Rhopressa (netarsudil mesylate)
Ophthalmic Antiglaucoma Agents Ophthalmic (Eye) Drops
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)
Drug class: Ophthalmic Antiglaucoma Agents
Therapeutic class: Ophthalmic Agents
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.
| Drug label | Dosing type | Instructions |
|---|---|---|
| Rhopressa 0.02% Ophth Solution | Maintenance | Instill 1 drop into affected eye(s) by ophthalmic route once daily inthe evening. |
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.
- Corneal edema
- Surgical procedure on eye proper
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.
Less Frequent
- Corneal edema
Rare or Very Rare
- Bacterial keratitis
More Frequent
- Conjunctival hemorrhage
- Conjunctival hyperemia
- Corneal verticillata
- Ocular pain
Less Frequent
- Blurred vision
- Corneal staining
- Eye tearing
- Eyelid erythema
- Reduced visual acuity
Precautions
No enhanced messaging available.
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
| Code | Type | Description |
|---|---|---|
| Ocular hypertension | ||
| H40.05 | ICD10CM | Ocular hypertension |
| H40.051 | ICD10CM | Ocular hypertension, right eye |
| H40.052 | ICD10CM | Ocular hypertension, left eye |
| H40.053 | ICD10CM | Ocular hypertension, bilateral |
| H40.059 | ICD10CM | Ocular hypertension, unspecified eye |
| Open angle glaucoma | ||
| H40.1 | ICD10CM | Open-angle glaucoma |
| H40.10 | ICD10CM | Unspecified open-angle glaucoma |
| H40.10x0 | ICD10CM | Unspecified open-angle glaucoma, stage unspecified |
| H40.10x1 | ICD10CM | Unspecified open-angle glaucoma, mild stage |
| H40.10x2 | ICD10CM | Unspecified open-angle glaucoma, moderate stage |
| H40.10x3 | ICD10CM | Unspecified open-angle glaucoma, severe stage |
| H40.10x4 | ICD10CM | Unspecified open-angle glaucoma, indeterminate stage |
| H40.11 | ICD10CM | Primary open-angle glaucoma |
| H40.111 | ICD10CM | Primary open-angle glaucoma, right eye |
| H40.1110 | ICD10CM | Primary open-angle glaucoma, right eye, stage unspecified |
| H40.1111 | ICD10CM | Primary open-angle glaucoma, right eye, mild stage |
| H40.1112 | ICD10CM | Primary open-angle glaucoma, right eye, moderate stage |
| H40.1113 | ICD10CM | Primary open-angle glaucoma, right eye, severe stage |
| H40.1114 | ICD10CM | Primary open-angle glaucoma, right eye, indeterminate stage |
| H40.112 | ICD10CM | Primary open-angle glaucoma, left eye |
| H40.1120 | ICD10CM | Primary open-angle glaucoma, left eye, stage unspecified |
| H40.1121 | ICD10CM | Primary open-angle glaucoma, left eye, mild stage |
| H40.1122 | ICD10CM | Primary open-angle glaucoma, left eye, moderate stage |
| H40.1123 | ICD10CM | Primary open-angle glaucoma, left eye, severe stage |
| H40.1124 | ICD10CM | Primary open-angle glaucoma, left eye, indeterminate stage |
| H40.113 | ICD10CM | Primary open-angle glaucoma, bilateral |
| H40.1130 | ICD10CM | Primary open-angle glaucoma, bilateral, stage unspecified |
| H40.1131 | ICD10CM | Primary open-angle glaucoma, bilateral, mild stage |
| H40.1132 | ICD10CM | Primary open-angle glaucoma, bilateral, moderate stage |
| H40.1133 | ICD10CM | Primary open-angle glaucoma, bilateral, severe stage |
| H40.1134 | ICD10CM | Primary open-angle glaucoma, bilateral, indeterminate stage |
| H40.119 | ICD10CM | Primary open-angle glaucoma, unspecified eye |
| H40.1190 | ICD10CM | Primary open-angle glaucoma, unspecified eye, stage unspecified |
| H40.1191 | ICD10CM | Primary open-angle glaucoma, unspecified eye, mild stage |
| H40.1192 | ICD10CM | Primary open-angle glaucoma, unspecified eye, moderate stage |
| H40.1193 | ICD10CM | Primary open-angle glaucoma, unspecified eye, severe stage |
| H40.1194 | ICD10CM | Primary open-angle glaucoma, unspecified eye, indeterminate stage |
| H40.12 | ICD10CM | Low-tension glaucoma |
| H40.121 | ICD10CM | Low-tension glaucoma, right eye |
| H40.1210 | ICD10CM | Low-tension glaucoma, right eye, stage unspecified |
| H40.1211 | ICD10CM | Low-tension glaucoma, right eye, mild stage |
| H40.1212 | ICD10CM | Low-tension glaucoma, right eye, moderate stage |
| H40.1213 | ICD10CM | Low-tension glaucoma, right eye, severe stage |
| H40.1214 | ICD10CM | Low-tension glaucoma, right eye, indeterminate stage |
| H40.122 | ICD10CM | Low-tension glaucoma, left eye |
| H40.1220 | ICD10CM | Low-tension glaucoma, left eye, stage unspecified |
| H40.1221 | ICD10CM | Low-tension glaucoma, left eye, mild stage |
| H40.1222 | ICD10CM | Low-tension glaucoma, left eye, moderate stage |
| H40.1223 | ICD10CM | Low-tension glaucoma, left eye, severe stage |
| H40.1224 | ICD10CM | Low-tension glaucoma, left eye, indeterminate stage |
| H40.123 | ICD10CM | Low-tension glaucoma, bilateral |
| H40.1230 | ICD10CM | Low-tension glaucoma, bilateral, stage unspecified |
| H40.1231 | ICD10CM | Low-tension glaucoma, bilateral, mild stage |
| H40.1232 | ICD10CM | Low-tension glaucoma, bilateral, moderate stage |
| H40.1233 | ICD10CM | Low-tension glaucoma, bilateral, severe stage |
| H40.1234 | ICD10CM | Low-tension glaucoma, bilateral, indeterminate stage |
| H40.129 | ICD10CM | Low-tension glaucoma, unspecified eye |
| H40.1290 | ICD10CM | Low-tension glaucoma, unspecified eye, stage unspecified |
| H40.1291 | ICD10CM | Low-tension glaucoma, unspecified eye, mild stage |
| H40.1292 | ICD10CM | Low-tension glaucoma, unspecified eye, moderate stage |
| H40.1293 | ICD10CM | Low-tension glaucoma, unspecified eye, severe stage |
| H40.1294 | ICD10CM | Low-tension glaucoma, unspecified eye, indeterminate stage |
| H40.13 | ICD10CM | Pigmentary glaucoma |
| H40.131 | ICD10CM | Pigmentary glaucoma, right eye |
| H40.1310 | ICD10CM | Pigmentary glaucoma, right eye, stage unspecified |
| H40.1311 | ICD10CM | Pigmentary glaucoma, right eye, mild stage |
| H40.1312 | ICD10CM | Pigmentary glaucoma, right eye, moderate stage |
| H40.1313 | ICD10CM | Pigmentary glaucoma, right eye, severe stage |
| H40.1314 | ICD10CM | Pigmentary glaucoma, right eye, indeterminate stage |
| H40.132 | ICD10CM | Pigmentary glaucoma, left eye |
| H40.1320 | ICD10CM | Pigmentary glaucoma, left eye, stage unspecified |
| H40.1321 | ICD10CM | Pigmentary glaucoma, left eye, mild stage |
| H40.1322 | ICD10CM | Pigmentary glaucoma, left eye, moderate stage |
| H40.1323 | ICD10CM | Pigmentary glaucoma, left eye, severe stage |
| H40.1324 | ICD10CM | Pigmentary glaucoma, left eye, indeterminate stage |
| H40.133 | ICD10CM | Pigmentary glaucoma, bilateral |
| H40.1330 | ICD10CM | Pigmentary glaucoma, bilateral, stage unspecified |
| H40.1331 | ICD10CM | Pigmentary glaucoma, bilateral, mild stage |
| H40.1332 | ICD10CM | Pigmentary glaucoma, bilateral, moderate stage |
| H40.1333 | ICD10CM | Pigmentary glaucoma, bilateral, severe stage |
| H40.1334 | ICD10CM | Pigmentary glaucoma, bilateral, indeterminate stage |
| H40.139 | ICD10CM | Pigmentary glaucoma, unspecified eye |
| H40.1390 | ICD10CM | Pigmentary glaucoma, unspecified eye, stage unspecified |
| H40.1391 | ICD10CM | Pigmentary glaucoma, unspecified eye, mild stage |
| H40.1392 | ICD10CM | Pigmentary glaucoma, unspecified eye, moderate stage |
| H40.1393 | ICD10CM | Pigmentary glaucoma, unspecified eye, severe stage |
| H40.1394 | ICD10CM | Pigmentary glaucoma, unspecified eye, indeterminate stage |
| H40.14 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens |
| H40.141 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye |
| H40.1410 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye, stage unspecified |
| H40.1411 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye, mild stage |
| H40.1412 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye, moderate stage |
| H40.1413 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye, severe stage |
| H40.1414 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, right eye, indeterminate stage |
| H40.142 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye |
| H40.1420 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye, stage unspecified |
| H40.1421 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye, mild stage |
| H40.1422 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye, moderate stage |
| H40.1423 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye, severe stage |
| H40.1424 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, left eye, indeterminate stage |
| H40.143 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral |
| H40.1430 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral, stage unspecified |
| H40.1431 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral, mild stage |
| H40.1432 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral, moderate stage |
| H40.1433 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral, severe stage |
| H40.1434 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, bilateral, indeterminate stage |
| H40.149 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye |
| H40.1490 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye, stage unspecified |
| H40.1491 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye, mild stage |
| H40.1492 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye, moderate stage |
| H40.1493 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye, severe stage |
| H40.1494 | ICD10CM | Capsular glaucoma with pseudoexfoliation of lens, unspecified eye, indeterminate stage |
| H40.15 | ICD10CM | Residual stage of open-angle glaucoma |
| H40.151 | ICD10CM | Residual stage of open-angle glaucoma, right eye |
| H40.152 | ICD10CM | Residual stage of open-angle glaucoma, left eye |
| H40.153 | ICD10CM | Residual stage of open-angle glaucoma, bilateral |
| H40.159 | ICD10CM | Residual stage of open-angle glaucoma, unspecified eye |
ICD code information from First Databank (FDB).
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Last reviewed · Source: First Databank (FDB) drug data
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