Deferoxamine remains the mainstay of iron chelation therapy

'Although we found that Ll {I,2-dimethyl-3-hydroxypyrid-4-oneJ is an effective oral chelator, we emphasise that its use as a therapeutic alternative to subcutaneous desferrioxamine {deferoxamineJ cannot yet be recommended.'

20 patients with moderate to severe transfusional iron overload, in whom deferoxamine therapy was failing or was not a therapeutic option. were randomised to receive oral 1.2-dimethyl-3-hydroxypyrid-4-one 50 mg/kg/day and SC deferoxamine 50 mg/kg/day for 3 days each in a crossover fashion after their monthly red cell transfusions. Adequate dietary ascorbic acid [vitamin C] and supplemental ascorbic acid 100 mg/day were given during chelation therapy.

Mean urinary iron excretion was 12.3 mg/day during 1.2-dimethyl-3-hydroxypyrid-4-one therapy compared with 18.2 mg/day during deferoxamine therapy. In 5 patients who were readmitted after a further transfusion and who received 1,2-dimethyl-3-hydroxypyrid-4-one 75 mg/kg/day, there was a significantly increased mean urinary iron excretion from 13.8 to 26.7 mg/day. which was comparable with the urinary iron excretion for these patients during deferoxamine therapy (24.9 mg/day).

A further 6 patients underwent measurement of total iron excretion (faecal and urinary): faecal iron excretion increased significantly from 8.5 to 12.2 mg/day during 1.2-dimethyl-3-hydroxypyrid-4-one 75 mg/kg/day therapy. The elimination half-life was 117-237 min in 4 patients who took part in pharmacokinetic studies. 01" !L'n NF. Koren (j, Hermann C. Iknlur y, Chung D, c'l al. Comparison of oral iron chC'ialor L1 and dc'sf~rrio .\aminc' on iron· loadc'c\ palic'nls, Lane"'1 336: I ~75·1 ~N, ~4 No, 1'1'10

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9 INPHARMA@I Dec 1990 _