Chelation Studies with 2,3‐Dihydroxybenzoic Acid in Patients with β‐Thalassaemia Major

Chelation Studies with 2,3‐Dihydroxybenzoic Acid in Patients with β‐Thalassaemia Major
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2,3-二羟基苯甲酸对重型 β-地中海贫血患者的螯合研究

DOI:
10.1111/j.1365-2141.1976.tb03566.x
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发表时间:
1976
影响因子:
6.5
通讯作者:
A. Cerami
A. Cerami
中科院分区:
医学2区
文献类型:
--
作者:
C. Peterson;J. Graziano;R. Grady;R. Jones;H. Vlassara;V. Canale;D. Miller;A. Cerami

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摘要通过在重型β地中海贫血患者中进行铁平衡研究,将2,3-二羟基苯甲酸评价为一种潜在有用的口服有效铁螯合药物。以25 mg/kg/d的剂量对5名患者给药8 d,导致铁排泄量平均增加4.5 mg/d。当药物以25 mg/kg q.i.d. 8例患者21 d铁排出量增加至6.5 mg/d。螯合作用对铁具有高度特异性,镁和钙排泄的变化微不足道。该药物耐受性良好,副作用仅限于胃肠道不适,当药物与食物一起服用时,副作用有所改善。这些研究为进一步评价2,3-二羟基苯甲酸在铁超负荷患者中的作用提供了依据。
Summary. 2,3‐Dihydroxybenzoic acid was evaluated as a potentially useful, orally effective iron‐chelating drug by performing iron balance studies in patients with β‐thalassaemia major. The administration of this substance at 25 mg/kg/d to five patients for 8 d caused an average increase in iron excretion of 4.5 mg/d. When the drug was administered at 25 mg/kg q.i.d. to eight patients for 21 d, iron excretion increased to 6.5 mg/d. Chelation was highly specific for iron with changes in magnesium and calcium excretion being insignificant. The drug was well tolerated with side effects limited to gastrointestinal complaints which ameliorated when the drug was taken with food. These studies provide a rationale for further evaluation of 2,3‐dihydroxybenzoic acid in patients with iron overload.