Pharmaco/ferrokinetic-related pro-oxidant activity of deferiprone in beta-thalassemia.

Abstract:

:The potential of free radical formation in serum of beta-thalassemia/Hb E patients receiving a single oral dose of 25 mg/kg body weight of deferiprone, a bidentate orally active iron chelator, was evaluated using EPR/spin trapping technique. In the presence of ascorbic acid and tert-butylhydroperoxide, EPR signals of ascorbyl radical (aH=0.18 mT) and DMPO-carbon centred adduct (aH=2.37 mT, aN=1.65 mT) were detected. Shortly after deferiprone administration, EPR signal intensities decreased concomitant with an increase in serum levels of deferiprone. Unfortunately, enhanced EPR signal intensities were observed at 300 min after dosing in patients with serum molar ratio of deferiprone to iron less than 3, suggesting the formation of incomplete iron-deferiprone complexes and consequently free radical formation. To avoid adverse effects of deferiprone, a dosage regimen should be designed according to iron status of the patients and aimed at maintaining an adequate ratio of serum chelator-to-iron concentration.

journal_name

Free Radic Res

journal_title

Free radical research

authors

Jirasomprasert T,Morales NP,Limenta LM,Sirijaroonwong S,Yamanont P,Wilairat P,Fucharoen S,Chantharaksri U

doi

10.1080/10715760902870611

subject

Has Abstract

pub_date

2009-05-01 00:00:00

pages

485-91

issue

5

eissn

1071-5762

issn

1029-2470

pii

910303718

journal_volume

43

pub_type

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