$29.50
Manufacturer: Greece
Increased intraocular pressure in patients with open-angle glaucoma or pseudoexfoliative glaucoma, when local use of beta-blockers alone is insufficient.
Description
Dorzitim Composition
active ingredients: dorzolamide; timolol;
1 ml of solution contains 20 mg of dorzolamide in the form of 22.26 mg of dorzolamide hydrochloride and 5 mg of timolol in the form of 6.830 mg of timolol maleate;
Dorzitim excipients:
benzalkonium chloride, mannitol (E 421), sodium citrate dihydrate, 1 M sodium hydroxide solution, hydroxyethyl cellulose, water for injection.
Dorzitim Dosage form.
Eye drops, solution.
Basic physical and chemical properties: almost colorless, slightly viscous, opalescent solution.
Pharmacotherapeutic group. Means used in ophthalmology. Antiglaucoma drugs and miotics. Beta-adrenergic blockers. ATX code S01E D51.
Pharmacological properties
Pharmacodynamics.
The drug contains two active ingredients: dorzolamide hydrochloride and timolol maleate. Each of these components reduces increased intraocular pressure by reducing the secretion of intraocular fluid, but due to a different mechanism of action.
Dorzolamide hydrochloride is a potent type II carbonic anhydrase inhibitor. Inhibition of carbonic anhydrase of the miliary body leads to a decrease in the secretion of intraocular fluid by slowing down the formation of bicarbonate ions, which, in turn, leads to a decrease in the transport of sodium and fluid.
Timolol maleate is a non-selective beta-adrenergic receptor blocker. The exact mechanism of action of timolol, which manifests itself in a decrease in intraocular pressure, is still unknown. Fluorometric and tonographic studies indicate that the effect of timolol is due to a decrease in the secretion of humoral fluid. In addition, timolol can increase moisture drainage.
The combination of the actions of the two components leads to a more pronounced decrease in intraocular pressure than monotherapy with these drugs.
After topical application, Dorzitim reduces intraocular pressure, regardless of whether its increase is associated with glaucoma. Increased intraocular pressure plays a significant role in the pathogenesis of optic nerve damage and loss of visual fields in glaucoma.
Dorzitim reduces intraocular pressure without the development of side effects characteristic of miotics, such as night blindness, accommodation spasm, pupil constriction.
Pharmacokinetics.
Dorzolamide hydrochloride. When applied topically, dorzolamide enters the systemic circulation. With prolonged use, dorzolamide accumulates in erythrocytes as a result of binding to type II carbonic anhydrase, maintaining very low plasma concentrations of the free drug. Due to metabolism, dorzolamide forms a single N-desethyl metabolite, which blocks type II carbonic anhydrase less pronounced than its original form, but also inhibits type I carbonic anhydrase, a less active isoenzyme. The metabolite also accumulates in erythrocytes, where it binds mainly to type I carbonic anhydrase. Approximately 33% of dorzolamide binds to blood plasma proteins. Dorzolamide is excreted in the urine unchanged and as a metabolite. After discontinuation of the drug, dorzolamide is excreted nonlinearly from erythrocytes, characterized by an initial rapid decrease in concentration and a subsequent phase of slow elimination with a half-life of about 4 months.
Timolol maleate. After topical ophthalmic application, timolol is absorbed systemically. Systemic exposure of timolol was determined after topical application of an ophthalmic 0.5% solution 2 times a day. The maximum plasma concentration after the morning dose was 0.46 ng / ml, and after the evening dose was 0.35 ng / ml.
Clinical characteristics.
Indications
Increased intraocular pressure in patients with open-angle glaucoma or pseudoexfoliative glaucoma when topical use of beta-blockers alone is insufficient.
Contraindications
· Hypersensitivity to one or both active substances or to any of the auxiliary components of the drug; · Diseases of the respiratory tract, including bronchial asthma and severe chronic obstructive pulmonary disease; Sinus bradycardia, antrioventricular block II or III degree, severe heart failure, cardiogenic shock; Severe renal impairment (creatinine clearance less than 30 ml / min) or hyperchloremic acidosis; · The period of pregnancy and lactation, children’s age.
Interaction with other medicinal products and other types of interactions.
In the case of the concomitant use of other topical ophthalmic drugs, Dorzitim should be used at intervals of at least 10 minutes.
Special studies of the interaction of Dorzitim and other drugs have not been conducted. No interactions were observed with the simultaneous use of the drug Dorzitim and other groups of systemic drugs: ACE inhibitors, calcium channel blockers, diuretics, NSAIDs (including acetylsalicylic acid) and hormones (estrogens, insulin, thyroxine).
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