Composition, form of production and packaging
Eye drops transparent, colorless.
latanoprost 0.05 mg
Excipients: benzalkonium chloride - 0.2 mg, sodium chloride - 4.1 mg, disodium hydrophosphate anhydrous - 4.74 mg, sodium dihydrogen phosphate monohydrate - 4.6 mg, water d / and - up to 1 ml.
2.5 ml - a bottle-dropper polyethylene (1) - packs cardboard.
2.5 ml - a bottle-dropper polyethylene (3) - packs cardboard.
5 ml - a bottle-droppers polyethylene (1) - packs cardboard.
5 ml - a bottle-droppers polyethylene (3) - packs cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
Latanoprost is an analogue of prostaglandin F2? - is a selective agonist of FP receptors 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.
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.
Latanoprost, being a prodrug form, is absorbed through the cornea, where its hydrolysis occurs to a biologically active acid. Concentration in watery moisture reaches a maximum about 2 hours after topical application.
V d is 0.16 В± 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, 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.
Latanoprost acid is rapidly removed from the plasma (T 1/2 = 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.
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 C max of latanoprost acid in blood plasma is 5 minutes for all age groups. T 1/2 acid latanoprost in children is the same as in adults. At equilibrium concentration no cumulation of latanoprost acid in the blood plasma occurs.
- Decreased increased intraocular pressure (IOP) in adults and children (over 1 year old) with open-angle glaucoma or an elevated ophthalmotonus.
Note: In children younger than 3 years with primary congenital glaucoma, first-line therapy remains surgical treatment (trabeculotomy / goniotomy).
In adults and children older than 1 year - one drop in the affected eye (a) 1 time per 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 the installation of each drop, it is recommended to apply pressure to the lower lacrimal point located at the inner corner of the eye in the lower eyelid. This must be done within 1 minute.
The following undesirable reactions related to the use of the drug were recorded:
From the side of the organ of vision: irritation of the eyes (burning sensation, sensation of sand in the eyes, itching, tingling and sensation of foreign body); blepharitis; hyperemia of the conjunctiva; Pain in the eyes; increased pigmentation of the iris; transient point erosions of the epithelium, edema of the eyelids, perforbital edema, edema and erosion of the cornea; conjunctivitis; lengthening, thickening, increasing the number and increasing pigmentation of eyelashes and gun hair; iritis / uveitis; keratitis; macular edema, incl. cystoid; changing the direction of growth of eyelashes, sometimes causing eye irritation; blurred vision, photophobia, dryness of the eye mucosa.
From the skin and subcutaneous tissues: a rash, darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal nskroliz.
From the nervous system: dizziness, headache.
On the part of the respiratory organs: bronchospasm (including acute attacks or exacerbation of the disease in patients with bronchial asthma in the anamnesis), shortness of breath.
From the musculoskeletal system and connective tissue: pain in the muscles / joints.
General and local reactions: nonspecific pain in the chest.
Infections and invasions: herpetic keratitis.
There were also cases of retinal artery embolism, retinal detachment and vitreous hemorrhage in patients with diabetic retinopathy.
The safety profile of Prolatan in children did not differ from the safety profile in adults. In comparison with the adult population, nasopharyngitis and fever were most frequently observed in children.
- hypersensitivity to latanoprost or other components of the drug;
- age up to 1 year (effectiveness and safety not established).
Afakia, pseudo-aphakia with a rupture of the posterior capsule of the lens, patients with known risk factors for macular edema (in the treatment with latanoprost, cases of development of macular edema, including cystoid) are described; inflammatory, neovascular or congenital glaucoma (due to lack of sufficient experience in the use of the drug); asthma; herpetic keratitis in the anamnesis.
Prolatan should be avoided in patients with active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin analogues. Prolatan should be used with caution in patients with risk factors for developing iritis / uveitis. There are limited data on the use of Prolatan in patients who are scheduled for surgery for cataracts. In connection with this, Prolatan should be used with caution in this group of patients.
PREGNANCY AND LACTATION
Adequate controlled studies in pregnant women have not been conducted. 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 into breast milk, so during breastfeeding the drug should be used with caution.
APPLICATION FOR CHILDREN
Contraindicated in children under 1 year of age. efficiency and safety are not established.
The safety profile of Prolatan in children older than 1 year did not differ from the safety profile in adults. In comparison with the adult population, nasopharyngitis and fever were most frequently observed in children.
Preparation Prolatan should be used not more often than once a day, as 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.
Preparation Prolatan can be used simultaneously 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 preparation Prolatan includes benzalkonium chloride, which can be absorbed by contact lenses. Before dropping drops, contact lenses must be removed and reinstalled after 15 minutes.
Prolatan 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 Prolatan can be continued 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 speed of progressing pigmentation decreases over time and stabilizes after 5 years. In more distant terms, the effects of increased iris pigmentation have not been 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.
Prolate preparation 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.
Patients who apply drops to only one eye may develop heterochromia.
The use of eye drops can cause a transient blurred vision.
Impact on the ability to drive and other mechanisms
It is necessary to drive with care or use complex equipment during the use of the drug.
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.
If the ProAltan preparation is taken orally orally, the following information should be considered: one bottle with 2.5 ml of solution contains 125 Ојg of latanoprost, 5 ml - 250 Ојg of latanoprost. More than 90% of the drug is metabolized at the first pass through the liver. Intravenous infusion in a dose of 3 Ојg / kg in healthy volunteers did not cause any symptoms, however, when a dose of 5.5-10 Ојg / 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.
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 incompatible with eye drops containing thiomersal - precipitation.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
Store at 2-8 В° C, in a place protected from light. The opened vial should not be stored for more than 45 days at a temperature not exceeding 25 В° C. Keep out of the reach of children. Shelf life - 2 years. 45 days after opening the bottle. Do not use after the expiration date printed on the package.