Pharmacokinetics and red cell utilization of ⁵²Fe/⁵⁹Fe‐labelled iron polymaltose in anaemic patients using positron emission tomography

Abstract

Summary. Parenteral iron–polysaccharide complexes are increasingly applied. The pharmacokinetics of iron sucrose have been assessed by our group using positron emission tomography (PET). A single intravenous injection of 100 mg iron as iron (III) hydroxide–polymaltose complex, labelled with a tracer in the form of 52Fe/59Fe, was similarly assessed in six patients using PET for about 8 h. Red cell utilization was followed for 4 weeks. Iron polymaltose was similarly distributed to the liver, spleen and bone marrow. However, a larger proportion of this complex was rapidly distributed to the bone marrow. The shorter equilibration phase for the liver, about 25 min, indicates the minimal role of the liver for direct distribution. Splenic uptake also reflected the reticuloendothelial handling of this complex. Red cell utilization ranged from 61% to 99%. Despite the relatively higher uptake by the bone marrow, there was no saturation of marrow transport systems at this dose level. In conclusion, high red cell utilization of iron polymaltose occurred in anaemic patients. The major portion of the injected dose was rapidly distributed to the bone marrow. In addition, the reticuloendothelial uptake of this complex may reflect the safety of polysaccharide complexes. Non‐saturation of transport systems to the bone marrow indicated the presence of a large interstitial transport pool, which might possibly be transferrin.

Comparative efficacy and safety of intravenous ferric carboxymaltose (Ferinject) and iron(III) hydroxide dextran (Cosmofer) in pregnancy

“…Although larger studies are needed to investigate this further, there is support for this possibility from a study by Beshara et al 9 This is a red cell utilization study comparing distribution of intravenous iron over four weeks of the hydroxide-polymaltose formulated intravenous iron (Ferinject), compared with distribution pattern of intravenous iron-sucrose. In both cases, intravenous iron was distributed to the liver, spleen and bone marrow, but a larger proportion of the complex was quickly distributed to the bone marrow in the polymaltose formulation, with the major portion of the injected dose rapidly distributed to the bone marrow.…”

The role of iron supplementation during epoietin treatment for cancer-related anemia

“…Uptake in the bone marrow was observed within hours, 68-97% of the labeled iron was utilized within 2 weeks, and labeled iron was incorporated in the erythrocytes after three weeks [53][54][55]. Most available data on the pharmacokinetics and pharmacodynamics of iron dextran are from an earlier formulation, not marketed today.…”

Anemia in Inflammatory Bowel Diseases in Children

“…Карбоксимальтозат железа после введе-ния быстро поступает в печень и селезенку, затем железо медленно высвобождается из комплексов и избиратель-но поступает в костный мозг, тем самым предупреждая риск развития синдрома вторичной перегрузки желе-зом. Применение препарата изучено в большом чис-ле клинических испытаний у разных групп пациентов, при этом феррокинетика проанализирована с помощью позитронной эмиссионной томографии с целью оценки распределения железа после введения препарата [90]. Эффективность лечения препаратом подтверждена дан-ными, приведенными в систематическом обзоре и мета-анализе результатов рандомизированных исследований [91].…”