Xalaprost

Approved Indications:

• Open-Angle Glaucoma (OAG): For the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma.
• Ocular Hypertension: To decrease IOP in patients with ocular hypertension where IOP elevation is a risk factor for optic nerve damage or visual field loss.

Clinically Accepted Off-Label Uses:

• Normal-Tension Glaucoma: Used in patients with normal baseline IOP who have documented glaucomatous progression.
• Secondary Glaucoma (e.g., Pseudoexfoliative, Pigmentary): As adjunctive treatment when IOP remains uncontrolled on other agents.
• Angle-Closure Glaucoma (Post-Iridotomy): Adjunct therapy after laser peripheral iridotomy in selected cases.

Adults (including Elderly):

• Recommended Dose: One drop in the affected eye(s) once daily in the evening.
• Route of Administration: Ophthalmic (topical).
• Note: More frequent administration may decrease efficacy.

Pediatric Patients (≥1 year):

• One drop in the affected eye(s) once daily in the evening.
• Safety and effectiveness in children <1 year have not been established.

Renal and Hepatic Impairment:

• No dose adjustment necessary, but use with caution. Monitor for systemic side effects due to potential accumulation.

Administration Guidelines:

• Remove contact lenses prior to instillation and wait at least 15 minutes before reinsertion.
• If using other ophthalmic medications, space at least 5 minutes apart.
• Avoid contamination by not touching the dropper tip to any surface.

Latanoprost is a prostaglandin F2α analog that selectively binds to prostanoid FP receptors in the ciliary muscle. This activation increases the outflow of aqueous humor through the uveoscleral pathway, thereby lowering intraocular pressure. The IOP-lowering effect begins within 3–4 hours, peaks at 8–12 hours, and lasts for at least 24 hours, making it suitable for once-daily dosing.

• Absorption: Rapidly absorbed through the cornea and hydrolyzed to its active form (latanoprost acid).
• Bioavailability: High local ocular bioavailability; minimal systemic absorption.
• Distribution: Confined mostly to ocular tissues.
• Metabolism: Metabolized primarily in the liver via beta-oxidation.
• Elimination: Excreted by the kidneys as inactive metabolites.
• Plasma Half-Life: Approximately 17 minutes.
• Onset of Action: Within 3–4 hours post-instillation.
• Duration of Action: Up to 24 hours.

Pregnancy:

• FDA Category C: Animal studies have shown adverse effects on the fetus; no well-controlled human studies. Use only if clearly needed.

Lactation:

• It is unknown whether latanoprost is excreted in human milk. Due to potential systemic absorption and risk to the infant, caution is advised. Consider discontinuing breastfeeding or the drug based on clinical need.

• Primary Class: Ophthalmic Antiglaucoma Agent
• Subclass: Prostaglandin F2α Analog

• Hypersensitivity to latanoprost or any component of the formulation
• Active intraocular inflammation (e.g., uveitis)
• History of herpes simplex keratitis

• Iris Pigmentation: May cause permanent increase in brown pigmentation of the iris.
• Eyelash Changes: Gradual increase in length, thickness, and number of eyelashes may occur.
• Macular Edema: Particularly in aphakic patients or those with posterior capsular rupture.
• Herpetic Eye Disease: May trigger recurrence of herpes simplex keratitis; avoid in susceptible patients.
• Intraocular Inflammation: Use cautiously in patients with a history of uveitis.
• Contact Lenses: Contains benzalkonium chloride which may discolor soft lenses. Remove lenses prior to use.
• Systemic Effects: Rare systemic absorption may cause musculoskeletal pain or respiratory symptoms.

Common (≥1%):

• Ocular: Iris pigmentation, conjunctival hyperemia, eyelash changes, eye irritation, blurred vision, dry eyes

Less Common (<1%):

• Ocular: Photophobia, eye pain, foreign body sensation
• Systemic: Headache, rash, upper respiratory tract symptoms

Serious (Rare):

• Macular edema
• Uveitis
• Reactivation of herpes keratitis

Onset & Severity:

• Iris color changes develop slowly and may be permanent.
• Eyelash and eyelid changes are reversible upon discontinuation.
• Most other effects are mild, transient, and dose-independent.

Common (≥1%):

• Ocular: Iris pigmentation, conjunctival hyperemia, eyelash changes, eye irritation, blurred vision, dry eyes

Less Common (<1%):

• Ocular: Photophobia, eye pain, foreign body sensation
• Systemic: Headache, rash, upper respiratory tract symptoms

Serious (Rare):

• Macular edema
• Uveitis
• Reactivation of herpes keratitis

Onset & Severity:

• Iris color changes develop slowly and may be permanent.
• Eyelash and eyelid changes are reversible upon discontinuation.
• Most other effects are mild, transient, and dose-independent.

• Guideline Endorsements: Continues to be a first-line agent in major international guidelines (AAO, NICE, EGS) for open-angle glaucoma and ocular hypertension.
• Safety Surveillance: Emphasis on regular monitoring for iris pigmentation and macular edema in high-risk patients.
• Combination Formulations: Increasing use of fixed-dose combinations (e.g., latanoprost + timolol) for enhanced IOP control and compliance.

• Unopened Bottle: Store at 2°C to 8°C (refrigerated). Protect from light.
• After Opening: May be stored at room temperature (up to 25°C) for up to 6 weeks.
• Do Not Freeze.
• Keep the bottle tightly closed and avoid contamination.
• Discard any unused solution after 6 weeks of opening.