latanoprost/netarsudil ophthalmic (Rx)

Brand and Other Names:Rocklatan
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Dosing & Uses


Dosage Forms & Strengths


ophthalmic solution

  • 0.02%/0.005% (0.2mg/mL and 0.05mg/mL)
  • Bottle: 2.5-mL fill in 4-mL container

Elevated Intraocular Pressure

Indicated for reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension

Instill 1 drop in affected eye(s) qDay in evening; not to exceed 1 dose/day

Dosing Considerations

May be used concomitantly with other topical ophthalmic drug products to lower IOP

If other topical ophthalmics are used, administer drops at least 5 minutes apart

Safety and efficacy not established



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            Adverse Effects


            Conjunctival hyperemia (59%)

            Instillation site pain (20%)

            Corneal verticillata (15%)

            Conjunctival hemorrhage (11%)


            Eye pruritus (5-8%)

            Reduced visual acuity (5-8%)

            Increased lacrimation (5-8%)

            Instillation site discomfort (5-8%)

            Blurred vision (5-8%)

            Frequency Not Defined (Netarsudil)

            Instillation site erythema

            Corneal staining

            Increased lacrimation

            Eyelid erythema

            Frequency Not Defined (Latanoprost)

            Foreign body sensation

            Punctate keratitis

            Burning and stinging


            Increased iris pigmentation

            Excessive tearing

            Eyelid discomfort

            Dry eye

            Eye pain

            Eyelid margin crusting

            Eyelid erythema/edema

            Upper respiratory tract infection/nasopharyngitis/influenza


            Myalgia/arthralgia/back pain

            Rash/allergic reactions






            Latanoprost reported to cause changes to pigmented tissues (owing to increased melanin content in melanocytes), including increased pigmentation of the iris, periorbital tissue, and eyelashes; pigmentation is expected to increase as long as latanoprost is administered; inform patients of possibility of increased pigmentation

            Latanoprost may gradually change eyelashes and vellus hair in the treated eye; changes include increased length, thickness, pigmentation, number of lashes or hairs, and misdirected growth of eyelashes; eyelash changes are usually reversible when treatment discontinued

            Caution with history of intraocular inflammation (iritis/uveitis); should generally not be used with active intraocular inflammation because latanoprost may exacerbate inflammation

            Macular edema, including cystoid macular edema, reported with latanoprost; caution in aphakic patients, pseudophakic patients with a torn posterior lens capsule, or those with known risk factors for macular edema

            Reactivation of herpes simplex keratitis reported with latanoprost; caution with history of herpetic keratitis; avoid with active herpes simplex keratitis as administration may exacerbate inflammation

            Risk of bacterial keratitis associated with use of multiple-dose containers of topical ophthalmic products

            Remove contact lenses before administration

            Drug interaction overview

            • In vitro studies show precipitation of latanoprost solution occurs when mixed with thimerosal-containing ophthalmic drops
            • Combining 2 or more prostaglandins or prostaglandin analogues is not recommended; administration of prostaglandin drug products more than once daily may mitigate the IOP-lowering effect or cause paradoxical elevations in IOP



            There are no available data regarding ophthalmic use in pregnant women

            Animal studies

            • Reproduction studies of latanoprost showed embryofetal lethality in rabbits; no embryofetal lethality was observed at a dose ~15 times higher than the recommended human ophthalmic dose (RHOD); in 4 of 16 pregnant rabbits, no viable fetuses were present at a dose ~80 times RHOD
            • IV administration of netarsudil to pregnant rats and rabbits during organogenesis did not produce adverse embryofetal effects at clinically relevant systemic exposures


            No data are available regarding the presence of netarsudil or latanoprost in human milk, the effects on the breastfed infant, or the effects on milk production

            Systemic exposure to netarsudil following topical ocular administration is low, and it is not known whether measurable levels of netarsudil would be present in maternal milk following topical ocular administration

            Consider the development and health benefits of breastfeeding along with the mother’s clinical need for the drug and any potential adverse effects on the breastfed child or from the underlying maternal condition

            Pregnancy Categories

            A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

            B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

            C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

            D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

            X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

            NA: Information not available.



            Mechanism of Action

            Latanoprost: Prostaglandin F2-alpha analog; increases outflow of aqueous humor

            Netarsudil: Dual inhibitor of Rho-kinase and the norepinephrine plasma membrane transport protein; increases trabecular outflow


            Netarsudil and active metabolite: Little to no quantifiable plasma concentrations measured during 8 days of daily use


            Latanoprost: 0.16 L/kg


            Netarsudil: Metabolized by esterases in the eye to an active metabolite, AR-13503

            Latanoprost: Hydrolyzed by esterases in the cornea to the biologically active acid; active acid that reaches systemic circulation is primarily metabolized by the liver to the 1,2-dinor and 1,2,3,4-tetranor metabolites via fatty acid beta-oxidation



            • Half-life: 17 minutes
            • Clearance: 7 mL/min/kg
            • Excretion: Urine 88%


            Ophthalmic Administration

            Instruct patient on proper technique of administering ophthalmic drops and how to avoid contaminating the container

            Concomitant use with other ophthalmics: Administer at least 5 minutes apart

            Contact lenses: Remove contacts before administering ophthalmic drops; may reinsert 15 minutes afterwards; contains benzalkonium chloride, which may be absorbed by soft contact lenses

            Missed dose: If dose is missed, continue treatment with the next dose in the evening; do not exceed 1 dose/day


            Protect from light

            Store at 2-8°C (36-46°F)

            During shipment, the bottle may be maintained at temperatures up to 40°C (104°F) for a period not exceeding 14 days

            After opening, bottle can be used until expiration date





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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.