Index of drugs

Reduction of elevated intraocular pressure in patients with open-angle glaucoma and intraocular hypertension who have insufficient response to beta-blockers or prostaglandin analogs.

1 ml drops contains 50 μg latanoprost and 5 mg Timolol as maleate and 0.20 mg 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 - it increases the flow of the choroid-scleral and reduces the resistance of the outflow through the trabecular mesh. 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. Bronchial hyperreactivity, including bronchial asthma currently or in history, severe chronic obstructive pulmonary disease. Sinus bradycardia, syndrome of a sick sinus-atrial node, atrio-ventricular block IIst. or IIIst. not controlled by a pacemaker, overt cardiac failure, cardiogenic shock.

In patients with cardiovascular problems (eg ischemic heart disease, Prinzmetal angina and heart failure) and hypotension, the potential for β-blocker therapy should be critically evaluated and the use of other active substances should be considered. Patients with cardiovascular disorders should be monitored for deterioration of these disorders and for the severity of side effects. Due to the negative effects on conduction time, β-blockers should be used with caution in patients with Ist heart block. Caution should be exercised in patients with severe peripheral circulatory disturbances (eg severe Raynaud's disease or Raynaud's syndrome). Some respiratory symptoms, including deaths due to sudden bronchospasm in patients with asthma, have been reported in the eye following the use of certain β-blockers. 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 may mask the signs and symptoms of hypoglycaemia - caution should be exercised in patients exposed to spontaneous hypoglycaemia and patients with unstable diabetes mellitus. β-blockers can mask the symptoms of hyperthyroidism. β-blockers may cause dry eyes - the product should be used with caution in patients with corneal diseases. Use of the preparation together with another systemic beta-blocker may lead to increased intraocular pressure or known effects associated with systemic β-adrenergic blockade - these patients should be closely monitored for response. Co-administration of two topically active β-blockers or two locally acting prostaglandins is not recommended. Patients with a history of atopic disease or severe anaphylactic reactions caused by a variety of allergens may be more sensitive to repeated allergen challenge and may show no response to the adrenaline dose used to treat anaphylactic reactions during beta blockers. When using agents that inhibit the production of aqueous humor (eg timolol, acetazolamide), cases of choroidal dissection have been reported after filtration. Β-blocker preparations administered to the eye may inhibit the systemic effect of β-agonists, eg adrenaline - before the surgery, the anesthetist should be informed that the patient is using timolol. During treatment, the pigmentation of the iris may change; treatment can be continued, however, patients should be regularly examined and if the clinical condition requires it, treatment should be discontinued. Due to the lack of documented experiments, caution should be exercised when using the preparation in patients with inflammatory glaucoma, neovascular glaucoma, closed-angle glaucoma, congenital glaucoma, open-angle glaucoma in patients with pseudophakia, pigmented glaucoma and acute attacks of glaucoma with closed angle. Latanoprost should be used with caution in patients who have had a history of herpetic keratitis. Avoid use in patients with existing herpes keratitis and in patients with recurrent herpetic keratitis associated with prostaglandin analogs. Due to the risk of macular edema (including cystic form), caution should be exercised when using latanoprost in patients with aphasia, pseudophakia with discontinued posterior capsule or in patients at risk of cystic macular edema. The benzalkonium chloride contained in the preparation may 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. Contact lenses should be removed before applying the preparation and do not wear earlier than after 15 minutes.

The preparation should not be used during pregnancy and breastfeeding.

Very common: increased pigmentation of the iris (most commonly in people with mixed iris color eg: blue-brown, gray-brown, yellow-brown and green-brown). Common: eye irritation (including pricking, burning, pruritus), eye pain. Uncommon: headache, conjunctival congestion, conjunctivitis, blurred vision, excessive tearing, eyelid inflammation, corneal disease, rash, pruritus. Additional side effects associated with the use of the individual components of the preparation: latanoprost: keratitis keratitis, dizziness, changes in the appearance of eyelashes (lengthening, thickening, darkening, increasing the amount), punctate epithelial defects, periorbital edema, iritis / uveitis, edema spots (in patients with aphasia, pseudoafakia with discontinued posterior capsule, as well as in patients at risk of macular edema), dry eye, keratitis, swelling and corneal defects, changes in the direction of eyelash growth (which may cause eye irritation), cyst iris, photophobia, changes in the orbita and eyelid leading to deepening the eyelid furrow.deterioration of pre-existing angina, palpitations, asthma, exacerbation of asthma, shortness of breath, dark eyelid skin, joint pain, muscle pain, pain in the chest area; timolol: systemic allergic reaction (including angioneurotic edema, urticaria, local or generalized rash, pruritus, anaphylactic reaction), hypoglycaemia, insomnia, depression, nightmares, memory loss, syncope, cerebral infarction, cerebral ischemia, worsening of signs and symptoms subjective myasthenia gravis, dizziness, paresthesia, headache, eye irritation symptoms (burning, pricking, pruritus, tearing, redness of the eyes), blepharitis, keratitis, blurred vision, choroidal detachment after filtration, reduction of corneal sensitivity, dry eyes, erosion cornea, eyelid droop, double vision, tinnitus, bradycardia, chest pain, palpitations, edema, arrhythmia, congestive heart failure, atrioventricular block, cardiac arrest, heart failure, decreased blood pressure, Raynaud's phenomenon, cold hands and feet, bronchospasm (p in patients with pre-existing bronchial spasticity), dyspnea, cough, taste disturbances, nausea, digestive disorders, diarrhea, dry mouth, epigastric pain, vomiting, hair loss, psoriasis-like rash or exacerbation of psoriasis, skin rash, pains muscle, sexual dysfunction, decreased libido, weakness / fatigue. In some patients with severe corneal damage, very rare cases of corneal calcification associated with the use of eye drops with phosphate content have been reported.

Adults (also elderly patients). The conjunctival: 1 drop administered to the affected eye (eyes) once a day. If a dose is missed, treatment should be continued with the Next scheduled dose. Do not exceed a dose of 1 drop in the affected eye (s) once a day.Special groups of patients. The safety and efficacy of use in children and adolescents have not been established.Way of giving. After instillation, it is recommended to compress the nasal-lacrimal canal or close the eyelid for 2 minutes. If the patient uses more than one eye medicine, each of these medicines should be given at least 5 minutes apart.