Ksalakom drops Ch. 2.5ml vial, cap.

$15.86

Ksalakom drops Ch. 2.5ml vial, cap.

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Description

Composition
Active substance:
1 ml of solution contains: latanoprost – 50 micrograms, timolol maleate – 6.83 mg (equivalent to 5 mg of timolol) ;.
Excipients:
Benzalkonium chloride (as a 50% solution), sodium hydrogen phosphate anhydrous, sodium dihydrogen phosphate monohydrate, sodium chloride, water for injection *.
* If necessary (for pH) was added a solution of hydrochloric acid or 10% sodium hydroxide, 10% solution – q.s.
Description:
Antiglaucoma agents (analogue prostaglandin F2 alpha + beta-blocker).
Product form:
Eye drops; 2.5 ml of a solution (ocular drops) in dropper vial (low density polyethylene) with a screw cap and a safety cap unthreaded from the control of the first opening; 1 bottle dropper with instructions for use in a cardboard package.
Contraindications
Reactive airway disease, including asthma (or indication of its presence in history), severe COPD; sinus bradycardia, atrioventricular block II-III level, symptomatic heart failure, cardiogenic shock; Hypersensitivity to latanoprost, timolol maleate or other components of the formulation.
Carefully
Inflammatory, neovascular, or congenital closure glaucoma, open-angle glaucoma in combination with psevdofakiey, pigmentary glaucoma (due to lack of enough experience with the drug); aphakia, psevdoafakiya with posterior lens capsule rupture, patients with known risk factors for macular edema (in treatment of latanoprost described cases of macular edema, including cystoid).
Dosage
50 mg + 5 mg / ml
Indications
Reduction of elevated intraocular pressure (IOP) in patients with open angle glaucoma or elevated intraocular with insufficient efficacy of other IOP lowering drugs for topical application.
Interaction with other drugs
The interaction of the drug Ksalakom® not been specifically studied with other drugs.
In applying the drug Ksalakom® patients receiving beta-blocker inwardly, possibly more significant IOP reduction or enhancement of systemic manifestations of beta-blockers, however simultaneous topical application of two or more beta-blockers is not recommended.
With simultaneous instillation into the eyes of two prostaglandin analogues described paradoxical increase in IOP, so simultaneous use of two or more prostaglandins, their analogs or derivatives not recommended.
With simultaneous application of timolol maleate with epinephrine sometimes developed mydriasis.
With the combination of timolol maleate with the following drugs is possible additive effect with the development of systemic hypotension and / or bradycardia: · calcium channel blockers; · means for causing reduction of catecholamines, or beta-blockers, antiarrhythmics · · cardiac glycosides.
Beta-blockers can enhance the hypoglycemic effect of antidiabetic agents.
Overdose
Below is information on the overdose of the two components of the preparation:
latanoprost
Apart from ocular irritation and conjunctival hyperemia, and other undesirable changes in the body of an overdose are not known latanoprost.
When receiving the random latanoprost inwardly to consider the following: One vial containing 2.5 ml of a solution containing 125 micrograms latanoprost. More than 90% of the drug is metabolized during the first pass through the liver. An intravenous infusion at a dose of 3 mcg / kg in healthy volunteers did not cause any symptoms but when administered dose 5,5-10 g / kg were observed nausea, abdominal pain, dizziness, fatigue, hot flushes and sweating. In patients with bronchial asthma, moderate administering latanoprost in the eye in a dose of 7 times exceeding the therapeutic one, does not cause bronchospasm.
timolol maleate
There are cases of unintentional overdose of timolol maleate eye drops, causing the observed systemic effects similar to those of systemic administration of beta-blockers: dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest. (See. Section “Side effects”).
In the in vitro study, it was shown that when dialysis timolol easily derived from plasma or whole blood.
In patients with renal insufficiency timolol dialyzed worse.
In the case of overdose symptomatic treatment.
pharmachologic effect
Pharmacodynamics:
The preparation Ksalakom® includes two active components – latanoprost and timolol maleate. The mechanism of lowering elevated intraocular pressure (IOP) of these components is different, which provides an additional reduction in IOP compared to the effect achieved in the application of each of these components in monotherapy.
Latanoprost – prostaglandin F2 alpha analogue – is a selective FP receptor agonist and a prostanoid lowers IOP by increasing the outflow of aqueous humor mainly uveoscleral route, as well as through the trabecular meshwork. Established that latanoprost has no significant effect on production of aqueous humor and blood aqueous barrier. During the short-term treatment is not latanoprost fluorescein leakage in the rear segment of the eye under psevdofakii. When used in therapeutic doses latanoprost has no significant pharmacological effects on the cardiovascular and respiratory systems.
Timolol – nonselective beta-1 and beta-2-adrenergic blocker, which has no significant intrinsic sympathomimetic activity, has no direct effect on myocardial depression or local anesthetic (membrane stabilizing) effect.
Blockade of beta-adrenergic receptors causes a decrease in cardiac output in healthy subjects and patients with heart disease. In patients with severe impairment of myocardial function, beta-blockers may inhibit the stimulatory effect of the sympathetic nervous system necessary for adequate heart.
Beta-adrenoceptor blockade in the bronchi and bronchioles leading to increased airway resistance under the influence of the parasympathetic nervous system. A similar effect can be dangerous for people with asthma and other diseases bronhospasticheskimi (see. Section “Contraindications” and “Special instructions”).
The use of timolol maleate eye drops causes a decrease in normal and elevated IOP, regardless of the presence or absence of glaucoma. Elevated intraocular pressure is a major risk factor for glaucomatous visual field loss. The higher the IOP, the greater the likelihood of glaucomatous visual field loss and optic nerve damage.
The exact mechanism of action of reducing IOP under timolol maleate is not installed. And flyurofotometrii tonography results indicate that the main mechanism of action may be associated with a decrease in the formation of aqueous humor. However, some studies also noted a slight increase in outflow.
Effect of the combination of latanoprost and timolol maleate begins within one hour and maximal effect occurs within 6-8 hours.
Repeated application of adequate IOP reduction maintained for 24 hours after administration.
Pharmacokinetics:
Pharmacokinetic interactions between latanoprost and timolol maleate is not set, although 1-4 hours after application of the combined preparation of latanoprost acid concentration in the aqueous humor was about two times higher than with monotherapy.
latanoprost:
Suction:
Latanoprost, as a prodrug, absorbed through the cornea where it is hydrolyzed to the biologically active acid. The concentration in the aqueous humor reached the maximum after about two hours after topical application.
Distribution:
The volume of distribution of 0.16 ± 0.02 L / kg. Latanoprost acid is determined in aqueous humor within the first 4 hours and plasma – only during the first hour after topical application.
Metabolism:
Latanoprost is hydrolyzed in the cornea by the action of esterase with the formation of a biologically active acid. Latanoprost acid entering the systemic circulation, it is metabolized mainly in the liver by the beta-oxidation of fatty acids to form the 1,2-dinor- and 1,2,3,4-tetranor-metabolites.
excretion:
latanoprost acid is rapidly eliminated from the plasma (t1 / 2 = 17 min). Systemic clearance is approximately 7 mL / min / kg. Metabolites derived mainly kidneys: after topical application with urine output approximately 88% of the administered dose.
Timolol maleate:
The concentration of timolol maleate in aqueous humor reaches a maximum after about 1 hour after application of eye drops. Part of the dose systemically absorption and peak plasma concentration was 1 ng / ml, is reached in 10-20 minutes after drug application, one drop in each eye once daily (300 ug / day). The half-life of timolol maleate from the plasma is about 6 hours. Timolol maleate is extensively metabolised in the liver. Metabolites, as well as some unchanged timolol maleate, excreted in the urine.
Pregnancy and breast-feeding
Adequate controlled studies have not been conducted in pregnant women. The drug should be used during pregnancy only if the potential benefit justifies potential risk to the fetus.
Latanoprost and its metabolites may be released into breast milk. Timolol maleate, when used in the form of eye drops, is also found in breast milk. Given the risk of serious adverse reactions in infants are breastfed and the importance of the drug to the mother should either stop breast-feeding or stop the drug.
Use in children:
Safety and effectiveness in children have not been established.
Conditions of supply of pharmacies
On prescription.
side effects
In applying the drug Ksalakom® account the following undesirable reaction with a frequency greater than 1%:
On the part of the organ of vision: visual disturbances, blepharitis, cataracts, conjunctivitis, lesions of the conjunctiva (follicles, papillary reaction conjunctiva, petechiae et al.), Corneal lesions (erosion, pigmentation, punctate keratitis, etc.), Refractive disorders hyperemia eyes, eye irritation, eye pain, increased pigmentation of the iris, keratitis, photophobia, visual field loss.
Infections: sinusitis, infections of the upper respiratory tract and other infections.
Metabolic and nutritional: diabetes mellitus, hypercholesterolaemia.
Psychiatric disorders: depression.
From the nervous system: headache.
Vascular disorders: hypertension.
For the skin and subcutaneous tissue disorders: hypertrichosis, rash, and skin changes (irritation dermatohalazion et al.).
On the part of the musculoskeletal system and connective tissue disorders: arthritis.
Listed below are other undesirable phenomena have been observed with monotherapy individual components Ksalakom® formulation (besides those mentioned above).
latanoprost:
From a sight organ: eye irritation (burning sensation, feeling of sand in the eyes, itching, stinging and foreign body sensation); transient point epithelial erosion, swelling of the eyelids, and corneal edema erosion; lengthening, thickening, increased number and increased pigmentation of eyelashes and vellus hair; iritis / uveitis; macular edema, including cystoid; a change in direction of growth of eyelashes sometimes cause irritation of the eyes; blurred vision.
For the skin and subcutaneous tissue: skin rash, darkening of the eyelid skin and the local skin reaction on the eyelids.
From the nervous system: dizziness.
From the respiratory system: asthma (including acute attacks or exacerbations in patients with a history of bronchial asthma), shortness of breath.
On the part of the musculoskeletal system and connective tissue disorders: pain in muscles / joints.
General and local reactions: non-specific chest pain.
Timolol maleate (in the form of eye drops):
Immune system: systemic allergic reactions, including anaphylaxis, angioedema, urticaria, localized and generalized rash.
Errors of Metabolism and Nutrition: anorexia, hidden symptoms of hypoglycemia in patients with diabetes.
Psychiatric disorders: behavioral and psychiatric disorders, including confusion, hallucinations, anxiety, disorientation, nervousness, memory loss, decreased libido, insomnia, and nightmares.
From the nervous system: cerebral ischemia, cerebrovascular accident, dizziness, increased symptoms of myasthenia gravis, paresthesia, drowsiness, fainting.
From a sight organ: cystoid macular edema, decreased corneal sensitivity; choroidal detachment following filtration surgery; ptosis, blurred vision, including refractive change, and diplopia.
On the part of the organ of hearing and vestibular: tinnitus.
Cardiac arrhythmias, bradycardia, cardiac arrest, heart failure, heart block, palpitation, angina progression.
Vascular disorders: intermittent claudication, cold hands and feet, hypotension, Raynaud’s syndrome.
On the part of the respiratory system: bronchospasm (mainly in patients with prior bronhospasticheskimi disease), cough, shortness of breath, nasal congestion, pulmonary edema and respiratory failure.
On the part of the gastrointestinal tract: diarrhea, dry mouth, dyspepsia, nausea, retroperitoneal fibrosis.
For the skin and subcutaneous tissue disorders: alopecia, psevdopemfigoid, psoriasiform rash or exacerbation of psoriasis.
On the part of the musculoskeletal system and connective tissue disorders: systemic lupus erythematosus.
Reproductive system and breast: impotence, Peyronie’s disease.
General and local: asthenia / fatigue, chest pain, edema.
special instructions
Ksalakom® drug should be used no more than once a day, as more frequent administration of latanoprost leads to weakening of the IOP-lowering effect.
Omitting a single dose, the next dose should be administered at the usual time.
If the patient simultaneously uses other eye drops, they should be applied at intervals of at least 5 minutes.
The composition includes a preparation Ksalakom® benzalkonium chloride which can be absorbed by contact lenses. Before burying drops contact lenses must be removed and re-install them in 15 minutes.
latanoprost
Latanoprost may cause a gradual increase in the content of brown pigment in the iris. Change eye color due to increased melanin content in the stromal melanocytes of the iris and not an increase in the number of melanocytes themselves. Typically, the brown pigmentation appears around the pupil spreads concentrically to the periphery of the iris. The entire iris or parts become brown. In most cases, the color change is small and can not be established clinically. Increased pigmentation of the iris of one or both eyes is mainly observed in patients with a mixed color of the iris, comprising at the base of a brown color. The drug has no effect on nevi and lentigo iris; Pigment accumulation in the trabecular meshwork or not observed in the anterior chamber.
In determining the degree of pigmentation of the iris for more than 5 years did not reveal adverse effects increased pigmentation even when continued treatment with latanoprost. Patients degree of IOP reduction was similar regardless of the presence or absence of amplification of iris pigmentation. Therefore, treatment with latanoprost can be continued in case of increased pigmentation of the iris. Such patients should be regularly monitored and, depending on the clinical situation, treatment can be discontinued.
Increased pigmentation of the iris usually occurs within the first year after the start 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 stabilized after 5 years. In more remote terms the effects of increased iris pigmentation has not been studied. After cessation of treatment gain brown pigmentation of the iris is not mentioned, but the change in eye color may be irreversible.
In connection with the application of latanoprost described cases of skin darkening age, which may be reversible.
Latanoprost may cause a gradual change eyelashes and vellus hair, such as lengthening, thickening, increased pigmentation, increased density and change in the direction of growth of eyelashes. Eyelash changes are reversible and disappear after cessation of treatment.
Patients who use the drops only in one eye, may develop heterochromia.
timolol maleate
When applied topically, beta-blockers may experience the same adverse reactions, as well as at their systemic administration. Patients with severe heart disease history should be constantly watching for timely detection of the symptoms of heart failure. The local application of timolol maleate can arise following the reaction of the heart and respiratory system: progression Prinzmetal angina, and also central and peripheral circulatory disorders, hypotension, heart failure fatal, severe reaction from the respiratory system, including bronchospasm with a fatal outcome in patients with asthma, bradycardia.
Before performing extensive surgery should discuss the desirability of gradual withdrawal of beta-blockers. Drugs in this group violate the ability of the heart to the reflex response to beta-adrenergic stimulation, which can increase the risk of general anesthesia. There are cases of protracted severe hypotension during anesthesia, and difficulty in restoring and maintaining heart rate. During surgery, the effects of beta-blockers may be eliminated using adequate doses adrenoceptor agonists.
Beta-blockers may enhance the hypoglycaemic effect of antidiabetic agents and mask the symptoms and manifestations of hypoglycemia. They should be used with caution in patients with spontaneous hypoglycemia or diabetes (particularly labile currents) receiving insulin or oral hypoglycemic agents.
Therapy with beta-blockers may mask some of the main symptoms and signs of hyperthyroidism. Abrupt discontinuation of treatment may cause a worsening of the disease.
In the treatment of beta-blockers in patients with severe atopy or anaphylactic reactions to various allergens may gain a history response when re-exposed to these allergens. Thus adrenaline in usual doses used for the relief of anaphylactic reactions, can be inefficient.
In rare cases, timolol maleate induced enhancement of muscle weakness in patients with myasthenia gravis or myasthenic symptoms (e.g., diplopia, ptosis, generalized weakness).
In applying means lowering IOP described choroidal detachment after filtration procedures.
Effects on ability to drive and use other mechanisms
The use of eye drops can cause a transient blurring of vision. While this effect persists, patients should not drive a car or use complex technology.
Storage conditions
Store at +2 – + 8 C protected from light.
After opening, the vial is stored at a temperature not higher than +25 C.
Dosing and Administration
Adults (including the elderly) – one drop into the affected eye (s) once a day.
Information
Appearance may differ from that depicted in the picture. There are contraindications. You need to read the manual or consult with a specialist

Additional information

Weight0.100 kg
Manufacturer

Pfizer

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