Rocklatan (Netarsudil and latanoprost) - Uses, Dosing, Side effects

Netarsudil and latanoprost are both medications used to treat glaucoma, a condition characterized by increased pressure within the eye that can lead to vision loss if left untreated.

  • Netarsudil: Netarsudil is a medication that works by increasing the drainage of fluid from the eye, thus reducing intraocular pressure (IOP). It is a Rho kinase inhibitor, which means it works by inhibiting the Rho kinase enzyme, leading to relaxation of the trabecular meshwork, a tissue in the eye responsible for draining aqueous humor. Netarsudil is typically administered as eye drops and is used once daily.
  • Latanoprost: Latanoprost belongs to a class of medications known as prostaglandin analogs. It works by increasing the outflow of aqueous humor from the eye, thereby lowering intraocular pressure. Latanoprost is also administered as eye drops and is usually taken once daily, typically in the evening.

Rocklatan is a combination of two drugs, Netarsudil and latanoprost, a Rho-kinase inhibitor and a prostaglandin analog.

Rocklatan (Netarsudil and latanoprost) Uses:

  • Elevated intraocular pressure:
    • reduction of elevated intraocular pressure in people with open-angle glaucoma or ocular hypertension

Rocklatan Dose in Adult

Rocklatan Dose in the therapy of Elevated intraocular pressure:

  • For both of these medications, the typical dose is one drop in the affected eye or eyes once a day, and it's usually done in the evening.
  • You only need to use one drop, and you don't need to use it more than once a day.

Rocklatan Dose in Children

Not indicated in children.

Pregnancy Risk Category: N (Not assigned)

  • When using eye drop medications, not much of the medicine gets into the bloodstream.
  • If you're pregnant and need to use these eye drops, it's important to use the smallest amount that still works well.
  • This helps minimize any potential risks to the baby.
  • You can also close your tear ducts after using the drops to reduce how much gets into your system.
  • Remember to check the specific instructions for each medication you use.

Use of netarsudil or latanoprost during breastfeeding

  • It's uncertain whether netarsudil or latanoprost pass into breast milk, but not much of the medication gets into your bloodstream when you use it in your eyes.
  • If you're breastfeeding and need to use these eye drops, you should weigh the potential risk of the baby being exposed to the medication against the benefits of breastfeeding for the baby and the benefits of treatment for you.

Rocklatan Dose in Kidney Disease:

  • The manufacturer's instructions don't mention any changes in dosage for people with kidney problems.
  • This is because the amount of the medication that gets into your bloodstream is very low when you use it in your eyes.
  • Therefore, it's unlikely that you would need to adjust the dosage based on kidney function.

Rocklatan Dose in Liver disease:

  • The manufacturer's instructions don't include any changes in dosage for individuals with liver issues.
  • This is because the medication is applied directly to the eyes, leading to minimal absorption into the bloodstream.
  • Consequently, it's improbable that dosage adjustments would be necessary based on liver function.

Typical Side Effects of Rocklatan (Netarsudil and latanoprost):

  • Local:
    • Application site pain
  • Ophthalmic:
    • Conjunctival hyperemia
    • Epithelial keratopathy
    • Conjunctival hemorrhage

Less Common Side Effects of Rocklatan (Netarsudil and latanoprost):

  • Ophthalmic:
    • Blurred vision
    • decreased visual acuity
    • eye discomfort
    • eye pruritus
    • increased lacrimation

Contraindications to Rocklatan (Netarsudil and latanoprost):

  • According to the manufacturer's information, there are no specific conditions or situations listed as contraindications for the use of this medication.

Cautions and alerts

Ocular effects

  • The use of these medications may cause changes in the color and increase the brown pigmentation of the iris (the colored part of the eye), the skin of the eyelids, and the eyelashes.
  • Additionally, the length and number of eyelashes may increase.
  • It's important to note that the pigmentation of the iris is likely to be permanent, although any color changes may not be noticeable for months to years.
  • However, changes in the pigmentation of the skin around the eyes and eyelashes may be reversible if you stop using the medication.

Ocular inflammation:

  • In some cases, using these medications may lead to inflammation inside the eye or worsen existing inflammation.
  • Therefore, it's important to be cautious when using them, especially if you have a history of conditions like iritis or uveitis, which involve inflammation inside the eye.
  • If you're currently experiencing active inflammation inside your eye.

Bacterial Keratitis

  • Bacterial keratitis can occur when there is accidental contamination of multiple-dose ophthalmic solutions.
  • This means that bacteria get into the eye drops, leading to an infection in the cornea.
  • It's crucial to follow proper hygiene practices when using any eye drops, including washing your hands before applying them and making sure the dropper tip doesn't touch any surfaces.
  • Additionally, avoid sharing eye drops with others to prevent the spread of bacteria.

Herpetic keratitis

  • If you have a history of herpes simplex keratitis, which is a viral infection of the eye caused by the herpes simplex virus, you should use these medications with caution.
  • There's a risk that using them might cause a reactivation of the virus.
  • It's crucial to avoid using these medications if you currently have an active outbreak of herpes simplex keratitis.

Ocular disease:

  • These medications should be used cautiously in certain individuals with specific ocular conditions.
  • For example, caution is advised when using them in individuals who have had cataract surgery without an artificial lens (aphakic), those who have had cataract surgery with a torn posterior lens capsule, or those who have risk factors for macular edema (swelling in the central part of the retina).
  • It's important to note that the safety and effectiveness of these medications have not been fully determined for individuals with certain types of glaucoma, such as angle-closure, inflammatory, or neovascular glaucoma.

Netarsudil and latanoprost: Drug Interaction

Note: Drug Interaction Categories:

  • Risk Factor C: Monitor When Using Combination
  • Risk Factor D: Consider Treatment Modification
  • Risk Factor X: Avoid Concomitant Use

Risk Factor C (Monitor therapy)

Bimatoprost

Latanoprost and Bimatoprost use concurrently has the potential to raise intraocular pressure. 

Nonsteroidal Anti-Inflammatory Agents

Prostaglandins' potential for healing effects might be diminished (Ophthalmic). The therapeutic benefits of prostaglandins may potentially be enhanced by nonsteroidal anti-inflammatory drugs (Ophthalmic). 

Nonsteroidal Anti-Inflammatory Agents (Ophthalmic)

Prostaglandins' potential for healing effects might be diminished (Ophthalmic). Nonsteroidal Anti-Inflammatory Drugs (Ophthalmic) may improve the prostaglandins' therapeutic impact (Ophthalmic).

Monitoring parameters:

Monitoring Intraocular Pressure (IOP) and Iris Pigmentation

  • Regular Monitoring: It's important to regularly check the pressure inside the eye (intraocular pressure or IOP) when using these medications.
  • Examine Iris Pigmentation: Keep an eye out for any changes in the color of the iris (the colored part of the eye). If you notice increased pigmentation (darkening) of the iris, make sure to examine the patient regularly to monitor these changes.
  • Consultation: If you observe any significant changes or have concerns about the patient's iris pigmentation, consult with a healthcare professional promptly for further evaluation and management.

How to administer Rocklatan (Netarsudil and latanoprost)?

Co-administration with Other Eye Drops

  • Combination Therapy: These eye drops can be used along with other eye drops to lower intraocular pressure (IOP) effectively.
  • Administer Separately: If using more than one type of eye drop, it's important to administer each medication at least 5 minutes apart to allow proper absorption and effectiveness.
  • Remove Contact Lenses: Before applying the eye drops, remove any contact lenses. Wait for at least 15 minutes after administering the drops before reinserting the lenses to avoid potential interactions or irritation.
  • Prevent Contamination: To minimize the risk of contamination, avoid touching the dropper tip with your fingers, eyes, eyelids, or the surrounding areas. This helps ensure the integrity of the medication and reduces the likelihood of introducing harmful bacteria.

Mechanism of action of Rocklatan (Netarsudil and latanoprost):

  • Netarsudil: Netarsudil works as a Rho kinase inhibitor. While the exact mechanism is not fully understood, it is believed to increase the outflow of aqueous humor by relaxing the trabecular meshwork, a tissue in the eye responsible for draining fluid, thus lowering intraocular pressure (IOP).
  • Latanoprost: On the other hand, Latanoprost is a prostaglandin F-alpha analog. It functions by increasing the outflow of aqueous humor through the uveoscleral pathway, another route for fluid drainage in the eye. By enhancing this drainage, latanoprost effectively reduces intraocular pressure.

Both medications work to lower intraocular pressure by facilitating the drainage of fluid from the eye, albeit through different pathways. Despite the exact mechanisms not being fully understood, their efficacy in reducing IOP has been well established in clinical practice.

Absorption:

  • The absorption of latanoprost is limited, primarily occurring through the cornea.
  • After absorption, it undergoes hydrolysis to form the biologically active acid, which can be detected in the aqueous humor within the first 4 hours and in the plasma within the first hour.

Distribution:

  • Latanoprost has a distribution volume (V) of approximately 0.16 L/kg, indicating its distribution throughout the body.

Metabolism:

  • Latanoprost is administered as an isopropyl ester prodrug, which is hydrolyzed to the active acid form in the cornea. Any biologically active acid that enters systemic circulation is primarily metabolized in the liver through fatty acid beta-oxidation.
  • Netarsudil, on the other hand, is metabolized by ophthalmic esterases to its active metabolite, AR-13503.

Half-life elimination:

  • The half-life of elimination for latanoprost is relatively short, at approximately 17 minutes, indicating rapid clearance from the body.

Excretion:

  • Latanoprost and its metabolites are primarily excreted in urine, with approximately 88% of the administered dose excreted in this way.

International Brands of Netarsudil and latanoprost:

  • Rocklatan

Netarsudil and latanoprost Brand Names in Pakistan:

No Brands Available in Pakistan.