Composition, form of production and packaging
Eye drops 0.005% in the form of a clear, colorless solution.
latanoprost 50 Ојg
Excipients: sodium chloride - 4.1 mg, sodium dihydrogen phosphate (monohydrate) - 4.6 mg, sodium hydrophosphate (anhydrous) - 4.74 mg, benzalkonium chloride - 0.2 mg, water q / and - 995 mg.
2.5 ml - a bottle-dropper polyethylene (1) - packs cardboard with the control of the first opening.
2.5 ml - a bottle-dropper polyethylene (3) - packs cardboard with the control of the first opening.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2015.
Antiglaucoma preparation, analogue of prostaglandin F 2? , is a selective agonist of FP receptors (prostaglandin F) and reduces intraocular pressure (IOP) by increasing the outflow of aqueous humor, mainly by the 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. C max oflatanoprost in aqueous humor is achieved approximately 2 hours after topical application of the preparation.
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 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: T 1/2 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 C max of latanoprost acid in blood plasma is 5 min 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 IOP in adults and children (over 1 year old) with open-angle glaucoma or an elevated ophthalmotonus.
Adults and children older than 1 year - 1 drop in the affected eye (a) 1 time / 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 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 min.
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 corneal epithelium, edema of the eyelids, periorbital 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 (including cystoid); changing the direction of growth of eyelashes, sometimes causing eye irritation; the growth of an additional number of eyelashes over the meibomian glands, changes in the periorbital region and in the eyelash region, leading to a deepening of the furrow of the upper eyelid; blurred vision, photophobia, dryness of the eye mucosa.
From the skin: a rash, darkening of the skin of the eyelids and local skin reactions on the eyelids, toxic epidermal necrolysis.
From the nervous system: dizziness, headache.
On the part of the respiratory system: bronchospasm (including acute attacks or exacerbation of the disease in patients with bronchial asthma in the anamnesis), dyspnea.
From the musculoskeletal system: pain in the muscles, pain in the joints.
Infections and invasions: herpetic keratitis.
Other: nonspecific chest pain.
There were also cases of retinal artery embolism, retinal detachment and vitreous hemorrhage in patients with diabetic retinopathy.
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.
The safety profile of Xalatan В® in children did not differ from the safety profile in adults. In comparison with the adult population, nasopharyngitis and fever were most common in children.
- age under 1 year (efficiency and safety not established);
- hypersensitivity to latanoprost or other components of the drug.
With caution should be used in patients with aphakia, pseudoafacies with rupture of the posterior capsule of the lens, in patients with risk factors for macular edema (in the treatment with latanoprost, cases of development of macular edema, including cystoid) are described; in patients with inflammatory, neovascular glaucoma (due to lack of sufficient experience in the use of the drug); at a bronchial asthma, a herpetic keratitis in the anamnesis.
Should you avoid using Xalatan В® in patients with active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin F 2 analogues ? .
Xalatan В® should be used with caution in patients with risk factors for developing iritis / uveitis.
There are limited data on the use of Xalatan В® in patients who are scheduled for surgery for cataracts. In this regard, in this group of patients Xalatan В® should be used with caution.
PREGNANCY AND LACTATION
Adequate controlled studies in pregnant women have not been conducted. The drug should be prescribed during pregnancy only in those cases when the expected benefit for the mother exceeds the possible risk to the fetus.
Latanoprost and its metabolites can be excreted in breast milk, so during breastfeeding the drug should be used with caution.
APPLICATION FOR CHILDREN
Contraindicated in children under 1 year.
Xalatan В® should not be prescribed more than 1 time / day, because more frequent use of latanoprost leads to a weakening of the IOP-lowering effect.
If you miss one dose, the next dose should be given 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 В® 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 may 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 is 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.
Symptoms: in addition to irritation of the mucous membrane of the eyes, conjunctival hyperemia or episclerosis, there were no other undesirable changes on the part of the eye in case of an overdose of latanoprost.
If you randomly take latanoprost inside, you should consider the following information: one bottle with 2.5 ml of solution contains 125 Ојg of latanoprost. More than 90% of the drug is metabolized by the "first pass" through the liver. IV 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.
Treatment: symptomatic therapy.
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.
Xalatan В® is incompatible with eye drops containing thiomersal (precipitation occurs).
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored out of reach of children, protected from light at a temperature of 2 В° to 8 В° C. Shelf life - 3 years.
After opening the bottle the drug should be used within 4 weeks, while the bottle should be stored at a temperature of no higher than 25 В° C.