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Xalatan eye drops - is an ophthalmic drug for reducing intraocular pressure in patients with ophthalmotonus and treating open-angle glaucoma. Improves the outflow of watery moisture, which leads to a decrease in intraocular pressure, thereby preventing the progression of glaucoma symptoms (which leads to an irreversible loss of vision - blindness). At the moment is one of the effective drugs for the treatment of glaucoma.
The antiglaucoma preparation, analogue of prostaglandin F2α, is a selective agonist of FP receptors (prostaglandin F) and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor mainly by uveoscleral route, and also through the trabecular network.
It has been established that latanoprost does not significantly affect the production of aqueous humor and the hemato-ophthalmic barrier.
When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems.
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 is a prodrug, absorbed through the cornea, where its hydrolysis occurs (under the action of esterases) to form a biologically active acid. Cmax of latanoprost in aqueous humor is achieved approximately 2 hours after topical application of the preparation.
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.
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.
Latanoprost acid is rapidly removed from the plasma: T1 / 2 is 17 minutes. 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 dose is excreted.
Pharmacokinetics in special clinical cases
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 Cmax of latanoprost acid in blood plasma is 5 minutes for all age groups. T1 / 2 acid latanoprost in children is the same as in adults. At equilibrium concentration no cumulation of latanoprost acid in the blood plasma occurs.
Decreased elevated intraocular pressure (IOP) in adults and children (over 1 year old) with open-angle glaucoma or an elevated ophthalmotonus.
The drug Xalatan should not be used more than once a day, as the more frequent introduction of latanoprost leads to a weakening of the IOP-lowering effect.
If you miss one dose, the next dose should be administered at the usual time.
Latanoprost can be used concurrently with other classes of ophthalmic drugs for topical use in order to reduce IOP. If the patient simultaneously uses other eye drops, they should be applied at intervals of at least 5 minutes.
The composition of the drug Xalatan includes benzalkonium chloride, which can be absorbed by contact lenses. Before dropping drops, contact lenses must be removed and reinstalled after 15 minutes.
Latanoprost can cause a gradual increase in the content of brown pigment in the iris. 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 parts of it become brown. In most cases, discoloration is negligible and may not be clinically established. The enhancement of the pigmentation of the iris of one or both eyes is observed, mainly, in patients with a mixed color of the iris, which is based on a brown color. The drug does not affect the nevi and lentigo iris; The accumulation of pigment in the trabecular network or in the anterior chamber of the eye was not noted. In determining the degree of pigmentation of the iris for more than 5 years, no undesirable effects of pigmentation enhancement have been detected even with the continuation of latanoprost therapy. In patients, the degree of IOP decrease was the same regardless of the presence or absence of enhancement of the pigmentation of the iris. Therefore, treatment with latanoprost can continue in cases of increased pigmentation of the iris. Such patients should be under regular supervision and, depending on the clinical situation, treatment can be discontinued. Increased pigmentation of the iris is usually observed during the first year after initiation of treatment, rarely - during the second or third year. After the fourth year of treatment this effect was not observed. The rate of progression of pigmentation decreases with time and stabilizes after 5 years. In more distant terms, the effects of increased iris pigmentation were not studied. After the cessation of treatment of the enhancement of brown pigmentation, the iris was not noted, however, the discoloration of the eyes may be irreversible.
In connection with the use of latanoprost, cases of darkening of the eyelid skin, which can be reversible, are described.
Latanoprost can cause gradual changes in eyelashes and fleece hair, such as lengthening, thickening, increasing pigmentation, increasing the density and changing the direction of growth of the eyelashes. The eyelash changes are reversible and pass after the cessation of treatment.
Patients who apply drops to only one eye may develop heterochromia.
Impact on the ability to drive vehicles and manage mechanisms
The use of eye drops can cause a transient blurred vision. It is necessary to drive with care or use complex equipment during the use of the drug.
Immediately after instillation, Xalatan eye drops can cause a temporary increase in symptoms of irritation of the mucous membrane of the eyes, which can manifest as lacrimation, slight tingling or burning, red eyes, transient visual acuity, corneal edema or eyelids. The drug can provoke the development of eye inflammation (uveitis, keratitis, conjunctivitis) and edema of the macula.
Very rarely the drug can cause allergic reactions, headache, dizziness, pain in the muscles and joints, bronchospasm.
It is necessary to warn the patient about the possibility of changing the color of the eyes, which is associated with increased pigmentation of the iris, as well as the possibility of darkening the skin of the eyelids and increasing eyelash growth. The above changes are reversible.
Symptoms: In addition to irritation of the mucous membrane of the eyes, conjunctival hyperemia or episclerosis, other undesirable changes from the side 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 at 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 adults and children older than 1 year: one drop in the affected eye (a) once a day. The optimal effect is achieved with the use of the drug in the evening.
As with any eye drops, in order to reduce the possible systemic effect of the drug, immediately after instillation each drop is recommended to press down the tear point located at the inner corner of the eye in the lower eyelid. This must be done within 1 minute.
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