Lumify: The Dangers of Lumify and Its Benefits. The Dangers of Benzalkonium chloride (BAK); Can You Use Lumify in Kids?


In 2017, The FDA approved brimonidine tartrate ophthalmic solution 0.025% (Lumify, Bausch + Lomb, Bridgewater, New Jersey) as an over-the-counter eye drop for ocular redness. 




The agent uses a lower dose of brimonidine tartrate. Brimonidine was first approved by the FDA in 1996 for reducing IOP in glaucoma patients. 

Unlike popular OTC eye drops like Visine and Clear Eyes that claim to “get the red out”, Lumify does not result in a “Rebound Redness” effect well known to occur with the chronic use of Visine and Clear Eyes.

Visine and similar drugs work by constricting blood vessels in the eye via the eye’s alpha-1 receptor. Lumify also constricts blood vessels, but it acts on a different receptor called the alpha-2 receptor which avoids the rebound redness effect.

Lumify has a much lower concentration of a long-standing, FDA-approved, prescription glaucoma medication called Alphagan which decreases eye pressure by constricting blood vessels. Lumify is four to eight times the strength of Lumify so it is considered relatively safe by the FDA as an OTC drop.

The issue with Lumify (as well as all preservative containing drops) is its preservative. It is unclear why they chose Benzalkonium Chloride (BAK), but this preservative is particularly irritating for many patients.


The Dangers of Benzalkonium chloride (BAK)

Benzalkonium chloride (BAK), a common preservative that has been used in ophthalmology since the 1940s and found in up to 70% of eye drops, is a quaternary ammonium compound which acts like a detergent, lysing cell membranes, and killing microorganisms. 

Preservatives are used in eye medications because they help make the drops more cost-effective: a large bottle of eye drops can last a month or more when a preservative is added compared with preservative free (PF) counterparts–which come in small, slighly frustrating, vials where you cannot put the top back on.

Many animal and human studies have shown that BAK is toxic to the ocular surface cells, particularly the cornea and conjunctiva (REF 1-6). Studies show BAK stimulated an apoptotic response to corneal cells and may even damage Meibomian Gland Cells. Some studies have also shown that at a molecular level, dose-dependent DNA damage is associated with BAK.


Preservative-Free Lumify would be lovely but that is NOT available yet. 


A patient asked, “if a patient is allergic to Lumify, can they use diluted Alphagan?”


Answer: theoretically diluted Alphagan could be used as the preservative is Purite which is less toxic according to some studies compared to BAK (but Purite is still a preservative); however there is a risk of contamination in diluting the Alphagan which could lead to a corneal infection




Six studies involving a total of approximately 600 participants reported a low risk for rebound redness with Lumify. The longest of these studies lasted about seven weeks; the effects of the drops, when used four times a day in the studies, lasted about eight hours.

Can You Use Lumify in Kids?
Lumify’s label says it is safe for patients over the age of 5, however, the FDA trials only included adults. I would avoid using Lumify in kids: it is imperative to find out why the child’s eye is red as it can be due to meibomian gland loss which can lead to significant issues in the future if left untreated.
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Reference 
1. Horsley MB, Kahook MY. Effects of prostaglandin analog therapy on the ocular surface of glaucoma patients. Clin Ophthalmol. 2009;3:291-295. Find Full Text [Context Link]

2. Kastelan S, Tomic M, Metez Soldo K, et al. How ocular surface disease impacts the glaucoma treatment outcome. Biomed Res Int. 2013;2013:696328. 
3. Baudouin C, Riancho L, Warnet JM, et al. In vitro studies of antiglaucomatous prostaglandin analogues: travoprost with and without benzalkonium chloride and preserved latanoprost. Investig Ophthalmol Vis Sci. 2007;48:4123-4128. Find Full Text Bibliographic Links [Context Link]

4. Bhagat P, Sodimalla K, Paul C, et al. Efficacy and safety of benzalkonium chloride-free fixed-dose combination of latanoprost and timolol in patients with open-angle glaucoma or ocular hypertension. Clin Ophthalmol. 2014;8:1241-1252. Find Full Text [Context Link]

5. European Medicines Agency. EMEA public statement on antimicrobial preservatives in ophthalmic preparations for human use. Doc. Ref.: EMEA/622721/2009. Available at:http://www.ema.europa.eu/docs/en_GB/document_library/Public_statement/2009/12/WC500017608.pdf
6.Steven DW, Alaghband P, Lim KS. Br J Ophthalmol Epub ahead of print: 2018 May 12. doi:10.1136/ bjophthalmol-2017-311544

7.
 2018 May;170:188-197. doi: 10.1016/j.exer.2018.02.020. Epub 2018 Feb 24.

Toxicity of cosmetic preservatives on human ocular surface and adnexal cells.

Chen X1, Sullivan DA2, Sullivan AG3, Kam WR2, Liu Y4.

Abstract

Cosmetic products, such as mascara, eye shadow, eyeliner and eye makeup remover are used extensively to highlight the eyes or clean the eyelids, and typically contain preservatives to prevent microbial growth. These preservatives include benzalkonium chloride (BAK) and formaldehyde (FA)-releasing preservatives. We hypothesize that these preservatives, at concentrations (BAK = 1 mg/ml; FA = 0.74 mg/ml) approved for consumer use, are toxic to human ocular surface and adnexal cells. Accordingly, we tested the influence of BAK and FA on the morphology, survival, and proliferation and signaling ability of immortalized human meibomian gland (iHMGECs), corneal (iHCECs) and conjunctival (iHConjECs) epithelial cells. iHMGECs, iHCECs and iHConjECs were cultured with different concentrations of BAK (5 μg/ml to 0.005 μg/ml) or FA (1 mg/ml to 1 μg/ml) under basal, proliferating or differentiating conditions up to 7 days. We used low BAK levels, because we found that 0.5 mg/ml and 50 μg/ml BAK killed iHMGECs within 1 day after a 15 min exposure. Experimental procedures included analyses of cell appearance, cell number, and neutral lipid content (LipidTox), lysosome accumulation (LysoTracker) and AKT signaling in all 3 cell types. Our results demonstrate that BAK and FA cause dose-dependent changes in the morphology, survival, proliferation and AKT signaling of iHMGECs, iHCECs and iHConjECs. Many of the concentrations tested induced cell atrophy, poor adherence, decreased proliferation and death, after 5 days of exposure. Cellular signaling, as indicated by AKT phosphorylation after 15 (FA) or 30 (BAK) minutes of treatment, was also reduced in a dose-dependent fashion in all 3 cell types, irrespective of whether cells had been cultured under proliferating or differentiating conditions. Our results support our hypothesis and demonstrate that the cosmetic preservatives, BAK and FA, exert many toxic effects on cells of the ocular surface and adnexa.

Experimental Eye Research

Volume 170, May 2018, Pages 188-197
Experimental Eye Research

Toxicity of cosmetic preservatives on human ocular surface and adnexal cells

Highlights

•
We hypothesize that BAK and FA at concentrations approved for consumer use, are toxic to human ocular cells.
•
We measured the impact of BAK and FA on the morphology, survival, and proliferation and signaling of human ocular cell lines.
•
Our results demonstrate that the cosmetic preservatives, BAK and FA, exert many toxic effects on human ocular cells.

Abstract

Cosmetic products, such as mascara, eye shadow, eyeliner and eye makeup remover are used extensively to highlight the eyes or clean the eyelids, and typically contain preservatives to prevent microbial growth. These preservatives include benzalkonium chloride (BAK) and formaldehyde (FA)-releasing preservatives. We hypothesize that these preservatives, at concentrations (BAK = 1 mg/ml; FA = 0.74 mg/ml) approved for consumer use, are toxic to human ocular surface and adnexal cells. Accordingly, we tested the influence of BAK and FA on the morphology, survival, and proliferation and signaling ability of immortalized human meibomian gland (iHMGECs), corneal (iHCECs) and conjunctival (iHConjECs) epithelial cells. iHMGECs, iHCECs and iHConjECs were cultured with different concentrations of BAK (5 μg/ml to 0.005 μg/ml) or FA (1 mg/ml to 1 μg/ml) under basal, proliferating or differentiating conditions up to 7 days. We used low BAK levels, because we found that 0.5 mg/ml and 50 μg/ml BAK killed iHMGECs within 1 day after a 15 min exposure. Experimental procedures included analyses of cell appearance, cell number, and neutral lipid content (LipidTox), lysosome accumulation (LysoTracker) and AKT signaling in all 3 cell types. Our results demonstrate that BAK and FA cause dose-dependent changes in the morphology, survival, proliferation and AKT signaling of iHMGECs, iHCECs and iHConjECs. Many of the concentrations tested induced cell atrophy, poor adherence, decreased proliferation and death, after 5 days of exposure. Cellular signaling, as indicated by AKT phosphorylation after 15 (FA) or 30 (BAK) minutes of treatment, was also reduced in a dose-dependent fashion in all 3 cell types, irrespective of whether cells had been cultured under proliferating or differentiating conditions. Our results support our hypothesis and demonstrate that the cosmetic preservatives, BAK and FA, exert many toxic effects on cells of the ocular surface and adnexa.
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