Iron sucrose complex

Sodium ferric gluconate complex and iron-sucrose complex are alternative parenteral iron preparations. These agents can be given only by the intravenous route. They appear to be less likely than high-molecular-weight iron dextran to cause hypersensitivity reactions. 

Iron dextran, iron sucrose complex, and sodium ferric gluconate complex Parenteral preparations can cause hypersensitivity reactions ... 

The efficiency of vitamin E in the suppression of free radical-mediated damage induced by iron overload has been studied in animals and humans. Galleano and Puntarulo [46] showed that iron overload increased lipid and protein peroxidation in rat liver. Vitamin E supplementation successfully suppressed these effects and led to an increase in a-tocopherol, ubiquinone-9, and ubiquinone-10 contents in liver. Important results were obtained by Roob et al. [47] who found that vitamin E supplementation attenuated lipid peroxidation (measured as plasma MDA and plasma lipid peroxides) in patients on hemodialysis after receiving iron hydroxide sucrose complex intravenously during hemodialysis session. These findings support the proposal that iron overload enhances free radical-mediated damage in humans. 

The challenge with parenteral iron therapy is that parenteral administration of inorganic free ferric iron produces serious dose-dependent toxicity, which severely limits the dose of that can be administered. However, when the ferric iron is formulated as a colloid containing particles with a core of iron oxyhydroxide surrounded by a core of carbohydrate, bioactive iron is released slowly from the stable colloid particles. In the USA, the three available forms of parenteral iron are iron dextran, sodium ferric gluconate complex, and iron sucrose. 

Parenteral (Iron dextran) (InFeD, DexFerrum) 50 mg elemental iron/mL Parenteral (Sodium ferric gluconate complex) (Ferrlecit) 12.5 mg elemental iron/mL Parenteral (Iron sucrose) (Venofer) 20 mg elemental iron/mL Oprelvekin (IL-11) (Neumega)... 

We have found, however, that the ferric complex with sucrose is suitable for this purpose. Although the complex does not represent a homogenous molecular species, it is stable and highly soluble in water at neutral pH at a ratio of iron sucrose <1 40 and has a favorable over-... 

Intravenous iron. Iron dextran inj. (ferric hydroxide complexed with dextrans 50 mg/ml) and iron sucrose inj. (ferric hydroxide complexed with sucrose 20 mg/ml) are administered by slow... 

Intravenous iron preparations differ in the composition of the complex to which elemental iron is bound. These differences affect the rate of dissociation of iron from the complex to the reticuloendothelial system and subsequent storage as ferritin. Iron sucrose is also delivered directly to transferrin. The half-life of these formulations also differ ferric gluconate 1 hour, iron sucrose 6 hours, and iron dextran 40 to 60 hours. However, there is minimal to no correlation between the pharmacokinetics of these formulations and their pharmacodynamic effects. ... 

FDA-approved preparations for parenteral therapy include sodium ferric gluconate complex in sucrose (ferrlecit), iron sucrose (venofer), and iron dextran (iNFED, DEXFERRUM). Unlike iron dextran, which requires macrophage processing that may require several weeks, -80% of sodium ferric gluconate is delivered to transferrin with 24 hours. Sodium ferric gluconate has a much lower risk of serious anaphylactic reactions than iron dextran. 

Iron sorbitol is a complex of iron, sorbitol and citric acid. It i.s not suitable for intravenous injection and is given by deep intramuscular injcction.s to minimi/c staining of the skin. Iron sorbitol may cause anaphylactoid reactions. Iron sucrose is a complex of ferric hydroxide with sucrose that is given by intravenous injection or infusion. Severe reactions may occur and drugs for resuscitation and anaphylaxis should be available. 

Pharmacology Sodium ferric gluconate complex in sucrose injection is a stable macromolecular complex used to replete the total body content of iron. 

Other sugars and polyols also complex with iron. Fructose is the most effective, but sorbitol, glucose, galactose, lactose, sucrose, pentoses and tetroses can also keep hydrolyzed ferric salts in solution. An excess of sugar must always be present in order to prevent ferric hydroxide precipitate. There appears to be a competition between the OH- and sugar hydroxyls for the Fe3+. 

Detailed kinetic measurements of the initial rates of iron uptake by rat liver mitochondria have been carried out in this laboratory during the last few years using 59Fe(III)-sucrose as the donor complex (23, 24, 27-32). The general features given in Table II support the concept that iron, like other cations, is accumulated by an energy-dependent as well as an energy-independent mechanism, and these two processes have different time, pH, and temperature dependencies. 

It has been generally assumed that iron is transported across biological membranes in the ferrous form and that ferric iron would have to be reduced before it can be used by the organism. Thus, based on nutritional studies it has long been recognized that Fe(II) is1 more effectively absorbed than Fe(III), and this has been attributed to differences in the thermodynamic and kinetic stability of the complexes and chelates formed by these cations (for review, see Ref. 2). The experimental proof of a transport in the ferrous form has, however, not been given until quite recently in studies of iron transport in isolated mitochondria (23) as well as in enterobacteria (33). In rat liver mitochondria we have found that Fe(III) donated from a metabolically inert water soluble complex of sucrose interacts with the respiratory chain at the level of cytochrome c (and possibly cytochrome a) (23, 32) (Figure 1 B), which has a oxidation-reduction potential of around +250 mV (34) and is localized to the outer phase of the mitochondrial inner membrane (35). 

Composition Ferric oxide hydrate bonded to sucrose chelates with gluconate in a molar rate of 2 iron molecules to 1 gluconate molecule Complex of ferric hydroxide and dextran Complex of polynuclear iron hydroxide in sucrose... 

Faich G, Strobos J. Sodium Fe + gluconate complex in sucrose safer IV 61. iron therapy than iron dextrans. Am J Kidney Dis 1999 33 464-470. 

The parenteral iron medications available include iron dextran (ferric hydroxide and high-molecular-weight dextran) for intramuscular use, dextriferron (a complex of ferric hydroxide and partially hydrolyzed dextran) for intravenous use, and saccharated iron oxide (a complex of ferric hydroxide and sucrose) for intravenous use. These preparations are reserved for those cases in which oral preparations are not tolerated, absorbed, or rapid enough in their onset of action, or are otherwise not suitable for noncompfiant patients. 

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