Premium Nahrungsergänzungsmittel | artgerecht

Diquafosol: Active Ingredient for Dry Eye Disease

Diquafosol is an active ingredient used to treat dry eye disease. It stimulates tear fluid production and improves the stability of the tear film.

Regular tips about health Regular tips about health

Things worth knowing about "Diquafosol"

Diquafosol is an active ingredient used to treat dry eye disease. It stimulates tear fluid production and improves the stability of the tear film.

What is Diquafosol?

Diquafosol is a synthetic active substance administered as eye drops for the treatment of dry eye disease (keratoconjunctivitis sicca). It belongs to the pharmacological class of P2Y2 receptor agonists and works by stimulating the natural production of tear fluid and mucin (a gel-like substance) on the ocular surface. Under the brand name Diquas, it is widely used in Japan and other Asian countries, and is also available in various European markets.

Mechanism of Action

Diquafosol selectively binds to P2Y2 purinergic receptors located on the epithelial cells of the conjunctiva and cornea, as well as on goblet cells. This binding triggers two key secretory processes:

Increased aqueous secretion: Conjunctival epithelial cells are stimulated to produce more water and electrolytes, thereby replenishing the aqueous layer of the tear film.
Enhanced mucin secretion: Goblet cells in the conjunctiva are activated to secrete more mucin. Mucin is essential for stabilizing the tear film and ensuring uniform wetting of the ocular surface.

This dual mechanism sets Diquafosol apart from simple artificial tears, which merely passively moisten the eye surface without promoting the eye's own secretory capacity.

Indications

Diquafosol is primarily used in the following conditions:

Dry eye disease (keratoconjunctivitis sicca): Both in cases of reduced tear production and in cases of excessive tear evaporation due to a disrupted tear film.
Mucin-deficient dry eye: Particularly effective in patients where a lack of mucin is the primary cause of ocular dryness.
Screen-related dry eye: Adjunctive treatment for symptoms associated with prolonged use of digital screens.

Dosage and Administration

Diquafosol eye drops are available in a 3% concentration. The standard dosage is 1 drop 6 times daily in each affected eye. The drops are applied directly to the ocular surface. When using multiple eye drops simultaneously, a minimum interval of 5 minutes should be maintained between different preparations. Exact dosing and duration of treatment should always be determined by an ophthalmologist.

Side Effects

Diquafosol is generally well tolerated. Possible side effects include:

Common: Temporary burning or stinging immediately after application, mild irritation of the ocular surface.
Occasional: Eye redness (hyperaemia), foreign body sensation, brief blurred vision after instillation.
Rare: Allergic reactions on the ocular surface, such as itching or swelling of the conjunctiva.

Serious systemic side effects are very rare due to the local application to the eye.

Contraindications and Precautions

Diquafosol should not be used in patients with known hypersensitivity to the active substance or any of the excipients. Contact lens wearers should remove their lenses before applying the eye drops and should wait at least 15 minutes before reinserting them. Data on use during pregnancy and breastfeeding are limited; the decision to use this medication should be made in consultation with the treating physician.

References

Kinoshita S. et al. - Randomized Controlled Phase 3 Study of Diquafosol Ophthalmic Solution for Dry Eye Disease. Ophthalmology, 2012.
Mori Y. et al. - Effects of Diquafosol Tetrasodium on the Ocular Surface Epithelium. Japanese Journal of Ophthalmology, 2015.
European Medicines Agency (EMA) - Assessment Report on Diquafosol-containing Medicinal Products, 2021.

Building Blocks for a Healthy Life

As an integrated manufacturer, we develop & produce evidence-based, patented, and non-patented formulations. We work exclusively with plant and natural extracts according to the strictest purity & quality standards.
The combination of science & modern technology with the laws of nature creates solutions consistently tailored to humans – for the highest good: health.