Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Solution, Ophthalmic:
Rocklatan: Netarsudil dimesylate 0.02% and latanoprost 0.005% (2.5 mL) [contains benzalkonium chloride]
Pharmacology
Mechanism of Action
Although the exact mechanism is unknown, netarsudil is a Rho kinase inhibitor and latanoprost is a prostaglandin F2-alpha analog, and both may reduce intraocular pressure by increasing the outflow of aqueous humor.
Pharmacokinetics/Pharmacodynamics
Absorption
Limited. Latanoprost is absorbed through the cornea and hydrolyzed to the biologically active acid (measurable in the aqueous humor during the first 4 hours and in the plasma during the first hour).
Distribution
Latanoprost: Vd: 0.16 ± 0.02 L/kg
Metabolism
Latanoprost: Isopropyl ester prodrug is hydrolyzed to the biologically active acid in the cornea. Biologically active acid reaching systemic circulation is primarily metabolized hepatically via fatty acid beta-oxidation.
Netarsudil: Metabolized by ophthalmic esterases to active metabolite, AR-13503
Excretion
Latanoprost: Urine: ~88% (as metabolites)
Half-Life Elimination
Latanoprost: 17 minutes
Use: Labeled Indications
Elevated intraocular pressure: Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension
Contraindications
There are no contraindications listed in the manufacturer's labeling.
Dosage and Administration
Dosing: Adult
Elevated intraocular pressure: Ophthalmic: One drop in the affected eye(s) once daily in the evening (maximum: 1 drop in affected eye(s) once daily).
Dosing: Geriatric
Refer to adult dosing.
Administration
Ophthalmic: May be used with other eye drops to lower IOP. If more than one topical ophthalmic drug is being used, administer the drugs at least 5 minutes apart. Remove contact lenses prior to administration and wait 15 minutes before reinserting. Avoid touching the dropper tip with fingers, eyes, eyelids, or surrounding areas to minimize contamination of the dropper tip.
Storage
Store at 2°C to 8°C (36°F to 46°F). Protect from light. May be maintained at temperatures up to 40°C (104°F) for up to 14 days during shipment.
Drug Interactions
Bimatoprost: The concomitant use of Latanoprost and Bimatoprost may result in increased intraocular pressure. Monitor therapy
Nonsteroidal Anti-Inflammatory Agents: May diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents may also enhance the therapeutic effects of Prostaglandins (Ophthalmic). Monitor therapy
Nonsteroidal Anti-Inflammatory Agents (Ophthalmic): May diminish the therapeutic effect of Prostaglandins (Ophthalmic). Nonsteroidal Anti-Inflammatory Agents (Ophthalmic) may enhance the therapeutic effect of Prostaglandins (Ophthalmic). Monitor therapy
Adverse Reactions
See individual agents.
>10%:
Local: Application site pain (20%)
Ophthalmic: Conjunctival hyperemia (59%), epithelial keratopathy (15%), conjunctival hemorrhage (11%)
1% to 10%: Ophthalmic: Blurred vision (5% to 8%), decreased visual acuity (5% to 8%), eye discomfort (5% to 8%), eye pruritus (5% to 8%), increased lacrimation (5% to 8%)
Warnings/Precautions
Concerns related to adverse effects:
- Bacterial keratitis: Inadvertent contamination of multiple-dose ophthalmic solutions has caused bacterial keratitis.
- Ocular effects: May change/increase brown pigmentation of the iris, the eyelid skin, and eyelashes; length and/or number of eyelashes may also be increased. Pigmentation of the iris is likely to be permanent although iris color change may not be noticeable for months to years; pigmentation of the periorbital tissue and eyelash changes may be reversible following discontinuation of therapy. Long-term consequences and potential injury to eye are not known.
- Ocular inflammation: Intraocular inflammation and exacerbation of inflammation may occur; use with caution in patients with a history of intraocular inflammation (eg, iritis/uveitis) and generally avoid use in patients with active intraocular inflammation.
Disease-related concerns:
- Herpetic keratitis: Use with caution in patients with a history of herpes simplex keratitis; reactivation may occur. Avoid use in patients with active herpes simplex keratitis.
- Ocular disease: Use with caution in aphakic patients, pseudophakic patients with a torn posterior lens capsule, or patients with risk factors for macular edema. Safety and efficacy have not been determined for use in patients with angle-closure, inflammatory, or neovascular glaucoma.
Special populations:
- Contact lens wearers: Solution contains benzalkonium chloride which may be absorbed by contact lenses. Remove contacts prior to administration and wait 15 minutes before reinserting.
Other warnings/precautions:
- Appropriate use: Avoid concurrent use of 2 or more prostaglandins or prostaglandin analogs or more frequent administration than once daily; may decrease the IOP lowering effect or cause paradoxical elevations in IOP.
Monitoring Parameters
Monitor IOP; regularly examine patients who develop increased iris pigmentation.
Pregnancy
Pregnancy Considerations
Systemic absorption is limited following ophthalmic application.
If ophthalmic agents are needed during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Samples 1988). Also refer to individual monographs.
Patient Education
- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
- Patient may experience blurred vision, increased tears, burning, stinging, eyelash growth, foreign body sensation in eye, or eyelash changes. Have patient report immediately to prescriber vision changes, eye pain, severe eye irritation, bleeding in the eye, or eye discoloration (HCAHPS).
- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.
