Allopurinol was first used to shift the metabolism of thiopurine compounds from 6-MMP to 6-TGN in poor responders to AZA or 6-MP
Afterward, the patient remained on 6-MP
therapy at the decreased dose of 50 mg/day, and aminotransferase levels normalized 1 month after the biopsy.
The incidence of prematurity was about 70% higher among the women treated with azathioprine or 6-MP
, compared with another control group of healthy women who were not treated with the drug.
The selection of AZA or 6-MP
and the dosage of the drug were at the discretion of the clinician.
9] Nonstandard abbreviations: AZA, azathioprine; 6-MP
, 6-mercaptopurine; 6-TGN, 6-thioguanine nucleotide; 6-MMP, 6-methyl mercaptopurine; TPMT, thiopurine S-methyltransferase; Ery, erythrocyte; CDAI, Crohn disease activity index; IBDQ, Inflammatory Bowel Disease Questionnaire; ITT, intention-to-treat; MCV, mean corpuscular volume.
10] Nonstandard abbreviafions: 6-MP
, 6-mercaptopurine; aza, azathioprine; IBD, inflammatory bowel disease; TPMT, thiopurine S-methyltransferase; TTPA, Inosine triphosphatase; ADR, adverse drug reacfion; 6-TGN, 6-thioguanosine nucleotide; OR, odds ratio; and CI, confidence interval.
It's unnecessary to routinely monitor 6-thioguanine nucleotide (6-TGN), the active metabolite of azathioprine and 6-MP
Erythrocyte TPMT activity was measured in EDTA blood as the conversion of 6-MP
to 6-MeMP (16) and expressed as picomoles of 6-MeMP formed per hour per milligram of hemoglobin [pmol 6-MeMP * [h.
To our knowledge, this is the first LC/MS/MS method developed to quantify 6-TGNs and 6-MMPNs, the 2 major metabolites of azathioprine and 6-MP
present in erythrocytes.
In February 2006, REMICADE was approved in the EU for the treatment of moderately-to- severely active UC in patients who have had an inadequate response to conventional therapy, including corticosteroids and 6-MP
or AZA, or who are intolerant to or have medical contraindications for such therapies.
The influence of 6-MP
and SAM concentrations on TPMT activity was assessed using eight concentrations of 6-MP
67), which catalyzes the conversion of a methyl moiety from S-adenosyl methionine to 6-MP
, yielding 6-methyl-MP.