Generic Name: Netarsudil Mesylate
Class: Antiglaucoma Agents, Miscellaneous
Chemical Name: [4-[(2S)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate;methanesulfonic acid
Molecular Formula: C30H35N3O9S2
CAS Number: 1422144-42-0
Netarsudil mesylate is an antiglaucoma agent.1
Uses for Rhopressa
Netarsudil mesylate has the following uses:
Netarsudil ophthalmic solution 0.02% is a Rho kinase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.1
Rhopressa Dosage and Administration
Netarsudil mesylate is available in the following dosage form(s) and strength(s):
Ophthalmic solution 0.02% containing 0.2 mg/mL of netarsudil.1
Dosage of netarsudil mesylate is expressed in terms of netarsudil.1
It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
One drop of a 0.02% solution into the affected eye(s) once daily in the evening.1
Cautions for Rhopressa
There have been reports of bacterial keratitis associated with the use of multiple-dose containers of topical ophthalmic products. These containers had been inadvertently contaminated by patients who, in most cases, had a concurrent corneal disease or a disruption of the ocular epithelial surface.1
Use With Contact Lenses
Contact lenses should be removed prior to instillation of netarsudil mesylate and may be reinserted 15 minutes following its administration.1
Risk Summary: There are no available data on netarsudil mesylate use in pregnant women to inform any drug associated risk; however, systemic exposure to netarsudil from ocular administration is low. Intravenous administration of netarsudil to pregnant rats and rabbits during organogenesis did not produce adverse embryofetal effects at clinically relevant systemic exposures.1
Animal Data: Netarsudil administered daily by intravenous injection to rats during organogenesis caused abortions and embryofetal lethality at doses ≥0.3 mg/kg/day (126-fold the plasma exposure at the recommended human ophthalmic dose [RHOD], based on Cmax). The no-observed-adverse-effect-level (NOAEL) for embryofetal development toxicity was 0.1 mg/kg/day (40-fold the plasma exposure at the RHOD, based on Cmax).1
Netarsudil administered daily by intravenous injection to rabbits during organogenesis caused embryofetal lethality and decreased fetal weight at 5 mg/kg/day (1480-fold the plasma exposure at the RHOD, based on Cmax). Malformations were observed at ≥3 mg/kg/day (1330-fold the plasma exposure at the RHOD, based on Cmax), including thoracogastroschisis, umbilical hernia and absent intermediate lung lobe. The NOAEL for embryofetal development toxicity was 0.5 mg/kg/day (214-fold the plasma exposure at the RHOD, based on Cmax).1
There are no data on the presence of netarsudil mesylate in human milk, the effects on the breastfed infant, or the effects on milk production. However, systemic exposure to netarsudil following topical ocular administration is low, and it is not known whether measurable levels of netarsudil would be present in maternal milk following topical ocular administration.1
The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for netarsudil mesylate and any potential adverse effects on the breast-fed child from netarsudil mesylate.1
Safety and effectiveness in pediatric patients below the age of 18 years have not been established.1
No overall differences in safety or effectiveness have been observed between elderly and other adult patients.1
Common Adverse Effects
The most common adverse reaction is conjunctival hyperemia (53%). Other common adverse reactions (approximately 20%) include: corneal verticillata, instillation site pain, and conjunctival hemorrhage.1
It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:
Please see product labeling for drug interaction information.
Mechanism Of Action
Netarsudil is a rho kinase inhibitor, which is believed to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork route. The exact mechanism is unknown.1
Advice to Patients
Handling the Container: Instruct patients to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to minimize contamination of the solution. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions.1
When to Seek Physician Advice: Advise patients that if they develop an intercurrent ocular condition (e.g., trauma or infection), have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician’s advice concerning the continued use of netarsudil mesylate.1
Use with Contact Lenses: Advise patients that netarsudil mesylate contains benzalkonium chloride, which may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of netarsudil mesylate and may be reinserted 15 minutes following its administration.1
Use with Other Ophthalmic Drugs: Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes between applications.1
Missed Dose: Advise patients that if one dose is missed, treatment should continue with the next dose in the evening.1
AHFS First Release. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.
Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.
Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.
0.02% (of netarsudil) (0.2 mg/mL)
Rhopressa (with benzalkonium chloride)
Aerie Pharmaceuticals Inc.
AHFS Drug Information. © Copyright 2018, Selected Revisions January 8, 2018. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
1. Aerie Pharmaceuticals, Inc. Rhopressa (netarsudil) ophthalmic prescribing information. 2017 Dec.
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- Drug class: ophthalmic glaucoma agents