Elevated IOP in open-angle glaucoma or ocular hypertension
1 drop in the affected eye(s) once daily in the evening
Lowers IOP 3.9 to 4.7 mm Hg from baseline, sustained over 6 months.
OFF-LABELNot in the FDA label for this product
Corneal edema from Fuchs endothelial corneal dystrophy
0.02%, 1 drop once daily for 8 weeks; twice daily was also studied, with no significant difference between the two regimens at any time point
Phase 2 open-label · n=40
Phase 2 randomized open-label parallel-group trial, 40 patients with central corneal thickness 600 micrometers or more: mean central corneal thickness fell 28.4 micrometers at week 4 on once-daily dosing (P=0.0021) and 20.1 micrometers on twice-daily (P=0.0335), 12.5% of patients had complete resolution of corneal edema, and 25% gained 10 or more letters at week 4 (5 patients in each arm). Reticular edema developed in one patient on twice-daily dosing and resolved on discontinuation; this indication is not FDA approved.
0.02% (0.2 mg/mL) ophthalmic solution, 2.5 mL fill in a 4 mL bottle
Mechanism of Action
Rho kinase and norepinephrine transporter inhibitor that lowers IOP by increasing aqueous outflow through the trabecular meshwork, with the exact mechanism unknown per the label. A phase 2 aqueous humor dynamics trial in open-angle glaucoma and ocular hypertension measured increased outflow facility (treatment difference 0.03 microliters/min/mm Hg) and lower episcleral venous pressure (treatment difference 0.89 mm Hg), placing the effect on both the proximal and distal conventional pathway.
Warnings & Precautions
Epithelial corneal edema: Honeycomb or bullous edema in eyes with pre-existing corneal stromal edema or after procedures that could affect corneal endothelial function; typically resolves after discontinuation, so new eye pain or decreased vision warrants prompt evaluation.
Bacterial keratitis: Reported with contaminated multidose containers, in most cases in eyes with concurrent corneal disease or a disrupted epithelial surface.
Soft contact lenses: Benzalkonium chloride 0.015% may be absorbed by soft lenses; remove before instillation and reinsert after 15 minutes.
Common Side Effects
Ocular: Conjunctival hyperemia 53%, the most common reaction, with 6% of patients discontinuing therapy for it; corneal verticillata, instillation site pain, and conjunctival hemorrhage each approximately 20%; instillation site erythema, corneal staining, blurred vision, increased lacrimation, eyelid erythema, and reduced visual acuity in 5% to 10%.
Corneal verticillata: First noted at 4 weeks of daily dosing, without apparent change in visual function, and resolving in most patients after discontinuation.
Postmarketing: Epithelial corneal edema in patients with pre-existing corneal stromal edema or after ocular procedures that could affect corneal endothelial function; frequency not estimable.
Pregnancy & Lactation
Pregnancy: No human data, and systemic exposure after ocular dosing is low; IV dosing of pregnant rats and rabbits through organogenesis produced no adverse embryofetal effects at clinically relevant systemic exposures. In rats, abortion and embryofetal lethality occurred at 126 times the plasma exposure at the recommended human ophthalmic dose by Cmax (NOAEL 40 times), and in rabbits, embryofetal lethality at 1480 times and malformations at 1330 times and above (NOAEL 214 times).
Lactation: No data on presence in human milk, effects on the breastfed infant, or effects on milk production; systemic exposure after ocular dosing is low.
Pediatric Use
Safety and effectiveness below age 18 not established.
Available Forms
Mechanism of Action
Pregnancy & Lactation
Pediatric Use