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medicalmeds.eu Medicines Protivoglaukomny means (F2α prostaglandin analog + beta adrenoblocker) Ксалаком®

Ксалаком®

Препарат Ксалаком®. Pfizer (Пфайзер) США


Producer: Pfizer (Pfayzer) of the USA

Code of automatic telephone exchange: S01ED51

Release form: Liquid dosage forms. Drops are eye.

Indications to use:


General characteristics. Structure:

Active agents: латанопрост 0,005%, Timololum of 0,5%.
Inactive excipients: chloride a benzalkoniya, hydrosodium phosphate (anhydrous), dihydrosodium phosphate (monohydrate), sodium chloride, water for injections.




Pharmacological properties:

Pharmacodynamics.

Action mechanism
Ksalak - the combined drug of a latanoprost and Timololum of a maleate. The mechanism of decrease in the increased intraocular pressure (VGD) at these components is various that provides additional decrease in VGD in comparison with the effect which is reached at use of each of these components as monotherapy. Латанопрост - F2α prostaglandin analog - is the selection agonist of prostaglandinovy F (FP) of receptors and reduces VGD due to increase in outflow of watery moisture. The main mechanism of its action is connected with increase in uveoskleralny outflow. Латанопрост has no significant effect on products of watery moisture and does not influence a blood-ocular barrier. Timololum is beta-1-and beta 2 - adrenoblocker (non-selective) which has no significant internal sympathomimetic activity, does not exert direct depressive impact on a myocardium and has no membrane stabilizing activity. Action of Timololum is connected with decrease in formation of watery moisture in a ciliary epithelium.
Effect of drug by Ksalak comes within the first hour after use, and the maximum effect is observed within 6-8 hours.

Pharmacokinetics.

Латанопрост
Латанопрост well gets through a cornea, at the same time there is its hydrolysis to biologically active form. Researches at the person showed that the maximum concentration in watery moisture is reached approximately in two hours after topical administration of a latanoprost as monotherapy.
After topical administration at monkeys латанопрост it is distributed preferential in an anterior chamber of an eye, in a conjunctiva and centuries. Only insignificant quantities of a latanoprost reach a back chamber of the eye.
In eye tissues acid of a latanoprost is practically not metabolized; metabolism happens mainly in a liver. At the person the elimination half-life of acid of a latanoprost makes 17 minutes. Researches on animals showed that the main metabolites - 1,2-dinor-and 1,2,3,4, - tetraholes metabolites do not possess at all or have weak biological activity and are removed generally with urine.

Timololum
The maximum concentration of Timololum in watery moisture is reached approximately in 1 hour. A part of a dose is exposed to system absorption, and the maximum concentration in plasma, equal 1 ng/ml, is reached in 10-20 minutes after topical administration on one drop in each eye once a day (300 mkg/days). Timololum elimination half-life in plasma makes about 6 hours. Timololum is extensively metabolized in a liver. Metabolites, and also a quantity of not changed Timololum are allocated with urine.

Ksalak
Pharmacokinetic interactions between latanoprosty and Timololum did not come to light though the tendency to increase in concentration of acid of a latanoprost in watery moisture in 1-4 hours after administration of drug by Ksalak in comparison with that came to light when performing monotherapy.


Indications to use:

Drug is intended for decrease in the increased intraocular pressure at patients with an open angle glaucoma and the raised intraocular tension.


Route of administration and doses:

The recommended dosage for adults (including patients of advanced age):
Dig in on one drop in an eye(s) once a day. If one dose was passed, then further it is necessary to continue treatment, entering the following dose as usual.
If to the patient more than one drug for local introduction concerning an ophthalmologic disease are appointed, then it is necessary to administer these drugs with an interval not less than five minutes.


Features of use:

The drug Ksalakom® 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. 

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 Ksalakom®. Before an instillation of drops contact lenses need to be removed and again to establish them in 15 minutes.


Латанопрост

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.


Timololum maleate

At topical administration of beta adrenoblockers the same undesirable reactions can be observed, as well as at their system use. Patients with a serious illness of heart in the anamnesis should be observed constantly for the purpose of early detection of symptoms of heart failure. At topical administration of Timololum of a maleate there can be following reactions from heart and system of breath: progressing of stenocardia of Printsmetal, and also peripheral and central circulator disturbances, hypotension, heart failure with a lethal outcome, heavy reactions from respiratory system, including a bronchospasm with a lethal outcome at patients with asthma, bradycardia.

Before carrying out extensive surgical intervention it is necessary to discuss expediency of gradual cancellation of beta adrenoblockers. Drugs of this group break ability of heart to response to reflex beta and adrenergic stimulation that can increase risk at the general anesthesia. Cases of long heavy hypotension are described during an anesthesia and difficulty at recovery and maintenance of cordial reductions. During operation effects of beta adrenoblockers can be liquidated by means of sufficient doses of agonists of adrenoceptors.

Beta adrenoblockers can strengthen hypoglycemic action of antidiabetic means and mask symptoms and manifestations of a hypoglycemia. They should be applied with care at the patients with a spontaneous hypoglycemia or a diabetes mellitus (especially labile current) receiving insulin or peroral antihyperglycemic means.

Therapy by beta adrenoblockers can mask some main symptoms and manifestations of a hyperthyroidism. The sharp termination of treatment can cause an exacerbation of this disease.

At treatment by beta adrenoblockers at patients with an atopy or heavy anaphylactic reactions to various allergens in the anamnesis strengthening of the answer at repeated contact with these allergens is possible. At the same time adrenaline in the usual doses which are applied to stopping of anaphylactic reactions can be inefficient.

In rare instances of Timololum the maleate caused strengthening of muscular weakness in patients with myasthenia gravis or myasthenic symptoms (for example, a diplopia, a ptosis, generalized weakness).

At use of the means reducing VGD choroid amotio after the filtrational procedures is described.

 

Influence on ability to drive the car and other mechanisms

Use of eye drops can cause passing misting of sight. Until this effect disappears, patients should not drive the car or to use a difficult technique.


Side effects:

At use of the drug Ksalakom® the following undesirable reactions with a frequency of ³1% are registered:

From an organ of sight: vision disorder, blepharitis, cataract, conjunctivitis, defeats of a conjunctiva (follicles, papillary reactions of a conjunctiva, dot hemorrhages, etc.), defeats of a cornea (erosion, pigmentation, dot keratitis, etc.), disturbances of a refraction, eye hyperemia, irritation of an eye, eye pain, strengthening of pigmentation of an iris, keratitis, photophobia, loss of fields of vision.

Infections: sinusitis, infections of upper parts of respiratory tracts and other infections.

Disturbances of metabolism and food: diabetes mellitus, hypercholesterolemia.

Mental disorders: depression.

From a nervous system: headache.

Vascular disorders: hypertensia.

From integuments and hypodermic fabrics: hypertrichosis, rash and changes of skin (irritation, дерматохалазион, etc.).

From a musculoskeletal system and connecting fabric: arthritis.

Other undesirable phenomena which were observed at monotherapy by separate components of the drug Ksalakom® (in addition to stated above) are listed below.

Латанопрост:

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); passing dot erosion of an epithelium, the century, hypostasis and erosion of a cornea swelled; lengthening, thickening, increase in number and strengthening of pigmentation of eyelashes and vellus hair; iritis/uveitis; macular hypostasis, including tsistoidny; change of the direction of growth of eyelashes, sometimes defiant irritation of an eye; the obscured sight.

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

From a nervous system: dizziness.

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.

General and local reactions: nonspecific stethalgias.


Timololum a maleate (in the form of eye drops):

From immune system: system allergic reactions, including an anaphylaxis, a Quincke's disease, the urticaria localized and generalized rash.

Disturbances of metabolism and food: anorexia, the larvate symptoms of a hypoglycemia at patients with a diabetes mellitus.

Mental disorders: changes of behavior and mental disorders, including confusion of consciousness, hallucination, alarm, disorientation, nervousness, memory loss, decrease libido, sleeplessness and nightmares.

From a nervous system: brain ischemia, acute disorders of cerebral circulation, dizziness, strengthening of symptoms myasthenia gravis, paresthesia, drowsiness, syncope.

From an organ of sight: tsistoidny macular hypostasis, decrease in sensitivity of a cornea; choroid amotio after filtrational surgical interventions; ptosis, vision disorders, including change of a refraction and diplopia.

From an acoustic organ and vestibular mechanism: sonitus.

From heart: arrhythmia, bradycardia, cardiac standstill, heart failure, heart block, heartbeat, progressing of stenocardia

Vascular disorders: the alternating lameness, a cold snap of hands and legs, hypotension, Reynaud's syndrome.

From a respiratory organs: a bronchospasm (generally at patients with the previous bronkhospastichesky diseases), cough, short wind, a nose congestion, a fluid lungs and respiratory insufficiency.

From digestive tract: diarrhea, dryness in a mouth, dyspepsia, nausea, retroperitoneal fibrosis.

From integuments and hypodermic fabrics: alopecia, pseudo-pemphigoid, psoriazopodobny rash or exacerbation of psoriasis.

From a musculoskeletal system and connecting fabric: system lupus erythematosus.

From reproductive system and mammary glands: impotence, Peyronye's disease.

The general and local: adynamy/fatigue, stethalgia, hypostases.


Interaction with other medicines:

Interaction of the drug Ksalakom® with other drugs specially was not studied.

At drug Ksalakom® use to the patients receiving beta adrenoblocker inside, perhaps more expressed decrease in VGD or strengthening of system shows of beta adrenoblockers therefore simultaneous topical administration of two and more beta adrenoblockers is not recommended.

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.

At simultaneous use of Timololum of a maleate with adrenaline the mydriasis sometimes developed.

At a maleate Timololum combination to the listed below drugs the perhaps additive action with development of system hypotension and/or the expressed bradycardia:

- blockers of calcium channels;

- the means causing decrease in level of catecholamines, or beta adrenoblockers;

- antiarrhytmic means;

- cardiac glycosides.

Beta adrenoblockers can strengthen hypoglycemic action of antidiabetic means.

 


Contraindications:

Reactive respiratory diseases, including bronchial asthma (or the instruction on its existence in the anamnesis), HOBL of a heavy current; a sinus bradycardia, an atrioventricular block of the II-III degree, clinically expressed heart failure, cardiogenic shock; hypersensitivity to a latanoprost, Timololum to a maleate or other components of drug.

With care

Inflammatory, neovascular, closed-angle or inborn glaucoma, open angle glaucoma in combination with a psevdofakiya, pigmental glaucoma (due to the lack of sufficient experience of use of drug); 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).

Pregnancy, period of a lactation and children's age
Adequate controlled researches at pregnant women were not conducted. It is necessary to appoint drug at pregnancy only when the potential advantage exceeds possible risk for a fruit.

Латанопрост and its metabolites can be allocated in breast milk. Timololum a maleate, at use in the form of eye drops, also found in breast milk. Considering risk of development of serious undesirable reactions in the newborns who are on breastfeeding and also importance of use of drug for mother, it is necessary either to stop breastfeeding, or to cancel drug.

Use for children:

Safety and efficiency at children are not established.


Overdose:

Information on overdose of two components of drug is included below:

Латанопрост

In addition to irritation of eyes and a hyperemia of a conjunctiva, 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. 

Timololum maleate

Cases of inadvertent overdose of eye drops of Timololum of a maleate therefore the system effects similar to those at system use of beta adrenoblockers were observed are described: dizziness, headache, short wind, bradycardia, bronchospasm and cardiac standstill. (see the section "Side effect").

In the research in vitro it was shown that at dialysis Timololum is easily brought out of plasma or whole blood.

At patients with a renal failure Timololum was dialyzed worse.

In case of overdose carry out a symptomatic treatment.


Storage conditions:

Period of validity 2 years. To use the opened bottle within 4 weeks. Not to use after the period of validity specified on packaging.
To store at a temperature + 2 - + 8ºС in the place protected from light. To store the opened bottle at a temperature not above +25ºС. To store in the place, unavailable to children.


Issue conditions:

According to the recipe


Packaging:

Drops are eye; on 2,5 ml of solution (drops eye) 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 bottle dropper with the application instruction in a cardboard pack.



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