Xalatan^® (Drops) Instructions for Use

Marketing Authorization Holder

Viatris Specialty, LLC (USA)

Manufactured By

Pfizer Manufacturing Belgium, NV (Belgium)

ATC Code

S01EE01 (Latanoprost)

Active Substance

Latanoprost (Rec.INN registered by WHO)

Dosage Form

Xalatan®

Eye drops 0.005%: bottle 2.5 ml 1 or 3 pcs.

Dosage Form, Packaging, and Composition

Eye drops in the form of a clear, colorless solution.

Excipients: sodium chloride, benzalkonium chloride, sodium dihydrogen phosphate monohydrate, anhydrous disodium hydrogen phosphate, water for injections.

2.5 ml – polyethylene bottles (1) with a dropper tip – cardboard packs^×.
2.5 ml – polyethylene bottles (3) with a dropper tip – cardboard packs^×.

^× on the front side of the cardboard pack, for the purpose of controlling the first opening, a perforated line resembling the outline of half-rings is applied; the side surfaces of the pack are tightly glued during packaging of the drug.
Note control of the first opening is ensured by attaching the protective cap to the bottle body with plastic bridges.
Not all package sizes may be marketed.

Clinical-Pharmacological Group

Antiglaucoma drug – synthetic prostaglandin F2α analogue

Pharmacotherapeutic Group

Antiglaucoma agent – synthetic prostaglandin F_2α analogue

Pharmacological Action

Antiglaucoma agent. An analogue of prostaglandin F_2α, it is a selective agonist of FP receptors. Reduces intraocular pressure by increasing uveoscleral outflow of aqueous humor. It does not significantly affect the production of aqueous humor and the blood-ophthalmic barrier.

It is an isopropyl ester – an inactive precursor, the hydrolysis of which leads to the formation of the pharmacologically active acid latanoprost.

Pharmacokinetics

Latanoprost is a prodrug, esterified with an isopropyl group, and is inactive; after hydrolysis to the acid form, it becomes biologically active.

The prodrug is well absorbed through the cornea and is completely hydrolyzed upon entering the aqueous humor. The C_max of latanoprost in the aqueous humor is reached 2 hours after instillation.

The active form of latanoprost is practically not metabolized in the eye, but undergoes biotransformation in the liver.

The T_1/2 from plasma is 17 minutes.

Indications

Reduction of elevated intraocular pressure in adults and children (over 1 year of age) with open-angle glaucoma or ocular hypertension.

ICD codes

Dosage Regimen

Instill one drop into the affected eye(s)once daily.

Administer the dose in the evening to maximize intraocular pressure reduction.

Do not exceed the recommended once-daily dosage; more frequent application reduces the hypotensive effect.

If a dose is missed, continue with the next scheduled dose; do not double the dose.

Prior to instillation, remove contact lenses; lenses may be reinserted 15 minutes after administration.

To minimize systemic absorption, apply gentle pressure to the lacrimal sac (at the inner corner of the eye) for one minute immediately after instillation.

If using other topical ophthalmic products, maintain an interval of at least 5 minutes between applications.

Avoid allowing the dropper tip to contact the eye or any other surface to prevent contamination of the solution.

Adverse Reactions

Infections and infestations frequency unknown – herpetic keratitis.

Eye disorders very common – iris hyperpigmentation, conjunctival hyperemia, mild to moderate eye irritation (burning sensation, gritty feeling, itching, tingling and foreign body sensation), eyelash changes (increased length, thickness, number and pigmentation); common – transient punctate epithelial erosions (mostly asymptomatic), blepharitis, eye pain; uncommon – eyelid edema, eye dryness, keratitis, blurred vision, conjunctivitis; rare – iritis/uveitis (mainly in predisposed patients), macular edema, eyelid edema, corneal edema, corneal erosion, periorbital edema, darkening of the eyelid skin, eyelid skin reactions, change in eyelash growth direction, thickening, darkening and lengthening of eyelashes, distichiasis, photophobia; very rare – changes in the periorbital area and eyelash area leading to deepening of the upper eyelid sulcus; frequency unknown – iris cyst, conjunctival pseudopemphigoid.

Nervous system disorders frequency unknown – dizziness, headache.

Cardiac disorders uncommon – angina pectoris, palpitations; frequency unknown – unstable angina.

Respiratory, thoracic and mediastinal disorders rare – bronchospasm (including exacerbation in patients with a history of bronchial asthma), dyspnea.

Skin and subcutaneous tissue disorders uncommon – rash; rare – skin itching.

Musculoskeletal and connective tissue disorders frequency unknown – myalgia, arthralgia.

General disorders and administration site conditions very rare – chest pain.

Contraindications

Hypersensitivity to latanoprost; children under 1 year of age (efficacy and safety not established).

With caution aphakia, pseudophakia with rupture of the posterior lens capsule; patients with risk factors for macular edema; inflammatory, neovascular glaucoma; bronchial asthma; history of herpetic keratitis.

The use of latanoprost should be avoided in patients with active herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin F2_α analogues.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding). If it is necessary to use during lactation, the issue of stopping breastfeeding should be decided.

Pediatric Use

Contraindicated for use in children under 1 year of age (efficacy and safety not established).

Special Precautions

Latanoprost should be used with caution in patients with risk factors for iritis/uveitis. There is limited data on the use of latanoprost in patients scheduled for cataract surgery. In this regard, Latanoprost should be used with caution in this group of patients.

Latanoprost may cause a gradual change in eye color due to an increase in brown pigment in the iris. This is observed mainly in patients with mixed-color irises and is not accompanied by any clinical symptoms or pathological changes, but may be irreversible.

Latanoprost does not affect nevi and lentigo of the iris. No accumulation of pigment in the trabecular meshwork or other parts of the anterior chamber of the eye has been noted. It has been shown that darkening of the iris does not lead to undesirable clinical consequences, so the use of latanoprost can be continued if such darkening occurs. Nevertheless, such patients should be under regular observation and, depending on the clinical situation, treatment may be discontinued.

Experience with the use of latanoprost in the treatment of angle-closure and congenital glaucoma, pigmentary glaucoma, open-angle glaucoma in patients with pseudophakia is limited. There is no information on the use of latanoprost in the treatment of secondary glaucoma due to inflammatory eye diseases and neovascular glaucoma.

Latanoprost does not affect pupil size.

Since information on the use of latanoprost in the postoperative period of cataract extraction is limited, caution should be exercised when using this agent in this category of patients.

Caution should be exercised when using latanoprost in patients with a history of herpetic keratitis. In acute herpetic keratitis, as well as in the case of a history of chronic recurrent herpetic keratitis, the appointment of latanoprost should be avoided.

Macular edema, including cystic, has been observed during therapy with latanoprost mainly in patients with aphakia, pseudophakia, rupture of the posterior lens capsule, or in patients with risk factors for cystic macular edema (in particular, with diabetic retinopathy and retinal vein occlusion). Caution should be exercised when using latanoprost in patients with aphakia, pseudophakia with rupture of the posterior capsule or anterior chamber intraocular lenses, as well as in patients with known risk factors for cystic macular edema.

Experience with the use of latanoprost in patients with bronchial asthma is limited, but in some cases, exacerbation of asthma and/or the appearance of shortness of breath have been noted. Caution should be exercised when using latanoprost in this category of patients.

Cases of darkening of the periorbital skin have been observed, which in some patients were reversible with continued latanoprost therapy.

Latanoprost can cause gradual changes in eyelashes and vellus hair, such as lengthening, thickening, increased pigmentation, increased density, and changes in the direction of eyelash growth. Eyelash changes were reversible and resolved after discontinuation of therapy.

Careful monitoring of patients with dry eye syndrome or other corneal diseases is required during long-term use of latanoprost.

Before using latanoprost, contact lenses must be removed and reinserted no earlier than 15 minutes after instillation.

Latanoprost should not be instilled more than once a day, as it has been shown that more frequent administration reduces the hypotensive effect.

If one dose is missed, treatment is continued according to the usual schedule. As with the use of any eye drops, in order to reduce the possible systemic effect of latanoprost, it is recommended to press on the lower lacrimal point, located at the inner corner of the eye on the lower eyelid, for 1 minute immediately after instillation of each drop. This procedure must be performed directly after instillation.

If it is necessary to use other eye drops at the same time, their use should be separated by a 5-minute interval.

Use in pediatrics

Information on the efficacy and safety of latanoprost in children under 1 year of age is limited. There is no experience with the use of the drug in premature infants (gestational age less than 36 weeks).

There is no information on the safety of long-term use of latanoprost in children. In primary congenital glaucoma in children from 0 to 3 years of age, surgical intervention (goniotomy/trabeculotomy) remains the standard treatment method.

Effect on ability to drive vehicles and operate machinery

As with the use of other ophthalmic drugs, temporary visual impairment is possible; until it is restored, it is not recommended to drive vehicles or operate machinery.

Drug Interactions

When two prostaglandin analogues are instilled into the eyes simultaneously, a paradoxical increase in intraocular pressure has been described, so the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

Pharmaceutically incompatible with eye drops containing thimerosal – precipitation.

Storage Conditions

Store at 2°C (36°F) to 8°C (46°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.