Research
Print page Print page
Switch language
The Capital Region of Denmark - a part of Copenhagen University Hospital
Published

Pharmacokinetics of Ferric bepectate - a new intravenous iron drug for treating iron deficiency

Research output: Contribution to journalJournal articleResearchpeer-review

DOI

  1. Drug-related challenges following primary total hip and knee arthroplasty

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Validation of registration of pharmacological treatment in the Danish Hip and Knee Arthroplasty Registers

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Camostat mesylate against SARS-CoV-2 and COVID-19-Rationale, dosing and safety

    Research output: Contribution to journalReviewResearchpeer-review

  4. Postponement of cardiovascular outcomes by statin use: A systematic review and meta-analysis of randomized clinical trials

    Research output: Contribution to journalJournal articleResearchpeer-review

  1. Using machine learning for predicting intensive care unit resource use during the COVID-19 pandemic in Denmark

    Research output: Contribution to journalJournal articleResearchpeer-review

  2. Variable oxygen administration in surgical and medical wards evaluated by 30-day mortality - an observational study

    Research output: Contribution to journalJournal articleResearchpeer-review

  3. Medication errors in residential facilities based on Danish Poison Information Center inquiries

    Research output: Contribution to journalJournal articleResearchpeer-review

  4. Developing and validating COVID-19 adverse outcome risk prediction models from a bi-national European cohort of 5594 patients

    Research output: Contribution to journalJournal articleResearchpeer-review

  5. One-year mortality increases four-fold in frail patients undergoing cardiac surgery

    Research output: Contribution to journalJournal articleResearchpeer-review

View graph of relations

IV iron is indicated in clinical conditions, where rapid anaemia alleviation and repletion of iron stores are required. The acute toxicity of IV iron is ascribed to the presence of labile iron in plasma. Thus, shorter plasma residence time might improve the safety profile, even for compounds holding-on the iron tightly. In this single-centre, open-label, single-dose escalation study, we evaluated the elimination kinetics of ferric bepectate (FBP) compared to those of ferric carboxymaltose (FCM). Thirty-three iron-depleted anaemic patients who had undergone cardiac surgery were included and received 200, 500 or 1500 mg FBP or 500 mg FCM. Plasma drug curves were subjected to model-free analysis. Because saturation kinetics was found, a compartmental model with limited elimination capacity was applied. Urinary iron excretion was also analysed. The initial non-compartmental analysis revealed an increasing AUC/dose ratio for FBP. For both drugs, the central distribution compartment corresponded to plasma volume, and elimination followed Michaelis-Menten saturation kinetics. Maximal elimination rates (Vmax) were 224 mg/hr and 81 mg/hr for FBP 500 mg and FCM 500 mg, respectively; drug concentrations at half Vmax (Km), 99 mg/L and 212 mg/L, respectively; and terminal plasma half-life (T½), 3.05 hr and 8.96 hr, respectively. Both drugs were equally effective in eliciting an early ferritin rise. Urinary iron excretion was measurable in all patients receiving FCM but not in those receiving FBP, which was well tolerated. Intravenous iron drugs are subject to capacity-limited elimination with different saturation thresholds. Urinary iron excretion can be used as a surrogate for labile plasma iron. This article is protected by copyright. All rights reserved.

Original languageEnglish
JournalBasic & clinical pharmacology & toxicology
Volume125
Issue number2
Pages (from-to)133-141
ISSN1742-7843
DOIs
Publication statusPublished - Aug 2019

Bibliographical note

© 2019 The Authors. Basic & Clinical Pharmacology & Toxicology published by John Wiley & Sons Ltd on behalf of Nordic Association for the Publication of BCPT (former Nordic Pharmacological Society).

    Research areas

  • intravenous iron drugs, labile iron, michaelis-menten kinetics, side effects, urinary iron, Prospective Studies, Anemia, Iron-Deficiency/blood, Ferric Compounds/administration & dosage, Humans, Middle Aged, Male, Maltose/administration & dosage, Renal Elimination, Dose-Response Relationship, Drug, Iron/blood, Aged, Infusions, Intravenous

ID: 56798991