Glauprost eye drops 0.005%, 2.5ml No. 3

Decrease in high intraocular pressure (IOP) in adults and children (over the age of 1 year) with open-angle glaucoma or ophthalmic hypertension.

Adults (including elderly patients)

1 drop into the affected eye (s) 1 time / day. The optimal effect is achieved when using the drug in the evening. Instillation of the drug should not be carried out more often than 1 time / day, since it has been shown that more frequent administration reduces the hypotensive effect. If one dose is missed, treatment is continued as usual. As with the use of any eye drops, in order to reduce the possible systemic effect of the drug, immediately after instillation of each drop, it is recommended to press for 1 minute on the lower lacrimal opening, located at the inner corner of the eye on the lower eyelid. This procedure must be performed immediately after instillation. Before instillation, it is necessary to remove contact lenses and install them no earlier than 15 minutes after insertion. If several ophthalmic dosage forms are used simultaneously,their use should be delimited by a 5-minute interval.

Children

Latanoprost is used in children at the same dose as in adults. There are no data on the use of the drug in premature infants (gestational age <36 weeks). Data for children under 1 year of age is severely limited.

Eye drops are transparent, colorless.

1 ml latanoprost 50 mcg

Excipients: disodium hydrogen phosphate dodecahydrate - 17 mg, sodium dihydrogen phosphate dihydrate - 7 mg, sodium chloride - 3 mg, benzalkonium chloride - 0.2 mg, purified water - up to 1 ml

• Hypersensitivity to the components of the drug;

• age up to 1 year (efficacy and safety have not been established);

• pregnancy;

• lactation period.

  The drug should be used with caution in patients with aphakia, pseudoaphakia with rupture of the posterior lens capsule, in patients with known risk factors for macular edema (in the treatment of latanoprost, cases of macular edema, including cystoid edema, have been described), in patients with inflammatory, neovascular or congenital glaucoma (due to lack of sufficient experience with the drug).

pharmachologic effect

Antiglaucoma drug. Is it an analogue of prostaglandin F2? and a selective FP (prostaglandin F) receptor agonist. Reduces intraocular pressure by increasing the outflow of aqueous humor.

A decrease in intraocular pressure begins 3-4 hours after the administration of the drug, the maximum effect is observed after 8-12 hours, the effect lasts for at least 24 hours.

Studies in animals and humans have shown that the main mechanism of action is an increase in uveoscleral outflow, in addition, an improvement in outflow (a decrease in outflow resistance) has also been described in humans.

It was found that latanoprost has no significant effect on the production of aqueous humor and on the blood-ophthalmic barrier.

Animal studies have shown that at therapeutic doses, latanoprost does not affect (or does not significantly affect) intraocular circulation.

When applied topically, conjunctival or episcleral injection of mild to moderate severity is possible. According to fluorescent angiography, long-term treatment with latanoprost after extracapsular cataract extraction in monkeys had no effect on retinal circulation.

With short-term use, latanoprost did not contribute to the leakage of fluorescein in the posterior segment of the eye of patients with an artificial lens.

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, inactive; after hydrolysis to an acidic form, it becomes biologically active.

Suction

It is well absorbed through the cornea and completely hydrolyzed when it enters the aqueous humor.

Distribution

Studies in humans have shown that Cmax in aqueous humor is reached 2 hours after instillation. After instillation in monkeys, latanoprost is distributed mainly in the anterior chamber of the eye, conjunctiva and eyelids. Only a small amount of latanoprost reaches the posterior chamber of the eye. In the equilibrium state, there is no cumulation of latanoprost acid in the blood plasma.

Metabolism

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

Withdrawal

T1 / 2 from plasma is 17 minutes. Animal studies have shown that the main metabolites (1,2-dinor- and 1,2,3,4-tetranormetabolites) do not have (or have low) biological activity and are excreted mainly in the urine.

Pharmacokinetics in special patient groups

Pharmacokinetic studies of latanoprost were carried out in 22 adults and 25 children (aged 0-18 years) with ophthalmic hypertension and glaucoma. All age groups received latanoprost at a concentration of 0.005%, 1 drop in each eye for at least 2 weeks. Latanoprost exposure is approximately 2 times higher in children aged 3 to 12 years compared with adult patients and 6 times higher in children under 3 years of age. However, the safety profile of the drug does not differ between children and adults. In all age groups, the duration of maintenance of Cmax of latanoprost acid in blood plasma is 5 minutes. T1 / 2 of latanoprost acid in children is the same as in adults (<20 min).

Side effect

Infections and invasions: frequency unknown - herpetic keratitis.

From the side of the organ of vision: very often - hyperpigmentation of the iris, conjunctival hyperemia, eye irritation from mild to moderate (burning sensation, feeling of sand in the eyes, itching, tingling and sensation of a foreign body), changes in eyelashes (increase in length, thickness, number and pigmentation); often - transient point erosion of the epithelium (mostly asymptomatic), blepharitis, pain in the eye; infrequently - edema of the eyelids, dryness of the mucous membrane of the eye, keratitis, blurred vision, conjunctivitis; rarely - iritis / uveitis (mainly in predisposed patients), macular edema, eyelid edema, corneal edema, corneal erosion, periorbital edema, darkening of the eyelid skin, eyelid skin reactions, changes in the direction of eyelash growth, thickening, darkening and lengthening of eyelashes, distichiasis , photophobia;very rarely - changes in the periorbital region and in the region of the eyelashes, leading to a deepening of the groove of the upper eyelid; frequency unknown - cyst of the iris.

From the side of the nervous system: the frequency is unknown - dizziness, headache.

From the side of the cardiovascular system: very rarely - aggravation of the course of angina pectoris in patients with concomitant angina pectoris; frequency unknown - palpitations.

From the respiratory system: rarely - bronchospasm (including exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath.

On the part of the skin and subcutaneous tissues: infrequently - rash; rarely - darkening of the skin of the eyelids and local skin reactions on the eyelids.

From the musculoskeletal system: the frequency is unknown - myalgia, arthralgia.

Others: very rarely - chest pain.

Children

According to the results of two short-term (?12 weeks) clinical studies in 93 children, the safety profile of latanoprost in children did not differ from that in adults. The safety profile between different age groups in children is comparable. Compared to the adult population, nasopharyngitis and fever were most common in children.

Application during pregnancy and lactation

The safety of using latanoprost in pregnant women has not been established. Latanoprost can have toxic effects on pregnancy, fetus and newborn. Use during pregnancy is contraindicated.

Latanoprost and its metabolites may be excreted in breast milk. Use during breastfeeding is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

The effect of latanoprost on male and female fertility has not been found in experimental animal studies.

Application in children

Contraindicated in children and adolescents under 1 year of age.

special instructions

The use of latanoprost can gradually change the color of the eyes by increasing the brown pigment content in the iris. Before starting treatment, patients should be informed of a possible irreversible change in eye color. The use of the drug in one eye can cause irreversible heterochromia. This effect is seen primarily in patients with mixed iris coloration, such as blue-brown, gray-brown, green-brown, or yellow-brown. In studies of latanoprost, darkening usually began within the first 8 months of treatment, rarely during the second or third year, and was not observed after 4 years of treatment. The progression of iris pigmentation decreased over time and stabilized after 5 years. There are no data on increased pigmentation over 5 years.In an open-label 5-year safety study of latanoprost, 33% of patients developed iris pigmentation. In most cases, the change in iris color was insignificant and, often, clinically not detected. The incidence ranges from 7% to 85% in patients with mixed iris coloration, prevailing in patients with yellow-brown irises. Changes were not observed in patients with uniformly colored blue iris; in rare cases, changes were noted with uniformly colored irises of gray, green and brown.Changes were not observed in patients with uniformly colored blue iris; in rare cases, changes were noted with uniformly colored irises of gray, green and brown.Changes were not observed in patients with uniformly colored blue iris; in rare cases, changes were noted with uniformly colored irises of gray, green and brown.

The change in eye color is due to an increase in the content of melanin in the stromal melanocytes of the iris, and not an increase in the number of melanocytes themselves. Typically, brown pigmentation appears around the pupil and spreads concentrically to the periphery of the iris. In this case, the entire iris or parts of it become brown. No further pigmentation was observed after discontinuation of therapy. According to the available clinical data, the color change was not associated with any symptoms or pathological abnormalities.

The drug has no effect on nevi and iris lentigo.

According to the results of 5-year clinical studies, the accumulation of pigment in the sclero-corneal trabecular meshwork or other parts of the anterior chamber of the eye was not observed. It has been shown that the darkening of the iris does not lead to undesirable clinical consequences, therefore, the use of latanoprost can be continued in the event of such darkening. However, such patients should be monitored regularly and, depending on the clinical situation, treatment may be discontinued.

The experience of using latanoprost in the treatment of angle-closure and congenital glaucoma, pigmentary glaucoma, 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 has no effect on pupil size. Due to the lack of experience in the use of latanoprost in the treatment of an acute attack of angle-closure glaucoma, the drug should be used with caution in such patients.

Due to the fact that information on the use of latanoprost in the postoperative period of cataract extraction is limited, care should be taken 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 acute herpetic keratitis, as well as in the case of a history of chronic recurrent herpetic keratitis, latanoprost should be avoided.

Macular edema, incl. cystic, was observed during latanoprost therapy mainly in patients with aphakia, pseudophakia, rupture of the posterior lens capsule or in patients with risk factors for the development of cystic macular edema (in particular, with diabetic retinopathy and retinal vein occlusion).

Caution should be exercised when using latanoprost in patients with aphakia, pseudoaphakia with rupture of the posterior capsule or anterior chamber intraocular lenses, as well as in patients with known risk factors for cystic macular edema.

Caution should be exercised when using latanoprost in patients with risk factors for iritis / uveitis.

The experience of using latanoprost in patients with bronchial asthma is limited, but in a number of cases in the post-registration period there was an exacerbation of asthma and / or the appearance of shortness of breath. Caution should be exercised when using latanoprost in this category of patients.

There were cases of darkening of the skin of the periorbital region, which in a number of patients were reversible with continued therapy with latanoprost.

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

Glauprost contains benzalkonium chloride, which is often used as a preservative in ophthalmic medicines. Benzalkonium chloride can cause eye irritation, punctate keratopathy and / or toxic ulcerative keratopathy, and can be absorbed and discolored by soft contact lenses. Careful monitoring of the condition of patients with dry eye syndrome or other corneal diseases is required with prolonged use of latanoprost. Before using the drug, it is necessary to remove contact lenses and reinstall them no earlier than 15 minutes after instillation.

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 are no data on the safety of long-term use of latanoprost in children. For primary congenital glaucoma in children aged 0 to 3 years, surgery (goniotomy / trabeculotomy) remains the standard treatment.

Influence on the ability to drive vehicles and use mechanisms

As with other ophthalmic drugs, temporary visual impairment is possible; until it is restored, it is not recommended to drive vehicles or work with mechanisms.

Overdose

Symptoms: in addition to irritation of the mucous membrane of the eyes and hyperemia, other adverse reactions from the organ of vision with an overdose of latanoprost have not been described.

In case of accidental ingestion of latanoprost inside, the following information should be taken into account: one bottle with 2.5 ml of solution contains 125 ?g of latanoprost. More than 90% of latanoprost is metabolized during the 'first pass' through the liver.

IV infusion at a dose of 3 mcg / kg in healthy volunteers did not cause any symptoms, however, when a dose of 5.5-10 mcg / kg was administered, nausea, abdominal pain, dizziness, fatigue, 'hot flashes' and sweating were observed. Intravenous administration of latanoprost to monkeys at a dose of 500 ?g / kg did not cause significant effects on the cardiovascular system. Intravenous administration of latanoprost to monkeys caused transient bronchospasm. In patients with moderate bronchial asthma, instillation of latanoprost into the eyes at a dose 7 times higher than the therapeutic dose did not cause bronchospasm.

Treatment: carrying out symptomatic therapy.

Drug interactions

There are no unambiguous data on the drug interactions of latanoprost.

With the simultaneous instillation of two prostaglandin analogues, a paradoxical increase in IOP has been described, therefore the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

In vitro studies have shown that when mixing eye drops containing thiomersal with eye drops containing latanoprost, a precipitate is formed. If necessary, the simultaneous use of these drugs, you should observe a 5-minute interval between their instillation.