Carboxymethylcellulose

Identification

Summary

Carboxymethylcellulose is a compound used as an ophthalmic lubricant.

Brand Names
Leader Lubricant Eye Drops, Refresh Drops, Refresh Liquigel, Refresh Optive Advanced, Refresh Optive Extended Therapy, Retaine, Thera Tears, Theratears
Generic Name
Carboxymethylcellulose
DrugBank Accession Number
DB11059
Background

Carboxymethylcellulose is a cellulose derivative that consists of the cellulose backbone made up of glucopyranose monomers and their hydroxyl groups bound to carboxymethyl groups. It is added in food products as a viscosity modifier or thickener and emulsifier. It is also one of the most common viscous polymers used in artificial tears, and has shown to be effective in the treatment of aqueous tear-deficient dry eye symptoms and ocular surface staining 1. The viscous and mucoadhesive properties as well as its anionic charge allow prolonged retention time in the ocular surface 1. Sodium carboxymethylcellulose is the most commonly used salt.

Type
Small Molecule
Groups
Approved, Investigational
Synonyms
  • Carbose
  • Carboxymethyl cellulose
  • Carmellose
  • Carmelosa
  • Cellulose carboxymethyl ether
  • Cellulose gum
  • Cellulose, carboxymethyl ether
  • Thylose

Pharmacology

Indication

Indicated for the symptomatic relief of burning, irritation and discomfort of the eyes due to dryness or exposure to wind or sun.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

In a randomized clinical study of patients with mild or moderate forms of eye dryness, ophthalmic treatment with sodium carboxymethylcellulose resulted in a diminished frequency of symptoms compared to the placebo group 2. Carboxymethylcellulose interacts with human corneal epithelial cells to facilitate corneal epithelial wound healing and attenuate eye irritation in a dose-dependent manner 1. It exhibits protective actions on the ocular surface in various applications; it mediates cytoprotective effects on the ocular surface when applied prior to contact lenses and reduces the incidence of epithelial defects during LASIK 1.

Mechanism of action

Carboxymethylcellulose binds to the surface of corneal epithelial cells via its glucopyranose subunits binding to glucose receptors GLUT-1 1. The residence time of carboxymethylcellulose bound to corneal cells is approximately 2 hours as indicated by a short-term binding assay 1. Binding of carboxymethylcellulose to the matrix proteins stimulated corneal epithelial cell attachment, migration, and re-epithelialization of corneal wounds 1.

TargetActionsOrganism
USolute carrier family 2, facilitated glucose transporter member 1
binder
Humans
Absorption

No pharmacokinetic data available.

Volume of distribution

No pharmacokinetic data available.

Protein binding

No pharmacokinetic data available.

Metabolism

No pharmacokinetic data available.

Route of elimination

No pharmacokinetic data available.

Half-life

No pharmacokinetic data available.

Clearance

No pharmacokinetic data available.

Adverse Effects
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Toxicity

Rat oral LD50, rabbit dermal LD50, and rat inhalation LC50 of sodium carboxymethyl cellulose are 27000 mg/kg, >2 g/kg, and >5800 mg/m^3 (4 hours), respectively MSDS.

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
AcetazolamideThe risk or severity of adverse effects can be increased when Acetazolamide is combined with Carboxymethylcellulose.
AclidiniumThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Aclidinium.
AlfentanilThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Alfentanil.
AlloinThe risk or severity of adverse effects can be increased when Carboxymethylcellulose is combined with Alloin.
AmantadineThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Amantadine.
AmilorideThe risk or severity of adverse effects can be increased when Amiloride is combined with Carboxymethylcellulose.
AmiodaroneThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Amiodarone.
AmitriptylineThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Amitriptyline.
AmlodipineThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Amlodipine.
AmobarbitalThe therapeutic efficacy of Carboxymethylcellulose can be decreased when used in combination with Amobarbital.
Interactions
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Food Interactions
No interactions found.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Carboxymethylcellulose sodiumK679OBS3119004-32-4Not applicable
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Acne PatchsPatch1.5 mg/1TopicalShenzhen Xing Ji Zhi Tong Technology Co.,Ltd2021-01-07Not applicableUS flag
Acne Pimple Master PatchPatch30 mg/10gTopicalCosrx Inc.2015-12-282015-12-31US flag
Artificial TearsLiquid10 mg/1mLOphthalmicDelsam Pharma Llc2020-07-23Not applicableUS flag
Artificial TearsSolution / drops10 mg/1mLOphthalmicAru Pharma Inc.2018-01-22Not applicableUS flag
Artificial Tears Lubricant Eye DropsSolution / drops10 mg/1mLOphthalmicEzricare Llc2020-11-22Not applicableUS flag
Biolle Gel TearsSolution / drops10 mg/1mLOphthalmicSage Ethnographic Research, Dba Biollé2015-06-01Not applicableUS flag
Biolle TearsSolution / drops5 mg/1mLOphthalmicSage Ethnographic Research, Dba Biollé2015-06-01Not applicableUS flag
Carboxymethylcellulose SodiumSolution / drops5 mg/1mLOphthalmicAvPAK2020-11-19Not applicableUS flag
Carboxymethylcellulose SodiumGel10 mg/1mLOphthalmicAvPAK2020-11-18Not applicableUS flag
Carboxymethylcellulose SodiumSolution / drops5 mg/1mLOphthalmicAvPAK2020-11-19Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Clear Eyes for Dry EyesCarboxymethylcellulose sodium (1.0 %) + Glycerin (0.25 %)SolutionOphthalmicPrestige Brands Inc2008-03-262014-03-20Canada flag
CVS Moisturizing Lubricating EyeCarboxymethylcellulose sodium (5 mg/100mg) + Glycerin (9 mg/100mg)Solution / dropsOphthalmicCVS Health2013-09-03Not applicableUS flag
CVS Moisturizing Lubricating Eye Twin PackCarboxymethylcellulose sodium (5 mg/1mL) + Glycerin (9 mg/1mL)Solution / dropsOphthalmicCVS Health2014-07-10Not applicableUS flag
Equate ComfortCarboxymethylcellulose sodium (2.5 mg/1mL) + Hypromellose (3 mg/1mL)GelOphthalmicWalmart Stores2014-04-10Not applicableUS flag
Equate Day and Night Restore TearsCarboxymethylcellulose sodium (5 mg/1mL) + Mineral oil (425 mg/1g) + Petrolatum (573 mg/1g)KitOphthalmicWalmart Stores2018-06-01Not applicableUS flag
Equate Lubricating EyeCarboxymethylcellulose sodium (5 mg/1mL) + Glycerin (9 mg/1mL)Solution / dropsOphthalmicWalmart Stores2012-04-01Not applicableUS flag
Equate Restore Dual LubricatingCarboxymethylcellulose sodium (5 mg/1mL) + Glycerin (9 mg/1mL)Solution / dropsOphthalmicWalmart2018-03-01Not applicableUS flag
Equate Restore Dual Sensitive LubricantCarboxymethylcellulose sodium (5 mg/1mL) + Glycerin (9 mg/1mL)Solution / dropsOphthalmicWalmart Stores2016-05-03Not applicableUS flag
Genteal GeldropsCarboxymethylcellulose sodium (0.25 %) + Hypromellose (0.3 %)SolutionOphthalmicAlcon, Inc.2007-01-032014-01-13Canada flag
GenTeal Moderate to SevereCarboxymethylcellulose sodium (2.5 mg/1mL) + Hypromellose (3 mg/1mL)GelOphthalmicNovartis Pharmaceutical Corporation2009-09-142018-06-30US flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Acne PatchsCarboxymethylcellulose (1.5 mg/1)PatchTopicalShenzhen Xing Ji Zhi Tong Technology Co.,Ltd2021-01-07Not applicableUS flag
Acne Pimple Master PatchCarboxymethylcellulose sodium (30 mg/10g)PatchTopicalCosrx Inc.2015-12-282015-12-31US flag
Cho-A DermCarboxymethylcellulose sodium (130 g/433g)DressingTopicalCho-A Pharm.Co.,Ltd.2018-06-19Not applicableUS flag
Mizon Bye Bye PimpleCarboxymethylcellulose (1.05 g/3.5g)PatchTopicalMizon Co.,Ltd.2018-05-01Not applicableUS flag
Thera-clearCarboxymethylcellulose (60 g/100g)PatchTopicalPeach Town Wholesale Inc.2020-11-06Not applicableUS flag
Trouble Clear SpotCarboxymethylcellulose sodium (36.87 mg/241)PatchTopicalSkinfood Co., Ltd.2016-04-012017-03-01US flag
Trouble Clear Spot 0.7cmCarboxymethylcellulose sodium (6.17 mg/101)PatchTopicalSkinfood Co., Ltd.2015-02-012017-03-01US flag
Trouble Clear Spot 1.0cmCarboxymethylcellulose sodium (12.58 mg/51)PatchTopicalSkinfood Co., Ltd.2015-02-012017-03-01US flag
Trouble Clear Spot 1.2cmCarboxymethylcellulose sodium (18.12 mg/91)PatchTopicalSkinfood Co., Ltd.2015-02-012017-03-01US flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
05JZI7B19X
CAS number
9000-11-7

References

General References
  1. Garrett Q, Simmons PA, Xu S, Vehige J, Zhao Z, Ehrmann K, Willcox M: Carboxymethylcellulose binds to human corneal epithelial cells and is a modulator of corneal epithelial wound healing. Invest Ophthalmol Vis Sci. 2007 Apr;48(4):1559-67. doi: 10.1167/iovs.06-0848. [Article]
  2. Bruix A, Adan A, Casaroli-Marano RP: [Efficacy of sodium carboxymethylcellulose in the treatment of dry eye syndrome]. Arch Soc Esp Oftalmol. 2006 Feb;81(2):85-92. [Article]
  3. DailyMed: Refresh Tears (carboxymethylcellulose) lubricating eye drops [Link]
PubChem Substance
347911098
RxNav
2062
ChEMBL
CHEMBL1909054
Wikipedia
Carboxymethyl_cellulose
AHFS Codes
  • 28:20.00 — Anorexigenic Agents & Respiratory and CNS Stimulants
  • 52:13.00* — Artificial Tears
  • 52:92.00 — EENT Drugs, Miscellaneous
MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentCataracts / Dry Eye Syndromes1
4CompletedTreatmentCervical Preparation / Medically induced abortion / Pain / Pregnancy Termination1
4CompletedTreatmentDry Eye Syndrome (DES)1
4CompletedTreatmentDry Eye Syndromes8
4CompletedTreatmentDry Eye Syndromes / Keratoconjunctivitis Sicca2
4CompletedTreatmentSeasonal Allergic Conjunctivitis1
4Enrolling by InvitationTreatmentDiabetic Macular Edema (DME) / Neovascular Age-Related Macular Degeneration / Retinal Vein Occlusion1
4RecruitingTreatmentIllness, Critical / Shock1
4Unknown StatusPreventionMyopia1
3CompletedTreatmentBilateral LASIK Surgery1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
PatchTopical1.5 mg/1
PatchTopical30 mg/10g
LiquidOphthalmic10 mg/1mL
Solution / dropsOphthalmic10 mg/1mL
SyrupOral
SolutionOphthalmic5 mg/1mL
SolutionConjunctival; Ophthalmic10 mg
LiquidOphthalmic0.5 %
Solution / dropsConjunctival
Solution / drops; suspension / dropsOphthalmic4 mg/0.4mL
Solution / dropsOphthalmic
DressingTopical130 g/433g
Solution / dropsOphthalmic2.5 mg/1mL
LiquidOphthalmic0.5 g/100mL
Solution / dropsOphthalmic
GelOphthalmic
KitOphthalmic
LiquidIntraocular5 mg/1mL
SolutionOphthalmic10 mg
SolutionIntraocular; Ophthalmic10 mg
Aerosol, sprayOral
Solution / dropsOphthalmic.5 g/100mL
Solution, gel forming / dropsOphthalmic0.5 g/100mL
SolutionOphthalmic
SolutionOphthalmic5 mg
LiquidOphthalmic5 mg/1mL
Solution, gel forming / dropsOphthalmic.5 g/100mL
SolutionOphthalmic0.5 mg
SolutionOphthalmic0.5 g/100mL
PatchTopical1.05 g/3.5g
SolutionOphthalmic0.5 % w/v
CapsuleOral300 mg
SolutionConjunctival; Ophthalmic
LiquidOphthalmic
LiquidOphthalmic5 mg/mL
OintmentOphthalmic; Topical
PasteOral; Topical
Solution / dropsOphthalmic0.25 % w/v
GelOphthalmic10 mg/1mL
Solution / dropsOphthalmic1 %
SolutionOphthalmic0.5 %
SolutionOphthalmic1 %
EmulsionOphthalmic
Solution / dropsOphthalmic0.5 %
Solution / dropsOphthalmic5 mg/1mL
Kit; solutionOphthalmic
AerosolOral
SprayOral
Solution / dropsOphthalmic0.5 %w/v
SolutionConjunctival; Ophthalmic5 mg
PatchTopical60 g/100g
SolutionOphthalmic0.25 % w/w
Solution / dropsOphthalmic0.5 g/100mL
PatchTopical36.87 mg/241
PatchTopical6.17 mg/101
PatchTopical12.58 mg/51
PatchTopical18.12 mg/91
Solution / dropsOphthalmic5.25 mg/1ml
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)300MSDS
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Xenobiotic transporter activity
Specific Function
Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including b...
Gene Name
SLC2A1
Uniprot ID
P11166
Uniprot Name
Solute carrier family 2, facilitated glucose transporter member 1
Molecular Weight
54083.325 Da
References
  1. Garrett Q, Simmons PA, Xu S, Vehige J, Zhao Z, Ehrmann K, Willcox M: Carboxymethylcellulose binds to human corneal epithelial cells and is a modulator of corneal epithelial wound healing. Invest Ophthalmol Vis Sci. 2007 Apr;48(4):1559-67. doi: 10.1167/iovs.06-0848. [Article]

Drug created on December 03, 2015 16:51 / Updated on June 22, 2021 09:25