Treatment of increased intraocular pressure in patients with: ocular hypertension, open-angle glaucoma, pellicular glaucoma. In adjunctive therapy in combination with beta-blockers. Monotherapy in patients who do not respond to β-blockers, or when the use of β-blockers is contraindicated.
Composition:
1 ml of solution contains 20 mg of dorzolamide in the form of hydrochloride. The preparation contains benzalkonium chloride.
Action:
A strong carbonic anhydrase II inhibitor for topical administration. Inhibition of carbonic anhydrase in the ciliary processes of the eye reduces the amount of aqueous humor released. As a result, the intraocular pressure is reduced. After topical ocular administration, dorzolamide lowers elevated intraocular pressure, regardless of whether it is associated with glaucoma. After topical application, dorzolamide passes into the systemic circulation. The drug and its metabolite - N-deethyl-dorzolamide - accumulate in erythrocytes. Dorzolamide is moderately bound to plasma proteins (approximately 33%). It is excreted mainly in urine in unchanged form. Upon completion of the drug, the concentration of dorzolamide in the erythrocytes decreases non-linearly. Initially, the drug concentration rapidly decreases, followed by a slower elimination phase with T0,5 approximately 4 months
Contraindications:
Hypersensitivity to the active substance or any of the excipients. Severe renal failure (creatinine clearance <30 ml / min). Hyperglycemic acidosis.
Precautions:
Caution should be exercised in patients with hepatic impairment (no study). The treatment of patients with acute angle-closure glaucoma, besides administering antihypertensive medications, also requires other therapeutic interventions. The use of dorzolamide in patients with acute angle-closure glaucoma has not been studied. After administration of the preparation, the same side effects that occur after the general administration of sulfonamides, including serious side effects, may occur. If severe side effects or signs of hypersensitivity are found, the preparation should be discontinued. Treatment based on oral carbonic anhydrase inhibitors is associated with the risk of urolithiasis due to disturbances of the acid-base balance, especially in patients with a history of renal calculi. Patients with pre-existing kidney stones may be at higher risk of developing urolithiasis during treatment with dorzolamide. If an allergic reaction is observed (eg conjunctivitis or eyelid irritation), the need to stop treatment should be considered. There is a possibility of increased general action when using carbonic anhydrase inhibitors in patients receiving oral carbonic anhydrase and dorzolamide. The concomitant use of dorzolamide and oral carbonic anhydrase inhibitors is not recommended. Patients with previous chronic corneal injury and / or ophthalmic surgery at the eye have reported cases of corneal edema and irreversible corneal decomposition when dorzolamide eye drops are used. Caution should be exercised when administering dorzolamide topically to such patients. After filtration, with the use of agents that inhibit the production of aqueous humor, cases of choroidal dissection with simultaneous intraocular hypotension have been reported. The preparation contains benzalkonium chloride, which may cause eye irritation. Before taking the medicine, remove the contact lenses and wait at least 15 minutes before putting them on again. Benzalkonium chloride was not found to discolor soft contact lenses. The use of dorzolamide has not been studied in patients less than 36 weeks of gestational age and less than 1 week of age. Patients with significantly immature renal tubules should receive dorzolamide only after careful consideration of the risk-benefit balance due to the risk of metabolic acidosis.
Pregnancy and lactation:
Dorzolamide should not be used during pregnancy. Breastfeeding is not recommended if treatment with dorzolamide is needed.
Side effects:
Very often: burning and stinging in the eye. Common: headache, superficial punctate keratitis, tearing, conjunctivitis, blepharitis, pruritus of the eye, eyelid irritation, blurred vision, nausea, bitter taste in the mouth, asthenia / asthenia. Uncommon: inflammation of the iris and ciliary body. Rarely: dizziness, paresthesia, irritation (including redness) of the eye, eye pain, scabs on the eyelids, transient myopia (receding after discontinuation of therapy), corneal edema, reduction of intraocular pressure, choroidal dissection after surgical filtration, nosebleed, irritation throat, dry mouth, contact dermatitis, Steven-Johnson syndrome and toxic epidermal necrolysis, urolithiasis, hypersensitivity reactions (local reactions related to the eyelids and symptoms of generalized allergic reactions, eg angioedema, urticaria, pruritus, rash, shortness of breath) , rarely bronchospasm). In children, there was a burning sensation in the eye, congestion and eye pain; less frequently (<4%) swelling and occlusion of the cornea occurred. In very young patients, particularly with immature or impaired renal function, metabolic acidosis has been reported.
Dosage:
Monotherapy: 1 drop into the conjunctival sac of the affected eye (eyes) 3 times a day. In adjunctive therapy in combination with the β-blocker used for the eyes: 1 drop into the conjunctival sac of the affected eye (eyes) twice a day. In patients treated with another antiglaucoma drug, dorzolamide is introduced the Next day after discontinuing previous treatment. When using several topical ophthalmic medications, a minimum of 10 minutes should be allowed between the instillation of subsequent medications. Children: Limited data are available on the use of dorzolamide 3 times a day.