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Netarsudil and Latanoprost

Medically reviewed by Drugs.com. Last updated on Aug 20, 2020.

Pronunciation

(ne TAR soo dil & la TA noe prost)

Index Terms

  • Latanoprost and Netarsudil
  • Netarsudil Dimesylate and Latanoprost

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]

Brand Names: U.S.

  • Rocklatan

Pharmacologic Category

  • Ophthalmic Agent, Antiglaucoma
  • Prostaglandin, Ophthalmic
  • Rho Kinase Inhibitor

Pharmacology

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.

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.

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). May be stored at 2°C to 25°C (36°F to 77°F) after opening for up to 6 weeks; if stored under refrigeration after opening, product can be used until expiration date. 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 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

What is this drug used for?

• It is used to treat glaucoma.

• It is used to lower high eye pressure.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Blurred vision

• Increased tears

• Burning

• Stinging

• Eyelash growth

• Foreign body sensation in eye

• Eyelash changes

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Vision changes

• Eye pain

• Severe eye irritation

• Bleeding in the eye

• Eye discoloration

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.