Active substanceLatanoprostLatanoprost
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  • Dosage form: & nbsptoapley eye
    Composition:

    1 ml of the solution contains:

    active substance: Latanoprost in terms of 100% substance - 0.05 mg;

    Excipients: Benzalkonium chloride 0.2 mg, sodium chloride 4.0 mg, sodium dihydrogen phosphate monohydrate 4.5 mg, sodium hydrophosphate anhydrous 4.7 mg, water for injection up to 1 ml.

    Description:Pcolorless liquid.
    Pharmacotherapeutic group:Antiglaucoma means - prostaglandin F2-alpha analogue synthetic
    ATX: & nbsp

    S.01.E.E   Prostaglandin analogues

    S.01.E.E.01   Latanoprost

    Pharmacodynamics:

    Active substance latanoprost, an analogue of prostaglandin F2α, is a selective proponoid FP receptor agonist. Latanoprost helps to reduce intraocular pressure by increasing the outflow of watery moisture, mainly by the uveoscleral route, and also through the trabecular network. Decrease in intraocular pressure begins approximately 3-4 hours after the administration of the drug, and the maximum effect occurs after 8-12 hours. The hypotensive effect lasts about 24 hours.

    Latanoprost has no significant effect on the production of aqueous humor, does not affect the hemato-ophthalmic barrier.

    Determined that latanoprost in therapeutic doses 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 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, entering the systemic bloodstream, is metabolized mainly in the liver by beta-oxidation of fatty acids to form 1,2-dinor- and 1,2,3,4-tetranor metabolites.

    Excretion

    Latanoprost acid is rapidly eliminated from the 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 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 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 or other components of the drug;

    - atozrast up to 1 year (efficiency and safety not established);

    - bThe periodicity and the period of breastfeeding (see the section on "Application during pregnancy and during breastfeeding").

    Carefully:

    Care should be taken when using the drug in patients with aphakia, pseudoafacies with rupture of the posterior capsule of the lens, in patients with known risk factors for macular edema (in the treatment with latanoprost, cases of development of macular edema, including cystic edema) are described; inflammatory, neovascular or congenital glaucoma (due to a lack of experience in the use of the drug).

    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 effect of latanoprost on male and female fertility was not found in animal studies.

    Dosing and Administration:

    Dosing regimen in adults (including the elderly)

    One drop to the affected eye (a) once a day. The optimal effect is achieved with Lanotan in the evening.

    Do not instillation of the drug more 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 the section "Special instructions").

    If several eye dosage forms are used simultaneously, their application should be delimited by a 5-minute interval.

    Dosage regimen in children

    The drug Lanotan 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:

    Most of the undesirable phenomena 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 / 10000, <1/1000); very rarely (<1/10000); 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

    Very often: hyperpigmentation of the iris, congestion of the conjunctiva, irritation of the eyes from mild to moderate (burning sensation, sensation of sand in the eyes, itching, tingling and foreign body sensation), eyelashes (increase in length, thickness, quantity and pigmentation).

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

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

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

    Very 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 iris.

    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.

    From the nervous system

    The frequency is unknown: dizziness, headache.

    From the heart

    Very rare: aggravation of angina pectoris in patients with concomitant angina.

    Frequency unknown: sensation of palpitations.

    On the part of the respiratory system

    Rare: bronchospasm (including disease exacerbation in patients with asthma disease), shortness of breath.

    From the skin and subcutaneous tissues

    Infrequent: rash.

    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

    The frequency is unknown: myalgia, arthralgia.

    Common violations and local reactions

    Very rarely: chest pain.

    Children

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

    Overdose:

    In addition to eye irritation and hyperemia, and other unwanted reaction from the body of an overdose of the drug Lanotan not described.

    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 latanoprost is metabolized by the "first pass" through the liver. Intravenous infusion at a dose of 3 μg / kg in healthy volunteers did not cause any symptoms, but with a dose of 5.5-10 μg / kg, nausea, abdominal pain, dizziness, fatigue, "hot flashes" and sweating were observed. Intravenous administration of latanoprost to monkeys at a dose of 500 μg / kg did not cause significant effects from the cardiovascular system.

    Intravenous introduction of latanoprost to monkeys caused a transient bronchospasm. In patients with moderate bronchial asthma, the instillation 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:

    There is no single-valued data on drug interactions of latanoprost.

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

    In studies in vitro It is shown that when mixing eye drops containing thiomersal with eye drops containing latanoprost, a precipitate is formed. If a simultaneous application of these drugs is necessary, a 5-minute interval between their instillations should be observed.

    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 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 four years of treatment. The progression of 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, predominating 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 Lanotan 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. In connection with the lack of experience with the use of latanoprost in the treatment of an acute attack of closed-angle glaucoma, caution should be used in such patients.

    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, observed during therapy latanoprost mainly in patients with aphakia, psevdoafakiey, rupture of posterior lens capsule, or in patients with risk factors for cystic macular edema (and particularly in 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 asthma and / or the appearance of dyspnea have been observed in the post-marketing 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.

    Lanotan contains 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 adsorbed by 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 Lanolot, it is necessary to remove 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:

    Like the use 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, 0.05 mg / ml.
    Packaging:

    For 2.5 ml in polyethylene bottles, ukuporennyh droppers and caps with polyethylene screw with the control of opening. Each label is labeled self-adhesive.

    One bottle together with the instruction for medical use is put in a pack of cardboard.

    Storage conditions:

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

    After opening, the vial should be stored at a temperature not exceeding 25 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Shelf life after opening the bottle is 42 days.

    Do not use after the expiration date printed on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-003796
    Date of registration:18.08.2016
    Expiration Date:18.08.2021
    The owner of the registration certificate:FARMAK, PAO FARMAK, PAO Ukraine
    Manufacturer: & nbsp
    Representation: & nbspFARMAK PAOFARMAK PAO
    Information update date: & nbsp14.02.2018
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