Xalacom drops eye bottle 2.5ml
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Active ingredients
Latanoprost + Timolol
Release form
Drops
Composition
Active ingredient: latanoprost 50 mcg, timolol 5 mg adjuvants: benzalkonium chloride (as a 50% solution) 200 mcg, sodium anhydrous hydrogen phosphate 2.89 mg, sodium dihydrogen phosphate monohydrate 6.39 mg, sodium chloride 4.10 mg, water for injection up to 1 ml. Concentration of active ingredient (mcg): 5050 mcg
Pharmacological effect
Antiglaucoma combination drug, which consists of two active ingredients - latanoprost and timolol. The mechanism of lowering IOP in latanoprost and timolol is different, which provides an additional reduction in IOP compared to the effect of using each of these components as monotherapy. Latanoprost is an analogue of prostaglandin F2α - is a selective agonist of the prostanoid FP receptors and reduces IOP by increasing the outflow of aqueous humor, mainly by uveoscleral route, as well as through the trabecular network. Latanoprost does not have a significant effect on the production of aqueous humor and the permeability of the blood-ophthalmic barrier. During short-term treatment, latanoprost does not cause fluorescene infiltration into the posterior segment of the eye during pseudophakia. When used in therapeutic doses, it does not have a significant pharmacological effect on the cardiovascular and respiratory systems. Timolol is a non-selective beta1- and beta2-adrenoblocker. It does not have significant internal sympathomimetic activity, has no direct depressive effect on the myocardium, does not possess membrane-stabilizing and local anesthetic activity. The blockade of β-adrenoreceptors causes a decrease in cardiac output in healthy people and patients with heart disease. In patients with severe myocardial dysfunction, beta-adrenergic blockers can inhibit the stimulating effect of the sympathetic nervous system necessary for adequate functioning of the heart. The blockade of β-adrenoreceptors in the bronchi and bronchioles leads to an increase in the resistance of the respiratory tract under the influence of the parasympathetic nervous system. A similar effect can be dangerous for patients with bronchial asthma and other bronchospastic diseases. The use of timolol maleate in the form of eye drops causes a decrease in elevated and normal IOP, regardless of the presence or absence of glaucoma. Elevated IOP is a major risk factor for glaucomatous loss of visual fields.The higher the IOP, the higher the likelihood of glaucomatous loss of visual fields and damage to the optic nerve. The exact mechanism for reducing IOP under the action of timolol maleate is not installed. The results of tonography and fluorometry suggest that the main mechanism of action may be associated with a decrease in the formation of aqueous humor. However, some studies have also noted a slight increase in the outflow of aqueous humor. In addition, inhibition of increased synthesis of cyclic AMP caused by endogenous β-adrenergic stimulation is possible. No effect of timolol on the permeability of the blood-ophthalmic barrier was noted. The effect of Xalacom occurs within the first hour after application, the maximum effect is noted within 6-8 hours. With repeated use, an adequate decrease in IOP persists for 24 hours after administration.
Pharmacokinetics
The pharmacokinetic interaction between latanoprost and timolol maleate has not been established, although 1-4 hours after Xalacom was applied, the concentration of latanoprost acid in aqueous humor was about 2 times higher than in monotherapy. biologically active form (acid). Cmax in aqueous humor is reached 2 hours after topical application. The systemic bioavailability of latanoprost acid after topical application of eye drops is 45%. The distribution of Vd is 0.16 ± 0.02 l / kg. Acid latanoprost is determined in watery moisture during the first 4 hours, and in plasma - only during the first hour after topical administration. Binding to plasma proteins is 87%. Metabolism Latanoprost undergoes hydrolysis in the cornea of the eye under the influence 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 Acid latanoprost is rapidly removed from blood plasma. T1 / 2 is 17 min. Plasma clearance is 0.4 l / h / kg. Systemic clearance is approximately 7 ml / min / kg.Metabolites are excreted mainly by the kidneys: after topical administration, about 88% of the dose is excreted in urine. Timolol maleate Absorption of Cmax of timolol maleate in aqueous humor is reached after 1 hour. each eye 1 time / day (300 mcg / day) in plasma is reached Cmax, which is 1 ng / ml. Metabolism and elimination of timolol maleate is actively metabolized in the liver. T1 / 2 timolol maleate from plasma is about 6 hours. Metabolites, as well as some unchanged timolol maleate, are excreted by the kidneys.
Indications
Reducing elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension with a lack of efficacy of monotherapy for individual components of the drug.
Contraindications
Reactive diseases of the respiratory tract, including bronchial asthma (or an indication of its presence in history), severe COPD; sinus bradycardia, sick sinus syndrome, sinoatrial block, grade II-III atrioventricular block without control of an artificial pacemaker, clinically severe heart failure, cardiogenic shock: hypersensitivity to latanoprost, timolol or other components of the drug, up to 18 years of age; not installed). With care: Inflammatory, neovascular, angle-closure glaucoma, open-angle glaucoma in combination with pseudophakia, pigmentary glaucoma (due to the lack of sufficient experience with the drug); aphakia, pseudophakia with a rupture of the posterior lens capsule, patients with known risk factors for macular edema (in the case of treatment with latanoprost, cases of macular edema, including cystoid, are described); a history of herpetic keratitis; atrioventricular block I degree (β-blockers negatively affect the time of the impulse in the heart muscle); peripheral circulatory disorders (for example, severe Raynaud's syndrome or Raynaud's disease). It is necessary to avoid the use of the drug Xalacom in patients with the active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with the use of prostaglandin F2α analogues.Timolol should be used with caution in patients with chronic obstructive pulmonary disease and only in cases where the potential benefit of using the drug for a patient exceeds the risk. Caution should be used Xalak in patients with diseases of the cornea, as the drug can cause dryness of the mucous membrane of the eyes.
Precautionary measures
Do not exceed the recommended dose. With caution, use the drug for inflammatory, neovascular, angle-closure glaucoma, open-angle glaucoma in combination with pseudophakia, pigmentary glaucoma (due to the lack of sufficient experience with the drug); aphakia, pseudophakia with a rupture of the posterior lens capsule; in patients with known risk factors for macular edema (in the case of treatment with latanoprost, cases of macular edema, including cystoid, are described); herpetic keratitis in history; AV blockade of I degree (beta-blockers negatively affect the time of the impulse in the heart muscle); peripheral circulatory disorders (for example, severe Raynaud's syndrome or Raynaud's disease); in patients with corneal diseases, because The drug can cause dryness of the mucous membrane of the eyes. It is necessary to avoid the use of Xalacom in patients with active form of herpetic keratitis and recurrent herpetic keratitis, especially associated with taking prostaglandin F2α analogues.
Use during pregnancy and lactation
Adequate controlled studies of the use of the drug in pregnant women have not been conducted. When conducting epidemiological studies with the use of beta-blockers orally, there were no cases of fetal malformations, but the risk of intrauterine growth retardation was increased. In addition, symptoms of beta-adrenergic blocking action (such as bradycardia, decreased blood pressure, impaired respiratory function, and hypoglycemia) were detected in newborns whose mothers took beta-blockers during pregnancy. If a pregnant woman received therapy with beta-blockers, you should carefully monitor the condition of the newborn in the first days after birth. In this regard, the use of the drug Xalacom during pregnancy is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus. Latanoprost and its metabolites may be excreted in breast milk; timolol maleate, when used in the form of eye drops, was also found in breast milk.Given the risk of serious adverse reactions in breastfed newborns, as well as the importance of using the drug for the mother, if you need to use the drug during lactation, you should decide whether to stop breastfeeding or discontinue the drug.
Dosage and administration
Adults (including elderly) - one drop in the affected eye (a) once a day. As with the use of any eye drops, in order to reduce the possible systemic effect of the drug, immediately after the installation of each drop, it is recommended to press on the lower lacrimal point located at the inner corner of the eye on the lower eyelid. This must be done within 2 minutes.
Side effects
The incidence of adverse reactions is presented according to the following classification: Very frequent ≥10% Frequent ≥1% and <10% Infrequent ≥0.1% and <1% Rare ≥0.01% and <0.1% Very rare <0.01% On the part of the organ of vision: very frequent - increased pigmentation of the iris; frequent - visual impairment, blepharitis, cataract, conjunctivitis, lesions of the conjunctiva (follicles, papillary conjunctival reactions, punctate hemorrhages, etc.), corneal lesions (erosion, pigmentation, keratitis, punctate keratitis, etc.), refractive disorders, erosion, pigmentation, keratitis, punctate keratitis, etc., disorders of refraction, imperatives, and in the presence of adipose tissue, ectopiasis eyes (including burning sensation and itching in the eyes), pain in the eyes, photophobia, loss of visual fields, increased tear formation. Infections: frequent - sinusitis, infections of the upper respiratory tract and other infections. Metabolic and nutritional disorders: frequent - diabetes mellitus, hypercholesterolemia. Mental disorders: frequent depression. On the part of the nervous system: frequent - headache. Vascular disorders: frequent increase in blood pressure. On the part of the skin and subcutaneous tissues: frequent - hypertrichosis, rash, pruritus and skin changes (irritation, dermatochalasion, etc.). On the part of the musculoskeletal system and connective tissue: frequent - arthritis. The following are the other adverse events that were observed during monotherapy with the individual components of Xalacom (in addition to the above). Latanoprost: On the part of the organ of vision: eye irritation (burning sensation, feeling of sand in the eyes, itching, tingling and foreign body sensation); transient point erosion of the corneal epithelium,eyelid edema, keratitis; lengthening, thickening, increasing the number and strengthening of the pigmentation of eyelashes and vellus hair; iritis / uveitis; macular edema (in patients with aphakia, in patients with pseudophakia with a ruptured posterior lens capsule, or in patients with risk factors for the development of macular edema), including cystoid; changing the direction of eyelash growth, sometimes irritating to the eyes; blurred vision, photophobia, changes in the periorbital area and eyelids, leading to a deepening of the furrows of the upper eyelid, periorbital edema, iris cysts. Since the cardiovascular system: exacerbation of angina in patients with coronary heart disease, palpitations. On the part of the skin and subcutaneous tissues: skin rash, darkening of the eyelid skin and local skin reactions on the eyelids. On the part of the nervous system: dizziness. On the part of the respiratory system: asthma (including acute attacks or exacerbation of the disease in patients with a history of bronchial asthma), shortness of breath. On the part of the musculoskeletal system and connective tissue: pain in the muscles / joints. General and local reactions: nonspecific chest pain. Infections: herpetic keratitis. Timolol (in the form of eye drops): On the part of the immune system: systemic allergic reactions, including anaphylaxis, angioedema, anaphylactic reactions, urticaria, pruritus, localized and generalized rash. Metabolic and nutritional disorders: anorexia, hidden symptoms of hypoglycemia in diabetic patients. Mental disorders: behavioral changes and mental disorders, including confusion, hallucinations, anxiety, disorientation, nervousness, symptoms of depression, memory loss, insomnia, depression and nightmares. From the nervous system: cerebral ischemia, acute disorders of cerebral circulation, dizziness, increased symptoms of myasthenia gravis, paresthesia, drowsiness, headache, fainting. On the part of the organ of vision: cystoid macular edema, decreased sensitivity of the cornea; symptoms and signs of eye irritation (eg, burning sensation, itching, feeling of sand in the eyes, increased tearing, redness), blepharitis, keratitis, blurred vision, dry eye mucosa, corneal erosion, choroidal detachment after filtration surgery; ptosis, visual disturbances, including changes in refraction and diplopia. From the organ of hearing and vestibular apparatus: tinnitus.Cardiac disorders: arrhythmia, bradycardia, atrioventricular block, chronic heart failure, cardiac arrest, blockade of intracardiac conduction, heartbeat, progression of angina. Vascular disorders: intermittent claudication, cold hands and feet, lower blood pressure, Raynaud's syndrome. On the part of the respiratory system: bronchospasm (mainly in patients with previous bronchospastic diseases), cough, shortness of breath, nasal congestion, pulmonary edema and respiratory failure. On the part of the gastrointestinal tract: diarrhea, dryness of the oral mucosa, impaired taste, dyspepsia, nausea, vomiting, abdominal pain, retroperitoneal fibrosis. On the part of the skin and subcutaneous tissues: alopecia, pseudopemfigoid, skin rash, psoriasis-like rash or exacerbation of psoriasis. On the part of the musculoskeletal system and connective tissue: systemic lupus erythematosus and myalgia. Reproductive system and mammary glands: decreased libido, impotence, impaired sexual function and Peyronie's disease. General and local: asthenia / fatigue, chest pain, edema. In some patients with significant corneal damage, very rare cases of corneal calcification were recorded in connection with the use of phosphate-containing eye drops.
Overdose
LatanoprostSymptomes: in addition to eye irritation and conjunctival hyperemia, other undesirable changes in the organ of vision in the case of latanoprost overdose are not known. More than 90% of the drug is metabolized during the first passage through the liver. In / in infusion at a dose of 3 mcg / kg in healthy volunteers did not cause any symptoms, but when administered at a dose of 5.5-10 mcg / kg, nausea, abdominal pain, dizziness, fatigue, hot flashes and sweating were observed. These symptoms are resolved 4 hours after stopping the infusion. In patients with moderate bronchial asthma, administration of latanoprost in a dose 7 times higher than therapeutic did not cause bronchospasm. Timolol maleate Symptoms: cases of unintentional overdose of eye drops of timolol maleate are described.as a result, effects similar to those observed with systemic use of beta-blockers: dizziness, headache, shortness of breath, bradycardia, bronchospasm, cardiac arrest were observed. In an in vitro study, it was shown that dialysis of timolol maleate is easily removed from plasma or whole blood. In patients with renal insufficiency, timolol maleate was worse dialysed. Treatment: for Xalacoma overdose, symptomatic therapy is carried out.
Interaction with other drugs
The interaction of Xalacom with other drugs was not specifically studied. It is not recommended to use other beta-blockers simultaneously with Xalacom, since a pronounced decrease in IOP or enhancement of the systemic effects of beta-blockers is possible. When two prostaglandin analogues are simultaneously instilled into the eyes, a paradoxical increase in IOP is observed, therefore simultaneous the use of two or more prostaglandins, their analogues or derivatives is not recommended. With simultaneous use of timolol maleate with e pinefrinom (adrenaline) is sometimes evolved midriaz.Vozmozhno additive effect with the development of systemic hypotension and / or severe bradycardia when timolol maleate combination with the following drugs: calcium channel blockers slow, means for causing reduction of catecholamines, beta-blockers, antaritmicheskie agents, cardiac glycosides , guanethidine. An increase in the action of systemic beta-blockers (for example, a decrease in heart rate, depression) was reported with the simultaneous use of an isofarm inhibitor nta CYP2D6 (for example, quinidine, fluoxetine, paroxetine) and timolol. Beta-adrenoblockers may increase the hypoglycemic effect of antidiabetic drugs. With the sudden cancellation of clonidine, an increase in blood pressure is observed. This reaction can be enhanced with simultaneous use with beta-blockers.
special instructions
Xalacom should be used no more than 1 time / day, since more frequent use leads to a weakening of the effect of reducing IOP. When you skip a single dose, the next dose should be administered at the usual time. If the patient simultaneously uses other eye drops, they should be used at intervals of at least 5 min. Xalacom contains benzalkonium chloride, which can be adsorbed on contact lenses.There are reports of the development of point keratopathy and / or toxic ulcerative keratopathy; eye irritation and discoloration of soft contact lenses may also occur when using benzalkonium chloride. It is recommended to conduct a thorough monitoring of the condition of patients who use Xalacom frequently or for a long time, in whom dryness of the mucous membrane of the eyes or conditions that damage the cornea is observed. Before dropping instillation of contact lenses should be removed, and then set after 15 min. Latanoprost Latanoprost can cause a gradual increase in the content of brown pigment in the iris. As with the use of latanoprost in the form of eye drops, with the use of Xalacom, the enhancement of iris pigmentation was noted in 16-20% of cases among all patients who received the drug during the year (assessed on the basis of photographs). The change in eye color is due to an increase in the number of melanin in the stromal melanocytes of the iris, and not an increase in the number of melanocytes themselves. In typical cases, brown pigmentation appears around the pupil and concentrically spreads to the periphery of the iris. In this case, the entire iris or its parts become brown. In most cases, the color change is minor and may not be established clinically. Increased pigmentation of the iris of one or both eyes is observed mainly in patients with mixed color of the iris, which is mainly based on brown color. The drug has no effect on nevi and lentigo iris; accumulation of pigment in the trabecular network or anterior chamber of the eye is not observed. When determining the pigmentation of the iris for more than 5 years, no undesirable effects of increased pigmentation were detected, even with continued therapy with latanoprostom. In patients, the degree of IOP reduction was the same regardless of the degree of pigmentation of the iris. Therefore, treatment with latanoprostom can be continued in cases of increased iris pigmentation, but patients should be monitored regularly and, depending on the clinical situation, treatment can be stopped. Increased iris pigmentation is usually observed during the first year after the start of treatment, rarely after 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 pigmentation of the iris have not been studied. After cessation of treatment, the enhancement of brown pigmentation of the iris was not observed, however, the change in eye color may be irreversible. In connection with the use of latanoprost, cases of darkening of the eyelid skin, which may be reversible, are described. increased pigmentation, increase in thickness and change the direction of growth of eyelashes. Changes to the eyelashes are reversible and disappear after stopping treatment. Patients using drops for the treatment of only one eye may develop heterochromia. Timolol maleate The topical application of beta-blockers may result in the same adverse reactions as systemic use. Patients with severe heart disease history should be constantly monitored in order to timely identify the symptoms of heart failure. The local application of timolol maleate may cause progression of Prinzmetal angina pectoris, peripheral and central circulatory disorders, arterial hypotension, bradycardia, fatal heart failure, and severe reactions of the respiratory system (including bronchospasm with a lethal outcome in patients with bronchial asthma) .Before extensive surgical intervention, the feasibility of phasing out beta-blockers should be discussed. Drugs in this group impair the ability of the heart to respond to reflex beta-adrenergic stimulation, which may increase the risk during anesthesia. Cases of prolonged severe hypotension during anesthesia and difficulties in restoring and maintaining cardiac activity are described. During surgery, the effects of beta-blockers can be eliminated with sufficient doses of adrenoreceptor agonists. Medicines with beta-blocking effect can block the systemic agonist effect of drugs such as epinephrine.Therefore, it is necessary to warn the anesthesiologist that the patient is receiving timolol. Beta-blockers can enhance the hypoglycemic effect of oral hypoglycemic agents and mask the symptoms of hypoglycemia. They should be used with caution in patients with spontaneous hypoglycemia or diabetes mellitus (especially labile), receiving insulin or oral hypoglycemic agents. Beta-adrenergic blocker therapy may mask the symptoms of hyperthyroidism, abrupt cessation of treatment can cause exacerbation of this disease. When treating beta-adrenergic blockers, patients with atopy or severe anaphylactic reactions to various allergens in the anamnesis, the response may be enhanced by repeated contact with these allergens. In this case, epinephrine (adrenaline) in the usual doses used to relieve anaphylactic reactions may not be effective. In rare cases, timolol maleate causes increased muscle weakness in patients with myasthenia gravis or myasthenic symptoms (for example, diplopia, ptosis, generalized weakness). agents that reduce IOP, described choroid detachment after filtration procedures - fistulizirovannyh operations (trabeculectomy and its modifications, sinusotomy with diatomotor tract, non-invasive I have deep sclerectomy and other fistulizing operations, which create new or stimulate existing ways of outflow of intraocular fluid). Impact on the ability to control vehicles and work with mechanisms. The use of eye drops can cause transient blurred vision. Until this effect disappears, patients should not drive or use sophisticated equipment.