Rhopressa netarsudil ophthalmic solution 0.02% eye drop bottle and box

Glaucoma treatment often focuses on lowering eye pressure, because eye pressure is one of the most important risk factors we can modify to help slow the progression of glaucoma.

Rhopressa (netarsudil 0.02%) is a relatively new type of glaucoma eye drop. It belongs to a class of medications known as Rho kinase (ROCK) inhibitors and is FDA-approved to lower eye pressure in people with open-angle glaucoma or ocular hypertension.

What makes Rhopressa particularly interesting is that it works differently from many of the glaucoma drops that came before it.

A Brief History of Rhopressa

For decades, glaucoma medications primarily lowered eye pressure either by reducing the amount of fluid the eye produces or by helping fluid leave the eye through alternative drainage pathways.

Researchers eventually began looking for medications that could more directly improve the eye’s natural drainage system.

This led to the development of netarsudil, originally known as AR-13324, by Aerie Pharmaceuticals. After several clinical trials demonstrated its ability to lower eye pressure, the FDA approved Rhopressa in December 2017.

Rhopressa became the first medication in the Rho kinase inhibitor class approved in the United States for glaucoma treatment, providing ophthalmologists with a new way to approach lowering eye pressure.

How Does Rhopressa Work?

Rhopressa netarsudil mechanism of action diagram showing the anterior chamber angle, trabecular meshwork, and Schlemm's canal

The eye constantly produces a clear fluid called aqueous humor. This fluid circulates through the front of the eye and then drains out.

Most of this fluid normally leaves through a microscopic drainage system called the trabecular meshwork.

You can think of this system somewhat like a drain. If it becomes more difficult for fluid to pass through, pressure inside the eye can increase.

Rhopressa blocks an enzyme called Rho kinase, or ROCK. Doing so relaxes and changes some of the cells within the eye’s drainage system, allowing fluid to pass through more easily.

In simple terms: Rhopressa helps improve the eye’s natural ability to drain fluid, which can lower eye pressure.

Research suggests that Rhopressa may also lower the pressure in the small veins into which the eye drains and may slightly reduce the amount of fluid produced inside the eye. These combined effects make its mechanism somewhat different from many traditional glaucoma medications.

How Is Rhopressa Used?

Rhopressa is available as netarsudil ophthalmic solution 0.02%.

The usual recommended dose is: One drop in the affected eye or eyes once daily in the evening.

Using the medication more than once per day is generally not recommended and may increase the likelihood of side effects.

Rhopressa can be used by itself, but it is also frequently used alongside other glaucoma medications when additional eye-pressure lowering is needed.

There is also a combination medication called Rocklatan, which contains both netarsudil and latanoprost. Because the two medications lower pressure in different ways, combining them can provide additional pressure lowering for some patients.

How Much Can Rhopressa Lower Eye Pressure?

Large clinical trials known as the ROCKET trials studied Rhopressa in patients with open-angle glaucoma or ocular hypertension.

These studies demonstrated that once-daily Rhopressa could produce meaningful reductions in eye pressure. In the ROCKET-2 study, for example, patients receiving Rhopressa once daily started with an average morning eye pressure of approximately 22.5 mmHg, with average morning pressures generally around 18 to 19 mmHg during treatment.

However, these numbers should not be interpreted as a prediction of exactly how much someone’s pressure will decrease.

Every patient responds differently to glaucoma medications. Some people experience substantial pressure reductions, while others may have a smaller response.

The important question is whether the medication helps an individual patient reach the eye-pressure goal established by their ophthalmologist.

What Are the Most Common Side Effects?

Rhopressa netarsudil ophthalmic side effects infographic: conjunctival hyperemia, conjunctival hemorrhage, instillation discomfort, eyelid redness

Like any medication, Rhopressa can cause side effects. Fortunately, most of its common side effects involve the surface of the eye rather than the rest of the body.

Eye Redness

The most common side effect of Rhopressa is redness of the eye.

This is quite common and occurred in roughly half or more of patients in some of the major clinical trials.

The redness occurs because Rhopressa affects the small blood vessels on the surface of the eye. It does not necessarily mean that the eye is infected or being damaged.

For some people, the redness is mild and not particularly bothersome. For others, it may be noticeable enough that a different glaucoma medication is preferred.

Changes on the Surface of the Cornea

Rhopressa can sometimes cause small deposits or changes on the clear front surface of the eye, called the cornea.

These changes are usually something an eye doctor notices during an examination rather than something a patient sees themselves. In clinical studies, these findings generally did not have a meaningful effect on vision.

They may also improve or disappear after the medication is discontinued.

Small Areas of Blood on the White of the Eye

Some patients using Rhopressa develop small areas of bleeding on the surface of the eye.

These can look like tiny red spots or occasionally a larger red area on the white part of the eye.

Although seeing blood on the surface of the eye can be concerning, these small surface hemorrhages are generally mild and do not necessarily indicate bleeding inside the eye.

Corneal Swelling

A less common but important side effect is swelling of the cornea, the clear window at the front of the eye.

This has been reported particularly in certain patients who already have problems with their cornea or who have undergone eye procedures that may affect the health of the cornea.

Significant corneal swelling can cause blurred or decreased vision. Patients using Rhopressa who develop a substantial new change in vision, eye pain, or other concerning symptoms should contact their eye doctor.

Where Does Rhopressa Fit Into Glaucoma Treatment?

Rhopressa provides ophthalmologists with another way to lower eye pressure.

Medications such as latanoprost and other prostaglandin eye drops remain common first treatments for glaucoma because they are effective, used once daily, and have been prescribed for many years.

However, many patients need more than one treatment to reach their desired eye pressure.

Rhopressa can be particularly useful because it works differently from many traditional glaucoma medications. This allows it to be added to another medication when additional pressure lowering is necessary.

One of its biggest drawbacks is eye redness, which can be significant for some patients. On the other hand, relatively little of the medication reaches the bloodstream, so systemic side effects are generally less of a concern than with certain other glaucoma medications.

Ultimately, there is no single glaucoma eye drop that is best for everyone. Choosing a medication depends on the type and severity of glaucoma, the desired eye pressure, other medical conditions, previous treatments, side effects, and how well an individual patient responds.

Works Cited

  1. U.S. Food and Drug Administration. Rhopressa (netarsudil ophthalmic solution) 0.02% Prescribing Information. Updated 2024.
  2. Serle JB, Katz LJ, McLaurin E, et al. Two Phase 3 Clinical Trials Comparing the Safety and Efficacy of Netarsudil to Timolol in Patients With Elevated Intraocular Pressure: ROCKET-1 and ROCKET-2. American Journal of Ophthalmology. 2018;186:116-127.
  3. Kahook MY, Serle JB, Mah FS, et al. Long-term Safety and Ocular Hypotensive Efficacy Evaluation of Netarsudil Ophthalmic Solution: ROCKET-2. American Journal of Ophthalmology. 2019;200:130-137.
  4. Hoy SM. Netarsudil Ophthalmic Solution 0.02%: First Global Approval. Drugs. 2018;78(3):389-396.
  5. Sturdivant JM, Royalty SM, Lin CW, et al. Discovery of the ROCK inhibitor netarsudil for the treatment of open-angle glaucoma. Bioorganic & Medicinal Chemistry Letters. 2016;26(10):2475-2480.
  6. Lin CW, Sherman B, Moore LA, et al. Discovery and Preclinical Development of Netarsudil, a Novel Ocular Hypotensive Agent for the Treatment of Glaucoma. Journal of Ocular Pharmacology and Therapeutics. 2018;34(1-2):40-51.

Medical Disclaimer

This article is intended for general educational and informational purposes only and is not a substitute for individualized medical advice, diagnosis, or treatment. Glaucoma treatment should be determined by an eye care professional based on each patient’s examination, medical history, disease severity, and other clinical factors.

Do not start, stop, or change a prescription eye medication without discussing it with your ophthalmologist or other qualified healthcare professional. Patients experiencing new or worsening eye pain, decreased vision, significant redness, or other concerning eye symptoms should seek appropriate medical evaluation.