Dorzolamide

Chemical name

4-(Этиламино)-5,6-дигидр��-6-метил-4Н-тиено[2,3-b]ти опиран-2- sulfonamid 7,7-dioksid (in the form of monogidrohlorida)

Gross

C10-H16-N2-O4-S3

Characteristics

White or no white crystalline powder, soluble in water and trudnorastvorimy in methanol and ethanol; Solution pH about 5.6.

Of drugs

The drugs-protivoglaucomnoe. Suppress activity izoenzima II carboangidraza (catalyzes obratimuu hydration reaction of carbon dioxide and dehydration coal acid) in the body ciliarnom eye. Decreases secretion vnutriglazna moisture (50%), education slows alkaline ions, and partly reducyruet transport of sodium and Voda.pronicaet inside the eye through rogovitsu (mostly), skler or limb. Partly absorbed by mucous membranes in the eyes of systemic vascular track (perhaps the emergence effects typical of sulfonamidov, including dioreticski). After getting stuck in the blood rapidly penetrate cells containing large numbers carboangidraza II. Stereoselekteven Cl. Linking plasma protein is about 33%. Transformed into N-dezetilirovanny metabolite less active against carboangidraza II, but can block carboangidrazou I. The plasma dorzolamid and its metabolites in the minimum concentrations. Excreted mainly kidneys, unedited, and partly in the form of metabolites. Following the rapid phase out slowly rotates due to the gradual release of drugs from the cells in T_1/2 about 4 months. In the long regular use accumulate in erythrocytes as a result of bonding with carboangidrazoy Ii.maximalny gipotenzivny effect is manifested through the two hours after instillation and maintained 12 hours Prolonged use reduces the risk of eye damage and nerve narrow fields of view. Impact inner pressure on the 9-21% at zacapawanyi twice a day, and 14-24% at 3-kratna instillation. Make it in a 2% solution of 4,5-6,1 mm Hg 3% solution less effective than 2% faster away from kongungualna cavity, as a matter of intense slezotechenie. When combined with a timololom within eight days has expressed additivoe effect in the 13-21%. Is drug of choice in cases where protivopokazana beta-adrenoblokatora as well as rejecting lexredstv, sujiwath position.

Indications

Increased inner pressure ofthalmogipertenzii, primary and secondary (incl. псевдоэксфолиативной ) open-glaucome.

Contraindications

Гиперчувствительност ь (including from other sulfon- and sulfanilamidam), the functions of the kidneys and liver, severe renal insufficiency (Cl creatinine 30 ml / min or less), pregnancy, breast-feeding (treatment must be accompanied by cessation of breastfeeding), children's age.

Side-Effects

Local : slezotechenie, pain, a sense of discomfort, pokalawania and itching in the eyes, irritation century fog of view refers, conjunctivitis, keratit, blefarit, iridotsyklit, increase in the thickness of cornea. System : bitterness in the mouth, nausea, headache, increased fatigability, nefrourolitiaz, syndrome Stevens-Johnson, toxic It'sa nekroliz, agranulozitos, aplastic anaemia, etc. discrazii of blood, skin irritation.

Patient interaction

Potenziruet effect antiglaucomnah other drugs. Socetannoe appointment inhibitors carboangidraza inside increases the risk of systemic side effects.

Overdosing

Symptoms : violation elektrolitnogo balance KHS (acidosis), Zns.lechenie disorder : symptoms.

Precautions

In old age may increase sensitivity to dorzolamidu (to be low dose). During the period of treatment not wearing contact lenses. Гиперчувствительност ь can be and after reassignment sulfonamidov, regardless of how they are received by the body, so if previously appointed interior sulfonamidnye drugs, it is necessary to have in mind the possibility of raising. In developing conjunctivitis should stop treatment.

Dosing and Administration

Kongungualno 1 drop three times a day in combination with бета-адреноблокатора��и on the one drop twice a day, 10 minutes after putting beta-adrenoblokator.

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