Treatment of elevated intraocular pressure in: ocular hypertension, open-angle glaucoma, pertussis glaucoma - in combination with β-blockers or monotherapy in patients not responding to β-blocker therapy or in patients in whom beta-blockers are 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 secretion of aqueous humor. As a result, the intraocular pressure is reduced. After topical administration, dorzolamide lowers the increased intraocular pressure, whether it is associated with glaucoma or not. After topical application, dorzolamide passes into the systemic circulation. During long-term use, it is deposited in the erythrocytes, as a result of selective binding to CA-II, while the extremely low concentration of free drug is maintained in the blood plasma. The parent form of the drug is metabolized to the sole N-deethyl derivative, which inhibits CA-II less than the parent compound, but also inhibits less active isoenzyme (CA-I). The metabolite also accumulates in erythrocytes, where it is mainly associated with CA-I. Dorzolamide is moderately bound to plasma proteins (in about 33%). It is excreted mainly in urine in unchanged form; the metabolite is also excreted in the urine followed by the phase of slower elimination with T0,5 about 4 months
Contraindications:
Hypersensitivity to the active substance or to any of the excipients. Severe renal failure (creatinine clearance <30 ml / min). Hyperlloric acidosis.
Precautions:
Caution should be exercised in patients with hepatic impairment (no study). The management of patients with acute angle-closure glaucoma requires additional therapeutic interventions in addition to use of ophthalmic hypotensive agents - the use of dorzolamide in patients with this diagnosis has not been studied. After topical administration of dorzolamide, there is a risk of side effects typical of sulfonamides. Dorzolamide is a sulphonamide and is absorbed systemically, although it is administered topically - side effects typical of sulfonamides may occur after topical administration. If severe symptoms of hypersensitivity develop, discontinue use. Patients with kidney stones in the past are at increased risk of urolithiasis during treatment. If allergic reactions occur (eg conjunctivitis or eyelid irritation) discontinuation of treatment should be considered. Co-administration of dorzolamide and oral carbonic anhydrase inhibitors is not recommended. Cases of corneal edema and irreversible corneal damage have been reported when dorzolamide is used in patients diagnosed with chronic corneal disorder and / or previous intraocular surgery - caution should be used in these patients. Cases of choroidal dissection with concomitant intraocular hypotonia after filtration with administration of agents that inhibit the production of aqueous humor have been reported. The preparation contains benzalkonium chloride, which may cause eye irritation and changes the color of soft contact lenses - avoid contact with soft contact lenses. Remove the contact lenses before giving the drops and replace them again after 15 minutes. Dorzolamide was not studied in preterm infants below 36 weeks of gestational age or in children less than 1 week of age. Patients with significant renal tubular immature should receive dorzolamide after careful consideration of the benefit / risk ratio, due to the possible risk of metabolic acidosis.
Pregnancy and lactation:
Do not use during pregnancy and during breastfeeding.
Side effects:
Very often: burning and stinging in the eye.Common: headache, superficial punctate keratitis, conjunctivitis, tearing, blurred vision, blepharitis, pruritus of the eye, eyelid irritation, nausea, bitter taste in the mouth, asthenia / fatigue. Uncommon: inflammation of the iris and ciliary body. Rarely: dizziness, paresthesia, corneal edema, choroidal detachment after filtration, intraocular hypotension, irritation (including redness) of the eye, eye pain, eyelid gluing, transient myopia (disappearing after cessation of therapy), nose bleed, throat irritation, dryness in the mouth, urolithiasis, contact dermatitis, hypersensitivity (systemic allergic reactions, including angioneurotic edema, urticaria and pruritus, rash, shortness of breath, rare bronchospasm and signs of local reactions within the eyelids). In children: burning and stinging in the eye, congestion and eye pain; less frequently (<4%) there was swelling and corneal opacity. In very young children, metabolic acidosis has been reported especially with immature or impaired renal function.
Dosage:
Monotherapy: 1 drop into the conjunctival sac of the affected eye (eyes) 3 times a day. In combination with the β-blocker used for the eye: 1 drop into the conjunctival sac of the affected eye (eyes), twice a day. When the preparation is to be used instead of another ophthalmic medicine used for the eye, discontinue using the other medicine after taking all doses on a given day and start using the product the Next day. If the patient uses more than one topical ophthalmic drug, each of the medicines should be administered separately, with a minimum of 10 minutes. break.