Latanoprost-Optic 0.005% Eye Drops

Indications

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

Method of application and doses

Locally.

Dosing regimen for adults (including the elderly)

One drop in the affected eye once a day. Optimal effect is achieved when the medication is used in the evening.

Instillation of the medication should not be performed more than once a day, as more frequent administration has been shown to reduce the hypotensive effect.

If a dose is missed, treatment should continue according to the usual schedule. As with any eye drops, to reduce the possible systemic effect of the medication, it is recommended to press on the lower tear duct located at the inner corner of the eye on the lower eyelid for 1 minute immediately after instilling each drop. This procedure should be performed right after instillation.

Before instillation, contact lenses must be removed and can be reinserted no earlier than 15 minutes after administration (see also the section "Special instructions"). If other eye drops need to be used simultaneously, their application should be separated by a 5-minute interval.

Dosing regimen for children

Latanoprost is used in children at the same dose as in adults. Data on the use of the medication in premature infants (gestational age < 36 weeks) is lacking. Data in children < 1 year is very limited.

Composition

Composition per 1 ml.

Active ingredient: latanoprost - 0.05 mg.

Excipients:

glycerol ricinoleate macrogol (polyoxyl-35-castor oil) - 0.40 mg, polydronium chloride - 0.025 mg, sodium chloride - 4.10 mg, sodium dihydrogen phosphate monohydrate - 4.60 mg, anhydrous sodium phosphate - 4.74 mg, purified water - up to 1.0 ml.

Description of the dosage form

Clear colorless liquid

Contraindications

Increased sensitivity to latanoprost or other components of the drug. Age under 1 year (efficacy and safety not established).
With caution

Aphakia, pseudoaphakia with rupture of the posterior capsule of the lens; patients with risk factors for macular edema (cases of macular edema, including cystoid, have been reported during treatment with latanoprost); inflammatory, neovascular glaucoma (due to lack of sufficient experience with the drug); bronchial asthma; history of herpetic keratitis.
The use of the drug should be avoided in patients with active herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin F2α analogs. The drug should be used with caution in patients with risk factors for the development of iritis/uveitis. There is limited data on the use of the drug in patients scheduled for cataract surgery. Therefore, in this group of patients, the drug should be used with caution.

Section: Special Instructions

Latanoprost may gradually change the color of the eyes due to an increase in the brown pigment content in the iris. Patients should be informed about the possible irreversible change in eye color before starting treatment. The use of the drug in one eye may cause irreversible heterochromia. Such changes in eye color have been predominantly noted in patients with unevenly colored irises, namely: brown-blue, gray-brown, yellow-brown, and green-brown. In studies of latanoprost, darkening typically began within the first 8 months of treatment, rarely during the second and third years, and was not observed after four years of treatment. The progression of iris pigmentation decreased over time and stabilized after 5 years. Data on the enhancement of pigmentation over 5 years is lacking. In an open 5-year safety study of latanoprost, 33% of patients developed iris pigmentation (see the "Side Effects" section). In most cases, the change in iris color was minor and often clinically undetectable. The incidence ranged from 7 to 85% in patients with irises of different colors, predominating in patients with yellow-brown irises. Changes in patients with uniformly colored blue irises were not observed; in rare cases, changes were noted in uniformly colored gray, green, and brown irises. The change in eye color is due to an increase in melanin content in the stromal melanocytes of the iris, rather than an increase in the number of melanocytes themselves. In typical cases, brown pigmentation appears around the pupil and concentrically spreads to the periphery of the iris. As a result, the entire iris or parts of it acquire a brown color. After discontinuation of therapy, further pigmentation was not observed. According to available clinical data, the change in color was not associated with any symptoms or pathological disorders. The drug does not affect nevi and lentigines of the iris. According to the results of 5-year clinical studies, no accumulation of pigment in the scleral-corneal trabecular meshwork or other parts of the anterior chamber of the eye was noted. It has been shown that darkening of the iris does not lead to undesirable clinical consequences, so the use of latanoprost can continue in the event of such darkening. However, 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, and open-angle glaucoma in patients with pseudoaphakia 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. Due to limited information on the use of latanoprost in the postoperative period following cataract extraction, caution should be exercised when using the drug in this category of patients. Caution should be exercised when using latanoprost in patients with a history of herpetic keratitis. In cases of acute herpetic keratitis, as well as in the presence of anamnesis of chronic recurrent herpetic keratitis, latanoprost should be avoided. Macular edema, including cystoid edema, has been noted during latanoprost therapy primarily in patients with aphakia, pseudoaphakia, posterior capsule rupture of the lens, or in patients with risk factors for developing cystoid macular edema (particularly in diabetic retinopathy and retinal vein occlusion). Caution should be exercised when using latanoprost in patients with aphakia, pseudoaphakia with posterior capsule rupture, or anterior chamber intraocular lenses, as well as in patients with known risk factors for cystoid macular edema. Caution should be exercised when using latanoprost in patients with risk factors for developing iritis/uveitis. Experience with the use of latanoprost in patients with bronchial asthma is limited, but in some cases, exacerbations of asthma and/or the appearance of shortness of breath have been noted during the post-registration period. Caution should be exercised when using latanoprost in this category of patients (see also the "Side Effects" section). Cases of darkening of the skin in the periorbital area have been noted, which in some patients were reversible with continued latanoprost therapy. Latanoprost may cause gradual changes in eyelashes and vellus hair, such as lengthening, thickening, increased pigmentation, increased density, and changes in the direction of eyelash growth. Changes in eyelashes were reversible and resolved after discontinuation of therapy. Latanoprost-Optic contains benzalkonium chloride, which is often used as a preservative in ophthalmic medications. Benzalkonium chloride may cause eye irritation, punctate keratopathy, and/or toxic ulcerative keratopathy, as well as be absorbed by soft contact lenses and discolor them. Careful monitoring of patients with "dry eye" syndrome or other corneal diseases is required during prolonged use of latanoprost. Contact lenses should be removed before using the drug and reinserted no earlier than 15 minutes after instillation (see also the "Method of Administration and Dosage" section). Children Information on the efficacy and safety of latanoprost in children under one year of age is limited. There is no experience with the drug in premature infants (gestational age less than 36 weeks). Data on the safety of long-term use of latanoprost in children is lacking. In cases of primary congenital glaucoma in children aged 0 to 3 years, the standard method of treatment remains surgical intervention (goniotomy/trabeculotomy).

Section: Side Effects

Most adverse reactions were noted from the visual organ. In an open 5-year safety study, 33% developed pigmentation of the iris (see "Special Instructions" section). Other adverse reactions from the visual organ are generally transient and are noted immediately after instillation. The grading of adverse reactions by frequency of occurrence was as follows: very common (≥1/10); common (≥1/100,

Section: Overdose

In addition to irritation of the mucous membrane of the eyes, hyperemia of the conjunctiva or episclera, other undesirable changes in the visual organ due to an overdose of latanoprost are not known. In the case of accidental ingestion of latanoprost, the following information should be considered: one bottle containing 2.5 ml of solution contains 125 mcg of latanoprost. More than 90% of the drug is metabolized on the first pass through the liver. An intravenous infusion at a dose of 3 mcg/kg in healthy volunteers did not cause any symptoms; however, doses of 5.5-10 mcg/kg resulted in nausea, abdominal pain, dizziness, fatigue, flushing, and sweating. In patients with moderate bronchial asthma, the administration of latanoprost in the eyes at a dose 7 times higher than the therapeutic dose did not cause bronchospasm. In case of overdose, symptomatic treatment is carried out.

Interaction

When two analogs of prostaglandins are instilled in the eyes simultaneously, a paradoxical increase in intraocular pressure has been reported; therefore, the simultaneous use of two or more prostaglandins, their analogs, or derivatives is not recommended.
Pharmaceutically incompatible with eye drops containing thimerosal - precipitation.

Pharmacodynamics

Latanoprost, a prostaglandin F2α analog, is a selective agonist of FP (prostaglandin F) receptors and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, primarily through the uveoscleral pathway, as well as through the trabecular meshwork. The reduction in IOP begins approximately 3-4 hours after administration of the drug, with maximum effect observed after 8-12 hours, and the action lasts for at least 24 hours. It has been established that latanoprost does not have a significant effect on the production of aqueous humor or on the blood-ocular barrier. When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems.

Pharmacokinetics

Latanoprost (molecular weight 432.58) is a prodrug, esterified with an isopropyl group, and is inactive; after hydrolysis to the acid form, it becomes biologically active.
Absorption
The prodrug is well absorbed through the cornea and is completely hydrolyzed upon entering the aqueous humor.
Distribution
Studies in humans have shown that the maximum concentration in the aqueous humor is reached 2 hours after instillation. After instillation in monkeys, latanoprost is predominantly distributed in the anterior chamber of the eye, conjunctiva, and eyelids. Only a small amount of latanoprost reaches the posterior chamber of the eye.
Biotransformation
The active form of latanoprost is practically not metabolized in the eye, but is subject to biotransformation in the liver.
Excretion
The half-life in plasma is 17 minutes.
Animal studies have shown that the main metabolites (1,2-dinor- and 1,2,3,4-tetranor metabolites) have no (or low) biological activity and are primarily excreted in the urine.
Children
The exposure to latanoprost is approximately 2 times higher in children aged 3 to 12 years compared to adult patients and 6 times higher in children under 3 years of age.
However, the safety profile of the drug is not different between children and adults. The time to reach the maximum concentration of latanoprost acid in plasma is 5 minutes for all age groups. The half-life of latanoprost acid in children is the same as in adults. There is no accumulation of latanoprost acid in plasma at steady-state concentration.

Storage conditions

Opened dropper bottle should be stored for no more than 30 days at a temperature not exceeding 25 °C