Treatment of increased intraocular pressure in patients with open-angle glaucoma or glaucoma in the course of epidural exfoliative syndrome, when beta-adrenoceptor therapy is insufficient.
Composition:
1 ml of solution contains 20 mg of dorzolamide (as hydrochloride) and 5 mg of Timolol (as maleate). The preparation 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 strongly inhibits human carbonate anhydrase II. Inhibition of carbonic anhydrase in the ciliary processes of the eye causes a reduction in the volume of secreted aqueous humor. This is probably due to a reduction in the rate of ion formation bicarbonate and the resulting reduction in sodium and liquid transport. Timolol is a non-selective antagonist of 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 dorzolamide, timolol or any of the excipients. Airway hyperreactivity, including bronchial asthma currently or in history, and 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 impairment (creatinine clearance <30 ml / min) or hyperchloraemic acidosis.
Precautions:
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 have an increased response to come back to these allergens, these patients may not respond to the dose of adrenaline commonly 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). When using agents that inhibit the production of aqueous humor (eg timolol, acetazolamide) after filtration, cases of choroidal dissection have been reported. In some patients, a decreasing response to timolol eye drops was found during long-term treatment (this was not observed in clinical trials). 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, eyelid inflammation, keratitis, decreased corneal sensation, dry eye symptoms. Uncommon: depression, dizziness, syncope, visual disturbances, including refraction disorders (in some cases due to discontinuation of the drug that constricts the pupil), bradycardia, shortness of breath, nausea, indigestion, weakness, fatigue. Rare: allergic reactions (including angioneurotic edema, urticaria, local and generalized rash, anaphylaxis), insomnia, nightmares, memory loss, paresthesia, worsening of myasthenia gravis, decreased sex drive, cerebrovascular incident, cerebral ischemia, eyelid drooping, 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: itching, hypoglycaemia, itchy eye, watery eyes, blurred vision, corneal ulceration, heart failure, atrioventricular block, abnormal taste, abdominal pain, vomiting, skin rash, muscle pain, sexual dysfunction.dorzolamide. Common: headache, eyelid inflammation, eyelid irritation, nausea, weakness, fatigue. Uncommon: inflammation of the iris and ciliary body. Rarely: dizziness, paresthesia, eye irritation (including redness), eye pain, eyelid stickiness, temporary myopia (disappearing after cessation of therapy), corneal edema, ocular hypotonia, choroidal detachment (after filtration procedures), nose bleed, throat irritation , dryness of the oral mucosa, rash.
Dosage:
1 drop into the conjunctival sac of the affected eye (eyes) 2 times a day.Children and youth. The effectiveness of the medicine in children has not been determined. The safety of the medicine in children aged <2 years has not been established. Limited data are available on the use of the preparation twice a day in children aged ≥2 and <6 years.Way of giving. 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. When using several topical ophthalmic medications, a minimum of 10 minutes should be allowed between the instillation of subsequent medications.