What is Diquafosol Eye Drops Used For?

October 7, 2025 •

4 min read

Originally approved in Japan in 2010, Diquafosol is a unique treatment for Dry Eye Disease that works by stimulating the natural secretion of tear components directly on the ocular surface. This provides a different approach compared to traditional artificial tears and has demonstrated effectiveness in improving both the signs and symptoms of dry eye. Understanding what is Diquafosol eye drops used for is crucial for patients exploring advanced treatment options.

Quick Summary

Diquafosol eye drops are primarily used to treat dry eye disease by acting as a P2Y2 receptor agonist. It works by stimulating the secretion of fluid and mucin from the ocular surface to stabilize the tear film. This helps alleviate symptoms and repair damage for patients with various forms of dry eye, including those with meibomian gland dysfunction and post-surgical dry eye.

Key Points

Stimulates Natural Tear Production: Diquafosol is a P2Y2 purinergic receptor agonist that promotes the natural secretion of aqueous fluid and mucin from the ocular surface, stabilizing the tear film.
Treats Both Aqueous and Evaporative Dry Eye: By increasing the fluid and mucin components and also stimulating lipid secretion from meibomian glands, Diquafosol effectively addresses multiple forms of dry eye disease.
Improves Ocular Surface Health: Clinical studies have shown that Diquafosol significantly reduces corneal and conjunctival staining, indicating a repair of the ocular surface damage often associated with dry eye.
Effective for Post-Surgical Recovery: It is particularly useful for managing and mitigating dry eye symptoms following procedures such as LASIK and cataract surgery.
Generally Well-Tolerated: The most common adverse effects, such as eye irritation and discharge, are typically mild and often decrease with continued use, and no serious drug-related adverse events have been reported.
Offers Longer-Term Benefits: Unlike simple artificial tears which offer only temporary relief, Diquafosol provides more sustained improvements in both subjective symptoms and objective signs over longer treatment periods.

Understanding Diquafosol's Mechanism of Action

At its core, Diquafosol is a dinucleotide polyphosphate that functions as a P2Y2 purinergic receptor agonist. These P2Y2 receptors are widely present on the cells of the ocular surface, including the corneal and conjunctival epithelium, goblet cells, and meibomian glands. When Diquafosol is administered, it binds to these receptors and triggers a cascade of cellular responses that promote the secretion of essential tear film components.

Unlike simple artificial tears, which merely supplement the tear film from the outside, Diquafosol actively works from within to increase the eye's natural production of tears and mucin. This twofold action is critical for restoring a stable and functional tear film, addressing both aqueous-deficient and evaporative types of dry eye.

The Tear Film and How Diquafosol Helps

The tear film is composed of three main layers: a lipid layer, an aqueous layer, and a mucin layer. A deficiency in any of these layers can lead to the symptoms of dry eye. Diquafosol works by stimulating P2Y2 receptors on conjunctival cells, goblet cells, and meibomian glands to increase secretion of aqueous fluid, mucin, and lipids, respectively, which are key components for spreading and retaining the tear film evenly across the eye.

Specific Uses of Diquafosol Eye Drops

Beyond general dry eye treatment, clinical studies demonstrate Diquafosol's efficacy in specific conditions, such as aqueous-deficient dry eye, including in patients with Sjögren's syndrome, by increasing aqueous tear fluid. For evaporative dry eye linked to obstructive meibomian gland dysfunction, it helps stabilize the tear film by stimulating lipid secretion. Diquafosol is also effective in managing post-surgical dry eye after procedures like LASIK and cataract surgery. It has been shown to improve tear film stability in patients with short tear film breakup time dry eye and is also used to address dry eye symptoms in contact lens wearers.

Diquafosol vs. Other Common Dry Eye Treatments

Comparing Diquafosol to other dry eye treatments highlights its unique position. The best choice depends on the individual patient and their specific condition. For a detailed comparison of Diquafosol with other therapies like Artificial Tears, Cyclosporine A, and Rebamipide Eye Drops, including their mechanisms, primary functions, speed of action, and common side effects, please see the full article on {Link: PMC website https://pmc.ncbi.nlm.nih.gov/articles/PMC4440420/}.

How to Use Diquafosol Eye Drops

Proper administration is essential for maximizing the effectiveness of Diquafosol and minimizing potential side effects. Patients should always follow their doctor's instructions, but general guidelines often include the following steps:

Wash your hands thoroughly before handling the eye drops.
Tilt your head back and gently pull down your lower eyelid to create a small pocket.
Instill one drop into the pocket. Do not let the tip of the bottle touch your eye or any other surface to prevent contamination.
Close your eye gently and press a finger against the inner corner for 1 to 5 minutes. This helps the medicine absorb and prevents it from draining into your tear duct.
If using other eye drops, wait at least 5 minutes before applying the next one.
If you wear contact lenses, remove them before use. Wait 5 to 10 minutes before reinserting them.

Side Effects and Considerations

While generally well-tolerated, some individuals may experience side effects with Diquafosol eye drops. The most common are typically mild and transient.

Common Side Effects:

Eye irritation or stinging upon application
Foreign body sensation
Eye discharge or mucus
Itching or redness of the eyes
Blepharitis (eyelid inflammation)

These side effects are most common during the first month of treatment and tend to subside with continued use. Patients should discuss any persistent or bothersome side effects with their eye care professional.

Important Considerations:

Pregnancy and breastfeeding: The safety of Diquafosol during pregnancy and breastfeeding has not been fully established. Use should be decided in consultation with a doctor.
Allergic reactions: Though rare, serious allergic reactions are possible. Discontinue use and seek medical attention immediately if you experience severe itching, swelling, or difficulty breathing.

Conclusion

Diquafosol eye drops offer a multi-faceted approach to treating dry eye disease by stimulating the eye's natural production of tears and tear components. Its mechanism, which targets the secretion of aqueous fluid, mucin, and lipids, aids in restoring tear film stability and alleviating both symptoms and signs of dry eye. It is beneficial for various types of dry eye, including post-surgical and MGD-related cases. While minor side effects can occur, they are generally transient. Diquafosol serves as a potent treatment option for dry eye, and should be used under the guidance of an eye care professional.

Frequently Asked Questions

Diquafosol eye drops are used to treat dry eye disease by stimulating the natural secretion of tear fluid and mucin from the ocular surface, helping to stabilize the tear film and alleviate symptoms.

Unlike artificial tears that simply add moisture to the eye, Diquafosol is a P2Y2 receptor agonist that stimulates the eye's own cells to produce more fluid and mucin naturally. This addresses the underlying cause of tear deficiency, providing more comprehensive and longer-lasting relief.

Yes, Diquafosol has been shown to be effective in treating dry eye in patients with Sjögren's syndrome, an autoimmune disorder that can cause severe aqueous-deficient dry eye.

Common side effects include mild eye irritation, stinging, conjunctival redness, and eye discharge. These are usually most noticeable in the first month of treatment and tend to decrease over time.

According to instructions, soft contact lenses should be removed before applying Diquafosol. It is generally recommended to wait 5 to 10 minutes before reinserting the lenses.

The frequency of use should be determined by your healthcare provider.

Clinical comparisons suggest that Diquafosol and sodium hyaluronate offer similar effectiveness for some outcomes, like improving corneal fluorescein staining. However, Diquafosol has shown superiority in improving Rose Bengal staining scores, indicating better efficacy on the conjunctival surface.

Yes, studies have shown that Diquafosol can significantly improve dry eye symptoms and ocular surface damage in patients following LASIK surgery, often providing more effective treatment than conventional artificial tears.