Brinzolamide (Brinzolamidum)

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

Ophthalmic products

Included in the formulation
  • Asopt®
    drops d / eye 
    Novartis Pharma AG     Switzerland
  • Brinzopt
    drops d / eye 
    K.O. Ромфарм Компани С.Р.Л.     Romania
    • АТХ:

    S.01.E.C   Inhibitors of carbonic anhydrase

    S.01.E.C.04   Brinzolamide

    Pharmacodynamics:

    The inhibitor of carbonic anhydrase II in the ciliary body, reduces the production of aqueous humor by slowing the formation of bicarbonate ions, followed by a decrease in the transport of sodium and liquid. Reduces intraocular pressure. When topical application enters the systemic circulation. With long-term use, it accumulates in erythrocytes due to its connection with carbonic anhydrase II. Metabolite N-dizetil also accumulates in erythrocytes, but due to the connection with carbonic anhydrase I.

    Pharmacokinetics:

    It is subject to systemic absorption. Due to its connection with carbonic anhydrase II, it accumulates in erythrocytes for a long time. Concentration in plasma with constant intake is less than 10 ng / ml. Metabolized to form N-desethyl Brinzolamide, N-demethoxypropyl, O-desmethyl. N-desethyl is accumulated due to a bond with carbonic anhydrase I. The connection with plasma proteins is 60%. Half-life is 111 days. It is excreted by the kidneys mainly unchanged.

    Indications:

    Increased intraocular pressure in ocular hypertension or open-angle glaucoma.

    ICD-10

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

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

    Contraindications:

    Individual intolerance to the components of the drug; Pkidney failure (creatinine clearance more than 30 ml per minute); breast-feeding.

    Carefully:

    Hepatic insufficiency, pregnancy, age under 18 years (efficacy and safety of use not established).

    Pregnancy and lactation:

    Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) - C. Studies in humans were not conducted. When used in rats and rabbits, a teratogenic effect is found. Before using the drug, it is necessary to assess the relationship between risk and benefit.

    It is recommended to stop breastfeeding in children whose mothers take the drug.

    Dosing and Administration:

    The instillation- 1 drop in the conjunctival sac of the affected eye 2 times a day. Other ophthalmic agents may be used at intervals of 10-15 minutes.

    Side effects:

    The central nervous system and sensory organs: blepharitis, keratitis, hyperemia, pain, separated from the eyes, sensation of foreign body, allergic reactions from the eyes, conjunctivitis,keratoconjunctivitis, keratopathy, double vision, burning or discomfort after instillation, dry eyes, transient blurred vision (after instillation), as well as headache and anxiety.

    Other: increased blood pressure, lower back pain, taste change, rhinitis, pharyngitis.

    Allergies: dermatitis, hives.

    Alopecia or focal hair loss.

    Overdose:

    When an overdose is noted electrolyte imbalance, acidosis, violations of the central nervous system. Symptomatic treatment is required.

    Interaction:

    It is possible to enhance the systemic effects associated with the inhibition of carbonic anhydrase, while using the means at the same time.

    Special instructions:

    Care should be taken when driving vehicles and working with machinery, as against the background of the use of the drug, a temporary deterioration view.

    Before using the drug, you need to remove contact lenses and wear them 15-20 minutes after instillation.

    Instructions
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