Dorzolamide (Dorzolamidum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Ophthalmic products

Enzymes and antiferments

Included in the formulation
  • Glaucopt
    drops d / eye 
    Rowecq Limited     United Kingdom
  • Dorzolamide-native
    drops d / eye 
    NATIVA, LLC     Russia
  • Dorzolamide-SOLOfarm
    drops d / eye 
    GROTEKS, LLC     Russia
  • Dorzopt
    drops d / eye 
    K.O. Ромфарм Компани С.Р.Л.     Romania
  • Trusopt®
    drops d / eye 
    Santen, AO     Finland
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    ONLS

    VED

    АТХ:

    S.01.E.C.03   Dorzolamide

    Pharmacodynamics:

    An antiglaucoma agent, an inhibitor of carbonic anhydrase. Inhibition of carbonic anhydrase in the ciliary body helps to reduce the formation of HCO ions3- with the subsequent slowing down of the transfer of sodium and liquid, which leads to a decrease in the secretion of the intraocular fluid.

    Pharmacokinetics:

    With topical application dorzolamide penetrates into the systemic circulation. At course use due to selective binding with carbonic anhydrase II accumulates in erythrocytes. At the same time, very low concentrations of unchanged active substance are determined in the blood plasma. Dorzolamide is metabolized to form a single N-desethylated metabolite, which also accumulates in red blood cells.

    The binding of dorzolamide with plasma proteins is about 33%.

    It is excreted mainly with urine in the form of unchanged substance and metabolite.

    After the end of dorzolamide administration, the process of elution from erythrocytes has a nonlinear character: first a rapid decrease in the concentration of the active substance takes place, then the elimination slows down, and the half-life is 4 months.

    Indications:For topical application in ophthalmology: increased intraocular pressure, open-angle glaucoma (including secondary glaucoma), pseudoexfoliation glaucoma.
    ICD-10

    VII.H40-H42.H40.5   Glaucoma secondary due to other eye diseases

    VII.H40-H42.H40.4   Glaucoma secondary due to inflammatory disease of the eye

    VII.H40-H42.H40.3   Glaucoma secondary posttraumatic

    VII.H40-H42.H40.1   Primary open angle glaucoma

    VII.H40-H42.H40.0   Suspicion of glaucoma

    Contraindications:

    Chronic renal failure (creatinine clearance less than 30 ml / min), hyperchloremic acidosis, pregnancy, lactation (breastfeeding), children and adolescents under 18 years old, simultaneous oral intake of inhibitors of carbonic anhydrase, hypersensitivity to dorzolamide.

    Carefully:

    Use with caution for violations of liver function.

    Caution is used in patients with diabetes mellitus, liver failure, with diseases of the cornea,after antiglaucomatous operations (risk of eye hypotension, retinal detachment).

    Pregnancy and lactation:

    Recommendations FDA category C. The drug is contraindicated in pregnancy and during breastfeeding.

    Dosing and Administration:

    1 drop in the affected eye 2-3 times a day; in combination with β-adrenoblockers for topical administration - 1 drop 2 times a day.

    Side effects:

    Local reactions: burning, crawling, itchy eyes, watery eyes, blurred vision, irritation and swelling of the eyelids, conjunctivitis, superficial punctate keratitis, blepharitis, photophobia; rarely - iridocyclitis, increasing the thickness of the cornea, allergic reactions, hypotension eye, retinal detachment in patients after antiglaukomatoznyh operations.

    Systemic reactions: bitterness in the mouth, nausea, headache, fatigue, nefrourolitiaz, malignant erythema multiforme (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), agranulocytosis, aplastic anemia, skin rashes.

    Overdose:

    The following symptoms may occur: electrolyte imbalance, acidosis, disorders of the nervous system.

    Treatment: symptomatic, monitoring the level of electrolytes (especially potassium) in the blood and monitoring the pH of the blood.

    Interaction:

    Antiglaucoma drugs (beta-blockers, pilocarpine, dipyvephrine, carbachole) enhance the effect of dorzolamide.

    With simultaneous use with acetazolamide, the risk of systemic side effects increases.

    It is possible to increase toxicity when taking acetylsalicylic acid in high doses.

    Special instructions:

    Because the dorzolamide can cause dizziness and nausea, during the treatment should be avoided potentially dangerous activities associated with the need for concentration and increased speed of psychomotor reactions.

    Instructions
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