Interaction between azathioprine and aminosalicylates: an in vivo study in patients with Crohn’s disease

Autor:	Jean-Pierre Desager, Robert Vanheuverzwyn, Yves Horsmans, Olivier Dewit
Rok vydání:	2002
Předmět:	medicine.medical_specialty Hepatology business.industry Metabolite Gastroenterology Azathioprine Pharmacology Drug interaction Aminosalicylate chemistry.chemical_compound Thiopurine S-Methyltransferase Endocrinology chemistry Mesalazine Pharmacokinetics Sulfasalazine Internal medicine medicine Pharmacology (medical) business medicine.drug
Zdroj:	Alimentary Pharmacology & Therapeutics. 16:79-85
ISSN:	0269-2813
Popis:	BACKGROUND: The inhibition of thiopurine methyltransferase activity, one of the enzymes responsible for azathioprine metabolism, by aminosalicylates has been described in an in vitro study. This could result in a higher risk of bone marrow depression when using the two drugs together. AIM: To investigate the in vivo interaction between azathioprine and aminosalicylates in quiescent Crohn's disease by measuring 6-thioguanine nucleotide levels, thiopurine methyltransferase activity and the plasma levels of the acetylated metabolite of 5-aminosalicylic acid. METHODS: Sixteen patients taking a stable dose of azathioprine, plus sulfasalazine or mesalazine, were enrolled and completed the study. They were not taking any drugs interfering with azathioprine metabolism. Four visits every 4 weeks were held over a 3-month period. Aminosalicylate administration was withdrawn after the second visit. At each visit, the blood cell count, inflammatory parameters, levels of 6-thioguanine nucleotide and the acetylated metabolite of 5-aminosalicylic acid and thiopurine methyltransferase activity were determined. RESULTS: After aminosalicylate withdrawal, mean 6-thioguanine nucleotide levels decreased significantly from 148 pmol (57-357 pmol) to 132 pmol (56-247 pmol) per 8 x 10(8) red blood cells (P=0.027), without significant changes in thiopurine methyltransferase activity or biological parameters. CONCLUSIONS: This in vivo study favours the existence of an interaction between azathioprine and aminosalicylates through a mechanism which remains unclear. This drug-drug interaction should be taken into account when using azathioprine and aminosalicylates simultaneously.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::a48dd31146664680c19d849ef83bb469 https://doi.org/10.1046/j.1365-2036.2002.01156.x Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
Nepřihlášeným uživatelům se plný text nezobrazuje	K zobrazení výsledku je třeba se přihlásit.