|Pronunciation||ne TAR soo dil|
|Trade names||Rhopressa, Rhokiinsa|
|Drug class||Rho kinase inhibitor|
|Main uses||Increased intraocular pressure, open-angle glaucoma|
|Side effects||Red eyes, conjunctival bleeding, blurry vision, tearing|
|Eye drops, topical|
|Duration of action||≥ 24 hrs|
|Metabolism||Esterases in the cornea|
|Metabolites||AR-13503 (active metabolite)|
|Elimination half-life||16–17 hrs|
|Chemical and physical data|
|Molar mass||453.542 g·mol−1|
|3D model (JSmol)|
Netarsudil was approved for medical use in the United States in 2017 and Europe in 2019. In the United States a 2.5 ml bottle costs about 305 USD as of 2021. It is also available as the combination netarsudil/latanoprost. It is not commercially available in Europe and the United Kingdom as of 2021.
It is used at a dose of one drop per day.
The most common side effects are hyperaemia (increased blood flow associated with redness, in 51% of patients) in the conjunctiva, cornea verticillata (drug deposits in the cornea, in 17%), and eye pain (in 17%). All other side effects occur in fewer than 10% of people. Hypersensitivity reactions occur in fewer than 1%.
Overdosing netarsudil is unlikely because concentrations in the body are so low that they are generally not detectable.
Mechanism of action
This drug's mechanism of action is not entirely clear. It inhibits the enzyme rho kinase. This appears to increase outflow of aqueous humor through the trabecular meshwork, and also to reduce pressure in the veins of the episcleral layer. The drug also inhibits the norepinephrine transporter.
After instillation into the eye, netarsudil is cleaved by esterases in the cornea to AR-13503, which is the active metabolite. Concentrations reached in the blood plasma are so low that they are generally not detectable. To judge from animal models, the drug acts for at least 24 hours. Its elimination half-life is 16 to 17 hours (in rabbits).
The drug is used in form of a salt, netarsudil dimesilate, which is a white to light yellow crystalline powder. It is a weak acid and moderately hygroscopic, freely soluble in water and soluble in methanol.
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