Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2020 Publisher: Pharmacosmos A/S, Roervangsvej 30, DK-4300 Holbaek, Denmark
Pharmacotherapeutic group: Iron parenteral preparation
ATC code: B03AC
Diafer solution for injection is a colloid with strongly bound iron in spheroidal iron-carbohydrate particles. The carbohydrate part of the complex constitutes derisomaltose, which consists of 3-5 glucose units with an average molecular weight of approximately 1000 kDa. The complex forms a stable matrix type structure with about 10 iron(III) atoms to one molecule of derisomaltose pentamers. Derisomaltose does not contain any reducing sugar residues, which can be involved in complex redox reactions.
INN name: Ferric derisomaltose (also known as iron(III) isomaltoside 1000).
The iron is available in a non-ionic water-soluble form in an aqueous solution with pH between 5.0 and 7.0.
Evidence of a therapeutic response can be seen within a few days of administration of Diafer as an increase in the reticulocyte count.
Serum ferritin peaks approximately 7 to 9 days after an intravenous dose of Diafer and slowly returns to baseline after about 3 weeks.
Pharmacokinetic studies are not available for Diafer. Information given is based on literature data from various parenteral iron preparations.
The Diafer formulation contains iron in a strongly bound complex that enables a controlled and slow release of bioavailable iron to iron-binding proteins with little risk of free iron.
Following intravenous administration, ferric derisomaltose is rapidly taken up by the cells in the reticuloendothelial system (RES), particularly in the liver and spleen from where iron is slowly released. The plasma half life is approximately 1 day for total iron (bound and circulating).
Circulating iron is removed from the plasma by cells of the reticuloendothelial system which split the complex into its components of iron and derisomaltose. The iron is immediately bound to the available protein moieties to form hemosiderin or ferritin, the physiological storage forms of iron, or to a lesser extent, to the transport molecule transferrin. This iron, which is subject to physiological control, replenishes haemoglobin and depleted iron stores.
Iron is not easily eliminated from the body and accumulation can be toxic. Due to the size of the complex, ferric derisomaltose is not eliminated via the kidneys. Small quantities of iron are eliminated in urine and faeces.
Derisomaltose is either metabolised or excreted.
Pharmacokinetic studies are not available for Diafer. Information given is based on literature data from various parenteral iron preparations.
Iron complexes have been reported to be teratogenic and embryocidal in non-anaemic pregnant animals at high single doses above 125 mg iron/kg body weight. The highest recommended dose in clinical use is 20 mg iron/kg body weight.
There are no other additional preclinical data of relevance to the prescriber than those already included in other sections of the SPC.
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