Nesudil

• Treatment of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
• Used as monotherapy or adjunctive therapy when additional IOP reduction is required.
• Aims to prevent optic nerve damage and visual field loss associated with elevated IOP.

• Route: Topical ophthalmic solution (eye drops).
• Adults:
• Instill 1 drop once daily in the evening into the affected eye(s).
• Do not exceed once daily dosing.
• Pediatrics: Safety and efficacy have not been established.
• Elderly: No dosage adjustment required.
• Renal and Hepatic Impairment: No dose adjustment necessary.
• Administration Instructions:
• Remove contact lenses prior to instillation; wait at least 15 minutes before reinsertion.
• Shake the bottle gently before use.
• Avoid touching the dropper tip to the eye or any surface to prevent contamination.

Netarsudil is a selective Rho kinase (ROCK) inhibitor that lowers intraocular pressure primarily by increasing aqueous humor outflow through the trabecular meshwork. It relaxes the trabecular meshwork and Schlemm's canal endothelial cells, reducing resistance to aqueous humor drainage. Additionally, netarsudil decreases episcleral venous pressure and inhibits the norepinephrine transporter, further contributing to the reduction of IOP.

• Absorption: Minimal systemic absorption following topical ocular administration; plasma concentrations remain low and transient.
• Distribution: Primarily localized in ocular tissues with negligible systemic exposure.
• Metabolism: Rapidly metabolized by esterases into an active metabolite, AR-13503.
• Elimination: Metabolites are excreted mainly via hepatic metabolism and renal excretion.
• Half-life: Systemic half-life is approximately 2 hours, but ocular IOP-lowering effects last about 24 hours.

• Pregnancy: No adequate well-controlled studies in pregnant women; animal studies indicate possible risk. Use only if the potential benefit justifies the potential risk to the fetus.
• Lactation: Unknown if netarsudil is excreted in human milk; exercise caution when administering to breastfeeding mothers.

• Ophthalmic antihypertensive agent
• Rho kinase (ROCK) inhibitor subclass

• Known hypersensitivity to netarsudil or any of its components.
• Active ocular infections, including herpetic keratitis.
• History of hypersensitivity to Rho kinase inhibitors.

• May cause conjunctival hyperemia (eye redness), typically mild to moderate and transient.
• Use cautiously in patients with ocular inflammation.
• Monitor for corneal verticillata (whorl-like corneal deposits).
• Avoid concomitant use with other ROCK inhibitors or prostaglandin analogues unless prescribed.

• Common: Conjunctival hyperemia, eye discomfort, blurred vision, eyelid erythema, corneal verticillata.
• Less Common: Eye pruritus, ocular pain, dry eyes.
• Rare: Hypersensitivity reactions, ocular inflammation.

• No significant systemic drug interactions are expected due to minimal systemic absorption.
• Potential additive effects when used with other intraocular pressure-lowering agents.
• Avoid concurrent use with other ROCK inhibitors or prostaglandin analogues unless clinically indicated.

• FDA-approved as a once-daily topical therapy for open-angle glaucoma and ocular hypertension.
• Recommended in clinical guidelines for patients inadequately controlled on other therapies.
• Ongoing studies continue to evaluate long-term safety and efficacy.

• Store at 20°C to 25°C (68°F to 77°F).
• Protect from light and moisture.
• Do not freeze.
• Keep the container tightly closed.
• Discard opened bottles after 4 weeks of use.