Netarsudil + Latanoprost

Allopathic
Indications
  • Treatment of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.
  • Indicated for patients who require additional IOP lowering when monotherapy with either agent is insufficient.
  • Used to prevent optic nerve damage and progression of visual field loss associated with glaucoma.
Dosage & Administration
  • 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 dose adjustment necessary.
  • Renal/Hepatic Impairment: No dose adjustment required.
  • Administration Tips:
    • Remove contact lenses prior to administration; wait at least 15 minutes before reinserting.
    • Shake the bottle gently before use.
    • Avoid touching the dropper tip to the eye or other surfaces to prevent contamination.
Mechanism of Action (MOA)

Netarsudil is a Rho kinase (ROCK) inhibitor that lowers intraocular pressure by increasing trabecular meshwork outflow and reducing episcleral venous pressure. It also inhibits the norepinephrine transporter, contributing further to IOP reduction. Latanoprost is a prostaglandin F2α analogue that lowers IOP by increasing uveoscleral outflow through remodeling the extracellular matrix of the ciliary muscle. The combination provides complementary and additive effects for lowering IOP.

Pharmacokinetics
  • Absorption: Minimal systemic absorption after ocular administration; peak plasma levels are low and transient.
  • Distribution: Primarily distributed in ocular tissues with minimal systemic exposure.
  • Metabolism:
    • Netarsudil is hydrolyzed to an active metabolite (AR-13503).
    • Latanoprost is hydrolyzed by corneal esterases to latanoprost acid, its active form.
  • Elimination:
    • Metabolites eliminated mainly via hepatic metabolism and renal excretion.
  • Half-life: Short systemic half-life (~2 hours), but ocular effects persist for 24 hours.
Pregnancy Category & Lactation
  • Pregnancy:
    • No adequate human studies; animal data suggest potential risk. Use only if clearly needed.
  • Lactation:
    • Unknown if excreted in breast milk; use with caution during breastfeeding.
Therapeutic Class
  • Ophthalmic antihypertensive agents — combination of Rho kinase inhibitor (Netarsudil) and prostaglandin analogue (Latanoprost).
Contraindications
  • Hypersensitivity to netarsudil, latanoprost, or any formulation excipients.
  • Active ocular infections including herpetic keratitis.
  • History of hypersensitivity reactions to prostaglandin analogues.
Warnings & Precautions
  • Potential for increased iris pigmentation and eyelash changes with latanoprost.
  • Use caution in patients with ocular inflammation or risk of macular edema.
  • Monitor for conjunctival hyperemia and ocular irritation.
  • Avoid concurrent use with other prostaglandin analogues.
Side Effects
  • Common: Conjunctival hyperemia, eye discomfort, blurred vision, increased eyelash growth, eye pain.
  • Less common: Corneal verticillata, dry eye symptoms.
  • Rare but serious: Macular edema, exacerbation of herpetic keratitis, hypersensitivity reactions.
Drug Interactions
  • No significant systemic interactions due to minimal systemic absorption.
  • Avoid concomitant use with other prostaglandin analogues or ROCK inhibitors.
  • Caution when combined with other ocular drugs affecting intraocular pressure.
Recent Updates or Guidelines
  • FDA-approved fixed-dose combination to improve adherence and provide enhanced IOP lowering.
  • Clinical guidelines endorse combination therapy in patients inadequately controlled on monotherapy.
  • Ongoing research into long-term safety and efficacy continues.
Storage Conditions
  • Store at 20°C to 25°C (68°F to 77°F).
  • Protect from light and moisture.
  • Do not freeze.
  • Keep container tightly closed.
  • Discard opened bottles after 4 weeks of use.