Usage
- Netarsudil is prescribed for the reduction of elevated intraocular pressure (IOP) in adult patients with primary open-angle glaucoma or ocular hypertension.
- Pharmacological classification: Rho kinase inhibitor.
- Mechanism of Action: Netarsudil increases trabecular outflow of aqueous humor, thereby reducing IOP. It also decreases episcleral venous pressure, further contributing to IOP reduction.
Alternate Names
- Netarsudil mesylate (International Nonproprietary Name - INN)
- Brand Names: Rhopressa, Rhokiinsa (in some regions), and in combination with latanoprost: Rocklatan, Roclanda.
How It Works
- Pharmacodynamics: Netarsudil primarily reduces IOP by enhancing trabecular outflow and decreasing episcleral venous pressure.
- Pharmacokinetics: Following topical ocular administration, systemic absorption is low. Netarsudil is metabolized in the eye by esterases to an active metabolite, AR-13503. Plasma concentrations of netarsudil are typically not quantifiable after topical ocular administration. The small amount that may enter systemic circulation is further metabolized, primarily in the liver. Elimination pathways have not been definitively characterized but is assumed to be through renal/hepatic routes.
- Mode of action: Netarsudil inhibits Rho kinase and norepinephrine transporter. Rho kinase inhibition leads to relaxation of the trabecular meshwork and Schlemm’s canal, facilitating aqueous humor outflow. Inhibition of the norepinephrine transporter results in decreased episcleral venous pressure.
Dosage
Standard Dosage
Adults:
- One drop in the affected eye(s) once daily in the evening.
- Do not exceed one drop per eye per day.
Children:
- The safety and efficacy of netarsudil in children below 18 years have not been established. No data are available. Off-label use for refractory pediatric glaucoma may occur under strict specialist supervision, but no established dosing guidelines exist.
Special Cases:
- Elderly Patients: No dose adjustment is necessary.
- Patients with Renal Impairment: No specific dose adjustment recommendations are available due to limited data. Caution advised.
- Patients with Hepatic Dysfunction: No specific dose adjustment recommendations are available due to limited data. Caution advised.
- Patients with Comorbid Conditions: Limited data are available; consider careful monitoring and potential interactions.
Clinical Use Cases
Netarsudil’s clinical use is primarily focused on managing open-angle glaucoma or ocular hypertension. Dosage recommendations for specific medical settings like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations are not specifically defined. Its use in such cases is not standard practice.
Dosage Adjustments
Limited data are available regarding dose modifications for specific patient factors, including renal/hepatic dysfunction, metabolic disorders, or genetic polymorphisms. Exercise caution and monitor closely in such cases.
Side Effects
Common Side Effects:
- Conjunctival hyperemia (eye redness)
- Corneal verticillata
- Instillation site pain
- Corneal staining
- Blurred vision
Rare but Serious Side Effects:
- Bacterial keratitis (corneal infection)
- Corneal edema
- Iritis/uveitis
- Vision changes/decreased vision
Long-Term Effects:
- Potential for increased pigmentation of the iris
- Effects of long-term use beyond 12 months have not been thoroughly studied.
Adverse Drug Reactions (ADR):
- Allergic reactions (rash, itching, hives, swelling)
Contraindications
- Hypersensitivity to netarsudil or any of its components.
Drug Interactions
- No significant drug interactions have been reported.
- If using other topical ophthalmic medications, administer at least 5 minutes apart. Apply other eye drops before Netarsudil due to its vasodilating properties, and eye ointments last.
Pregnancy and Breastfeeding
- Pregnancy: There are no adequate and well-controlled studies in pregnant women. Animal studies have shown potential for embryofetal toxicity at high doses. Use only if clearly needed.
- Breastfeeding: It is unknown if netarsudil is excreted in human milk. Systemic exposure is low after topical ocular administration. Use with caution and consider the developmental and health benefits of breastfeeding alongside the mother’s clinical need for the drug.
Drug Profile Summary
- Mechanism of Action: Rho kinase inhibitor, increasing trabecular outflow and decreasing episcleral venous pressure.
- Side Effects: Conjunctival hyperemia, corneal verticillata, instillation site pain, blurred vision.
- Contraindications: Hypersensitivity.
- Drug Interactions: No significant interactions reported.
- Pregnancy & Breastfeeding: Use with caution. Data is limited.
- Dosage: One drop in affected eye(s) once daily in the evening.
- Monitoring Parameters: Intraocular pressure, visual acuity, signs of ocular irritation or infection.
Popular Combinations
- Latanoprost and Netarsudil: This fixed-dose combination is available for patients who need additional IOP lowering beyond monotherapy.
Precautions
- General Precautions: Ensure proper administration technique to avoid contamination. Monitor for signs of infection.
- Specific Populations: As described above in sections related to dosage, pregnancy, and breastfeeding.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Netarsudil?
A: One drop in the affected eye(s) once daily in the evening for adults. Not recommended for children under 18.
Q2: How does Netarsudil lower IOP?
A: It increases trabecular outflow and reduces episcleral venous pressure.
Q3: Can Netarsudil be used with other glaucoma medications?
A: Yes, but administer at least 5 minutes apart.
Q4: What are the common side effects?
A: Conjunctival hyperemia (redness), corneal verticillata, instillation site pain, and blurred vision.
Q5: Is Netarsudil safe during pregnancy?
A: Data are limited. Consult with a specialist; only use if the potential benefits outweigh the risks.
Q6: Is Netarsudil safe during breastfeeding?
A: Data are limited. Use with caution and discuss the risks and benefits with a specialist.
Q7: Are there any contraindications for Netarsudil?
A: Hypersensitivity to netarsudil or its components.
Q8: How should Netarsudil be stored?
A: Refrigerate until opened. After opening, can be stored at room temperature for up to 6 weeks.
Q9: What should I do if I miss a dose?
A: Continue with the next scheduled dose in the evening. Do not double the dose.
