Treatment of increased intraocular pressure in patients with open-angle glaucoma or glaucoma in the course of exfoliative syndrome, in which monotherapy with the β-blocker administered topically is not sufficiently effective.
Composition:
1 ml of solution contains 20 mg of dorzolamide (as hydrochloride) and 5 mg of Timolol (as a maleate); the solution contains benzalkonium chloride.
Action:
The preparation contains two active substances that lower elevated intraocular pressure by reducing the secretion of aqueous humor through various mechanisms of action. The combined effect of both drugs results in a greater reduction in intraocular pressure compared to the treatment of each drug used separately. Dorzolamide hydrochloride strongly inhibits carbonic anhydrase II. Inhibiting the activity of this enzyme in the cilia reduces the secretion of aqueous humor, presumably by slowing the formation of bicarbonate ions, thereby reducing the transport of sodium and liquid. Timolol maleate is a non-selective drug blocking β-adrenergic receptors. The main action of timolol is associated with a decrease in aqueous humor production, and a slight increase in fluid outflow was also observed. After topical application, the preparation lowers elevated intraocular pressure, regardless of whether it is associated with glaucoma or not. After administration to the conjunctival sac, dorzolamide and timolol are absorbed through the cornea and penetrate into the systemic circulation.
Contraindications:
Hypersensitivity to any of the ingredients. Reactive airways disease, including bronchial asthma currently or in history or severe chronic obstructive pulmonary disease. Sinus bradycardia, sick sinus syndrome, sinus-atrioventricular block, atrio-ventricular block IIst. or IIIst. uncontrolled using a pacemaker, overt cardiovascular failure, cardiogenic shock. Severe renal failure (CCr <30 ml / min) or hyperchloraemic acidosis.
Precautions:
The effectiveness of the drug in children has not been confirmed. The safety of the medicine in children <2 years has not been confirmed. Data on the use of the drug in children aged ≥2 and <6 years are limited. The use of the drug in patients with hepatic failure has not been studied - use with caution. Due to the content of Timolol, caution should be exercised in patients with cardiovascular diseases such as ischemic heart disease, Prinzmetal angina, heart failure and hypotension (a critical evaluation of beta blocker therapy in these groups should be considered and consideration should be given to the use of other active substances observe the patient for signs of deterioration of these diseases and side effects); with heart block Ist. degree (adverse effect of β-blocker on the duration of electrical impulses); with severe peripheral circulation disorders, i.e. with severe Raynaud's disease or with Raynaud's syndrome; with mild or moderate chronic obstructive pulmonary disease (risk of bronchospasm, use the beta-blocker only if the benefits outweigh the risk); with unstable diabetes or hypoglycaemia (symptoms of hypoglycaemia may be masked); with hyperthyroidism (some symptoms of hyperthyroidism may be masked, sudden withdrawal of β-blocker may exacerbate symptoms of hyperthyroidism); with myasthenia gravis (worsening of symptoms). Ophthalmic drugs with β-blocking activity can inhibit the systemic effect of β receptor stimulation by drugs such as adrenaline; in case of anesthesia, please inform the anesthetist about taking timolol; moreover, when using β-blockers, patients with a history of atopy or a history of severe anaphylactic reactions to a variety of allergens may show an increased response to these allergens, both accidentally and during diagnostic or therapeutic procedures, these patients may not respond to the dose of adrenaline usually used to treat anaphylactic reactions.Due to the content of dorzolamide, caution should be used in patients who have been diagnosed with kidney stones in the past (risk of urolithiasis). The use of a combined drug containing dorzolamide and timolol has not been studied in patients with acute angle-closure glaucoma. Exercise caution in patients with existing chronic corneal injury and / or ophthalmic surgery (risk of corneal edema and irreversible corneal decompensation when using dorzolamide); with corneal diseases (timolol may cause dry eyes). After filtration treatments with the simultaneous use of agents that inhibit the production of aqueous humor (eg with the use of timolol, acetazolamide) cases of choroidal dissection with simultaneous intraocular hypotonia have been reported. The preparation should be discontinued in the event of hypersensitivity reactions or serious adverse reactions (adverse reactions typical of β-blockers for sulfonamides are possible). The drops contain benzalkonium chloride, which may cause eye irritation and discoloration of soft contact lenses; the contact lenses should be removed before instillation; they can be put on again 15 minutes after instillation.
Pregnancy and lactation:
Do not use during pregnancy and during breastfeeding.
Side effects:
Very often: burning and stinging, taste disturbances. Common: conjunctival injections, blurred vision, corneal erosions, eye itching, tearing, sinusitis. Uncommon: urolithiasis. Rare: systemic allergic reactions (including angioedema, urticaria, pruritus, rash, anaphylaxis), shortness of breath, respiratory failure, rhinitis, bronchospasm, contact dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis.timolol. Common: headache, eye irritation, blepharitis, keratitis, decreased corneal sensitivity and dry eye. Uncommon: depression, dizziness, syncope, visual disturbances, including refraction disorders (in some cases due to discontinuation of a miocile drug), bradycardia, shortness of breath, nausea, indigestion, asthenia, fatigue. Rare: allergic reactions (including angioneurotic edema, urticaria, local and generalized rash, anaphylaxis), insomnia, nightmares, memory loss, paraesthesia, worsening of myasthenia gravis, decreased libido, cerebrovascular event, cerebral ischemia, eyelid droop, double vision, choroidal detachment after filtration, tinnitus, chest pain, palpitations, edema, arrhythmia, congestive heart failure, cardiac arrest, heart block, hypotension, claudication, Raynaud's phenomenon, cold hands and feet, bronchospasm ( especially in patients with pre-existing bronchial spasticity), respiratory failure, cough, diarrhea, dry mouth, alopecia, psoriasis-like rash or exacerbation of psoriasis, systemic lupus erythematosus, Peyronie's disease, decreased libido. Not known: pruritus, hypoglycaemia, itching, watery eyes, redness, blurred vision, corneal ulceration, heart failure, atrioventricular block, taste disturbances, abdominal pain, vomiting, muscle pain, sexual dysfunction.dorzolamide. Common: headache, blepharitis, eyelid irritation, nausea, asthenia, fatigue. Uncommon: inflammation of the iris and ciliary body. Rarely: dizziness, paresthesia, irritation (including redness), pain, eyelid gluing, transient myopia (receding after discontinuation of therapy), corneal edema, ocular hypotonia, choroidal detachment (after filtration procedures), nosebleeds, throat irritation, dryness in the mouth, rash.
Dosage:
1 drop into the conjunctival sac of the affected eye (eyes) 2 times a day. Children: limited data are available on the use of the preparation twice a day in children aged ≥2 and <6 years. When using several topical ophthalmic medications, a minimum of 10 minutes should be allowed between the instillation of subsequent medications. It is recommended to gently close the eyelid and / or compress the nasolabial duct after instillation to reduce the absorption of the drug into the systemic circulation.