lodoxamide ophthalmic

Action and Spectrum

Actions and Spectrum: 

Actions 

lodoxamide exerts its primary action by stabilizing mast cells in the conjunctiva. Mast cells release histamine and other inflammatory mediators in response to an allergic trigger. By stabilizing mast cells, lodoxamide prevents the release of these inflammatory substances, thereby reducing the allergic response.  

lodoxamide provides relief from itching (pruritus) associated with allergic conjunctivitis. By reducing the release of histamine and other itch-inducing substances, lodoxamide helps alleviate the discomfort and itching sensation in the eyes.  

Spectrum 

lodoxamide ophthalmic is primarily effective in treating allergic conjunctivitis, including seasonal allergic conjunctivitis (hay fever conjunctivitis) and perennial allergic conjunctivitis (year-round allergies). It is specifically designed to target the allergic inflammation of the conjunctiva, which is triggered by environmental allergens such as pollen, dust mites, animal dander, and certain irritants. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10%  

Transient local burning and discomfort (15%) 

1-10%  

Headache (1.5%) 

Blurred vision (1-5%) 

Tearing/discharge (1-5%) 

Hyperemia (1-5%) 

Dry eye (1-5%) 

Foreign body sensation (1-5%) 

Ocular itching/pruritus (1-5%) 

Crystalline deposits (1-5%) 

<1% 

Heat sensation 

Dizziness 

Dry nose 

Nausea 

Stomach discomfort 

Somnolence 

Sneezing 

Rash 

Corneal erosion/ulcer 

Ocular edema/swelling 

Ocular warming sensation 

Ocular fatigue 

Scales on lid/lash 

Eye pain 

Chemosis 

Corneal abrasion 

Keratopathy/keratitis 

Sticky sensation 

Epitheliopathy 

Blepharitis 

Allergy 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

• Hypersensitivity 
• Contact lenses 
• Children 
• Pre-existing conditions 
• Pregnancy 
• Breastfeeding 
• Ocular Herpes Simplex 
• Cataracts 
• Increased Intraocular Pressure 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy category: C 

Breastfeeding warnings:  

Unknown if topical administration of corticosteroids can lead to sufficient systemic absorption. 

Pregnancy category: 

Category A: well-controlled and satisfactory studies show no risk to the fetus in the first or later trimester. 

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: No data is available for the drug under this category. 

Pharmacology

Pharmacology:  

lodoxamide ophthalmic is a medication used as eye drops for allergic conjunctivitis, which is an inflammation of the conjunctiva (the clear tissue covering the white part of the eye and lining the inner surface of the eyelids) due to allergies.  

Pharmacodynamics: 

The pharmacodynamics of lodoxamide ophthalmic refers to how the medication affects the body and the underlying mechanisms of action. lodoxamide is a mast cell stabilizer, and its primary pharmacodynamic effects are seen locally in the eye. 

lodoxamide works by inhibiting the release of inflammatory substances, such as histamine, from mast cells.  

Pharmacokinetics: 

Absorption 

lodoxamide ophthalmic is applied topically as eye drops directly onto the eye’s surface. The medication is absorbed into the conjunctiva lining the inner surface of the eyelids. Distribution 

After absorption, lodoxamide is distributed within the tissues of the eye. Its distribution is primarily localized to the conjunctiva, where it exerts its pharmacological effects. There needs to be more information available on the extent of distribution beyond the eye. 

Metabolism 

lodoxamide ophthalmic undergoes minimal metabolism in the body. It is primarily eliminated in its unchanged form. The metabolism of lodoxamide is not considered a significant pathway in its elimination. 

Elimination and Excretion 

The elimination of lodoxamide occurs mainly through the tear drainage system. Tears carry the medication out of the eye, eventually reaching the nasal cavity and throat. From there, it is swallowed and eliminated from the body through the gastrointestinal tract. 

Adminstartion

Administration: 

The medication is typically available as eye drops for ocular conditions, such as vernal conjunctivitis, keratoconjunctivitis, keratitis, or eye infections. Instil the eyedrops in your lower eyelid to create a small pocket and instil the prescribed number of drops into the eye.

Close your eyes gently and press your finger against the corner of your eye near the nose for about 1-2 minutes to prevent the medication from draining into the tear duct. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: lodoxamide ophthalmic 

Pronounced as: loe-DOX-a-mide-off-THAL-mik 

Why do we use lodoxamide ophthalmic? 

lodoxamide ophthalmic is used to treat allergic conjunctivitis, an inflammation of the conjunctiva that lines the inner surface of the eyelids) caused by allergies. Allergic conjunctivitis can be triggered by allergens such as pollen, dust mites, pet dander, or certain chemicals.