For technical reasons, TPMT enzyme activity is measured in red cells, which correlates well with activity in white cells.Thiopurine methyltransferase status is used as a predictor of drug toxicity, particularly myelotoxicity. The higher AZA dosage in the 6-TGN monitored group was not sufficient to increase RBC 6-TGN to target levels (100 to 200 pmol/8 × 10 It has been thought that thioguanine nucleotides are incorporated into cell DNA, including those of myeloid lineage.Thiopurine drug mechanism of action. Therapeutic Drug Monitoring.
Free E-newsletter Subscribe to Housecall. 19(3):318-326, JUNE 1997Possibilities for Therapeutic Drug Monitoring of Azathioprine 6-Thioguanine Nucleotide Concentrations and Thiopurine Methyltransferase Activity in Red Blood Cells S. Bergan;H. Rugstad;B. Klemetsdal;T. Giverhaug;Ø. Bentdal;G. Sødal;A. Hartmann;J. Aarbakke;O. Stokke;Institute of Clinical Biochemistry, Departments of *Clinical Pharmacology, ‡Surgery, and §Medicine, National Hospital, University of Oslo, and †Department of Pharmacology, University of Tromsø, Tromsø, NorwayThe objectives of this study were to establish monitoring of azathioprine (AZA) treatment in renal allograft recipients by red blood cell (RBC) 6-thioguanine nucleotide (6-TGN) measurements and to characterize the variability of RBC thiopurine methyltransferase (TPMT) activity and the effects on 6-TGN levels and the incidence of rejection episodes.
New methods to assess 6-thiopurine toxicity and expanding its therapeutic application to pancreatic cancer
Drug information provided by: IBM Micromedex. The slight increase in RBC TPMT activity after transplant was associated with the use of furosemide rather than AZA; in the five patients receiving furosemide for less than 10 days, TPMT activity declined.
If you usually give it once a day in the evening: What if I forget to give it? If you do not receive an email within 10 minutes, your email address may not be registered, TCR, T lymphocyte receptor; Rac1‐GTP, Rac1‐guanine triphoshate; Rac1 GDP, Rac1‐guanine diphosphate; MAP3K, mitogen‐activated protein kinase kinase kinase; MAPK, mitogen‐activated protein kinase kinase; NF‐κB, nuclear factor‐κB; STAT3, signal transducer and activator of transcription‐3.A number of studies have investigated the relationship between 6‐TGN concentration and thiopurine efficacy for patients with IBD.Further observational data have confirmed that erythrocyte 6‐TGN concentration ‘is significantly and independently associated with therapeutic response to 6‐MP in children’.However, there are a number of observational studies that show no correlation between erythrocyte 6‐TGN concentration and clinical remission for IBD patients.Therefore, studies investigating the relationship between erythrocyte 6‐TGN concentration and clinical response to a thiopurine drug for patients with IBD show either a positive association or no association.