Cyclosporine Eye Drops

Anti-Inflammatory Eye Drops

Inflammation is a key factor in dry eye disease. If left untreated, inflammation drives increased dry eyes and damage to your eyes.

There are two main classes of anti-inflammatory eye drops:

Cyclosporine eye drops
Lifitegrast eye drops

💡 These are prescription eye drops prescribed by your eye care professionals!

💡 Bare in mind that all these eye drops sting a little upon instillation. Use of artificial tears before instillation of these eye drops may decrease the stinging.

Cyclosporine Eye Drops

What is cyclosporine?

Ciclosporin is a calcineurin inhibitor and an immunosuppressant that has been shown to both reduce inflammatory mediators in the tears and increase tear production.

How do cyclosporine eye drops work?

It functions through interaction with cyclophilin, thereby inhibiting the phosphatase activity of calcineurin. Consequently, there's a reduction in the generation of inflammatory cytokines by T lymphocytes, leading to its anti-inflammatory properties.

Ciclosporin is characterized by its hydrophobic nature, indicating its high solubility in lipids but poor solubility in water. This characteristic poses a constraint on its transport across the tear film to the ocular surface, thereby restricting the achievable concentration at the ocular surface.

What are the benefits of using cyclosporine eye drops?

Cyclosporine eye drops can be very effective in treating dry eye disease and other eye conditions. They can help to improve the symptoms of dry eye, such as burning, stinging, and irritation. Cyclosporine eye drops can also help to improve the vision of people with dry eye disease.

What are the side effects of cyclosporine eye drops?

The most common side effects of cyclosporine eye drops are mild and temporary. They can include burning, stinging, redness, and itching of the eyes. Less common side effects can include allergic reactions, eye infections, and increased tear production.

In contrast to various topical anti-inflammatories, notably steroids, Ciclosporin stands out for its ability to avoid elevating intraocular pressure or causing cataracts. This unique trait grants it a significant safety edge over these medications when utilized as an anti-inflammatory remedy for dry eye conditions.

How to use cyclosporine eye drops

Cyclosporine eye drops are usually used twice a day. To use them, simply tilt your head back and pull down your lower eyelid. Apply one drop of the medication to the inside of your lower eyelid. Close your eye and gently press on the inner corner of your eye for about a minute to prevent the medication from draining out.

Are cyclosporine eye drops safe for everyone?

Cyclosporine eye drops are generally safe for most people. However, they should not be used by people who are allergic to cyclosporine or who have certain eye conditions, such as glaucoma or keratitis.

Restasis

Restasis (Cyclosporine 0.05%) works by binding to proteins in the cells called immunophilins. This reduces activation and inflammation in dry eye disease. Cyclosporine increases tear production and goblet cell density.

On PBS via SAS; In NZ must be prescribed by Doctors only

Dosages: Twice a day, once in the morning and once at night.

❗People start noticing a difference with Restasis within 2-6 months.

Cequa & Ikervis

✅ Preservative-free formulas

These are newer formulations of cyclosporine. Cequa and Ikervis eye drops use coatings of nano-particles to help them travel through the tear film and reach the surface of the eye. The theory is that these coatings make Cequa or Ikervis more effective than compounded cyclosporine or Restasis.

They both have been engineered to deliver ciclosporin where it is needed most, using nanomicelles composed of polymers that encapsulate the ciclosporin molecule. The ciclosporin molecule is dissolved in a hydrophobic core, which in turn is coated in a hydrophilic shell. This hydrophilic shell allows transport through the tear film to the ocular surface. This improves both the tolerability and clinical efficacy of the compound.

Dosages:
- Cequa (Cyclosporine 0.09%) (PBS), twice a day
- Ikervis (Cyclosporine 0.1%) (PBS), once a day in the evening

❗People start noticing a difference as soon as 1 month but usually around 4-6 months.

Xiidra Eye Drops: Lifitegrast 5%

Lifitegrast blocks a protein called LFA-1. This also reduces activation and inflammation in dry eye disease. Up to a quarter of patients experience irritation and an unusual taste sensation.

Dosages: Twice a day, once in the morning and once at night.

Some may start to notice a difference after 2-12 weeks. It is also possible to switch from cyclosporine to Xiidra.

❗Xiidra discontinued in Australia but 5.0% ointment can be compounded in Australia and NZ

Unfortunately these drugs haven't been directly compared in clinical studies, but studies have found they all to be effective for treating dry eye.

💡 It is important to remember that Restasis, Cequa, Ikervis and Xiidra do not cure other causes of dry eyes - for example, blepharitis, Meibomian Gland Dysfunction or other medical causes of dry eyes. It is also important to work with an optometrist to identify other dry eye causes.