Active substanceLatanoprostLatanoprost
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  • Dosage form: & nbsptoapley eye
    Composition:

    Per 1 ml:

    Active substance: latanoprost-0.05 mg;

    Excipients: benzalkonium chloride 50% solution - 0.4 mg **, sodium chloride - 4.1 mg, sodium dihydrogen phosphate dihydrate - 5.2 mg, sodium hydrogen phosphate dodecahydrate - 11.95 mg ***, purified water - from 0.99 to 1.01 ml.

    ** corresponds to 0.2 mg of benzalkonium chloride,

    *** corresponds to 4.74 mg of anhydrous disodium phosphate.

    Description:A clear, colorless solution with no visible inclusions.
    Pharmacotherapeutic group:Antiglaucoma means - prostaglandin F2-alpha 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 watery moisture, 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.

    Latanoprost has no 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:

    Suction. Latanoprost, being a prodrug, is absorbed through the cornea, where its hydrolysis occurs to a biologically active acid. Concentration in watery moisture reaches a maximum about two hours after topical application. Distribution. The volume of distribution 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 to form a biologically active acid. Latanoprost acid, which enters the systemic bloodstream, is metabolized mainly in the liver by beta-oxidation of fatty acids with the formation of 1,2-dinor- and 1,2,3,4-tetranor metabolites.

    Excretion. Latanoprost acid is rapidly removed from the plasma (tl/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 with urine, approximately 88% of the administered dose is excreted.

    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. At equilibrium concentration no cumulation of latanoprost acid in the blood plasma occurs.

    Indications:Reduction of elevated intraocular pressure (IOP) in adults and children (over the age of 1 year) with open angle glaucoma or ocular hypertension.
    Contraindications:

    Hypersensitivity to latanoprost and other components of the drug.

    Age to 1 year (efficacy and safety not established).

    Pregnancy and the period of breastfeeding (see section "Application during pregnancy and during breast-feeding").

    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) are described; inflammatory, neovascular glaucoma (due to lack of sufficient experience in the use of the drug); bronchial asthma; herpetic keratitis in the anamnesis. It should avoid the use of the drug Latanoprost-Teva in patients with active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin analogues F2α. Latanoprost-Teva should be used with caution in patients with risk factors for developing iritis / uveitis.There are limited data on the use of the drug Latanoprost-Teva in patients who are scheduled surgical intervention for cataracts. In this regard, in this group of patients the drug Latanoprost-Teva 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 in the period of 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 the of adults

    One drop to the affected eye (s) 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, as 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 the lower tear point located at the inner corner of the eye in the lower eyelid.

    Before instillation it is necessary to remove contact lenses and to establish them not earlier, than in 15 minutes after introduction.

    When joint application of latanoprost with other drugs, the interval between instillations should be at least 5 minutes.

    Dosing regimen the 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 incidence of side effects is classified according to the recommendations of the World Health Organization: very often (≥ 1/10); often (≥ 1/100, but <1/10); infrequently (≥ 1/1000, but <1/100); rarely (≥ 1/10000, but <1/1000); very rarely (<1/10000), including individual messages; the frequency is unknown - the frequency can not be estimated from the available data.

    From the side of the organ of vision: very often - increased pigmentation of the iris, mild to moderate conjunctival hyperemia, eye irritation (burning sensation, sensation of sand in the eyes, itching, tingling and foreign body sensation), lengthening, thickening, increase in the number and intensification of pigmentation of eyelashes and gun hair; often - blepharitis, pain in the eyes, transient point erosions of the corneal epithelium, photophobia; infrequently - edema of the eyelids, dryness of the mucous membrane of the eyes, keratitis, conjunctivitis, blurred vision; rarely iritis / uveitis, macular edema, periorbital edema, edema and erosion of the cornea, a change in the direction of growth of the eyelashes, sometimes causing eye irritation, the growth of an additional number of eyelashes over the meibomian glands (distichiasis); very rarely - changes in the periorbital region and in the lash area, leading to a deepening of the furrow of the upper eyelid; the frequency is unknown - the iris cyst.

    From the skin and subcutaneous tissues: infrequent - rash; rarely - darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal necrolysis.

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

    From the heart: very rarely - unstable angina; frequency unknown - sensation of palpitations.

    On the part of the respiratory system: rarely - bronchospasm (including acute attacks or exacerbation of the disease in patients with bronchial asthma in history), dyspnea.

    From the side of the musculoskeletal system and connective tissue: frequency unknown - pain in the muscles / joints.

    General and local reactions: very rarely - nonspecific pain in the chest.

    Infections and invasions: frequency unknown - herpetic keratitis.

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

    In some patients with significant damage to the cornea, very rare cases of calcification of the cornea due to the use of phosphate-containing eye drops were recorded.

    Children

    The safety profile of latanoprost in children did not differ from the safety profile in adults. In comparison with the adult population, nasopharyngitis and fever were most common in children.

    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.

    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 latanoprost It is incompatible with eye drops containing thiomersal - a precipitate is formed.

    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 be informed of the possible irreversible change 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 the study of latanoprost, darkening usually began within the first 8 months of treatment, rarely - during the second or third year and was not observed after four years of treatment. Progression of the iris pigmentation decreased with time and stabilized after 5 years. 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 composition of the drug Latanoprost-Teva is benzalkonium chloride, often used as a preservative in ophthalmic drugs. Benzalkonium chloride can cause eye irritation, spot keratopathy and / or toxic ulcer keratopathy, and also be absorbed by soft contact lenses and discolored. 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 contact lenses and re-install them not earlier than 15 minutes after instillation (see also section "Dosing and Administration").

    There were cases of discoloration of the skin of the periorbital region, which in some patients were reversible in the continuation of latanoprost therapy.

    In connection with the use of latanoprost, cases of reversible darkening of the skin of the eyelids are described. 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 the eyelashes. The eyelash changes are reversible and pass after the cessation of treatment. The use of eye drops can cause a transient blurred vision.

    The experience of using the drug Latanoprost-Teva in chronic closed-angle glaucoma,open-angle glaucoma in patients with pseudophakia, aphakia, inflammatory, neovascular glaucoma, as well as in patients with cataracts undergoing surgical treatment, is limited, so use the drug Latanoprost-Teva in these patient groups with caution.

    There have been reports of cases of development of macular edema in patients with aphakia, pseudoafacies, with a rupture of the posterior capsule of the lens, as well as with known risk factors for macular edema, therefore, Latanoprost-Teva should be used with caution in these patient groups.

    In patients with risk factors for the development of iritis, uveitis, as well as with a history of herpetic keratitis, bronchial asthma, Latanoprost-Teva should be used with caution.

    Children

    Data on efficacy and safety in children in the age group <1 year are limited. Data of latanoprost in preterm infants (less than 36 weeks of gestational age) are not available. Information about the safety of long-term use of latanoprost in children is absent.

    In children aged 0 to 3 years with primary congenital glaucoma, surgical treatment (eg trabeculotomy / goniotomy) is still the method of choice.

    Effect on the ability to drive transp. cf. and fur:Due to a decrease in vision clarity, it is not recommended to perform actions requiring an increased concentration of attention and speed of psychomotor reactions within a few minutes after using the drug Latanoprost-Teva.
    Form release / dosage:Eye drops, 0.005%.
    Packaging:

    By 2.5 ml per dropper of low-density polyethylene with a screw cap and safety cap without thread with the control of the first opening.

    1 or 3 bottles of a dropper along with the instruction for use are placed in a cardboard box.

    Storage conditions:

    Store in a dark place at a temperature of 2-8 ° C.

    Keep out of the reach of children.

    Shelf life:

    3 years.

    After opening the vial, the drug should be used within 4 weeks.

    Do not use after the expiration date.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003775
    Date of registration:10.08.2016
    Expiration Date:10.08.2021
    The owner of the registration certificate:Teva Pharmaceutical Enterprises Co., Ltd.Teva Pharmaceutical Enterprises Co., Ltd. Israel
    Manufacturer: & nbsp
    Representation: & nbspTeva Teva Israel
    Information update date: & nbsp12.03.2018
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