Rhopressa (netarsudil mesylate)

Ophthalmic Antiglaucoma Agents Ophthalmic (Eye) Drops

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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.

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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.

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.

Contraindications

The manufacturer states there are no known contraindications to the use of netarsudil mesylate.

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.

Precautions

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ICD codes

CodeTypeDescription
Ocular hypertension
H40.05ICD10CMOcular hypertension
H40.051ICD10CMOcular hypertension, right eye
H40.052ICD10CMOcular hypertension, left eye
H40.053ICD10CMOcular hypertension, bilateral
H40.059ICD10CMOcular hypertension, unspecified eye
Open angle glaucoma
H40.1ICD10CMOpen-angle glaucoma
H40.10ICD10CMUnspecified open-angle glaucoma
H40.10x0ICD10CMUnspecified open-angle glaucoma, stage unspecified
H40.10x1ICD10CMUnspecified open-angle glaucoma, mild stage
H40.10x2ICD10CMUnspecified open-angle glaucoma, moderate stage
H40.10x3ICD10CMUnspecified open-angle glaucoma, severe stage
H40.10x4ICD10CMUnspecified open-angle glaucoma, indeterminate stage
H40.11ICD10CMPrimary open-angle glaucoma
H40.111ICD10CMPrimary open-angle glaucoma, right eye
H40.1110ICD10CMPrimary open-angle glaucoma, right eye, stage unspecified
H40.1111ICD10CMPrimary open-angle glaucoma, right eye, mild stage
H40.1112ICD10CMPrimary open-angle glaucoma, right eye, moderate stage
H40.1113ICD10CMPrimary open-angle glaucoma, right eye, severe stage
H40.1114ICD10CMPrimary open-angle glaucoma, right eye, indeterminate stage
H40.112ICD10CMPrimary open-angle glaucoma, left eye
H40.1120ICD10CMPrimary open-angle glaucoma, left eye, stage unspecified
H40.1121ICD10CMPrimary open-angle glaucoma, left eye, mild stage
H40.1122ICD10CMPrimary open-angle glaucoma, left eye, moderate stage
H40.1123ICD10CMPrimary open-angle glaucoma, left eye, severe stage
H40.1124ICD10CMPrimary open-angle glaucoma, left eye, indeterminate stage
H40.113ICD10CMPrimary open-angle glaucoma, bilateral
H40.1130ICD10CMPrimary open-angle glaucoma, bilateral, stage unspecified
H40.1131ICD10CMPrimary open-angle glaucoma, bilateral, mild stage
H40.1132ICD10CMPrimary open-angle glaucoma, bilateral, moderate stage
H40.1133ICD10CMPrimary open-angle glaucoma, bilateral, severe stage
H40.1134ICD10CMPrimary open-angle glaucoma, bilateral, indeterminate stage
H40.119ICD10CMPrimary open-angle glaucoma, unspecified eye
H40.1190ICD10CMPrimary open-angle glaucoma, unspecified eye, stage unspecified
H40.1191ICD10CMPrimary open-angle glaucoma, unspecified eye, mild stage
H40.1192ICD10CMPrimary open-angle glaucoma, unspecified eye, moderate stage
H40.1193ICD10CMPrimary open-angle glaucoma, unspecified eye, severe stage
H40.1194ICD10CMPrimary open-angle glaucoma, unspecified eye, indeterminate stage
H40.12ICD10CMLow-tension glaucoma
H40.121ICD10CMLow-tension glaucoma, right eye
H40.1210ICD10CMLow-tension glaucoma, right eye, stage unspecified
H40.1211ICD10CMLow-tension glaucoma, right eye, mild stage
H40.1212ICD10CMLow-tension glaucoma, right eye, moderate stage
H40.1213ICD10CMLow-tension glaucoma, right eye, severe stage
H40.1214ICD10CMLow-tension glaucoma, right eye, indeterminate stage
H40.122ICD10CMLow-tension glaucoma, left eye
H40.1220ICD10CMLow-tension glaucoma, left eye, stage unspecified
H40.1221ICD10CMLow-tension glaucoma, left eye, mild stage
H40.1222ICD10CMLow-tension glaucoma, left eye, moderate stage
H40.1223ICD10CMLow-tension glaucoma, left eye, severe stage
H40.1224ICD10CMLow-tension glaucoma, left eye, indeterminate stage
H40.123ICD10CMLow-tension glaucoma, bilateral
H40.1230ICD10CMLow-tension glaucoma, bilateral, stage unspecified
H40.1231ICD10CMLow-tension glaucoma, bilateral, mild stage
H40.1232ICD10CMLow-tension glaucoma, bilateral, moderate stage
H40.1233ICD10CMLow-tension glaucoma, bilateral, severe stage
H40.1234ICD10CMLow-tension glaucoma, bilateral, indeterminate stage
H40.129ICD10CMLow-tension glaucoma, unspecified eye
H40.1290ICD10CMLow-tension glaucoma, unspecified eye, stage unspecified
H40.1291ICD10CMLow-tension glaucoma, unspecified eye, mild stage
H40.1292ICD10CMLow-tension glaucoma, unspecified eye, moderate stage
H40.1293ICD10CMLow-tension glaucoma, unspecified eye, severe stage
H40.1294ICD10CMLow-tension glaucoma, unspecified eye, indeterminate stage
H40.13ICD10CMPigmentary glaucoma
H40.131ICD10CMPigmentary glaucoma, right eye
H40.1310ICD10CMPigmentary glaucoma, right eye, stage unspecified
H40.1311ICD10CMPigmentary glaucoma, right eye, mild stage
H40.1312ICD10CMPigmentary glaucoma, right eye, moderate stage
H40.1313ICD10CMPigmentary glaucoma, right eye, severe stage
H40.1314ICD10CMPigmentary glaucoma, right eye, indeterminate stage
H40.132ICD10CMPigmentary glaucoma, left eye
H40.1320ICD10CMPigmentary glaucoma, left eye, stage unspecified
H40.1321ICD10CMPigmentary glaucoma, left eye, mild stage
H40.1322ICD10CMPigmentary glaucoma, left eye, moderate stage
H40.1323ICD10CMPigmentary glaucoma, left eye, severe stage
H40.1324ICD10CMPigmentary glaucoma, left eye, indeterminate stage
H40.133ICD10CMPigmentary glaucoma, bilateral
H40.1330ICD10CMPigmentary glaucoma, bilateral, stage unspecified
H40.1331ICD10CMPigmentary glaucoma, bilateral, mild stage
H40.1332ICD10CMPigmentary glaucoma, bilateral, moderate stage
H40.1333ICD10CMPigmentary glaucoma, bilateral, severe stage
H40.1334ICD10CMPigmentary glaucoma, bilateral, indeterminate stage
H40.139ICD10CMPigmentary glaucoma, unspecified eye
H40.1390ICD10CMPigmentary glaucoma, unspecified eye, stage unspecified
H40.1391ICD10CMPigmentary glaucoma, unspecified eye, mild stage
H40.1392ICD10CMPigmentary glaucoma, unspecified eye, moderate stage
H40.1393ICD10CMPigmentary glaucoma, unspecified eye, severe stage
H40.1394ICD10CMPigmentary glaucoma, unspecified eye, indeterminate stage
H40.14ICD10CMCapsular glaucoma with pseudoexfoliation of lens
H40.141ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye
H40.1410ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye, stage unspecified
H40.1411ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye, mild stage
H40.1412ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye, moderate stage
H40.1413ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye, severe stage
H40.1414ICD10CMCapsular glaucoma with pseudoexfoliation of lens, right eye, indeterminate stage
H40.142ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye
H40.1420ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye, stage unspecified
H40.1421ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye, mild stage
H40.1422ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye, moderate stage
H40.1423ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye, severe stage
H40.1424ICD10CMCapsular glaucoma with pseudoexfoliation of lens, left eye, indeterminate stage
H40.143ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral
H40.1430ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral, stage unspecified
H40.1431ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral, mild stage
H40.1432ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral, moderate stage
H40.1433ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral, severe stage
H40.1434ICD10CMCapsular glaucoma with pseudoexfoliation of lens, bilateral, indeterminate stage
H40.149ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye
H40.1490ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye, stage unspecified
H40.1491ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye, mild stage
H40.1492ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye, moderate stage
H40.1493ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye, severe stage
H40.1494ICD10CMCapsular glaucoma with pseudoexfoliation of lens, unspecified eye, indeterminate stage
H40.15ICD10CMResidual stage of open-angle glaucoma
H40.151ICD10CMResidual stage of open-angle glaucoma, right eye
H40.152ICD10CMResidual stage of open-angle glaucoma, left eye
H40.153ICD10CMResidual stage of open-angle glaucoma, bilateral
H40.159ICD10CMResidual 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