Index of drugs

Decrease in intraocular pressure in patients with open-angle glaucoma and elevated intraocular pressure, in whom the response to topically applied beta-blockers or prostaglandin analogs is insufficient.

1 ml drops contain 0.05 mg latanoprost and 5 mg Timolol (as maleate). Drops contain benzalkonium chloride.

The product contains two active substances that reduce intraocular pressure due to different mechanisms of action. The combined effects of both drugs cause a greater decrease in intraocular pressure compared to the treatment of each drug used separately. Latanoprost is an analog of prostaglandin F_2α, a selective prostanoid FP receptor agonist. It lowers the intraocular pressure by increasing the outflow of aqueous humor - increases the choroidal scleral flow and reduces the resistance of outflow. It does not affect the production of aqueous humor and the blood-liquid barrier as well as the intraocular blood circulation. After application to the conjunctival sac, the preparation is absorbed through the cornea and is hydrolysed to the biologically active latanoprost acid. The maximum concentration of the drug in the aqueous humor occurs 2 hours after administration. After topical administration, the systemic bioavailability of latanoprostic acid is 45%. Latanoprost acid binds to plasma proteins in 87% and is practically not metabolized. Metabolism is mainly in the liver. Inactive metabolites are mainly excreted in the urine. T_0,5 it is about 17 min. Timolol is a non-selective beta-blocker, lacking intrinsic sympathomimetic activity and specific membrane function. Timolol reduces intraocular pressure by reducing the production of aqueous humor in the ciliary epithelium. There was no significant effect on the permeability of the blood-liquid barrier to plasma proteins. The maximum concentration in the aqueous humor occurs after 1 hour after local instillation of the drug. Part of the dose penetrates into the bloodstream - the maximum plasma concentration is reached after 10-20 min. Metabolism is in the liver. Timolol metabolites are excreted in the urine along with part of the drug in unchanged form. T_0,5 is 6 hours.

Hypersensitivity to the components of the preparation. Diseases with airway hyperresponsiveness (including bronchial asthma, history of asthma, severe chronic obstructive pulmonary disease). Sinus bradycardia, sinoatrial block caused by sick sinus syndrome, atrio-ventricular block IIst. or IIIst. uncontrolled with a pacemaker, overt cardiac failure, cardiogenic shock.

In patients with cardiovascular disease (eg ischemic heart disease, Prinzmetal's angina, heart failure) and hypotension, treatment with other substances should be considered. Patients with cardiovascular disease should be monitored for signs of deterioration and undesirable effects. Particularly cautiously, β-blockers should be used in patients with Ist block of heart. (negative effect on conduction time), with severe peripheral circulatory disturbances / diseases (eg severe forms of Raynaud's disease or Raynaud's syndrome). The drug should be used with caution in patients with mild / moderate COPD and only if the potential benefit outweighs the potential risk. Β-blockers should be used with caution in patients at risk of spontaneous hypoglycaemia or in patients with unstable diabetes because they may mask the symptoms of acute hypoglycaemia. Β-blockers can mask the symptoms of hyperthyroidism. When using β-blockers, patients with a history of atopic disease or severe anaphylactic reactions due to a variety of allergens may have a higher reactivity to repeated contact with these allergens and no response to the adrenaline dose usually used to treat anaphylactic reactions. Use of the preparation concomitantly with another oral β-blocker may lead to enhanced intraocular pressure-lowering effects or known activities associated with systemic β-adrenergic blockade. Carefully observe the patients' response to such treatment. Co-administration of two topically active β-blockers or two locally acting prostaglandins is not recommended.Due to the lack of sufficient data, caution should be exercised when using the drug in: inflammatory glaucoma, neovascular, chronic closed angle, congenital, open angle glaucoma in patients with pseudophakia, pigmented glaucoma. The drug does not affect or exert a minor effect on the pupils, but there is no documented experience regarding the use of acute attacks of closed-angle glaucoma. In these patients, caution should be exercised when using the drug until complete data is available. Patients should be closely monitored for frequent or long-term use in patients with dry eye syndrome or corneal injury. Because of the risk of macular edema and cystoid macular edema, use caution in patients with aphasia and pseudoaphacia with an interrupted posterior capsule and in patients at risk for macular edema. As a result of the use of drugs that lower the intraocular pressure (eg Timolol, acetazolamide) choroidal detachment after filtration was observed. During treatment, the pigmentation of the iris may change; patients should be tested regularly, if required by the clinical condition, treatment should be discontinued. Β-blockers applied to the eye may block systemic β-agonist activity, e.g. adrenaline. The anesthetist should be informed that the patient is taking timolol. Before starting treatment, the patient should be informed about the possibility of a permanent change in the color of the iris of the treated eye (treatment of one eye may lead to permanent heterochromia). The preparation contains benzalkonium chloride, which can cause point keratopathy, toxic ulcerative keratopathy, eye irritation, can be absorbed by contact lenses and change the color of soft contact lenses - do not use the product when using this type of lenses. Contact lenses should be removed before instillation and re-inserted no earlier than 15 minutes after instillation. There are no data on the safety and efficacy of the preparation in children and adolescents.

Do not use during pregnancy and during breastfeeding.

Very common: increased iris pigmentation (mainly in patients with iris of mixed color, eg green-brown, yellow-brown or blue / gray-brown, iris color change is very slow, it does not involve any side effects or pathological changes , it can be durable). Common: eye irritation (including stinging, burning and itching), eye pain. Uncommon: headache, eye congestion, conjunctivitis, blurred vision, increased tearing, blepharitis, corneal disorders, skin rash, pruritus. Additional side effects associated with the use of individual components of the preparation (frequency unknown). Latanoprost: dizziness, change of eyelashes and primary hair (increased length, thickness, pigmentation and quantity), punctate epithelial defects, periorbital edema, iritis / uveitis, macular edema, dry eyes, keratitis, edema and corneal errosion, incorrectly directed eyelashes (sometimes leading to eye irritation and iris cyst formation), exacerbation of angina in patients with pre-existing disease, palpitations, chest pain, asthma, exacerbation of asthma, shortness of breath, dark eyelid skin, joint pain, muscle pain. Timolol: hypersensitivity reactions (including angioneurotic edema, urticaria, skin rash), depression, insomnia, nightmares, memory loss, decreased libido, dizziness, paresthesia, cerebral ischemia, stroke, exacerbation of myasthenia gravis, syncope, signs and symptoms eye irritation including keratitis, decreased corneal sensation, dry eyes, visual disturbances including refractive changes (conditioned in some cases by interruption of miosis), double vision, ptosis, choroidal detachment (a consequence of a surgical filtration procedure), tinnitus, palpitations , bradycardia, arrhythmias, cardiac arrest, heart block, congestive heart failure, congestive heart failure, low blood pressure, Raynaud's symptom, cold hands and feet symptom, bronchospasm (mainly in patients with pre-existing disorder and bronchospasm), shortness of breath, cough, nausea, diarrhea, indigestion, dry mouth, a psoriatic rash similar to psoriasis or worsening of psoriasis symptoms, weakness, fatigue, chest pain, swelling.Timolol can cause the same types of cardiovascular disorders, respiratory disorders and other adverse reactions as in the case of β-blockers administered generally, the incidence of side effects after topical administration being lower than for systemic administration. Serious respiratory adverse reactions (including deaths due to sudden bronchoconstriction) may occur after administration of β-blockers. Additional side effects reported with β-adenolytic drugs that may occur during treatment: anaphylactic reactions, hypoglycaemia, signs and symptoms of eye irritation (eg tearing, redness), atrioventricular block, heart failure, abnormal taste, abdominal pain , vomiting, muscle pain, sexual dysfunction.

Adults: 1 drop to the affected eye (eyes) once a day. If the patient uses more than one eye medicine, each of these medicines should be given at least 5 minutes apart. If you miss one dose, continue with the Next scheduled dose. Blockage of the nasal-lacrimal gland or occlusion of the eyelids for 2 minutes reduces the systemic absorption of the drug. This can lead to relief of systemic side effects and increase the local activity of the drug.