Index of drugs

Treatment of elevated intraocular pressure in patients with open-angle glaucoma or pertussis glaucoma when beta-blocker monotherapy is insufficient.

1 ml of solution contains 20 mg of dorzolamide (as hydrochloride) and 5 mg of Timolol (as maleate).

A medicament lowering the increased intraocular pressure, which is a combination of a carbonic anhydrase inhibitor with a non-selective β-adrenergic receptor blocker. The combined effect of both substances results in a greater decrease in intraocular pressure than each one given separately. Dorzolamide hydrochloride is a potent inhibitor of carbonic anhydrase II. Inhibition of carbonic anhydrase in the ciliary processes of the eye reduces the secretion of aqueous humor, probably by slowing the rate of formation of bicarbonate ions with the consequent reduction of sodium transport and fluid. Timolol is a non-selective drug blocking β-adrenergic receptors. The action of timolol may be associated with a decrease in the production of aqueous humor, as well as a slight facilitation of the outflow of liquid. After topical administration, the preparation reduces elevated intraocular pressure, regardless of whether it is associated with glaucoma. Topical administration of dorzolamide allows the drug to work directly in the eye at much lower doses, and therefore with lower systemic exposure, resulting in a reduction in intraocular pressure without disturbing the acid-base balance and no changes in electrolyte concentrations characteristic of oral carbonic anhydrase inhibitors. After administration to the conjunctival sac, dorzolamide and timolol are absorbed through the cornea and penetrate into the systemic circulation.

Hypersensitivity to the components of the preparation. Airway hyperreactivity, 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 with a pacemaker, overt cardiac failure, cardiogenic shock. Severe renal failure (creatinine clearance <30 ml / min), hyperchloraemic acidosis.

The safety of the preparation in children <2 years has not been established. There are limited data on the safety of the medicine in children ≥2 and <6 years - in a small group of patients, the formulation administered twice daily was generally well tolerated. The effectiveness of the preparation in children has not been established. The use of the preparation in patients with acute angle-closure glaucoma has not been studied. The drug has not been studied in patients with impaired liver function - use caution. Due to the content of Timolol, in patients with cardiovascular disease (eg coronary disease, Prinzmetal's apnea or heart failure) or hypotension, the use of the preparation should be critically evaluated and treatment should be considered with other drugs that do not contain β-blockers. Exercise caution in patients with atrioventricular block Ist; with severe peripheral circulation disorders (e.g., severe forms of Raynaud's disease or Raynaud's syndrome); with mild to moderate chronic obstructive pulmonary disease (risk of β-blocker-induced bronchoconstriction - these drugs should only be used if the potential benefit outweighs the potential risk); with poorly controlled diabetes or spontaneous episodes of hypoglycaemia, with hyperthyroidism (beta-blockers can mask the symptoms of these diseases); with corneal diseases (beta-blockers may cause the eyeball to dry). The anesthetist should be informed that the patient is taking timolol because of the possible blockade of systemic β-agonistic activity, e.g. adrenaline. When using β-blockers, patients with a history of atopy or history of severe anaphylactic reactions to a variety of allergens may have an increased response to re-exposure to these allergens; these patients may not respond to the doses of adrenaline usually used to treat anaphylactic reactions. Treatment with β-blockers may increase symptomsmyasthenia gravis. As with systemic β-adrenergic drugs, if it is necessary to discontinue timolol eye drops in patients with coronary artery disease, the drug should be discontinued gradually. 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); with previous chronic corneal lesions and / or ophthalmic surgery (history of edema and irreversible corneal decompensation with dorzolamide in these patients). After application of drugs that inhibit the production of aqueous humor, choroidal dissection has been found after filtration. 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). Drops contain benzalkonium chloride, which may cause eye irritation. Benzalkonium chloride discolor soft contact lenses - before using the medicine, contact lenses should be removed and replaced again after at least 15 minutes.

Do not use during pregnancy. However, if the medicine is used until delivery, the condition of the newborn should be closely monitored during the first days of life, due to the risk of β-adrenergic blocking symptoms (bradycardia, hypotension, respiratory disorders, hypoglycaemia). There is no information on the excretion of dorzolamide in human milk; in animals, a reduction in body weight gain was observed in offspring. Β-blockers are excreted in breast milk. When timolol is used in therapeutic doses in the form of eye drops, it is unlikely that milk secretion of timolol will cause clinical signs of blocking β-adrenergic receptors in the child.

Very often: burning sensation and pinching in the eye, taste disturbances. Common: conjunctival injection, visual acuity, corneal erosion, itching in the eye, tearing, sinusitis. Uncommon: urolithiasis. Rare: symptoms of allergic reactions (including angioedema, urticaria, pruritus, rash, anaphylaxis, less frequent bronchospasm), shortness of breath, respiratory failure, rhinitis, contact dermatitis. Undesirable effects on individual components may be potential adverse events when using a combined preparation.timolol. Common: headache, eye irritation symptoms (eg burning sensation, pinching, itching, tearing, redness), blepharitis, keratitis, decreased corneal sensitivity, dry eyeball. Uncommon: dizziness, syncope, visual disturbances (including refractive changes, in some cases as a result of discontinuation of miocinatics), bradycardia, shortness of breath, nausea, indigestion, asthenia, fatigue. Rare: paresthesia, worsening of symptoms and occurrence of myasthenia gravis (myasthenia gravis), cerebrovascular episode, local hypoxia of the brain tissue, insomnia, nightmares, memory loss, eyelid droop, diplopia, choroidal detachment (after filtration procedures), tinnitus, chest pain, palpitations, edema, arrhythmias heart, congestive heart failure, atrioventricular block, cardiac arrest, hypotension, claudication, Raynaud's syndrome, cold hands and feet, bronchospasm (mainly in people with pre-existing bronchospasm), cough, diarrhea, dry mouth, alopecia, psoriasis-like rash or exacerbation of psoriasis, systemic lupus erythematosus, decreased sex drive, Peyronie's disease. Not known: systemic allergic reactions (including angioneurotic edema, urticaria, local and generalized rash, pruritus, anaphylactic reaction), hypoglycaemia, depression, corneal erosion, taste disorder, abdominal pain, vomiting, skin rash, 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, formation of scabs on the eyelids, transient myopia (receding after discontinuation of the drug), corneal edema, reduced intraocular pressure, choroidal detachment (after filtration procedures), epistaxis, throat irritation, dry mouth, rash.

1 drop into the conjunctival sac of the affected eye (eyes) 2 times a day. Occlusion of the naso-lacrimal duct or closure of the eyelids for 2 minutes reduces systemic absorption; this reduces the frequency of side effects and increases local effects. When using several topical ophthalmic medications, a gap of at least 10 minutes should be allowed between instillations of subsequent medications.