Xalatan eye drops 0.005% 2.5ml, 3pcs

Composition

>1 ml of the solution contains: Active ingredient: latanoprost – 50 mcg; excipients: sodium chloride, sodium dihydrogen phosphate (monohydrate), sodium hydrophosphate (anhydrous), benzalkonium chloride, water for injection.

Pharmacological action

Pharmacodynamicalatanoprost, an analog of prostaglandin F2a, is a selective agonist of FP (prostaglandin F) 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 use of the drug, the maximum effect is observed after 8-12 hours, and the effect persists for at least 24 hours. It was found that latanoprost does not significantly affect the production of aqueous humor and the blood-ophthalmic barrier. When used in therapeutic doses, latanoprost does not have a significant pharmacological effect on the cardiovascular and respiratory systems. Pharmacokineticsabsorption Latanoprost, being a prodrug, is absorbed through the cornea, where it is hydrolyzed to a biologically active acid. The concentration in the aqueous humor reaches a maximum about two hours after topical application. Distributionthe volume of distribution is 0.16 ± 0.02 l / kg. Latanoprost acid is detected in aqueous humor during the first 4 hours, and in plasma-only during 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 circulation is mainly metabolized in the liver by beta-oxidation of fatty acids to form 1,2-dinor-and 1,2,3,4-tetranor-metabolites. Elimination Latanoprost acid is rapidly eliminated from plasma (t1 / 2 =17 min). The systemic clearance is approximately 7 ml / min / kg. After beta-oxidation in the liver, metabolites are mainly excreted by the kidneys: after topical application, approximately 88% of the administered dose is excreted in the urine. Children’s exposure to latanoprost is approximately 2 times higher in children aged 3 to 12 years compared to adult patients and 6 times higher in children under 3 years of age. However, the safety profile of the drug does not differ 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 acid in children is the same as in adults. No accumulation of latanoprost acid in the blood plasma occurs at the equilibrium concentration.

Indications

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

Use during pregnancy and lactation

No adequate controlled trials have been conducted in pregnant women. The drug should be prescribed during pregnancy only in cases where the potential benefit to the mother exceeds the possible risk to the fetus. Latanoprost and its metabolites can be excreted in breast milk, so the drug should be used with caution during breast-feeding.

Contraindications

• age up to 1 year (efficacy and safety have not been established);
• hypersensitivity to latanoprost or other components of the drug.

The drug should be used with caution in patients with aphakia, pseudoaphakia with rupture of the posterior lens capsule, in patients with risk factors for macular edema (cases of macular edema, including cystoid edema, have been described during treatment with latanoprost); in patients with inflammatory, neovascular glaucoma (due to lack of sufficient experience with the drug); in patients with bronchial asthma, herpetic keratitis in the anamnesis.

The use of Xalatan should be avoided in patients with active herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin f2a analogues.

Xalatan should be used with caution in patients with risk factors for iritis/uveitis.

There are limited data on the use of Xalatan in patients who are planning cataract surgery. Therefore, Xalatan should be used with caution in this group of patients.

Side effects

The following adverse reactions related to the use of the drug have been reported: From the side of the visual organ:  eye irritation (burning sensation, sand sensation in the eyes, itching, tingling and foreign body sensation); blepharitis; conjunctival hyperemia; eye pain; increased iris pigmentation; transient pinpoint erosion of the corneal epithelium, eyelid edema, periorbital edema, corneal edema and erosion; conjunctivitis; elongation, thickening, increase in the number and strengthening of pigmentation of eyelashes and downy hair; iritis/uveitis; keratitis; macular edema, including cystoid; changes in the direction of eyelash growth, sometimes causing eye irritation; growth of an additional row of eyelashes over the Meibomian glands, changes in the periorbital area and in the area of the eyelashes, leading to a deepening of the furrow of the upper eyelid; blurred vision, photophobia, dryness of the eye mucosa. Skin and subcutaneous tissue disorders:  rash, darkening of the eyelid skin and local skin reactions on the eyelids, toxic epidermal necrolysis. Nervous system disorders:  dizziness, headache. Respiratory system disorders:  bronchospasm (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath. Musculoskeletal and connective tissue disorders:  muscle/joint pain. General and local reactions:  non-specific chest pain. Infections and infestations:  herpetic keratitis. Retinal artery embolism, retinal detachment, and vitreous hemorrhage have also been reported in patients with diabetic retinopathy. In some patients with significant corneal damage, very rare cases of corneal calcification have been reported due to the use of phosphate-containing eye drops. Xalatan®Safety Detyprofil the safety profile in children did not differ from that in adults. Compared to the adult population, children had the most frequent cases of nasopharyngitis and fever.

Interaction

When two prostaglandin analogues are simultaneously instilled into the eyes, a paradoxical increase in IOP has been described, so the simultaneous use of two or more prostaglandins, their analogues or derivatives is not recommended.

Pharmaceutical interaction

Xalatan is incompatible with eye drops containing thiomersal (precipitation occurs)

How to take, course of use and dosage

In adults and children older than 1 year – one drop in the affected eye (s) once a day. The optimal effect is achieved when using the drug in the evening. As with 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 point located at the inner corner of the eye on the lower eyelid. This must be done within 1 minute.

Overdose

In addition to irritation of the eye mucosa, conjunctival or episcleral hyperemia, other undesirable changes on the part of the visual organ with an overdose of latanoprost are not known. In case of accidental ingestion of latanoprost, the following information should be taken into account: one bottle with 2.5 ml of the solution contains 125 mcg of latanoprost. More than 90% of the drug is metabolized at the first pass through the liver. Intravenous infusion at a dose of 3 mcg / kg in healthy volunteers did not cause any symptoms, but with a dose of 5.5-10 mcg/kg, 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 overdose, symptomatic treatment is performed.

Special instructions

Xalatan® should be prescribed no more than 1 time / day, since more frequent use 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.

Latanoprost can be used simultaneously with other classes of topical ophthalmic medications to reduce IOP. If the patient is using other eye drops at the same time, they should be applied at intervals of at least 5 minutes.

Xalatan® contains benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, the contact lenses must be removed and re-installed after 15 minutes.

Latanoprost can cause a gradual increase in the content of brown pigment 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. In typical cases, brown pigmentation appears around the pupil and extends concentrically to the periphery of the iris. In this case, the entire iris or parts of it turn brown. In most cases, the discoloration is minor and may not be detected clinically. Increased pigmentation of the iris of one or both eyes is observed mainly in patients with mixed iris color, containing brown in the base. The drug does not affect the nevi and lentigo of the iris; pigment accumulation in the trabecular network 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, there were no undesirable consequences of increased pigmentation, 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 latanoprost can be continued in cases of increased pigmentation of the iris. Such patients should be monitored regularly and, depending on the clinical situation, treatment may be discontinued.

Increased iris pigmentation is usually observed during the first year after starting treatment, rarely during the second or third year. After the fourth year of treatment, this effect is not observed. The rate of pigmentation progression decreases over time and stabilizes after 5 years. In the longer term, the effects of increased iris pigmentation have not been studied. After discontinuation of 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 skin of the eyelids, which can be reversible, have been described.

Latanoprost can cause gradual changes in the eyelashes and downy hair, such as lengthening, thickening, increasing pigmentation, increasing density, and changing the direction of lash growth. Changes to the eyelashes are reversible and disappear after treatment is stopped.

Patients who use drops in only one eye may develop heterochromia.

Influence on the ability to drive motor vehicles and manage mechanisms

The use of eye drops may cause temporary blurred vision. Drive a car or use complex equipment during the use of the drug should be used with caution.

Form of production

Xalatan. Eye drops

Storage conditions

Store at room temperature + 2 – + 8 °C in a dark place. Store the opened bottle at a temperature not exceeding + 25 °C.

Expiration date

Shelf life: 3 years Service life: 1 month

Active ingredient

Latanoprost

Conditions of release from pharmacies

By prescription

Dosage form

eye drops