 0031-6970 49:5<393 1996 49 228 https://doi.org/10.1007/BF00203784 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00203784 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Lysaa R. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut NATIONALLICENCE 700 1- Giverhaug T. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut NATIONALLICENCE 700 1- Libæk Wold H. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut NATIONALLICENCE 700 1- Aarbakke J. Department of Pharmacology, Institute of Medical Biology, University of Tromsø, MH-bygget, N-9037, Tromsø, Norway aut NATIONALLICENCE 773 0- European Journal of Clinical Pharmacology Springer-Verlag 49/5(1996-02-01), 393-396 0031-6970 49:5<393 1996 49 228 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer