Rhopressa (netarsudil mesylate)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Netarsudil mesylate, a rho kinase (ROCK) inhibitor and norepinephrine transporter (NET) inhibitor, is an ocular hypotensive agent.
Netarsudil mesylate, a rho kinase (ROCK) inhibitor and norepinephrine transporter (NET) inhibitor, is an ocular hypotensive agent.
Although the exact mechanism of action of netarsudil in the reduction of intraocular pressure (IOP) is unknown, multiple mechanisms appear to be involved. The active metabolite of netarsudil appears to reduce IOP by increasing the outflow of aqueous humor through the trabecular meshwork and by decreasing episcleral venous pressure through its inhibitory effect on rho kinases. The drug also appears to decrease the production of aqueous humor through its inhibitory effect on the norepinephrine transporter.
Netarsudil mesylate is a prodrug that is absorbed through the cornea and into the aqueous humor following ocular instillation; the drug is metabolized by corneal esterases to its active form (netarsudil-M1; AR-13503). Topical administration of netarsudil mesylate to the eyes does not produce clinically important systemic exposure to the drug or its active metabolite. Following topical administration of 1 drop of netarsudil 0.02% solution to each eye once daily for 8 days in 18 healthy adults, plasma concentrations of netarsudil were undetectable (lower limit of quantitation 0.1 ng/mL) on days 1 and 8.
Netarsudil-M1 was detected in the plasma of only one individual in this study and only at one time point (0.11 ng/mL at 8 hours post-dose on day 8). Data from a study in rabbits indicate that the elimination half-life of netarsudil from aqueous humor is 16-17 hours and the effects of the drug on IOP persist for up to 24 hours or longer.
USES: Netarsudil is used to treat high pressure inside the eye due to certain eye conditions (such as open-angle glaucoma, ocular hypertension). This medication is thought to work by increasing the flow of fluid out of the eye. This helps lower pressure inside the eye.
Lowering high pressure inside the eye can help prevent loss of vision or blindness.
Generic name: netarsudil mesylate
Pronunciation: (ne-TAR-soo-dil)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Rhopressa
Indications
The following indications are listed for Rhopressa:
- Ocular Hypertension
- Open Angle Glaucoma
Also known as: Chronic Glaucoma, Compensated Glaucoma, Glaucoma Simplex, Increased Intraocular Pressure, Increased Iop, Open-Angle Glaucoma, Raised Intraocular Pressure, Simple Glaucoma.
Dosing
Dosage and concentration of netarsudil mesylate are expressed in terms of netarsudil.
For the treatment of open-angle glaucoma or ocular hypertension in adults, 1 drop of netarsudil 0.02% ophthalmic solution should be instilled in the affected eye(s) once daily in the evening. Twice-daily dosing of netarsudil ophthalmic solution is not well tolerated and is not recommended.
If the target intraocular pressure (IOP) is not achieved, alternative or additional ocular hypotensive agents may be required. (See Uses: Ocular Hypertension and Glaucoma.) When netarsudil is used in fixed combination with latanoprost, the usual adult dosage is 1 drop of an ophthalmic solution containing netarsudil 0.02% and latanoprost 0.005% in the affected eye(s) once daily in the evening. The fixed combination should not be administered more frequently than once daily.
Netarsudil mesylate administered alone or in fixed combination with latanoprost is applied topically to the eye(s) as an ophthalmic solution.
Care should be taken to avoid contaminating the solution container. (See Bacterial Keratitis under Cautions: Warnings/Precautions.)
Contact lenses should be removed prior to administration of netarsudil ophthalmic solution or netarsudil and latanoprost fixed-combination ophthalmic solution; contact lenses may be reinserted 15 minutes following administration of the drug. (See Use with Contact Lenses under Cautions: Warnings/Precautions.)
If the patient is receiving more than one topical ophthalmic preparation, the preparations should be administered at least 5 minutes apart.
If a dose is missed, the dose should be skipped and treatment should be resumed with the next scheduled dose.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
No formal drug interaction studies using topical ophthalmic netarsudil mesylate have been performed to date. However, interactions are not expected because of limited systemic exposure following topical application to the eye.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
The manufacturer states there are no known contraindications to the use of netarsudil mesylate.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effect of netarsudil ophthalmic solution is conjunctival hyperemia, which was reported in 53% of patients receiving the drug in clinical trials; 6% of patients required discontinuance of therapy because of this adverse effect. Other common adverse ocular effects of the drug include corneal verticillata, instillation site pain, and conjunctival hemorrhage, which were reported in approximately 20% of patients. Instillation site erythema, corneal staining, blurred vision, increased lacrimation, eyelid erythema, and reduced visual acuity were reported in 5-10% of patients.
In controlled clinical trials evaluating netarsudil and latanoprost fixed-combination ophthalmic solution, conjunctival hyperemia was reported in 59% of patients receiving the fixed-combination ophthalmic solution; 5% of patients required discontinuance of therapy because of this adverse effect. Instillation site pain, corneal verticillata, and conjunctival hemorrhage were reported in 11-20% of patients receiving the fixed-combination ophthalmic solution. Ocular pruritus, decreased visual acuity, increased lacrimation, instillation site discomfort, and blurred vision were reported in 5-8% of patients.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Safety and efficacy of topical ophthalmic netarsudil in pediatric patients younger than 18 years of age have not been established.
There are no data available regarding topical ophthalmic use of netarsudil in pregnant women to inform any drug-associated risk; however, systemic exposure to the drug following topical application to the eye is low.
In pregnant rats and rabbits, IV netarsudil administered during organogenesis did not produce adverse embryofetal effects at clinically relevant systemic exposures. However, abortions and embryofetal lethality occurred in rats at IV dosages of 0.3 mg/kg daily or greater (126 times the human plasma exposure at the recommended daily ophthalmic dosage). In rabbits, malformations (thoracogastroschisis, umbilical hernia, absent intermediate lung lobe) occurred at IV dosages of 3 mg/kg daily or greater (1330 times the human plasma exposure at the recommended daily ophthalmic dosage) and embryofetal lethality and decreased fetal weight occurred at IV dosages of 5 mg/kg daily (1480 times the human plasma exposure at the recommended human daily ophthalmic dosage).
It is not known whether netarsudil and/or its metabolite are distributed into human milk following topical application to the eye. Data also are not available on the effects of the drug on the breast-fed child or on milk production. However, systemic exposure to the drug following topical application to the eye is low.
The benefits of breast-feeding should be considered along with the importance of netarsudil to the woman and any potential adverse effects on the breast-fed child from the drug.
No overall differences in safety or efficacy of topical ophthalmic netarsudil have been observed between geriatric patients and younger adults.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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