Sodium ferric gluconate complex

Identification

Name
Sodium ferric gluconate complex
Accession Number
DB09517
Description

Sodium ferric gluconate complex is an iron replacement product for treatment of iron deficiency anemia. The stable macromolecular complex is negatively charged at alkaline pH with an apparent molecular weight of 289,000 – 440,000 daltons on gel chromatography. It is composed of iron (III) oxide hydrate directly bonded to sucrose with a chelating gluconate function in a molar ratio of two iron molecules to one gluconate. It is used in adult and in pediatric patients over the age of 6 years with chronic kidney disease (CKD) receiving hemodialysis and receiving supplemental epoetin therapy.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 2089.309
Monoisotopic: 2088.47592
Chemical Formula
C66H121Fe2NaO65
Synonyms
  • Ferric sodium gluconate complex
  • Sodium ferric gluconate complex

Pharmacology

Indication

Used to replete the total body content of iron during iron deficiency anemia in patients age 6 years and older with chronic kidney disease receiving hemodialysis and receiving supplemental epoetin therapy.

Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

Sodium ferric gluconate complex is an exogenous epoetin that acts to restore the body's content of iron, which is essential for normal hemoglobin synthesis, oxygen transport and enzymatic processes. The complex increases red blood cell production and increased iron utilization.

Mechanism of action

The complex is endocytosed by macrophages of the reticuloendothelial system. Within an endosome of the macrophage , lysosome fuses with the endosome creating an acidic environment leading to the cleavage of the complex from iron. Iron is then incorporated in ferritin, transferrin or hemoglobin. Sodium ferric gluconate also normalizes RBC production by binding with hemoglobin

TargetActionsOrganism
AFerritin light chain
binding
Humans
UHemoglobin subunit alpha
binding
Humans
AHemoglobin subunit beta
binding
Humans
Absorption

Peak drug levels (Cmax) varied significantly by dosage and by rate of administration. Highest Cmax value is observed in the regimen in which 125 mg was administered in 7 minutes (19.0 mg/L).

Volume of distribution

The initial volume of distribution is 6L which correlates well with the calculated blood volume.

Protein binding

It is bind to transferrin, ferritin and hemoglobin.

Metabolism
Not Available
Route of elimination

It is renally eliminated if it is greater than 18,000 Daltons.

Half-life

The terminal elimination half-life for drug bound iron was approximately 1 hour, with the value varying by dose but not by rate of administration. In adults, the shortest terminal elimination half-life of 0.825h occurs with the 62.5 mg/4 min dosing regimen and the longest value of 1.45h is achieved with 125 mg/7 min regimen. In pediatric patients, the half-life was 2 hours following administration of 1.5 mg/kg dose and 2.5 hours following administration of 3.0mg/kg dose.

Clearance

Total clearance ranges from 3.02 to 5.35 L/h in adult patients.

Adverse Effects
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Toxicity

Overdosage of iron causes cardiovascular toxicity and hepatic necrosis. The lowest lethal dose (LDLo) following intravenous administration is 78.8mg/kg in rats and 250mg/kg in dogs. Adverse effects from sodium ferric gluconate therapy include hypersensitivity reactions, nausea, vomiting, diarrhea, pain, peripheral swelling and hypotension. Dosages in excess of iron needs may lead to accumulation of iron in iron storage sites and hemosiderosis.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
CinoxacinSodium ferric gluconate complex can cause a decrease in the absorption of Cinoxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CiprofloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
DelafloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
EnoxacinSodium ferric gluconate complex can cause a decrease in the absorption of Enoxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
GatifloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Gatifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
GemifloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Gemifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
GrepafloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Grepafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
LevofloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Levofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
LomefloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Lomefloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
MoxifloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Moxifloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

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  • Action
    Action

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Food Interactions
No interactions found.

Products

Active Moieties
NameKindUNIICASInChI Key
IronunknownE1UOL152H77439-89-6XEEYBQQBJWHFJM-UHFFFAOYSA-N
Ferric cationionic91O4LML61120074-52-6VTLYFUHAOXGGBS-UHFFFAOYSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FerrlecitLiquid12.5 mgIntravenousSanofi Aventis2005-03-02Not applicableCanada flag
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC1999-02-182010-01-04US flag
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC2014-07-07Not applicableUS flag
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC2011-03-01Not applicableUS flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
NulecitInjection12.5 mg/1mLIntravenousActavis Pharma Company2011-03-312013-05-31US flag
Sodium Ferric Gluconate ComplexInjection12.5 mg/1mLIntravenousActavis Pharma, Inc.2011-03-312019-06-30US flag
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousHikma Pharmaceuticals USA Inc.2011-03-31Not applicableUS flag
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousWest-Ward Pharmaceuticals Corp2011-03-31Not applicableUS flag
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousActavis Pharma, Inc.2012-08-232019-06-30US flag
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as sugar acids and derivatives. These are compounds containing a saccharide unit which bears a carboxylic acid group.
Kingdom
Organic compounds
Super Class
Organic oxygen compounds
Class
Organooxygen compounds
Sub Class
Carbohydrates and carbohydrate conjugates
Direct Parent
Sugar acids and derivatives
Alternative Parents
C-glycosyl compounds / Disaccharides / O-glycosyl compounds / Medium-chain hydroxy acids and derivatives / Medium-chain fatty acids / Beta hydroxy acids and derivatives / Hydroxy fatty acids / Ketals / Oxanes / Oxolanes
show 13 more
Substituents
Acetal / Alcohol / Aliphatic heteromonocyclic compound / Beta-hydroxy acid / C-glycosyl compound / Carbonyl group / Carboxylic acid / Carboxylic acid derivative / Carboxylic acid salt / Disaccharide
show 25 more
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
CC9149U2QX
CAS number
34089-81-1
InChI Key
MQBDAEHWGRMADS-XNHLMZCASA-M
InChI
InChI=1S/5C12H22O11.C6H12O7.2Fe.Na.3O/c5*13-1-4-6(16)8(18)9(19)11(21-4)23-12(3-15)10(20)7(17)5(2-14)22-12;7-1-2(8)3(9)4(10)5(11)6(12)13;;;;;;/h5*4-11,13-20H,1-3H2;2-5,7-11H,1H2,(H,12,13);;;;;;/q;;;;;;2*+3;+1;3*-2/p-1/t5*4-,5-,6-,7-,8+,9-,10+,11-,12+;2-,3-,4+,5-;;;;;;/m111111....../s1
IUPAC Name
diiron(3+) ion sodium pentakis((2R,3R,4S,5S,6R)-2-{[(2S,3S,4S,5R)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]oxy}-6-(hydroxymethyl)oxane-3,4,5-triol) (2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanoate trioxidandiide
SMILES

References

Synthesis Reference

Geisser, Peter, and Susanna Burckhardt. "The Pharmacokinetics And Pharmacodynamics Of Iron Preparations". Pharmaceutics 3.4 (2011): 12-33. Web. 14 Apr. 2017.

General References
  1. Tenenbein M: Hepatotoxicity in acute iron poisoning. J Toxicol Clin Toxicol. 2001;39(7):721-6. [PubMed:11778670]
  2. Warady BA, Seligman PA, Dahl NV: Single-dosage pharmacokinetics of sodium ferric gluconate complex in iron-deficient pediatric hemodialysis patients. Clin J Am Soc Nephrol. 2007 Nov;2(6):1140-6. Epub 2007 Oct 17. [PubMed:17942782]
  3. Faich G, Strobos J: Sodium ferric gluconate complex in sucrose: safer intravenous iron therapy than iron dextrans. Am J Kidney Dis. 1999 Mar;33(3):464-70. [PubMed:10070910]
  4. Henry DH, Dahl NV, Auerbach M, Tchekmedyian S, Laufman LR: Intravenous ferric gluconate significantly improves response to epoetin alfa versus oral iron or no iron in anemic patients with cancer receiving chemotherapy. Oncologist. 2007 Feb;12(2):231-42. [PubMed:17296819]
  5. Warady BA, Zobrist RH, Wu J, Finan E: Sodium ferric gluconate complex therapy in anemic children on hemodialysis. Pediatr Nephrol. 2005 Sep;20(9):1320-7. Epub 2005 Jun 22. [PubMed:15971073]
  6. SODIUM FERRIC GLUCONATE COMPLEX IN SUCROSE MONOGRAPH [Link]
PubChem Compound
76968835
PubChem Substance
347827872
ChemSpider
34989638
RxNav
261435
Wikipedia
Sodium_ferric_gluconate_complex
AHFS Codes
  • 20:04.04 — Iron Preparations
FDA label
Download (86.7 KB)
MSDS
Download (957 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentAnemia2
4CompletedTreatmentChronic Renal Failure (CRF) / Iron Deficiency Anemia (IDA) / Iron-Deficiency Anemias2
4CompletedTreatmentHeart Failure / Iron Deficiency Anemia (IDA)1
4Not Yet RecruitingTreatmentHeart Failure1
4Unknown StatusTreatmentAnemia1
3CompletedSupportive CareAnemia / Disorders, Lymphoproliferative / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Precancerous Conditions / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAnemia1
2WithdrawnTreatmentAnemia1
2, 3CompletedTreatmentIron Deficiency Anemia (IDA)1
1CompletedBasic ScienceChronic Renal Failure (CRF) / Iron Deficiency Anemia (IDA) / Iron-Deficiency Anemias1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
LiquidIntravenous12.5 mg
InjectionIntravenous12.5 mg/1mL
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility824.0 mg/mLALOGPS
logP-2.6ALOGPS
logP-4.5ChemAxon
logS0.38ALOGPS
pKa (Strongest Acidic)11.84ChemAxon
pKa (Strongest Basic)-3ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count11ChemAxon
Hydrogen Donor Count8ChemAxon
Polar Surface Area189.53 Å2ChemAxon
Rotatable Bond Count30ChemAxon
Refractivity68.77 m3·mol-1ChemAxon
Polarizability30.86 Å3ChemAxon
Number of Rings10ChemAxon
Bioavailability0ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binding
General Function
Iron ion binding
Specific Function
Stores iron in a soluble, non-toxic, readily available form. Important for iron homeostasis. Iron is taken up in the ferrous form and deposited as ferric hydroxides after oxidation. Also plays a ro...
Gene Name
FTL
Uniprot ID
P02792
Uniprot Name
Ferritin light chain
Molecular Weight
20019.49 Da
References
  1. The Pharmacokinetics And Pharmacodynamics Of Iron Preparations [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binding
General Function
Oxygen transporter activity
Specific Function
Involved in oxygen transport from the lung to the various peripheral tissues.
Gene Name
HBA1
Uniprot ID
P69905
Uniprot Name
Hemoglobin subunit alpha
Molecular Weight
15257.405 Da
References
  1. The Pharmacokinetics And Pharmacodynamics Of Iron Preparations [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binding
General Function
Oxygen transporter activity
Specific Function
Involved in oxygen transport from the lung to the various peripheral tissues.LVV-hemorphin-7 potentiates the activity of bradykinin, causing a decrease in blood pressure.Spinorphin: functions as an...
Gene Name
HBB
Uniprot ID
P68871
Uniprot Name
Hemoglobin subunit beta
Molecular Weight
15998.34 Da
References
  1. The Pharmacokinetics And Pharmacodynamics Of Iron Preparations [Link]

Drug created on November 30, 2015 12:10 / Updated on September 22, 2020 02:10

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