Sodium ferric gluconate complex

Identification

Name
Sodium ferric gluconate complex
Accession Number
DB09517
Type
Small Molecule
Groups
Approved
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.

Structure
Thumb
Synonyms
  • Ferric sodium gluconate complex
  • Sodium ferric gluconate complex
Active Moieties
NameKindUNIICASInChI Key
IronunknownE1UOL152H77439-89-6XEEYBQQBJWHFJM-UHFFFAOYSA-N
Ferric cationionic91O4LML61120074-52-6VTLYFUHAOXGGBS-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
FerrlecitLiquidIntravenousSanofi Aventis2005-03-02Not applicableCanada
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC2014-07-07Not applicableUs
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC2011-03-01Not applicableUs
FerrlecitInjection12.5 mg/1mLIntravenoussanofi-aventis U.S. LLC1999-02-182010-01-04Us
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.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
NulecitInjection12.5 mg/1mLIntravenousActavis Pharma Company2011-03-312013-05-31Us
Sodium Ferric Gluconate ComplexInjection12.5 mg/1mLIntravenousActavis Pharma, Inc.2011-03-312019-06-30Us
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousWest-Ward Pharmaceuticals Corp2011-03-31Not applicableUs
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousWest-Ward Pharmaceuticals Corp2011-03-31Not applicableUs
Sodium Ferric Gluconate Complex in SucroseInjection12.5 mg/1mLIntravenousActavis Pharma, Inc.2012-08-232019-06-30Us
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.

    Learn more
Categories
UNII
CC9149U2QX
CAS number
34089-81-1
Weight
Average: 2089.309
Monoisotopic: 2088.47592
Chemical Formula
C66H121Fe2NaO65
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
[O--].[O--].[O--].[Na+].[Fe+3].[Fe+3].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O.OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O.OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O.OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O.OC[C@H]1O[C@@](CO)(O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@@H]1O

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
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
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
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.

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.
DifloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Difloxacin 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.
EnrofloxacinSodium ferric gluconate complex can cause a decrease in the absorption of Enrofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
FleroxacinSodium ferric gluconate complex can cause a decrease in the absorption of Fleroxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
FlumequineSodium ferric gluconate complex can cause a decrease in the absorption of Flumequine resulting in a reduced serum concentration and potentially a decrease in efficacy.
GarenoxacinSodium ferric gluconate complex can cause a decrease in the absorption of Garenoxacin 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.
Additional Data Available
  • Extended Description
    Extended Description

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

    Learn more
  • Severity
    Severity

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

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
No interactions found.

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]
External Links
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
1CompletedBasic ScienceChronic Renal Failure (CRF) / Iron Deficiency Anemia (IDA) / Iron-Deficiency Anemias1
2WithdrawnTreatmentAnemia1
2, 3CompletedTreatmentIron Deficiency Anemia (IDA)1
3CompletedSupportive CareAnemia / Disorders, Lymphoproliferative / Leukemias / Malignant Lymphomas / Multiple Myeloma and Plasma Cell Neoplasm / Precancerous Conditions / Unspecified Adult Solid Tumor, Protocol Specific1
3CompletedTreatmentAnemia1
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
Not AvailableUnknown StatusTreatmentRenal Failure Chronic Requiring Hemodialysis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
LiquidIntravenous
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

Taxonomy

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
Gluconic_acid / O-glycosyl compound / C-glycosyl compound / Disaccharide / Glycosyl compound / Medium-chain hydroxy acid / Medium-chain fatty acid / Hydroxy fatty acid / Beta-hydroxy acid / Ketal
show 25 more
Molecular Framework
Not Available
External Descriptors
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 July 11, 2020 00:05

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates