11/17/2019 Artificial Tears: A Primer

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Artificial Tears: A Primer

Author: Tressa Larson, OD (../bio/authors/Larson-Tressa.htm)
Posted on: November 23, 2016

Disclaimer:  The author has no financial interest in any product presented in this tutorial. Information
presented here is for educational purposes only and does not constitute an endorsement of any of
these products by the author nor by EyeRounds or The University of Iowa.

Outline
Formalization of the Active Ingredients (Artificial-Tears.htm#Formalization)
FDA Monography (Artificial-Tears.htm#FDA)
Goals of Artificial Tear Treatment (Artificial-Tears.htm#Goals)
Demulcents (Artificial-Tears.htm#Demulcents)
Emollients (Artificial-Tears.htm#Emollients)
Inactive Ingredients (Artificial-Tears.htm#Inactive Ingredients)
Homeopathic drops (Artificial-Tears.htm#Homeopathic drops)
Preservatives (Artificial-Tears.htm#Preservatives)
Companies listed in this article (Artificial-Tears.htm#Companies)

Lubricants are the first-line treatment for many causes of ocular irritation, in particular for dry eye. There
are a multitude of artificial tear choices available. The goal of this tutorial is to provide information about
the components that make up artificial tears, to discuss the functions of these components, and to
explain which commercially available drops contain those components. The list is not exhaustive and you
may feel free to send Dr. Tressa Larson (../bio/authors/Larson-Tressa.htm) (tressa-larson@uiowa.edu
(mailto:tressa-larson@uiowa.edu)) information on additional drops.

Formalization of the Active Ingredients

The first important point when considering the large variety of artificial tears is that the Food and Drug
Administration (FDA) created a drug monograph in the late 1980's to provide artificial tears a fast track to
FDA approval [1]. The monograph states that an over-the-counter ophthalmic drug product in a form
suitable for topical administration is generally recognized safe, e ective and not misbranded if it contains

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the following ingredients and ingredient combinations.

This tutorial aims to familiarize the reader with the FDA approved active ingredients and then to discuss
"inactive" ingredients.

FDA Monograph
1. Ophthalmic Astringent: A locally acting pharmacologic agent which, by precipitating protein, helps
to clear mucous from the surface of the eye
1. Zinc sulfate 0.25%
2. Ophthalmic Demulcent: An agent, usually a water soluble polymer, which is applied topically to
the eye to protect and lubricate mucous membranes
1. Cellulose derivatives
1. Carboxymethcellulose sodium 0.2 to 2.5%
2. Hydroxyethyl cellulose 0.2 to 2.5%
3. Hydroxypropyl methylcellulose 0.2 to 2.5%
4. Methylcellulose 0.2 to 2.5%
2. Dextran 70: 0.1% when used with another polymeric demulcent agent in this section
3. Gelatin 0.01%
4. Polyols, liquid
1. Glycerin 0.2 to 1%
2. Polyethylene glycol 300: 0.2 to 1%
3. Polyethylene glycol 400: 0.2 to 1%
4. Polysorbate 80: 0.2 to 1%
5. Polyvinyl alcohol 0.1 to 4%
6. Povidone 0.1 to 2%
3. Ophthalmic emollients: An agent, usually a fat or oil which is applied locally to eyelids to protect
or so en tissues and to prevent drying and cracking.
1. Lanolin preparations
1. Anhydrous lanolin 1 to 10% in combination with one or more oleaginous emollient
agents included here
2. Lanolin 1 to 10% in combination with one or more oleaginous emollient agents
included here
2. Oleaginous ingredients
1. Light mineral oil up to 50% in combination with one or more other emollient agents
included here
2. Mineral oil up to 50% in combination with one or more other emollient agents
included here
3. Para in up to 5% in combination with one or more other emollient agents included
here
4. Petrolatum up to 100%
5. White ointment up to 100%
6. White petrolatum up to 100%
7. White wax up to 5% in combination with one or more other emollient agents
included here
8. Yellow wax up to 5% in combination with one or more other emollient agents
included here
4. Ophthalmic hypertonicity agent: Sodium chloride 2 to 5%
5. Ophthalmic vasoconstrictors
1. Ephedrine hydrochloride 0.123%
2. Naphazoline hydrochloride 0.01 to 0.03%
3. Phenylephrine hydrochloride 0.08 to 0.2%
4. Tetrahydrazoline hydrochloride 0.01 to 0.05%
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6. Eyewashes: contain water tonicity agents and agents for establishing pH

7. Permitted combinations
1. Any astringent + any vasoconstrictor
2. Any 2-3 demulcents
3. Any single demulcent + any single vasoconstrictor
4. Any astringent + any vasoconstrictor + any demulcent
5. Any 2+ emollients
8. Permitted Indications (Demulcents or emollients)
1. For temporary relief of burning and irritation due to dryness of the eye
2. For temporary relief of discomfort due to minor irritations of the eye
3. For use as a protectant against further ocular irritation
4. For use as a lubricant to prevent further ocular irritation

Goals of Artificial Tear Treatment

Although there are many patient related treatment goals, the most common purpose of artificial tears is
to decrease dryness. Humectants are compounds which promote hydration and feel good upon
application. Artificial tears are also lubricants meaning they decrease friction on the ocular surface caused
by the eyelid. Another treatment goal in ocular surface disease is to increase tear retention. Artificial tears
do this by increasing tear viscosity, increasing the adherence of the tears to the ocular surface, decreasing
tear evaporation, and decreasing tear clearance. Additionally, inflammation is known to play a role in
causing dry eyes and there are artificial tear components that decrease inflammation by disrupting the
processes which promotes the recruitment of cytokines [2]. Artificial tears may also reduce redness and
swelling and serve to protect the eye from hyperosmolarity. High osmolarity of the tear film causes water
to di use out of epithelial cells, further dehydrating the surface. Finally, artificial tears may serve to so en
and moisturize the ocular surface by forming an oily layer that traps existing moisture present in the
tissues.

Demulcents
A demulcent is a soothing, usually mucilaginous substance that is used to relieve pain in inflamed or
irritated mucous membranes.

Polyethylene glycol (PEG) is a demulcent that forms a protective layer over a mucous membrane to
relieve inflammation or irritation and to preserve the ocular surface microenvironment. Demulcents are
high molecular weight polymers that mimic mucins and act to lubricate, protect and provide viscosity to
eye drops. Examples of artificial tears containing PEG are Blink Tears (Abbott), Blink Gel Tears (Abbott),
Systane gel (Alcon), Systane preservative free (Alcon), and Soothe (B+L).

Propylene glycol also forms a protective layer over mucous membranes to relieve inflammation and/or
irritation. It also increases the viscosity of the eye drop. In addition to its demulcent properties, propylene
glycol is a humectant because it holds up to three times its own weight in water. Examples of artificial
tears containing propylene glycol are B+L Advanced Eye Relief, Systane Balance, and Systane gel drops
(Alcon).

Glycerin is a demulcent and lubricant as well as a humectant. Glycerin has the added properties of
promoting epithelial cell growth and blunting the damaging e ects of high osmolarity on the ocular
surface. Povidone is a lipid that integrates with the existing oil layer of the tear film, thickening it to reduce
evaporation. Dextran is a low molecular weight hydrophilic polymer that increases the mechanical
strength of the tear film. Its low viscosity means that it is not useful in an artificial tear without a
thickening agent. Examples of artificial tears containing Glycerin are Refresh Optive and Refresh Optive
Advanced (Allergan), Oasis Tears (Oasis Medical Inc), Clear Eyes Pure Relief (Prestige Brands Inc.), and Tears
Naturale Forte (Alcon).

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There are a number of compounds that are cellulose derivatives that are approved for use in artificial
tears. Carboxymethylcellulose (CMC) is the most commonly used polymeric viscosity agent in the United
States. CMC binds to and is retained by corneal epithelial cells. It increases the viscosity and clearance
times of an eye drop and is also widely used in foods, pharmaceuticals and non-food products such as
tooth paste and detergents. Examples of artificial tears containing CMC are Thera Tears family (Advanced
Vision Research), Refresh Tears and Refresh Plus tears (Allergan).

Hydroxymethylcellulose (HMC), hydroxypropylcellulose (HPC), and hydroxypropylmethylcellulose

(HPMC, aka. hypromellose) are all hydrophilic polymers that coat and protect the eye. They are hydrogels
that crosslink upon contact with the ocular surface to increase tear clearance times. They must be mixed
with other compounds because they are too viscous to instill alone onto the ocular surface. HMC is
restores the protective e ect of the mucous layer of the tears. Examples of artificial tears containing HMC
and its related compounds are Tears Naturale II, Genteal Gel, and Genteal Liquid Gel Drops (Alcon) and in
Clear Eyes Pure Relief (Prestige Brands Inc). Lacrisert is a solid piece of HPMC that is inserted into the
fornix and le to dissolve slowly onto the surface of the eye.

Polyvinyl alcohol (PVA) is a demulcent that lowers the viscosity of a solution. Not found in any of the
most up to date artificial tear brands due to the availability of more e icacious compounds, PVA is found
in many older artificial tear preparations such as Refresh Classic (Allergan), Hypotears (Alcon), Fresh Kote
(Focus Laboratories), and Visine Tears for Dry Eye and Visine for Contacts (Johnson + Johnson). PVA is also
incorporated into Alcon's Dailies Aqua Comfort Plus contact lenses. The company claims that this daily
disposable lens releases PVA for about twenty hours of wear to increase comfort. This in turn is thought
to increase compliance with daily use since the lens becomes less comfortable once the PVA has di used
out of the lens.

Demulcents Conc. Range Function

Carboxymethylcellulose sodium 0.2 to 2.5% Increase Viscosity (thickener)

Stabilize emulsions

Dextran 70 0.1% when used with Increase mechanical strength of tear film.
another Demulcent Requires thickener due to low viscosity of
compound

Gelatin 0.01% seldom included

gelling agent

Glycerin 0.2 to 1% Blunts the damaging e ects of high

osmolarity on the ocular surface.
Lubricant, humectant
Promote epithelial cell growth

Hydroxyethyl cellulose 0.2 to 2.5% Cross links upon contact with tear film due
Hydroxypropyl-methylcellulose 0.2 to 2.5% to pH di erence to increase viscosity.
Methylcellulose 0.2 to 2.5% Too viscous to instill easily alone

Polyethylene glycol 300 0.2 to 1% Increases viscosity

 Polyethylene glycol 400 0.2 to 1% Forms protective layer over mucous
membrane to relieve irritation

Polysorbate 80 0.2 to 1% Stabilizes oil emulsions

Polyvinyl alcohol 0.1 to 4% Lowers tear viscosity

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Povidone 0.1 to 2% Lubricating and soothing

Lipid that integrates with existing oil layer,
thickening it and reducing evaporation

Propylene glycol 0.2 to 1% Forms a protective layer over mucous

membranes relieving inflammation.
Increases viscosity
Holds up to 3x own weight in water

Emollients
Emollients are oily or fat based agents which are used to so en and protect tissues to prevent cracking or
drying. Emollients are non-moisturizing, but they do function to seal in existing moisture. Mineral oils
thicken or replace the lipid layer of the tear film to increase tear stability and tear break up time. White
petrolatum and the lanolin preparations are lubricants. The majority of products containing mineral oil
and white petrolatum contain only those two components in varying proportions. Examples of artificial
tears containing these products include Systane Balance, Genteal PM, Hypotears Ointment, Systane
Nighttime (Alcon), Soothe XP and Soothe PM (B+L), Retaine MGD and Retaine PM Nighttime Ointment
(Ocuso ), and Refresh PM and Refresh Lacilube (Allergan)

Emollients Conc. Range Function

Anhydrous lanolin 1-10% in combo with one+ listed Lubrication and soothing
Lanolin oleaginous emollient Contributes to oil layer

Light mineral oil up to 50% in combo with one+ Replace or thicken lipid layer to
Mineral oil listed emollient increase tear stability and TBUT.
 Non-moisturizing, but does seal
in existing moisture.

Para in up to 5% in combo with one or Waxy consistency

more emollient Seal in moisture

Petrolatum up to 100% Lubricant

White Ointment Contributes to oil layer
White Petrolatum

 White Wax up to 5% in combo with one+ Contributes to oil layer

 Yellow Wax listed emollient

Inactive Ingredients
Sorbitol lowers the viscosity of gelling agents such as HP Guar (see below) and HPMC (see above) which
are too viscous to instill directly on to the eye. Once instilled on the eye, sorbitol dissipates quickly which
allows the solution to be more viscous than it is in the bottle. Sorbitol was the main addition to the
solution Systane to produce Systane Ultra.

Hyaluronic Acid is a humectant that binds multiples of its weight in water to lower tear osmolarity. It also
adheres to the ocular surface to stabilize the thickness of the tear film. This naturally highly viscous
solution is thinned out by the blink action of the eyelids. It also improves cell-cell adhesions. While not

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currently found in any of the US artificial tear preparations, it is found in all of the Hylo-care products
from Ursa Pharmaceuticals and is available in Europe.

Sodium hyaluronate is a derivative of hyaluronic acid and shares many of its beneficial properties.
Sodium hyaluronate is a humectant, lubricant, and hypo-osmotic. It is found naturally in the eye where it
is produced as a response to ocular surface damage. This hydrophilic polymer plays an important role in
corneal wound healing as it promotes corneal epithelial repair and helps control localized inflammation.
Sodium hyaluronate is also a lubricant with flow and deformation characteristics similar to those of the
tear aqueous layer. Additionally, it reduces mucous strands in tears and is better at lowering tear
osmolarity than glycerin. Examples of artificial tears containing sodium hyaluronate are Blink Tears, Blink
Gel Tears, and Blink Tears Preservative free from Abbott and in Oasis Tears (Oasis Medical Inc).

L-carnitine and Erythritol are always seen in combination as osmoprotectants. Osmoprotectants blunt
the damaging e ects of high osmolarity on the ocular surface by preventing the activation of the stress
cascade. L-carnitine and erythritol are absorbed by dehydrated cells where they promote hydration and
prevent cell shrinkage and inflammation. Examples of artificial tears containing these compounds are
Optive products from Allergan, Refresh Optive and Refresh Optive Advanced (added emollient).

Hydroxypropyl Guar (HP Guar) is a bean protein that is used as a thickening agent in both foods and
pharmaceuticals. As a component in an artificial tear, it readily stabilizes the tear film by increasing
viscosity. HP Guar mimics the mucin layer of the tears by binding to the cornea and strengthening the
attachment of the aqueous layer to the glycocalyx-mucin interface. This attachment thickens the
aqueous layer. HP Guar partially achieves this because it is pH sensitive, cross-linking and gelling when
the pH is above 7. HP Guar also potentiates the active ingredients by prolonging their e icacy. Examples
of artificial tears containing HP Guar are the entire Systane family of artificial tears from Alcon including
Systane, Systane Ultra, Systane Balance, Systane gel, Systane Preservative Free, and Systane Nighttime.

Polyacrylic Acid has a longstanding reputation for being more e icacious to dry eye patients than PVA. It
increases the viscosity and retention time of the artificial tear. Examples of artificial tears containing
Polyacrylic Acid are Genteal gel and Genteal Liquid Gel Drops (Alcon) and in Viscotears (Novartis UK).

Tyloxapol is a surfactant, detergent, and mucolytic agent used to thin sputum in inhalation aerosols. As
an artificial tear component, it helps to remove lipid and mucous from the surface of contact lenses. An
example of an artificial tear containing Tyloxapol is Soothe Long Lasting (B+L). It is also in the contact lens
rewetting drop Blink-n-Clean (Abbott).

Tromethamine, which is also found in the rewetting drop Blink-n-Clean, is an organic amine proton
acceptor. It is most frequently used as an emulsifying agent for cosmetics, but it is also an alkalizer and
biological bu er.

Inactive Ingredients Function

Sorbitol Lowers the viscosity of gelling agents Dissipates quickly, optimizing

viscosity.

Hyaluronic acid Binds multiples of its weight in water Lowers tear osmolarity
Adheres to ocular surface
Stabilizes and evens out the tear film
Highly viscous until blink thins it out
Improves cell-cell adhesion

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Sodium Hyaluronate Protects and promotes healing of corneal epithelium

Changes viscosity upon blinking- more viscous while the eye is open
Improves tear film break-up time and helps spreading
Helps control localized inflammation
Reduces mucous strands
Lowers tear osmolarity
Retains water, increasing surface wettability.

L-carnitine Blunts the damaging e ects of high osmolarity by preventing stress

Erythritol activation.
Absorbed by dehydrated cells to promote hydration
Prevent cell shrinkage and inflammation

Hydroxypropyl Guar Increasing viscosity

Mimics the mucin layer of the eye
Binds to cornea and aqueous layer       Prolongs the e icacy of active
ingredients
Actively cross links/gels at pH above pH 7

Polyacrylic acid  Increases viscosity/retention time of tears

Tyloxapol Surfactant and mucolytic agent

Tromethamine Organic amine proton acceptor. Emulsifying agent (thins waxy agents)

Boric acid Bu er systems used to obtain a pH for the artificial tear that is healthy
Borate Bu er and comfortable for the eye.
Sodium-citrate pH ~8.5 is most comfortable for dry eye patients (normal tear pH is about
Phosphate 7.5)
Phosphate-acetate
Phosphate-citrate
Phosphate-citrate-
bicarbonate
Sodium hydroxide

Calcium chloride Electrolytes are added to maintain or lower tear osmolarity as high
Magnesium chloride osmolarity products pull water from epithelial cells, interfering with
Potassium chloride metabolism.
Zinc chloride Some of the added electrolytes are also important for corneal epithelial
Sodium chloride metabolism.
Sodium citrate Some electrolytes are part of bu er systems.
Sodium lactate
Sodium bicarbonate

Preservatives
Preservatives are the component of artificial tears that may cause harm to the eye. Preservatives are
important in eye drops because they prevent bacterial growth and subsequent infection.
There are three main types of preservatives: detergent type, oxidative type, and ionic bu ering systems.
Detergent-type preservatives cause bacterial cell death by interrupting the lipids in their cell membranes
which causes the cells to break apart. These preservatives have a very broad spectrum of action making
them fairly toxic to human cells [4]. Oxidative-type preservatives penetrate bacterial cell membranes to
damage DNA, proteins, and lipids. Oxidative preservatives are less toxic to human cells than detergent

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preservatives. They are also e ective against bacteria at very low concentrations which helps to minimize
damage [5]. Ionic bu ering systems are similar to oxidative preservatives, but have both antibacterial and
antifungal properties [6]. SofZia, found in Travatan Z (Alcon), is the only ophthalmic preparation which
uses an ionic bu ering system type preservative.

Benzalkonium chloride (BAK) is the preservative currently in use in topical ocular preparations that is
most likely to cause irritation, inflammation, and serious side e ects. [4, 7, 8] This detergent-type
preservative is a quaternary ammonium cationic surfactant that has a very long shelf life and is very
e ective against a broad spectrum of organisms. Additionally, it increases drug penetration.
Unfortunately, BAK disrupts the tight junctions between human cells and accelerates desquamation of
the epithelium. BAK promotes apoptosis at low concentrations and necrosis at higher concentrations [8].
It stimulates the production of inflammatory cytokines and causes reversible and non-reversible
neurotoxicity which reduces cell density.[9, 10] BAK also decreases aqueous production. Many studies
have shown that BAK is more toxic to the ocular surface than other preservatives such as Polyquad,
SofZia, Purite, Gen Aqua, etc. [7, 11] BAK is found in more than 70% of all ophthalmic medications, but its
use is much less frequent in artificial tears due to its surface toxicity. Examples of artificial tears that
contain BAK are the Visine family of drops (Johnson and Johnson), the Clear Eyes family of drops
(Prestige Brands Inc.), Rohto (Metholatum Company), Hypotears (Alcon), and Soothe Long Lasting (B+L).
Polyquad (Polyquaternium-1) is a detergent-type preservative derived from BAK. It is unique because
bacterial cells attract Polyquad while human corneal epithelial cells tend to repel it. Despite causing
some superficial epithelial damage, reducing goblet cell density, and decreasing aqueous production it
results in less corneal epithelial staining and is better tolerated than Polyhexamethylene Biguanide
(PHMB) or BAK [12]. Polyquad is very e ective in contact lens solutions because the contact lens serves as
a reservoir to slowly release the compound without it becoming excessively concentrated in the lens.
Examples of artificial tears that contain Polyquad are most of the Alcon products, Tears Naturale II and
Tears Naturale Forte as well as the entire Systane family of preserved drops. Polexitonium
(Polyquaternium-42), the preservative found in Freshkote (Focus Laboratories), is closely related to
Polyquad.

Sodium Perborate, known by the brand names GenAqua (Genteal family, Alcon) and Dequest (Thera
Tears, Advanced Vision Research), is an oxidative-type preservative that releases hydrogen peroxide in a
reversible reaction. Sodium perborate is broadly toxic to many pathogens by altering bacterial protein
synthesis, oxidizing cell membranes, and altering membrane bound enzymes [12]. When exposed to the
aqueous environment of the ocular surface, the reversible bacteriotoxic bu ering reaction allows the
sodium perborate to break down into hydrogen peroxide, oxygen, and water. Hydrogen peroxide is a very
e icient antimicrobial, but in even small amounts, such as 30 parts per million (0.003%), is known to be
harmful to the eye [12].

Stabilized Oxychloro Complex (Purite) is another oxidative-type preservative. When exposed to light,
Purite degrades to water, oxygen, sodium, and chlorine free radicals. Purite has antibacterial, antifungal,
and antiviral e ects. It is e ective at unusually low concentrations (0.005%). Chlorine free radicals inhibit
microorganism protein synthesis within cells by oxidation of glutathione which causes cell death [10].
Examples of artificial tears that contain Purite are Refresh Tears, Refresh Optive, and Refresh Optive
Advanced (Allergan).
Ocupure is a preservative closely related to Purite that is a stabilized oxychloro complex with sodium
chlorite. Upon exposure to light, this preservative breaks down into sodium and chloride ions, oxygen,
and water [13]. Mammalian cells have oxidases, catalases, and antioxidants that readily neutralize the
small amount of stabilized oxychloro complex generally utilized as a preservative. Examples of artificial
tears that contain Ocupure are Blink (Abbott) family of tears.

Polyhexamethylene Biguanide (PHMB) is the most commonly used preservative in contact lens solutions
and historically has been a component of pool cleaners, skin disinfectants, and urinary catheter flush
solutions. PHMB integrates into bacterial cell walls, disrupting the membrane and lethally altering DNA

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transcription in both bacteria and Acanthemoeba. PHMB is non-irritating to human corneal cells and also
has limited antifungal activity [10]. PHMB is found in the artificial tear Soothe XP (B+L).

Chlorobutanol, a combination of acetone and chloroform, is a detergent-type preservative which is both

less toxic and less e ective than BAK [14]. It has broad anti-microbial activity. Its usefulness is limited by
the need to be stored at lower temperatures than most drops. Chlorobutanol it is only found in Refresh
Lacrilube (Allergan).

Edetate Disodium (EDTA) is a chelating agent that is used in a wide variety of products including hair
conditioner, facial cleansers, a ershaves, deodorants, and ophthalmic drops. When added to topical
medications, EDTA inactivates heavy metals, which prevents bacteria from using them to reproduce. EDTA
is also used to remove corneal deposits in band keratopathy. Examples of artificial tears that contain
EDTA are Soothe XP (B+L), Systane Ultra, Systane Balance (Alcon), and the Oasis Tears family (Oasis Medical
Inc.)

Some of the information above is in table form in an article written by Christiansen and Larson for Review
of Cornea & Contact Lens available from
http://www.reviewofcontactlenses.com/content/d/featured_articles/i/3554/c/59277/
(http://www.reviewofcontactlenses.com/content/d/featured_articles/i/3554/c/59277/) [15]

Preservative Conc. Range Additional E ects (+/-)

Benzalkonium chloride (BAK) 0.004 – 0.02% Increases drug penetration

Long shelf life
Disrupts tight junctions
Accelerate epithelial desquamation.
Promotes apoptosis at lower conc. and
necrosis at higher conc.
Stimulates production of inflammatory
cytokines.
Reduces aqueous production.
Causes reversible and non-reversible
neurotoxicity, reducing nerve fiber
density.

Polyquaternium-1 (Polyquad ®) 0.001% Bacterial cells attract Polyquad, but

human corneal epithelial cells tend to
repel it.
Causes superficial epithelial damage.
Reduces the density of conjunctival
goblet cells which decreases aqueous
tear film production.

Sodium Perborate (Dequest ®, and   Vanishing preservative: Upon exposure to

GenAqua ®) an aqueous environment, it is catalyzed
into hydrogen peroxide, water and
oxygen.
Alters protein synthesis within bacterial
cells by oxidizing cell membranes and
altering membrane-bound enzymes,
causing enzymatic inhibition.

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Stabilized oxychloro complex (Purite 0.005%  Degrades to water, oxygen, sodium and
®) chlorine free radicals when exposed to
light.
 Chlorine free radicals are thought to
inhibit microorganism protein synthesis
within cells by way of glutathione
oxidation, which causes microbe cell
death.
 Broad antimicrobial activity- includes
antibacterial, antifungal and antiviral
e ects.

Sodium Chlorite (Ocupure ®) 0.005% A mixture of 80% chlorite, 11% sodium

chloride, water and trace electrolytes, it
breaks down into sodium and chloride
ions, oxygen and water when exposed to
light.

Polyhexamethylene biguanide 0.02% Has activity against bacteria and

(PHMB) Acathemoeba, however, its antifungal
activity is limited. Lethally alters the
transcription of bacterial DNA.
Nonirritating to human corneal cells.
Integrates into bacterial cell walls,
disrupting the membrane.

Chlorobutanol   Alcohol that increases lipid solubility and

is able to cross the bacterial lipid layer.
Has extensive anti-bacterial action,
causing cell lysis by disruption of
microbial cell membrane lipid
configuration.
Causes significant keratitis and irritation
to the ocular surface, but less than BAK.

EDTA (Edetate disodium or 1% Chelating agent that binds metals which

EthyleneDiameneTetraacetic Acid) inactivates them.
Enhances the activity of quaternary
ammonium bases and sorbate.

Companies listed in this article

Advanced Vision Research, Lake Forest, IL, part of Akorn Inc.
Alcon Laboratories Inc., Fort Worth, TX, a subsidiary of Novartis
Allergan Inc., Irvine, CA
Abbott (formerly Abbott Medical Optics formerly Advanced Medical Optics (AMO)), Abbott Park, IL.
Bausch + Lomb (B+L) , Bridgewater, NJ, a subsidiary of Valeant Pharmaceuticals International Inc.
Focus Laboratories, North Little Rock, AR
Johnson and Johnson Consumer Companies, Skillman, NJ
Metholatum Company Orchard Park, NY, owned by Rohto Pharmaceutical Co.,

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Oasis Medical Inc., Glendora, CA

Ocuso Inc., Rosenberg, TX
Prestige Brands Inc., Tarrytown, NY
Similasan Inc., Highlands Ranch, CO
Ursa Pharmaceuticals, Saarbrücken, Germany

References
1. Food and Drug Administration: "Ophthalmic Drug Products for Over-the-counter Human use; Final
Monograph" 21 CFR Parts 349 and 369. Federal Register 1988, 53(43):7076-7093 Available from
http://www.fda.gov/downloads/Drugs/DevelopmentApprovalProcess/DevelopmentResources/Over-the-
CounterOTCDrugs/StatusofOTCRulemakings/ucm094081.pdf
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Larson T. Artificial Tears: A Primer. EyeRounds.org. November 23, 2016; Available from
http://EyeRounds.org/tutorials/artificial-tears.htm

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