Active substanceLatanoprostLatanoprost
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  • Dosage form: & nbspeye drops
    Composition:

    1 ml of the preparation contains:

    Active substance:

    Latanoprost 0.05 mg

    Excipients:

    Benzalkonium chloride 0.20 mg

    Sodium chloride 4.10 mg

    Sodium dihydrogen phosphate monohydrate 4.60 mg

    Sodium hydrophosphate anhydrous 4.74 mg

    Water for injection up to 1 ml.

    Description:

    Transparent colorless liquid.

    Pharmacotherapeutic group:Antiglaucoma means - prostaglandin F2α analogue synthetic
    ATX: & nbsp

    S.01.E.E   Prostaglandin analogues

    S.01.E.E.01   Latanoprost

    Pharmacodynamics:

    Latanoprost - an analogue of prostaglandin F2α - is a selective receptor agonist FP (prostaglandin F) and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly by the uveoscleral route, and also through the trabecular network. Decrease in IOP begins approximately 3-4 hours after the administration of the drug, the maximum effect is observed after 8-12 hours, the effect is maintained for at least 24 hours.

    Determined that latanoprost does not have a significant effect on the production of aqueous humor and on the hemato-ophthalmic barrier.

    When used in therapeutic doses latanoprost has no significant pharmacological effect on the cardiovascular and respiratory systems.
    Pharmacokinetics:

    Latanoprost (molecular weight 432.58) is a prodrug esterified with an isopropyl group, is inactive; after hydrolysis to acid form becomes biologically active.

    Suction

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

    Distribution

    Studies in humans have shown that the maximum concentration in aqueous humor is achieved 2 hours after instillation. After instillation to 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.

    Biotransformation

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

    Excretion

    The half-life of the plasma is 17 min.

    Studies in animals have shown that the main metabolites (1,2-dinor- and 1,2,3,4-tetranormetabolites) do not (or have low) biological activity and are excreted mainly in the urine.

    Children

    Exposure of latanoprost is approximately 2 times higher in children aged 3 to 12 years than in adult patients and 6 times higher in children younger than 3 years.

    However, the safety profile of the drug is not different in children and adults. The time to reach the maximum concentration of latanoprost acid in blood plasma is 5 minutes for all age groups. The half-life of latanoprost in children is the same as in adults. In the equilibrium concentration there is no accumulation of latanoprost acid in the blood plasma.

    Indications:

    Decreased elevated intraocular pressure in adults and children (over 1 year old) with open-angle glaucoma or increased ophthalmotonus.

    Contraindications:

    Hypersensitivity to latanoprost or other components of the drug. Age to 1 year (efficacy and safety not established).

    Carefully:

    Afakia, pseudo-aphakia with a rupture of the posterior capsule of the lens; patients with risk factors for macular edema (in the treatment with latanoprost, cases of development of macular edema, including cystoid edema); inflammatory, neovascular glaucoma (due to lack of sufficient experience in the use of the drug); bronchial asthma; herpetic keratitis in the anamnesis.

    It should be avoided in patients with active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin analogues F2α. The drug should be used with caution in patients with risk factors for the development of iritis / uveitis. There are limited data on the use of the drug in patients who are scheduled surgery for cataracts. In this regard, in this group of patients the drug should be used with caution.

    Pregnancy and lactation:

    Pregnancy

    The safety of latanoprost during pregnancy is not established in humans. Latanoprost can have toxic effects on the course of pregnancy, fetus and newborn. Application during pregnancy is contraindicated.

    Breastfeeding period

    Latanoprost and its metabolites can penetrate into breast milk. Application during breastfeeding is contraindicated. If it is necessary to use the drug, breastfeeding should be discontinued.

    Fertility

    The effects of latanoprost on male and female fertility in animal studies have not been revealed.

    Dosing and Administration:

    Dosing regimen in adults (including the elderly)

    But one drop in the affected eye (a) once a day. The optimal effect is achieved with the use of the drug in the evening.

    Do not instillation of the drug more often than once a day, because it is shown that more frequent administration reduces the hypotensive effect.

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

    Before instillation it is necessary to remove contact lenses and install them not earlier than 15 minutes after the administration (see also section "Special instructions"). If other eye drops need to be used simultaneously, their application should be delimited by a 5-minute interval.

    Dosage regimen in children

    Latanoprost is used in children in the same dose as in adults. Data on the use of the drug in prematurity (gestational age <36 weeks) are absent. Data for children <1 year are severely limited.

    Side effects:

    The majority of undesirable reactions were noted by the organ of vision. In an open 5-year safety study, pigmentation of the iris developed in 33% (see section "Special instructions"). Other undesirable reactions from the side of the organ of vision are usually transient and are noted immediately after instillation. The gradation of unwanted reactions by frequency was as follows: very often (≥1 / 10); often (≥1 / 100, <1/10); infrequently (≥1 / 1000, <1/100); rarely (≥1 / 10,000, <1/1000); very rarely (<1/10 000); the frequency is unknown (it is impossible to estimate the frequency from the available data).

    Infections and invasions

    Frequency unknown: herpetic keratitis.

    From the side of the organ of vision

    Often: hyperpigmentation of the iris, conjunctival hyperemia, eye irritation from mild to moderate degree (burning sensation, sensation of sand in eyes, itching, tingling and sensation of foreign body), eyelash changes (increase in length, thickness, quantity and pigmentation).

    Often: transient point erosions of the epithelium (mostly asymptomatic), blepharitis, pain in the eye.

    Infrequently: swelling of the eyelids, dryness of the mucous membrane of the eye, keratitis, blurred vision, conjunctivitis.

    Rarely: iritis / uveitis (mainly in predisposed patients), edema of the macula, edema of the eyelids, corneal edema, corneal erosion, periorbital edema, darkening of the skin of the eyelids, reactions of the eyelid skin, changes in the direction of eyelash growth, thickening, darkening and lengthening of eyelashes, distichiasis, photophobia .

    Rarely: Changes in the periorbital region and in the lash area, leading to a deepening of the furrow of the upper eyelid.

    Frequency unknown: cyst of the iris, pseudo-pemphigoid of the conjunctiva.

    From the nervous system

    Frequency unknown: dizziness, headache.

    From the heart

    Infrequently: angina, feeling of palpitations.

    Frequency unknown: unstable angina.

    On the part of the respiratory system

    Rarely: bronchospasm (including exacerbation of the disease in patients with bronchial asthma in the anamnesis), dyspnea.

    From the skin and subcutaneous tissues

    Infrequently: rash.

    Rarely: itching.

    Rarely: darkening of the skin of the eyelids and local skin reactions on the eyelids.

    From the side of the musculoskeletal system and connective tissue

    Frequency unknown: myalgia, arthralgia.

    Common violations and local reactions

    Rarely: chest pain.

    Overdose:

    In addition to irritation of the eye mucosa, conjunctival hyperemia or episclerosis, other undesirable changes on the part of the eye in case of an overdose of latanoprost are not known.

    If you randomly take Latanoprost inwards, you should consider the following information: one bottle with 2.5 ml of solution contains 125 μg of latanoprost. More than 90% of the drug is metabolized on the first pass through the liver. Intravenous infusion in a dose of 3 μg / kg in healthy volunteers did not cause any symptoms, however, when a dose of 5.5-10 μg / kg was administered, nausea, abdominal pain, dizziness, fatigue, hot flashes and sweating were observed.In patients with bronchial asthma of moderate severity, the administration of latanoprost in the eye at a dose 7 times higher than the therapeutic dose did not cause bronchospasm.

    In case of an overdose, symptomatic treatment is performed.

    Interaction:

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

    Pharmaceutically incompatible with eye drops containing thiomersal - precipitation.

    Special instructions:

    Latanoprost can gradually change the color of the eyes by increasing the content of brown pigment in the iris. Before starting treatment, patients should inform about possible irreversible changes in eye color. The use of a drug on one eye can cause irreversible heterochromy. This change in eye color was predominantly noted in patients with unevenly colored irises, namely: quads-blue, gray-brown, yellow-brown and green-brown. In studies of latanoprost, darkening usually began within the first 8 months of treatment, rarely - during the second and third years and was not observed after four years of treatment.

    Progression of the iris pigmentation decreased with time and stabilized after 5 years. Data on the increase in pigmentation for 5 years are absent. In an open 5-year study of latanoprost safety, pigmentation of the iris developed in 33% of the patients (see the "Side effect" section). In most cases, the change in the color of the iris was insignificant and, often, was not clinically detected. Frequency of occurrence ranged from 7 to 85% in patients with unequal iris, prevailing in patients with yellow-brown irises. Changes in patients with uniformly colored irises of blue color were not observed, in rare cases Changes were noted with uniformly colored irises of gray, green and brown color.

    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 concentrates on the periphery of the iris. In this case, the entire iris or its parts acquire a brown color. After the treatment was canceled, no further pigmentation was noted.According to the available clinical data, the color change was not associated with any symptoms or pathological disorders.

    The drug does not affect the nevi and lentigo iris. According to the results of 5-year clinical trials, pigment accumulation in the sclerogoric trabecular network or other parts of the anterior chamber of the eye was not noted. It is shown that iris darkening does not lead to undesirable clinical consequences, therefore, the use of latanoprost in case of such darkening can be continued. Nevertheless, such patients should be under regular supervision and, depending on the clinical situation, treatment may be discontinued.

    The experience of latanoprost in the treatment of closed-angle and congenital glaucoma, pigmentary glaucoma, open-angle glaucoma in patients with pseudo-pharmacies 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 the size of the pupil.

    Due to the fact that information about 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.

    Care should be taken when using latanoprost in patients with herpetic keratitis in history. For acute herpetic keratitis, as well as if there is anamnestic information about chronic recurrent herpetic keratitis, it is necessary to avoid the appointment of latanoprost.

    Macular edema, including cystic, was noted during latanoprost treatment mainly in patients with aphakia, pseudoafaky. rupture of the posterior capsular lens, or in patients with risk factors for cystic macular edema (in in particular, with diabetic retinopathy and retinal vein occlusion). Caution must be exercised when applying latanoprost patient with aphakia, psevdoafakiey with rupture of the posterior capsule or anterior chamber intraocular lenses, as well as patients with known risk factors cystic macular edema.

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

    The experience of using latanoprost in patients with bronchial asthma is limited, but in a number of cases, the exacerbation of the course of asthma and / or the appearance of dyspnea was noted in the postgrade period.Caution should be exercised when using latanoprost in this category of patients (see also the "Side effect" section). There were cases of darkening of the skin of the periorbital region, which in a number of patients were reversible in the continuation of latanoprost therapy.

    Latanoprost can cause gradual changes in eyelashes and fleece hair, such as lengthening, thickening, increased pigmentation, increased density and a change in the direction of growth of eyelashes. The changes in the eyelashes were reversible and passed after the cessation of therapy.

    Trilactan® contains benzalkonium chloride, often used as a preservative in ophthalmic drugs. Benzalkonium chloride may cause eye irritation, punctate keratopathy and / or toxic ulcerative keratopathy and absorbed soft contact lenses and discolor them. It requires careful monitoring of the condition of patients with dry eye syndrome or other corneal diseases with long-term use of latanoprost. Before using the drug, it is necessary to remove the contact lenses and re-install them no earlier than 15 minutes after instillation.See also "Method of administration and dose".

    Children

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

    Information about the safety of long-term use of latanoprost in children is absent. In primary congenital glaucoma in children from 0 to 3 years of age, surgical intervention (goniotomy / trabeculotomy) remains the standard method of treatment.

    Effect on the ability to drive transp. cf. and fur:

    As with the application of other ophthalmic drugs, a temporary visual impairment is possible; before it is restored to operate vehicles or work with mechanisms is not recommended.

    Form release / dosage:

    Eye drops 0.005%.

    Packaging:

    2.5 ml into a bottle with a dropper, low density polyethylene and the lid from the first control opening of the vial or dropper, high density polyethylene together with the lid and screwed plug-dropper.

    1 or 3 vials together with instructions for use, resistant device whether or not a pack of cardboard.

    Storage conditions:

    At a temperature of 2 to 8 ° C.

    The opened vial should be stored at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    After opening the bottle - 1 month.

    Do not use after the expiration date!

    Terms of leave from pharmacies:On prescription
    Registration number:LP-004254
    Date of registration:19.04.2017
    Expiration Date:19.04.2022
    The owner of the registration certificate:GROTEKS, LLC GROTEKS, LLC Russia
    Manufacturer: & nbsp
    Information update date: & nbsp11.05.2017
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