Ксалатан®

General characteristics. Structure:

International unlicensed name: латанопрост
Active agent: латанопрост - 50 mkg; excipients: sodium chloride, sodium dihydrophosphate (monohydrate), sodium hydrophosphate (anhydrous), a benzalkoniya chloride, water for injections.

Pharmacological properties:

Pharmacodynamics. Латанопрост - F2α prostaglandin analog - is the selection agonist of receptors of FP and reduces the intraocular pressure (VGD) due to increase in outflow of watery moisture, mainly, in the uveoskleralny way, and also through trabecular network. Decrease in VGD begins approximately in 3 – 4 h after administration of drug, the maximum effect is observed in 8 – 12 h, action remains during not less than 24 h.

It is established what латанопрост has no significant effect on products of watery moisture and on a blood-ocular barrier.

At use in therapeutic doses латанопрост does not render significant pharmacological effect on cardiovascular and respiratory systems.

Pharmacokinetics
Absorption:

Латанопрост, being a pro-dosage form, it is soaked up through a cornea where there is its hydrolysis to biologically active acid. Concentration in watery moisture reaches a maximum approximately in two hours after topical administration.

Distribution:

The volume of distribution makes 0,16 ± 0,02 l/kg. Acid of a latanoprost is defined in watery moisture within the first 4 hours, and in plasma – only within the first hour after topical administration.

Metabolism:

Латанопрост, being a pro-dosage form, is exposed to hydrolysis in a cornea under the influence of esterases with formation of biologically active acid. The acid of a latanoprost coming to a system blood stream is metabolized, generally in a liver by beta oxidation of fatty acids with education 1,2-dinor-and 1,2,3,4-tetraholes-metabolites.

Removal:

Acid of a latanoprost is quickly removed from plasma (t1/2 =17 min.). The system clearance makes about 7 ml/min. After beta oxidation in a liver metabolites are removed, generally by kidneys: after topical administration with urine about 88% of the entered dose are removed.

Indications to use:

Decrease in the increased intraocular pressure (VGD) at patients with an open angle glaucoma or the raised intraocular tension.

Route of administration and doses:

The adult (including elderly) - on one drop in the affected eye(s) once a day. The optimum effect is reached at drug use in the evening.

Features of use:

The drug Ksalatan® should be used not more often than once a day as more frequent introduction of a latanoprost leads to weakening of the reducing effect VGD.

At the admission of one dose, the following dose should be entered into usual time.

Латанопрост it is possible to apply along with other classes of ophthalmologic drugs to topical administration for the purpose of decrease in VGD. If the patient at the same time uses other eye drops, then they should be applied with an interval at least 5 minutes.

The benzalkoniya chloride which can be absorbed by contact lenses is a part of the drug Ksalatan®. Before an instillation of drops contact lenses need to be removed and again to establish them in 15 minutes.

Латанопрост can cause gradual increase in maintenance of a brown pigment in an iris. Discoloration of eyes is caused by increase in content of melanin in stromal melanocytes of an iris, but not increase in number of melanocytes. In typical cases brown pigmentation appears around a pupil and concentrically extends to the periphery of an iris. At the same time all iris or its parts gain brown color. In most cases discoloration is insignificant and can be not established clinically. Strengthening of pigmentation of an iris of the eye of one or both eyes is observed, mainly, at patients with the mixed color of an iris containing brown color in a basis. Drug does not exert impact on a nevus and лентиго an iris of the eye; accumulation of a pigment in trabecular network or in an anterior chamber of an eye is noted.

When determining extent of pigmentation of an iris within more than 5 years undesirable effects of strengthening of pigmentation even are not revealed at therapy continuation latanoprosty. Patients had an identical extent of decrease in VGD regardless of existence or lack of strengthening of pigmentation of an iris. Therefore, treatment latanoprosty can be continued also in cases of strengthening of pigmentation of an iris. Such patients have to be under regular observation and, depending on a clinical situation, treatment can be stopped.

Strengthening of pigmentation of an iris is usually observed within the first year after an initiation of treatment, is rare – within the second or third year. After the fourth year of treatment this effect was not observed. Pigmentation progressing speed decreases and stabilized in 5 years over time. In more remote terms effects of the increased pigmentation of an iris were not studied. After the termination of treatment of strengthening of brown pigmentation of an iris it was not noted, however discoloration of eyes can be irreversible.

Due to the use of a latanoprost cases of darkening of skin a century which can be reversible are described.

Латанопрост can cause gradual changes of eyelashes and vellus hair, such as lengthening, thickening, pigmentation strengthening, increase in density and change of the direction of growth of eyelashes. Changes of eyelashes are reversible and take place after the treatment termination.

At the patients applying drops only in one eye development of a heterochromia is possible.

Use of eye drops can cause passing misting of sight.

It is necessary to drive the car or to use a difficult technique during drug use with care.

Side effects:

The following undesirable reactions relating to drug use are registered:

From an organ of sight: irritation of eyes (burning sensation, feeling of sand in eyes, an itch, a pricking and feeling of a foreign body); blepharitis; conjunctiva hyperemia; eye pain; strengthening of pigmentation of an iris; passing dot erosion of an epithelium, the century, hypostasis and erosion of a cornea swelled; conjunctivitis; lengthening, thickening, increase in number and strengthening of pigmentation of eyelashes and vellus hair; iritis/uveitis; keratitis; macular hypostasis, including tsistoidny; change of the direction of growth of eyelashes, sometimes defiant irritation of an eye; sight misting.

From integuments and hypodermic fabrics: rash, darkening of skin a century and local skin reactions on centuries.

From a nervous system: dizziness, headache.

From a respiratory organs: asthma (including bad attacks or an exacerbation of a disease at patients with bronchial asthma in the anamnesis), an asthma.

From a musculoskeletal system and connecting fabric: muscle/joints pains.

Nonspecific reactions: nonspecific stethalgias.

Interaction with other medicines:

At a simultaneous instillation in eyes of two analogs of prostaglandins paradoxical increase in VGD therefore simultaneous use of two and more prostaglandins, their analogs or derivatives are not recommended is described.

Pharmaceutical it is incompatible with the eye drops containing tiomersat – precipitation.

Contraindications:

Hypersensitivity to a latanoprost or other components of drug. Age up to 18 years.

With care. An aphakia, a pseudo-aphakia with a rupture of the back capsule of a crystalline lens, patients with the known risk factors of macular hypostasis (at treatment latanoprosty cases of development of macular hypostasis, including tsistoidny are described); inflammatory, neovascular or inborn glaucoma (due to the lack of sufficient experience of use of drug).

Pregnancy and lactation
Adequate controlled researches at pregnant women were not conducted. It is necessary to appoint drug at pregnancy only when the potential advantage for mother exceeds possible risk for a fruit.

Латанопрост and its metabolites can be allocated in breast milk therefore during feeding by a breast drug should be used with care.

Overdose:

In addition to irritation of a mucous membrane of eyes, a hyperemia of a conjunctiva or an episclera, other undesirable changes from an organ of sight at overdose of a latanoprost are not known.

At accidental reception of a latanoprost inside it is necessary to consider the following information: one bottle from 2,5 ml of solution contains 125 mkg of a latanoprost. More than 90% of drug are metabolized at the first passing through a liver. Intravenous infusion in a dose of 3 mkg/kg did not cause any symptoms in healthy volunteers, however at introduction of a dose of 5,5-10 mkg/kg nausea, an abdominal pain, dizziness, fatigue, inflows and perspiration were observed. Introduction of a latanoprost to eyes in the dose, by 7 times exceeding therapeutic did not cause a bronchospasm in patients with bronchial asthma of moderate severity.

In case of overdose carry out a symptomatic treatment.

Storage conditions:

At a temperature + 2 ºС - + 8 ºС in the place protected from light. To store the opened bottle at a temperature not higher than + 25 ºС. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Drops eye 0,005%; on 2,5 ml of solution (eye drops) in a bottle dropper (polyethylene of low density) with the screwing-up cap and a safety cap without carving with control of the first opening; on 1 or 3 bottles droppers with the application instruction in a cardboard pack.