Prolatan eye drops 0.005%, 2.5 ml No. 3

Reduction of increased intraocular pressure (IOP) in adults and children (over the age of 1 year) with open-angle glaucoma or increased ophthalmotonus.

Note: In children under 3 years of age with primary congenital glaucoma, surgical treatment (trabeculotomy / goniotomy) remains the first-line therapy.

In adults and children over 1 year old - one drop into the affected eye (s) once a day. The optimal effect is achieved when using the drug in the evening. As with the use of any eye drops, in order to reduce the possible systemic effect of the drug, immediately after the installation of each drop, it is recommended to press on the lower lacrimal opening, located at the inner corner of the eye on the lower eyelid. This must be done within 1 minute.

Eye drops are transparent, colorless.

1 ml

latanoprost 0.05 mg

Excipients: benzalkonium chloride - 0.2 mg, sodium chloride - 4.1 mg, disodium hydrogen phosphate anhydrous - 4.74 mg, sodium dihydrogen phosphate monohydrate - 4.6 mg, water d / i - up to 1 ml.

• Hypersensitivity to latanoprost or other components of the drug;

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

  With caution, Afakia, pseudoaphakia with rupture of the posterior lens capsule, patients with known risk factors for macular edema (with latanoprost treatment, cases of macular edema, including cystoid edema, have been described; inflammatory, neovascular or congenital glaucoma (due to lack of sufficient experience with the drug); asthma; history of herpetic keratitis. Avoid the use of the drug Prolatan in patients with active herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin analogues. Prolatan should be used with caution in patients with risk factors for iritis / uveitis. There are limited data on the use of Prolatan in patients undergoing surgery for cataracts.In this regard, Prolatan should be used with caution in this group of patients.

pharmachologic effect

Latanoprost - an analogue of prostaglandin F2? - is a selective agonist of FP receptors and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly by the uveoscleral route, as well as through the trabecular network. A decrease in IOP begins approximately 3-4 hours after drug administration, the maximum effect is observed after 8-12 hours, the effect lasts for at least 24 hours.

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

When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems.

Pharmacokinetics

Suction

Latanoprost, being a prodrug, is absorbed through the cornea, where it is hydrolyzed to a biologically active acid. The concentration in aqueous humor reaches a maximum approximately 2 hours after topical application.

Distribution

Vd is 0.16 ± 0.02 l / kg. Latanoprost acid is determined in aqueous humor during the first 4 hours, and in plasma - only within the first hour after topical application.

Metabolism

Latanoprost, being a prodrug, undergoes hydrolysis in the cornea under the action of esterases with the formation of biologically active acid. Latanoprost acid, entering the systemic circulation, is metabolized mainly in the liver by beta-oxidation of fatty acids to form 1,2-dinor- and 1.2.3,4-tetranor metabolites.

Withdrawal

Latanoprost acid is rapidly eliminated from plasma (T1 / 2 = 17 min).

Systemic clearance is approximately 7 ml / min / kg. After beta-oxidation in the liver, metabolites are excreted mainly by the kidneys: after topical application, approximately 88% of the administered dose is excreted in the urine.

Children

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. The time to reach Cmax of latanoprost acid in blood plasma is 5 minutes for all age groups. T1 / 2 of latanoprost acid in children is the same as in adults. At the equilibrium concentration, there is no cumulation of latanoprost acid in the blood plasma.

Side effect

The following adverse reactions related to the use of the drug have been reported:

From the side of the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itching, tingling and foreign body sensation); blepharitis; hyperemia of the conjunctiva; Pain in the eyes; increased pigmentation of the iris; transient punctate erosion of the epithelium, edema of the eyelids, perporbital edema, edema and erosion of the cornea; conjunctivitis; lengthening, thickening, increasing the number and increasing pigmentation of eyelashes and vellus hair; iritis / uveitis; keratitis; macular edema, incl. cystoid; a change in the direction of eyelash growth, sometimes causing eye irritation; blurred vision, photophobia, dryness of the mucous membrane of the eyes.

On the part of the skin and subcutaneous tissues: rash, darkening of the eyelid skin and local skin reactions on the eyelids, toxic epidermal nskrolysis.

From the nervous system: dizziness, headache.

Respiratory system: bronchospasm (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath.

From the musculoskeletal system and connective tissue: muscle / joint pain.

General and local reactions: nonspecific chest pain.

Infections and invasions: herpetic keratitis.

There have also been cases of retinal artery embolism, retinal detachment and vitreous hemorrhage in patients with diabetic retinopathy.

Children

The safety profile of Prolatan in children did not differ from the safety profile in adults. Compared to the adult population, nasopharyngitis and fever were most common in children.

Application during pregnancy and lactation

There have been no adequate controlled studies in pregnant women. The drug should be prescribed during pregnancy only in cases where the potential benefit to the mother outweighs the possible risk to the fetus.

Latanoprost and its metabolites can be excreted in breast milk, therefore, the drug should be used with caution during breastfeeding.

Application in children

Contraindicated in children under 1 year of age, because efficacy and safety have not been established.

The safety profile of Prolatan in children over 1 year of age did not differ from the safety profile in adults. Compared to the adult population, nasopharyngitis and fever were most common in children.

special instructions

The drug Prolatan should be used no more than once a day, since more frequent administration of latanoprost leads to a weakening of the IOP-lowering effect.

If one dose is missed, the next dose should be administered at the usual time.

Prolatan can be used concomitantly with other classes of topical ophthalmic drugs to lower IOP. If the patient is using other eye drops at the same time, then they should be applied at intervals of at least 5 minutes.

Prolatan contains benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, contact lenses must be removed and reinserted after 15 minutes.

Prolatan can cause a gradual increase in the brown pigment content in the iris. The change in eye color is caused by an increase in the content of melanin in the stromal melanocytes of the iris, and not by 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. In most cases, discoloration is minor and may not be clinically apparent. Increased pigmentation in the iris of one or both eyes is observed mainly in patients with a mixed iris color with a brown base. The drug has no effect on nevi and iris lentigo; accumulation of pigment in the trabecular meshwork or in the anterior chamber of the eye was not noted.

When determining the degree of pigmentation of the iris for more than 5 years, no undesirable consequences of increased pigmentation were revealed even with continued therapy with latanoprost. In patients, the degree of IOP reduction was the same regardless of the presence or absence of increased iris pigmentation. Therefore, treatment with Prolatan can be continued in cases of increased iris pigmentation. Such patients should be monitored regularly and, depending on the clinical situation, treatment may be discontinued.

Increased iris pigmentation is usually observed within the first year after starting treatment, rarely during the second or third year. After the fourth year of treatment, this effect was not observed. The rate of pigmentation progression decreases over time and stabilizes after 5 years. In more distant terms, the effects of increased iris pigmentation have not been studied. After stopping treatment, there was no increase in brown pigmentation of the iris, but the change in eye color may be irreversible.

In connection with the use of latanoprost, cases of darkening of the eyelid skin have been described, which can be reversible.

Prolatan 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 are reversible and disappear after stopping treatment.

In patients using drops in only one eye, heterochromia may develop.

Eye drops may cause transient blurred vision.

Influence on the ability to drive a car and other mechanisms

Drive a car or use complex equipment while using the drug with caution.

Overdose

In addition to irritation of the mucous membrane of the eyes, hyperemia of the conjunctiva or episclera, other undesirable changes on the part of the organ of vision in case of an overdose of latanoprost are not known.

In case of accidental intake of the drug Prolatan inside, the following information should be taken into account: one bottle with 2.5 ml of solution contains 125 ?g of latanoprost, 5 ml - 250 ?g of latanoprost. More than 90% of the drug is metabolized during the first passage through the liver. Intravenous infusion at a dose of 3 ?g / kg in healthy volunteers did not cause any symptoms, however, when a dose of 5.5-10 ?g / kg was administered, nausea, abdominal pain, dizziness, fatigue, hot flashes and sweating were observed. In patients with moderate bronchial asthma, the introduction of latanoprost into the eyes at a dose 7 times higher than the therapeutic dose did not cause bronchospasm.

In case of an overdose, symptomatic treatment is performed.

Drug interactions

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

Pharmaceutically incompatible with eye drops containing thiomersal - precipitation.