Prolatan - instructions for use, dose, side effects, contraindications

benzalkonium chloride 0.2 mg, sodium chloride 4.10 mg, disodium hydrogen phosphate anhydrous 4.74 mg, sodium dihydrogen phosphate monohydrate 4.60 mg, water for injection up to 1 ml.

Description:A clear, colorless solution.

Pharmacotherapeutic group:Antiglaucoma means - prostaglandin F2α analogue synthetic

ATX: & nbsp

S.01.E.E Prostaglandin analogues

S.01.E.E.01 Latanoprost

Pharmacodynamics:

Latanoprost - an analogue of prostaglandin F₂_α - is a selective receptor agonist FP 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 ARI begins approximately 3 to 4 hours after drug administration, the maximum effect is observed after 8 to 12 hours, the effect persists for at least 24 hours. It is established that latanoprost does not have a significant effect on the production of aqueous humor and on the hemato-ophthalmic barrier.

When used in therapeutic doses latanoprost has no significant pharmacological effect on the cardiovascular and respiratory systems.

Pharmacokinetics:

Suction

Latanoprost, being a prodrug form, is absorbed through the cornea, where it is hydrolyzed to a biologically active acid. Concentration in watery moisture reaches a maximum about two hours after topical application.

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 within 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. Acid latanoprost, 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 removed from the plasma (T1 / 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.

Children

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 the maximum concentration of latanoprost acid in blood plasma is 5 minutes for all age groups. The half-life of latanoprost in children is the same as in adults. At equilibrium concentration no cumulation of latanoprost acid in the blood plasma occurs.

Indications:

Decreased elevated 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 old with primary congenital glaucoma, first-line therapy remains surgical treatment (trabeculotomy / goniotomy).

Contraindications:

Hypersensitivity to latanoprost or other components of the drug. Age to 1 year (efficacy and safety not established).

Carefully:

Aphakia, psevdoafakiya with rupture posterior lens capsule, patients with known risk factors for macular edema (in treatment of latanoprost described cases of macular edema, including cystoid); 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 this regard, in this group of patients Prolatan® 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 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.

Dosing and Administration:

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.

Side effects:

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, 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, 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 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 side of the musculoskeletal system and connective tissue: pain in muscles / joints.

General and local reactions: nonspecific pain in the chest.

Infections and infestations: herpetic keratitis.

There were also cases of retinal artery embolism, retinal detachment and vitreous hemorrhage in patients with diabetic retinopathy.

Children

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.

Overdose:

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 Prolatan® preparation is taken orally, the following information should be considered: one bottle with 2.5 ml of solution contains 125 μg of latanoprost, 5 ml - 250 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, pain in stomach, dizziness, fatigue, hot flashes and sweating. 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.

Interaction:

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.

Special instructions:

Prolatan® 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.

Prolatan® can be used concomitantly 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 preparation of Prolatan® is included 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 iris pigmentation 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 has no effect on 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. Consequently, 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.

Strengthening of the pigmentation of the iris is usually observed during the first year after the 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.

Prolatan® can cause gradual changes in eyelashes and fleece hair, such as lengthening, thickening, increased pigmentation, increased density and changes 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.

Effect on the ability to drive transp. cf. and fur:

It is necessary to drive with care or use complex equipment during the use of the drug.

Form release / dosage:

Eye drops 0.005%.

Packaging:

For 2.5 ml or 5 ml in a polyethylene bottle with a dropper cap and a turquoise screw cap with the control of the first autopsy. For 1 and 3 vials with instructions for use in a cardboard pack.

Storage conditions:

At a temperature of 2 - 8 ° 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 ° 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.

Terms of leave from pharmacies:On prescription

Registration number:LP-002748

Date of registration:10.12.2014

The owner of the registration certificate:Sentiss Pharma Pvt. Ltd.Sentiss Pharma Pvt. Ltd. India

Manufacturer: & nbsp

SENTISS PHARMA Pvt. Ltd India

Representation: & nbspSENTISS RUSS LLCSENTISS RUSS LLCRussia

Information update date: & nbsp16.11.2015

Illustrated instructions

Instructions

Prolatan® (Prolatan®)