Index of drugs

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

1 ml drops contains 50 μg latanoprost and 5 mg timolol (as maleate). The preparation contains 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 intra-ocular pressure by increasing the outflow of aqueous humor - increases the flow of the choroid-scleral and reduces the resistance of the outflow through the trabecular meshwork. It has no significant effect on the production of aqueous humor and on the blood-liquid water barrier as well as on intraocular blood circulation. After application to the conjunctival sac, it 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 approximately 2 hours after administration. T_0,5 in plasma is about 17 min. After topical administration, the systemic bioavailability of latanoprostic acid is 45%. Latanoprost acid binds to plasma proteins in 87%. Metabolism occurs mainly in the liver. Inactive metabolites are mainly excreted in the urine. Timolol is a non-selective beta-blocker, lacking intrinsic sympathomimetic activity, direct inhibition of myocardial function and nonspecific stabilizing of the membrane. 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 aqueous humor occurs after about 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. T_0,5 in plasma is 6 h. Metabolism occurs in the liver. Timolol metabolites are excreted in the urine along with part of the drug in unchanged form. There is a tendency to maintain a 2-fold higher concentrations of latanoprost in the aqueous humor after 1-4 hours from the administration of eye drops containing latanoprost and Timolol, compared to monotherapy.

Hypersensitivity to the active substance or to any of the excipients. Diseases with bronchial hyperreactivity, including bronchial asthma, history of asthma, severe chronic obstructive pulmonary disease. Sinus bradycardia, sick sinus syndrome, atrio-ventricular block IIst. and III. without a pacemaker, overt cardiac failure, cardiogenic shock.

Due to the content of β-blocker during the application of the preparation, adverse reactions occurring during the general use of β-blockers may occur (less frequently than after the general administration). In patients with cardiovascular disease (eg coronary heart disease, Prinzmetal's angina and heart failure) and hypotension, β-blocker therapy should be carefully evaluated and other medication should be considered. Patients with cardiovascular disease should be monitored for deterioration of existing diseases and side effects. In patients with heart block Ist. β-blockers should be used with caution due to their adverse effect on conduction time. Caution should be exercised in patients with severe peripheral circulatory disturbances (eg severe Raynaud's disease or Raynaud's syndrome). In patients with mild to moderate chronic obstructive pulmonary disease, the product should be used with caution and only if the potential benefit outweighs the risk.β-blockers should be used with caution in patients prone to self-hypoglycaemia or patients with unstable diabetes (beta-blockers may mask the symptoms of acute hypoglycaemia). Β-blockers can also mask the symptoms of hyperthyroidism. Ophthalmologic preparations containing β-blockers may cause dry eye - care should be taken in patients with corneal diseases. Co-administration of timolol with another β-adrenergic with a general effect may lead to increased intraocular pressure or known effects associated with systemic β-adrenergic blockade - patients' reactions should be carefully monitored. During treatment with beta-blockers, patients with a history of atopic disease or severe anaphylactic reactions caused by a variety of allergens may be more sensitive to re-exposure to these allergens and show no response to the doses of epinephrine usually used to treat anaphylactic reactions. When using agents that inhibit the production of aqueous humor (eg timolol, acetazolamide), cases of choroidal dissection have been reported after filtration. Ophthalmic preparations containing β-blockers can suppress the systemic effects of β-agonists, e.g. adrenaline - inform the anesthetist if the patient is using timolol. Co-administration of two topically administered β-blockers or two topically-applied preparations containing prostaglandins is not recommended. Latanoprost can gradually change the eye color by increasing the amount of brown pigment in the iris. It has not been proven that the change in the color of the iris is accompanied by other side effects or pathological changes. Color changes can be permanent. Patients should be tested regularly and if the iris pigmentation increases and the clinical condition so requires treatment should be discontinued. There is no documented experience regarding the use of latanoprost in inflammatory and neovascular glaucoma, or glaucoma of a closed angle or congenital glaucoma, open-angle glaucoma in patients with pseudophakia and pigmented glaucoma. Latanoprost has no effect on the pupil or is insignificant, however, there is no experience regarding the use of acute glaucoma attacks with a closed angle. Therefore, caution should be exercised when administering the preparation in these disease states until complete data are available. Latanoprost should be used with caution in patients who have had a history of herpetic keratitis. The use of latanoprost should be avoided in patients with current herpetic keratitis and in patients with a history of recurrent herpetic keratitis, particularly related to the use of prostaglandin analogues. Due to the risk of macular edema, including its cystic form in patients with aphasia, pseudophakia with discontinued posterior capsule, as well as patients at risk of macular edema, the preparation should be used with caution. The preparation contains benzalkonium chloride, which can cause punctate keratopathy and / or toxic ulcerative keratopathy, eye irritation and discoloration of soft contact lenses. Patients with dry eye syndrome or those with corneal injury that use the product frequently or for long periods of time should be carefully monitored. Before using the product, the contact lenses should be removed and not worn earlier than after 15 minutes. The safety and efficacy of the preparation in children and adolescents have not been established.

The preparation should not be used during pregnancy and breastfeeding.

Very common: increased pigmentation of the iris (especially in patients with iris of mixed color, eg green-brown, yellow-brown or blue / gray-brown, change in the color of the iris is very slow, not associated with other symptoms or pathological changes, can be stable, in patients with a homogeneous blue, gray, green or brown eye color, a change of color is rare). Common: eye irritation (including pricking, burning and pruritus), 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.Latanoprost: herpetic keratitis, dizziness, change of eyelashes and follicular hair (increased length, thickness, pigmentation and quantity), punctate epithelial defects, periorbital edema, iritis / uveitis, macular edema (in patients with aphasia, pseudophacia and broken back bag of the lens, or in patients at risk of macular edema), dry eye, keratitis, corneal edema and erosions, incorrectly directed eyelashes which sometimes lead to eye irritation, iris cyst, photophobia, orbital and eyelid changes leading to deepening of the eyelid furrow, deterioration of pre-existing angina, palpitations, asthma, asthma exacerbation, shortness of breath, dark eyelid skin, joint pain, muscle pain, chest pain. Timolol: systemic allergic reactions (including angioneurotic edema, urticaria, local or generalized rash, pruritus, anaphylactic reactions), hypoglycaemia, insomnia, depression, nightmares, memory loss, syncope, cerebrovascular episode, cerebral ischaemia, exacerbation of signs and symptoms myasthenia gravis, dizziness, paresthesia, headache, signs and symptoms of eye irritation (eg burning and pinching sensation, pruritus, tearing, redness), blepharitis, keratitis, blurred vision and choroidal detachment following surgical filtration, reduction of the sensation cornea, dry eyes, corneal erosion, ptosis, double vision, tinnitus, bradycardia, chest pain, palpitations, edema, arrhythmia, congestive heart failure, atrioventricular block, cardiac arrest, heart failure, reduced blood pressure blood , Raynaud's symptom, cold hands and feet, bronchospasm (mainly in patients with pre-existing bronchospasm), dyspnea, cough, change in taste, nausea, indigestion, diarrhea, dry mouth, abdominal pain, vomiting, baldness , psoriasis-like rash or worsening of psoriasis symptoms, skin rash, muscle pain, sexual dysfunction, reduced sex drive, weakness, fatigue.

Adults (including the elderly): 1 drop for the eye or both eyes covered by the disease once a day. If you miss one dose, continue with the Next scheduled dose. Compression of the nasolabial canal or closing of the eyelids for 2 min reduces the systemic absorption of the drug. If other topical ophthalmic medications are used, a break of at least 5 minutes should be allowed between administrations.