From the musculoskeletal system.
Antiglaucoma agent - an analogue of prostaglandin F2a. To reduce elevated intraocular pressure in adults and children (over 1 year of age) with open-angle glaucoma or increased ophthalmotonus. Apply 1 drop 1 time per day.
Latanoprost- prostaglandin F2a analogue - is a selective FP receptor agonist and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly through the uveoscleral route, as well as through the trabecular meshwork.
The decrease in IOP begins approximately 3-4 hours after administration of the drug, the maximum effect is observed after 8-12 hours, the effect lasts for at least 24 hours.
It has been established that latanoprost does not have a significant effect on 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.
Reduction of elevated intraocular pressure (IOP) in adults and children (over 1 year of age) with open-angle glaucoma or increased ophthalmotonus.
Note: In children under 3 years of age with primary congenital glaucoma, surgical treatment (trabeculotomy/goniotomy) remains the first-line treatment.
In adults and children over 1 year of age, one drop into the affected eye(s) once a day. The optimal effect is achieved when using the drug in the evening.
As when using any eye drops, in order to reduce the possible systemic effect of the drug, immediately after instillation of each drop it is recommended to press on the lower lacrimal opening, located at the inner corner of the eye on the lower eyelid. This must be done within 1 minute.
From the side of the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itching, tingling and foreign body sensation); blepharitis; conjunctival hyperemia; Pain in the eyes; increased pigmentation of the iris; transient punctate erosions of the epithelium, eyelid edema, periorbital edema, edema and erosions of the cornea; conjunctivitis; lengthening, thickening, increasing the number and increasing pigmentation of eyelashes and vellus hair; iritis/uveitis; keratitis; macular edema, incl. cystoid; change in the direction of eyelash growth, sometimes causing eye irritation; blurred vision, photophobia, dry eye mucosa.
For the skin and subcutaneous tissues: rash, darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal necrolysis.
From the nervous system: dizziness, headache.
From the respiratory system: bronchospasm (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath.
From the musculoskeletal system and connective tissue: muscle/joint pain.
General and local reactions: nonspecific chest pain.
Infections and infestations: herpetic keratitis.
Cases of retinal artery embolism, retinal detachment and vitreous hemorrhage have also been reported in patients with diabetic retinopathy.
Children
The safety profile of the drug in children did not differ from the safety profile in adults. Compared with the adult population, nasopharyngitis and fever were most frequently reported in children.
Hypersensitivity to latanoprost or other components of the drug.
Age up to 1 year (efficacy and safety have not been established).
The drug should be used no more than once a day, since more frequent administration 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.
The drug can be used concomitantly with other classes of topical ophthalmic drugs to reduce IOP. If the patient is using other eye drops at the same time, they should be used at least 5 minutes apart.
The drug contains benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, contact lenses must be removed and reinserted after 15 minutes.
The drug 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 melanin content 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 become brown. In most cases, the color change is minor and may not be clinically detectable.
Increased pigmentation of the iris of one or both eyes is observed mainly in patients with mixed iris color, containing a brown color as a base.
The drug has no effect on nevi and lentigines of the iris; no accumulation of pigment in the trabecular meshwork or in the anterior chamber of the eye was noted.
When two prostaglandin analogues are instilled into the eyes simultaneously, a paradoxical increase in IOP has been described, so the simultaneous use of two or more prostaglandins, their analogues or derivatives Not recommended.
Pharmaceutically incompatible with eye drops containing thiomersal- precipitation.
Instructions for use
Xalatan drops hl. 0.005% 2.5ml No. 3
Dosage forms
eye drops 0.005% 2.5ml
Synonyms
Glaumax
Glauprost
Xalatamax
Latanomol
Prolatan
Group
Antiglaucoma drugs
International nonproprietary name
Latanoprost
Compound
The active substance is latanoprost.
Manufacturers
Pfizer MFG. Belgium N.V. (Belgium), Pharmacia and Upjohn (Belgium), Pharmacia N.V./S.A. (Belgium)
pharmachologic effect
Latanaprost, a prostaglandin F 2 alpha analogue, is a selective FP (prostaglandin F) receptor agonist and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly through the uveoscleral pathway, as well as through the trabecular meshwork. The decrease in IOP begins approximately 3-4 hours after administration of the drug, the maximum effect is observed after 8-12 hours, the effect lasts for at least 24 hours. It has been established that latanoprost does not have a significant effect on 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. Pharmacokinetics. Suction. Latanoprost is a prodrug, absorbed through the cornea, where it is hydrolyzed (under the action of esterases) to form a biologically active compound - latanoprost acid. Concentration in aqueous humor reaches a maximum approximately two hours after topical application of the drug. 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 during the first hour after topical application. Metabolism. Latanoprost acid entering the systemic circulation 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 cleared from plasma: the half-life 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, approximately 88% of the dose is excreted in the urine. Pharmacokinetics in special clinical cases. 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 between children and adults. The time to reach the maximum concentration of latanoprost acid in the blood plasma is 5 minutes for all age groups. The half-life of latanoprost acid in children is the same as in adults. At equilibrium concentration, latanoprost acid does not accumulate in the blood plasma.
Side effect
The following adverse reactions related to the use of the drug have been registered. From the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itching, tingling and foreign body sensation), blepharitis, conjunctival hyperemia, eye pain, increased pigmentation of the iris, transient point erosions of the corneal epithelium, eyelid edema, periorbital edema, swelling and erosion of the cornea, conjunctivitis, lengthening, thickening, increase in the number and intensification of pigmentation of eyelashes and vellus hair, iritis/uveitis, keratitis, macular edema (including cystoid), change in the direction of eyelash growth, sometimes causing eye irritation, additional growth row of eyelashes above the meibomian glands, changes in the periorbital region and in the eyelash area, leading to a deepening of the furrow of the upper eyelid, blurred vision, photophobia, dry mucous membrane of the eyes. From the skin: rash, darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal necrolysis. From the nervous system: dizziness, headache. From the respiratory system: bronchospasm (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath. From the musculoskeletal system: muscle pain, joint pain. Other: nonspecific chest pain, herpetic keratitis. Cases of retinal artery embolism, retinal detachment and vitreous hemorrhage have also been reported in patients with diabetic retinopathy. Children. The safety profile of the drug in children did not differ from the safety profile in adults. Compared with the adult population, nasopharyngitis and fever were most frequently reported in children.
Indications for use
Reduction of elevated intraocular pressure IOP in adults and children (over 1 year of age) with open-angle glaucoma or increased ophthalmotonus.
Contraindications
Hypersensitivity to latanoprost or other components of the drug. Age up to 1 year (efficacy and safety have not been established).
Directions for use and dosage
In adults and children over 1 year of age - 1 drop into the affected eye(s) 1 time per day. The optimal effect is achieved when using the drug in the evening. As when using any eye drops, in order to reduce the possible systemic effect of the drug, immediately after installing each drop, it is recommended to press on the lower lacrimal opening, located at the inner corner of the eye on the lower eyelid. This must be done within 1 minute.
Overdose
Apart from irritation of the mucous membrane of the eyes, hyperemia of the conjunctiva or episclera, no other undesirable changes in the organ of vision are known with an overdose of latanoprost. If you accidentally take latanoprost orally, the following information should be taken into account: one bottle of 2.5 ml of solution contains 125 mcg of latanoprost. More than 90% of the drug is metabolized during the first passage through the liver. Intravenous infusion at a dose of 3 mcg/kg in healthy volunteers did not cause any symptoms, however, when a dose of 5.5-10 mcg/kg was administered, nausea, abdominal pain, dizziness, fatigue, hot flashes and sweating were observed. In patients with moderate bronchial asthma, administration of latanoprost into the eyes at a dose 7 times higher than the therapeutic dose did not cause bronchospasm. Treatment: symptomatic therapy.
Interaction
When two prostaglandin analogs are instilled into the eyes simultaneously, a paradoxical increase in IOP has been described, therefore the simultaneous use of two or more prostaglandins, their analogs or derivatives is not recommended. Pharmaceutically incompatible with eye drops containing thiomersal (precipitation occurs).
special instructions
Carefully. Aphakia, pseudophakia with rupture of the posterior capsule of the lens, patients with risk factors for macular edema (cases of the development of macular edema, including cystoid, have been described during treatment with latanoprost); inflammatory, neovascular glaucoma (due to lack of sufficient experience in using the drug); history of bronchial asthma, herpetic keratitis. The use of the drug should be avoided in patients with active herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin F2 alpha analogues. The drug should be used with caution in patients with risk factors for developing iritis/uveitis. There is limited data on the use of the drug in patients undergoing cataract surgery. In this regard, it should be used with caution in this group of patients. Pregnancy and lactation. There have been no adequate controlled studies in pregnant women. The drug should be prescribed during pregnancy only in cases where the potential benefit to the mother outweighs the possible risk to the fetus. Latanoprost and its metabolites can be excreted into breast milk, so the drug should be used with caution during breastfeeding. The drug should be prescribed no more than once a 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 concomitantly with other classes of topical ophthalmic medications to lower IOP. If the patient is using other eye drops at the same time, they should be used at least 5 minutes apart. The drug contains benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, contact lenses must be removed and reinserted after 15 minutes. Latanoprost may cause a gradual increase in brown pigment in the iris. The change in eye color is caused by an increase in the melanin content 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 become brown. In most cases, the color change is minor and may not be clinically detectable. Increased pigmentation of the iris of one or both eyes is observed mainly in patients with mixed iris color, containing a brown color as a base. The drug has no effect on nevi and lentigines of the iris; no accumulation of pigment in the trabecular meshwork or in the anterior chamber of the eye was noted. When determining the degree of pigmentation of the iris for more than 5 years, no undesirable consequences of increased pigmentation were revealed, 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 treatment may be discontinued depending on the clinical situation. Increased pigmentation of the iris is usually observed during the first year after the start of 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 stopping treatment, no increase in brown pigmentation of the iris was noted, 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 have been described, which may be reversible. Latanoprost may cause gradual changes in eyelashes and vellus hairs, such as lengthening, thickening, increased pigmentation, increased thickness, and a change in the direction of eyelash growth. Changes in eyelashes are reversible and disappear after cessation of treatment. Patients using drops in only one eye may develop heterochromia. Influence on the ability to drive vehicles and operate machinery. The use of eye drops may cause transient blurred vision. Driving a car or using complex machinery while using the drug should be done with caution.
Storage conditions
Store in a place protected from light, out of reach of children, at a temperature of 2 to 8 C. Store an opened bottle at a temperature not exceeding 25 C.
Reduction of elevated intraocular pressure IOP in adults and children (over 1 year of age) with open-angle glaucoma or increased ophthalmotonus.
Contraindications Xalatan eye drops 0.005% 2.5ml
Hypersensitivity to latanoprost or other components of the drug. Age up to 1 year (efficacy and safety have not been established).
Directions for use and dosage Xalatan eye drops 0.005% 2.5ml
Dosage regimen for adults (including the elderly). One drop into the affected eye(s) once daily. The optimal effect is achieved when using the drug in the evening. The drug should not be instilled more often than once a day, since more frequent administration has been shown to reduce the hypotensive effect. If one dose is missed, treatment is continued as usual. As when using any eye drops, in order to reduce the possible systemic effect of the drug, immediately after instillation of each drop, it is recommended to press for 1 minute on the lower lacrimal opening, located at the inner corner of the eye on the lower eyelid. This procedure must be performed immediately after instillation. Before instillation, it is necessary to remove contact lenses and install them no earlier than 15 minutes after insertion. If it is necessary to use other eye drops at the same time, their use should be separated by a 5-minute interval. Latanoprost is used in children at the same dose as in adults. Data on the use of the drug in premature infants (gestational age
Xalatan ® should be prescribed no more than 1 time/day, because 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 concomitantly with other classes of topical ophthalmic medications to lower IOP. If the patient is using other eye drops at the same time, they should be used at least 5 minutes apart.
Xalatan ® contains benzalkonium chloride, which can be absorbed by contact lenses. Before instilling drops, contact lenses must be removed and reinserted after 15 minutes.
Latanoprost may cause a gradual increase in brown pigment in the iris. The change in eye color is caused by an increase in the melanin content 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 become brown. In most cases, the color change is minor and may not be clinically detectable. Increased pigmentation of the iris of one or both eyes is observed mainly in patients with mixed iris color, containing a brown color as a base. The drug has no effect on nevi and lentigines of the iris; no accumulation of pigment in the trabecular meshwork or in the anterior chamber of the eye was noted.
When determining the degree of pigmentation of the iris for more than 5 years, no undesirable consequences of increased pigmentation were revealed, 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 treatment may be discontinued depending on the clinical situation.
Increased pigmentation of the iris is usually observed during the first year after the start of 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 stopping treatment, no increase in brown pigmentation of the iris was noted, 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 have been described, which may be reversible.
Latanoprost may cause gradual changes in eyelashes and vellus hairs, such as lengthening, thickening, increased pigmentation, increased thickness, and a change in the direction of eyelash growth. Changes in eyelashes are reversible and disappear after cessation of treatment.
Patients using drops in only one eye may develop heterochromia.
Impact on the ability to drive vehicles and operate machinery
The use of eye drops may cause transient blurred vision. Driving a car or using complex machinery while using the drug should be done with caution.
Composition and release form
Eye drops 0.005% - 1 ml latanoprost - 50 mcg excipients: sodium chloride; sodium dihydrogen phosphate (monohydrate); sodium hydrogen phosphate (anhydrous); benzalkonium chloride; water for injection in 2.5 ml dropper bottles; There are 1 or 3 bottles in a cardboard pack.
Description of the dosage form
Transparent colorless solution.
Characteristic
Analogue of PG F2-alpha (with molecular weight 432.58).
pharmachologic effect
It is a selective agonist of receptors for PG F2-alpha.
Pharmacokinetics
Increases the uveoscleral outflow of aqueous humor but does not have a significant effect on its production. In the form of an inactive precursor (latanoprost is an isopropyl ether), it penetrates well through the cornea, hydrolyzing to the biologically active acid latanoprost. Cmax in aqueous humor is reached approximately 2 hours after application. In the tissues of the eye, the active form is almost not metabolized; metabolism occurs mainly in the liver. T1/2 - 17 min. The 2 main metabolites are inactive and are excreted mainly in the urine.
Pharmacodynamics
By increasing uveoscleral outflow, it reduces the aqueous humor content in the internal media of the eye and reduces intraocular pressure. The effect begins 3-4 hours after administration, reaches a maximum after 8-12 hours and lasts for at least 24 hours. It does not affect the production of aqueous humor or the permeability of the blood-ophthalmic barrier.
Indications for use
Glaucoma
Contraindications for use
hypersensitivity to the drug.
Use during pregnancy and children
Contraindicated during pregnancy, breastfeeding and childhood.
Side effects
- sensation of a foreign body in the eye, redness of the eye;
- change in iris color;
- skin rash.
Drug interactions
The decrease in intraocular pressure increases when combined with beta-blockers (timolol), adrenergic agonists (dipivalyl adrenaline), carbonic anhydrase inhibitors (acetazolamide); with cholinomimetics - weaker. Pharmaceutically incompatible with thiomersal (precipitation).
Dosage
in the evening, 1 drop into the affected eye, once; if a dose is missed, the next one is administered as usual, i.e. 1 drop. When used together with other drugs in drops, they are administered at intervals of at least 5 minutes.
Overdose
Symptoms: episclera or conjunctival hyperemia, irritation of the mucous membrane of the eyes.
Symptomatic therapy is used as treatment.
Precautionary measures
Before treatment, it is necessary to inform the patient about a possible change in eye color. During treatment, mandatory regular examinations of iris pigmentation are required, because color changes develop slowly and may not be noticeable for several months; If there is an intense increase in pigmentation, treatment is stopped.
