Netarsudil is a topical Rho kinase inhibitor indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. In clinical studies, up to 5 mmHg reductions in IOP were observed in patients treated with netarsudil ophthalmic solution. Netarsudil was similar in efficacy to timolol 0.5% for patients with baseline IOP less than 25 mmHg; however, for patients with IOP of 25 mmHg or more, netarsudil resulted in smaller mean IOP reductions at morning time points compared with timolol. The most common adverse reaction reported in clinical studies with netarsudil was conjunctival hyperemia.
General Administration Information
For storage information, see the specific product information within the How Supplied section.
Route-Specific Administration
Ophthalmic Administration
-For ophthalmic use only.
-Avoid allowing the tip of the container to contact the eye, surrounding structures, fingers, or any other surface to minimize contamination of the solution.
-If use concomitantly with other ophthalmic products, the drugs should be administered at least 5 minutes apart.
-Contact lenses should be removed prior to instillation of netarsudil ophthalmic solution; they may be reinserted 15 minutes following administration of netarsudil.
The most common ocular adverse reaction reported in clinical studies with netarsudil was conjunctival hyperemia (53%; 6% discontinued therapy due to conjunctival hyperemia). Corneal verticillata (vortex keratopathy) was reported in approximately 20% of patients. This was first observed after 4 weeks of daily dosing and did not result in any apparent visual functional changes in patients. Most cases resolved upon discontinuation of treatment. Other common ocular adverse reactions reported in approximately 20% of patients receiving netarsudil included instillation ocular pain and conjunctival or ocular hemorrhage. Instillation site erythema, corneal staining, blurred vision, increased lacrimation, eyelid erythema, and reduced visual acuity were reported in 5% to 10% of patients.
The use of multiple dose containers of ophthalmic products has been associated with bacterial keratitis. Inadvertent contamination of the netarsudil container may increase the risk of infection in patients with concurrent corneal disease or a disruption of the ocular epithelial surface.
Netarsudil ophthalmic solution is formulated with the preservative benzalkonium chloride, which may be absorbed by soft contact lenses. Users of soft contact lenses should not administer netarsudil while wearing the lenses; lenses may be reinserted 15 minutes after netarsudil instillation.
There are no data available on netarsudil use in human pregnancy to inform a drug-associated risk; however, systemic exposure to netarsudil after ophthalmic administration is low. Animal data have shown that intravenous administration of netarsudil during organogenesis did not produce adverse embryofetal effects at clinically relevant systemic exposures.
There are no data available on the presence of netarsudil in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to netarsudil after ophthalmic administration is low and it is unknown whether measurable concentrations of netarsudil would be present in maternal milk following topical ocular administration. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for netarsudil and any potential adverse effects on the breast-fed infant from netarsudil.
For the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension:
Ophthalmic dosage:
Adults: Instill 1 drop into affected eye(s) once daily in the evening. If a dose is missed, continue with the next dose in the evening; twice daily dosing is not well tolerated and is not recommended. If more than 1 topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes apart.
Maximum Dosage Limits:
-Adults
1 drop/day/affected eye.
-Geriatric
1 drop/day/affected eye.
-Adolescents
Safety and efficacy have not been established.
-Children
Safety and efficacy have not been established.
-Infants
Safety and efficacy have not been established.
-Neonates
Safety and efficacy have not been established.
Patients with Hepatic Impairment Dosing
Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.
Patients with Renal Impairment Dosing
Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.
*non-FDA-approved indication
There are no drug interactions associated with Netarsudil products.
Netarsudil is a rho kinase inhibitor, which is believed to reduce intraocular pressure by increasing the outflow of aqueous humor through the trabecular meshwork route. The exact mechanism is unknown.
Netarsudil is administered topically to the eye. Systemic exposure after topical administration is low. In a study in 18 healthy subjects who received topical administration of netarsudil 0.02% once daily (1 drop bilaterally in the morning) for 8 days, there were no quantifiable plasma concentrations of netarsudil (lower limit of quantitation (LLOQ) 0.1 ng/mL) post dose on day 1 and day 8. Only 1 plasma concentration of 0.11 ng/mL for the active metabolite was noted for 1 subject on day 8, at 8 hours post dose. After topical ocular administration, netarsudil is metabolized by esterases in the eye.
Affected cytochrome P450 isoenzymes: none