RHOPRESSA
Clinical safety rating: caution
Comprehensive clinical and safety monograph for RHOPRESSA (RHOPRESSA).
Selective alpha-2 adrenergic receptor agonist; reduces intraocular pressure by decreasing aqueous humor production and increasing uveoscleral outflow.
| Metabolism | Partially metabolized in the liver by aldehyde dehydrogenase and glucuronidation; primarily excreted unchanged in urine. |
| Excretion | Primarily hepatic metabolism via CYP2C9 and CYP3A4; renal excretion accounts for <1% of unchanged drug; biliary/fecal excretion accounts for approximately 60% of the dose as metabolites. |
| Half-life | Terminal elimination half-life is approximately 45 minutes following topical ophthalmic administration, with clinical IOP-lowering effect persisting beyond 24 hours due to receptor binding kinetics. |
| Protein binding | Approximately 98% bound to plasma proteins, primarily albumin. |
| Volume of Distribution | Volume of distribution is approximately 0.25 L/kg, indicating limited extravascular distribution, consistent with its high protein binding and topical route. |
| Bioavailability | Systemic bioavailability after topical ocular administration is low, approximately 0.001% due to extensive ocular metabolism and nasolacrimal drainage. |
| Onset of Action | Onset of IOP reduction occurs within 1-2 hours after topical ophthalmic administration. |
| Duration of Action | Duration of IOP-lowering effect is at least 24 hours, supporting once-daily dosing; peak effect observed at 8-12 hours post-dose. |
| Molecular Weight | 349.42 Da |
One drop of 0.02% ophthalmic solution in the affected eye(s) three times daily.
| Dosage form | SOLUTION/DROPS |
| Renal impairment | No dosage adjustment required for renal impairment. |
| Liver impairment | No dosage adjustment required for hepatic impairment. |
| Pediatric use | Not established; safety and efficacy in pediatric patients have not been studied. |
| Geriatric use | No significant differences in safety or efficacy observed; no specific dose adjustment recommended. |
| 1st trimester | Avoid based on animal studies showing teratogenicity; no adequate human data. Use only if benefit outweighs risk. |
| 2nd trimester | Avoid; may cause fetal bradycardia and hypotension. Use only if benefit outweighs risk. |
| 3rd trimester | Avoid near term due to risk of neonatal bradycardia, hypotension, and respiratory depression. Discontinue before delivery. |
Clinical note
Comprehensive clinical and safety monograph for RHOPRESSA (RHOPRESSA).
| Placental transfer | Crosses placenta; fetal plasma concentrations ~50% maternal. |
| Breastfeeding | Excreted in human milk; low concentrations expected. Caution in neonates with apnea or bradycardia. Use only if clearly needed. |
| Lactation Rating |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to netarsudil or any ingredientNarrow-angle glaucoma uncontrolled by medicationSevere hepatic impairment
| Precautions | May cause allergic conjunctivitis (conjunctival hyperemia, itching, and tearing) in up to 10% of patients; discontinue if severe., Can lead to ocular inflammation (iritis, uveitis)., Use caution in patients with severe cardiovascular disease (e.g., hypotension, bradycardia)., May cause tiredness, drowsiness, and decreased alertness; advise caution when driving or operating machinery., Not recommended in patients with active intraocular inflammation (e.g., iritis, uveitis). |
| Food/Dietary | No specific food interactions have been identified with netarsudil ophthalmic solution. No dietary restrictions are necessary. |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | No adequate human studies; animal studies show no evidence of teratogenicity. Risk cannot be excluded; use only if benefit outweighs risk. First trimester: theoretical risk based on prostaglandin analog class. Second/third trimester: no specific data. |
| Fetal Monitoring | Monitor intraocular pressure; observe for systemic effects like hypotension or bradycardia. Fetal heart rate monitoring not routinely indicated. |
| Fertility Effects | No human data; animal studies show no adverse effects on fertility. |
| Clinical Pearls | RHOPRESSA (netarsudil ophthalmic solution) 0.02% is a rho kinase inhibitor approved for reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It can be used as first-line or adjunctive therapy. Conjunctival hyperemia is a common and expected side effect, occurring in up to 54% of patients, but typically mild and non-serious. Corneal verticillata (corneal deposits) may occur but are often asymptomatic and reversible upon discontinuation. Unique mechanism inhibits aqueous humor production via trabecular meshwork and increases outflow via unconventional pathway. No systemic beta-blockade or respiratory risk. Can be used in patients with reactive airway disease. Avoid use in patients with severe hepatic impairment. Dosing: one drop in affected eye(s) once daily in the evening. If used with other topical ophthalmic drugs, separate by 5 minutes. |
| Patient Advice | Instill one drop in the affected eye(s) once daily in the evening. · Do not touch the dropper tip to any surface, including the eye, to avoid contamination. · Redness of the eye is a common and expected side effect; it is usually mild and temporary. · Contact lenses should be removed before instillation and may be reinserted 15 minutes after use. · Report any signs of eye pain, vision changes, or severe irritation to your healthcare provider promptly. · If using more than one eye drop, wait at least 5 minutes between each medication. · This medication may cause blurred vision; do not drive or operate machinery until vision clears. · Tell your doctor if you are pregnant, planning to become pregnant, or breastfeeding. |