Index of drugs

Reduction of intraocular pressure in patients with open-angle glaucoma and elevated intraocular pressure, in whom the response to topically applied β-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 preparation 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 17 min. After systemic administration, the systemic bioavailability of latanoprostal 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 β₁ and β₂-adrenolytic, which does not have intrinsic sympathomimetic activity or nonspecific effects that reduce myocardial function or cell membrane stabilization activity. Timolol lowers 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 about 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. Reactive respiratory diseases, including bronchial asthma or bronchial asthma, severe chronic obstructive pulmonary disease. Sinus bradycardia, sick sinus syndrome, sinoatrial block, atrio-ventricular block IIst. or IIIst. decomposed with a pacemaker. Heart failure with symptoms, 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 ischemic heart disease, Prinzmetal's angina, cardiac insufficiency) and hypotension, β-blockers should be evaluated with particular care and consideration should be given to the use of other active substances; these patients should be monitored for signs of deterioration of these diseases and side effects. Due to the negative effect on the conduction time, β-blockers can be administered to patients with a heart block Ist. only with caution. Caution should be exercised in patients with severe or peripheral circulatory disorders (ie severe forms of Raynaud's disease or Raynaud's syndrome). It should be used with caution in patients with mild or moderate chronic obstructive pulmonary disease and only if the expected benefit outweighs the potential risk.Exercise caution in patients predisposed to spontaneous hypoglycaemia or in patients with unstable diabetes, because beta-blockers may mask the signs and symptoms of acute hypoglycaemia. β-blockers can mask the symptoms of hyperthyroidism. Patients with corneal diseases should be treated with caution. Co-administration of two topically administered β-blockers or two locally acting prostaglandins is not recommended. When using β-blockers, patients with a history of atopic disease or severe anaphylactic reactions due to a variety of allergens may be more sensitive to repeated exposure to the allergen and not respond to the usual doses of adrenaline administered to treat anaphylactic reactions. Latanoprost may gradually change the eye color by increasing the amount of brown pigment in the iris; this is not associated with any adverse or pathological symptoms. The change in color may be permanent. Patients should be tested regularly and if iris pigmentation increases, depending on the clinical condition, discontinuation may be considered. Due to limited data, caution should be used when using latanoprost in inflammatory, neovascular, chronic obstructed-angle, congenital, open-angle glaucoma in patients with pseudophakia, pigmented glaucoma and acute attacks of closed-angle glaucoma. 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. During the treatment with latanoprost, macular edema has been observed, including its cystic form. This symptom was detected mainly in patients with aphasia, pseudophakia with discontinued posterior capsule, as well as in patients at risk of macular edema - the preparation should be used with caution in these patients. As a result of the use of drugs that lower the intraocular pressure (eg timolol, acetazolamide) choroidal detachment after filtration was observed. β-blockers administered in the form of eye preparations may block the action of general β-agonists, e.g. adrenaline - an anesthesiologist should be informed that the patient is using the preparation. There are no data on the safety and efficacy of the preparation in children and adolescents. The preparation contains benzalkonium chloride, which may cause the cornea to break and / or toxic, ulcerative corneal defects; it can also cause eye irritation and discoloration of soft contact lenses. During frequent or long-term use of the preparation, close monitoring of patients with dry eye or damaged cornea is necessary. Contact lenses can absorb benzalkonium chloride. The lenses should be removed before the medicine is sprayed on, they can be re-inserted after 15 minutes.

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, the change in the color of the iris is very slow, does not involve other symptoms or pathological changes, can be stable, in patients with one-colored iris of the color blue, gray, green or brown the change of color is rare). Common: eye irritation (including pricking, burning and pruritus), eye pain. Uncommon: headache, conjunctival hyperemia, conjunctivitis, blurred vision, tearing, blepharitis, corneal diseases, rash, pruritus. Additional side effects specific for the individual active ingredients of the preparation. Latanoprost: herpetic keratitis, dizziness, changes in eyelashes and hairs (increase in length, thickness, discoloration and quantity), punctate erosive epithelium, edema around the eyes, iritis or uveitis, macular edema (in patients with aphasia, pseudophakia and discontinued posterior capsule or patients at risk for macular edema), dry eye, keratitis, corneal edema and erosion, abnormally growing eyelashes (which may cause eye irritation), iris cyst, exacerbation of pre-existing angina, palpitations , asthma, worsening asthma, shortness of breath, dark eyelid skin, joint pain, muscle pain, chest pain. Timolol: symptoms and systemic allergic reactions (including angioneurotic edema, urticaria and local and general rash, pruritus, anaphylactic reaction), hypoglycaemia.depression, memory disorders, decreased libido, insomnia, nightmares, dizziness, paresthesia, cerebral ischaemia, cerebral infarction, increased myasthenia gravis, syncope, headache, signs and symptoms of eye irritation (burning, pricking, pruritus, tearing, redness) , blepharitis, keratitis, visual impairment, choroidal detachment after filtration, reduction of corneal sensation and eye dryness, corneal erosion, visual disturbances including refractive changes (conditioned in some cases by interruption of miotics), double vision, ptosis, noise in the ears, palpitations, arrhythmias, bradycardia, chest pain, cardiac arrest, edema, block of the heart, congestive heart failure, atrioventricular block, heart failure, hypotension, Raynaud's, cold hands and feet, contraction bronchi (mainly in patients with existing ones previously bronchial spastic disorders), dyspnea, cough, taste disorders, nausea, diarrhea, indigestion, dry mouth, abdominal pain, vomiting, alopecia, psoriasis-like rash or exacerbation of psoriasis, skin rash, muscle pain, sexual dysfunction, decreased libido, weakness / fatigue.

Adults (including the elderly): 1 drop for the eye (s) affected by the disease process, once a day. If you miss one dose, continue with the Next scheduled dose. If other topical ophthalmic medications are used, a break of at least 5 minutes should be allowed between administrations. Compression of the nasolabial canal or gentle closing of the eyelids for 2 min limits the systemic absorption of the drug and increases the local effect of the preparation.