Nesudil0.02%

Nesudil ophthalmic solution is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. This is the sole FDA-approved (established) indication for Nesudil.

• Established/approved use: Once-daily reduction of elevated IOP in open-angle glaucoma and ocular hypertension, used either as a first-line agent or as an add-on to other IOP-lowering eye drops when target pressure is not achieved on existing therapy.

Nesudil is not approved and should not be used for angle-closure glaucoma, acute angle-closure attacks, or any non-ophthalmic condition.

Each mL of ophthalmic solution contains Netarsudil Dimesylate equivalent to 0.02% netarsudil base, formulated as a sterile, preserved (benzalkonium chloride) ophthalmic solution for topical application to the eye.

Nesudil is the mesylate salt of netarsudil, a Rho kinase (ROCK) inhibitor developed specifically for ophthalmic use. It is formulated as a sterile topical eye drop solution used once daily to lower intraocular pressure in people with open-angle glaucoma or ocular hypertension.

Unlike older IOP-lowering agents that primarily reduce aqueous humor production, Nesudil works mainly by increasing aqueous humor outflow through the eye's natural drainage pathway.

Nesudil belongs to the Rho kinase (ROCK) inhibitor class of ophthalmic anti-glaucoma agents. It is used topically in the eye and is distinct in mechanism from prostaglandin analogues, beta-blockers, alpha agonists, and carbonic anhydrase inhibitors used for the same indication.

Mechanism of action: Netarsudil Dimesylate is thought to lower intraocular pressure by inhibiting Rho kinase (ROCK), which relaxes the trabecular meshwork and increases aqueous humor outflow through the conventional (trabecular) drainage pathway, the eye's primary route for fluid egress. It may also reduce episcleral venous pressure and, to a lesser extent, decrease aqueous humor production.

Pharmacokinetics: Following topical ocular administration, netarsudil is metabolized by esterases in the eye to an active metabolite. Systemic exposure is minimal due to the small topical dose and extensive local metabolism, which limits systemic pharmacologic effects.

Administer Nesudil as a single drop into the conjunctival sac of the affected eye(s), once daily in the evening. Wash hands before instillation, avoid touching the dropper tip to the eye or surrounding structures to prevent contamination, and replace the cap after use. If using other topical ophthalmic products, space administration at least 5 minutes apart.

Formal drug-drug interaction studies with Nesudil are limited given its minimal systemic absorption; clinically significant systemic interactions have not been well established.

• Other topical ophthalmic agents: When used with other eye drops, separate administration by at least 5 minutes to prevent one drop washing out another.
• Prostaglandin analogues (e.g., latanoprost): No clinically significant pharmacodynamic interaction precluding combined use has been established; combination use is common in practice to achieve additional IOP lowering.

The most common adverse reaction with Nesudil is conjunctival hyperemia (eye redness), which is very common and is the leading cause of treatment discontinuation.

• Very common: Conjunctival hyperemia (redness).
• Common: Corneal verticillata (whorl-like corneal deposits; generally asymptomatic and typically reversible upon discontinuation), instillation-site pain, conjunctival hemorrhage, and instillation-site erythema.
• Less common: Blurred vision, increased lacrimation, erythema of the eyelid, reduced visual acuity, and dry eye.

Patients should be informed that corneal verticillata may occur and should be counseled to report any change in vision.

Pregnancy: There are no adequate and well-controlled studies of Nesudil in pregnant women. Nesudil should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult a physician before use if pregnant or planning pregnancy.

Lactation: It is not known whether Nesudil or its metabolites are excreted in human milk. Because systemic absorption after topical ocular administration is expected to be minimal, risk to a breastfeeding infant is likely low, but a physician should be consulted before use while breastfeeding, weighing the benefit of treatment against any potential risk to the infant.

• Conjunctival hyperemia: Very common; usually mild and does not typically require discontinuation, but is the most common reason patients stop treatment.
• Corneal verticillata: Whorl-like corneal epithelial deposits have been observed with chronic use; generally does not affect visual function and is typically reversible with discontinuation. Patients should be monitored and advised to report visual changes.
• Contact lens use: The solution contains benzalkonium chloride, which can be absorbed by soft contact lenses. Contact lenses should be removed before instillation and may be reinserted 15 minutes after administration.
• Instillation-site pain: Reported commonly; usually transient.
• Bacterial keratitis: As with other topical ophthalmic products, multiple-dose containers of eye drops have been associated with bacterial keratitis from inadvertent contamination; care should be taken to avoid contaminating the dropper tip.

Specific data on overdose with Nesudil are limited. Ocular overdose (excessive instillation) may increase local side effects such as conjunctival hyperemia or instillation-site pain. In case of accidental ingestion or significant overdose, seek immediate medical attention or contact a poison control center; do not attempt unsupervised specific home treatment.

Store unopened bottles refrigerated at 2°C to 8°C. After opening, the bottle may be stored at room temperature (15°C to 25°C) for up to 6 weeks. Protect from light and moisture, and keep out of reach of children.

• Pediatric use: Safety and efficacy of Nesudil in pediatric patients have not been established.
• Geriatric use: No overall differences in safety or efficacy have been observed between elderly and younger adult patients; no dose adjustment is required based on age alone.
• Renal impairment: No specific studies conducted; systemic exposure is minimal, so clinically significant effects are not expected.
• Hepatic impairment: No specific studies conducted; systemic exposure is minimal, so clinically significant effects are not expected.

Nesudil is generally used long-term as a chronic, once-daily therapy for as long as needed to control intraocular pressure in open-angle glaucoma or ocular hypertension. Duration should be determined and periodically reassessed by an ophthalmologist based on IOP control, tolerability, and visual field/optic nerve monitoring. Treatment should not be stopped or interrupted without consulting a physician.

Netarsudil Dimesylate is classified as an ophthalmic Rho kinase (ROCK) inhibitor, a class of anti-glaucoma agents distinct from prostaglandin analogues, topical beta-blockers, alpha-2 agonists, and carbonic anhydrase inhibitors.

Netarsudil Dimesylate inhibits Rho kinase (ROCK), leading to relaxation of the trabecular meshwork and Schlemm's canal endothelium, which increases conventional (trabecular) outflow of aqueous humor, the eye's primary drainage pathway. It may also lower episcleral venous pressure and modestly reduce aqueous humor production, together lowering intraocular pressure.

The safety and efficacy of Nesudil have not been established in pediatric patients. Use in children is not currently recommended outside of the guidance of a pediatric ophthalmologist, and only if no suitable alternative is available and potential benefits are judged to outweigh risks.