Asopt® (Azopt®)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceBrinzolamideBrinzolamide
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  • Asopt®
    drops d / eye 
    Novartis Pharma AG     Switzerland
  • Brinzopt
    drops d / eye 
    K.O. Ромфарм Компани С.Р.Л.     Romania
    • Dosage form: & nbspeye drops
    Composition:
    Per 1 ml of the preparation:
    Active substance: Brenzolamide 10.0 mg
    Excipients: benzalkonium chloride solution, equivalent to benzalkonium chloride 0.1 mg; disodium edetate 0.1 mg; sodium chloride 2.5 mg; tyloxapol 0.25 mg; mannitol 33.0 mg; carbomer (974P) 4.0 mg; sodium hydroxide and / or hydrochloric acid concentrated to pH adjustment; water purified to 1.0 ml.
    Description:

    Homogeneous suspension of white or almost white color.

    Pharmacotherapeutic group:Antiglaucoma preparation, inhibitor of carbonic anhydrase
    ATX: & nbsp

    S.01.E.C   Inhibitors of carbonic anhydrase

    S.01.E.C.04   Brinzolamide

    Pharmacodynamics:

    Brinzolamide is an inhibitor of carbonic anhydrase II. Due to inhibition of carbonic anhydrase II, the formation of bicarbonate ions slows down, followed by a decrease in the transport of sodium and liquid, which leads to a decrease in the production of intraocular fluid in the ciliary body of the eye. As a result, there is a decrease in intraocular pressure (IOP).

    Pharmacokinetics:

    With topical application brenzolamide penetrates into the systemic circulation. Brinzolamide Adsorbed in erythrocytes as a result of selective binding.There is a metabolite - N-desethyl Brinzolamide, which also binds to carbonic anhydrase and accumulates in erythrocytes. In the presence of brinzolamide, the metabolite binds mainly to carbonic anhydrase I.

    In plasma, the concentrations of Brinzolamide and its metabolite are below the limit of quantification (<10 ng / ml). The half-life is 111 days. Binding to plasma proteins is about 60%.

    Brinzolamide is excreted in the main with urine unchanged. The main metabolite (N-de-ethylbenzenamide) and low concentrations of other metabolites (N- desmethoxypropyl and O-desmethyl) are also found in the urine.

    Indications:

    Decreased elevated intraocular pressure at open-angle glaucoma; ocular hypertension.

    Contraindications:

    Individual hypersensitivity to the components of the drug;

    Because Azopt® and its metabolites are excreted mainly by the kidneys, it is not recommended to be prescribed to patients with severe impairment of renal function (creatinine clearance <30 mL / min).

    Carefully:

    The use of the drug has not been studied in patients with closed-angle glaucoma.

    The use of the drug has not been studied in patients with severe liver disease, so such patients should be prescribed with caution.

    Sensitization of the body with sulfonamides can develop if the drug is administered repeatedly in violation of the instructions for its use. If serious adverse reactions or signs of hypersensitivity occur, the drug should be discontinued.

    Pregnancy and lactation:

    Adequate and well-controlled studies in pregnant women were not conducted. It is possible to use the drug to treat pregnant women as prescribed by the treating doctor if the expected curative effect exceeds the risk of developing potential side effects to the fetus.

    Breastfeeding should be interrupted when using the drug.

    Pediatric Use

    It is not recommended to use in childhood, since at the moment the safety and effectiveness of the drug for children are not established.

    Dosing and Administration:

    Locally. Vial before use shake.

    Instilled 1 drop into the conjunctival sac twice a day.

    Side effects:

    In 5-10% of cases; blurred vision, a bitter, sour or unusual taste in

    In 1-5% of cases: blepharitis, dermatitis, dry eye, foreign body sensation, headache, conjunctival hyperemia, discharge from the eyes, discomfort in the eyes, keratitis, pain and itching in the eyes, rhinitis.

    Less than 1% of cases: local reactions - conjunctivitis, keratoconjunctivitis, diplopia, keratopathy, lacrimation, asthenopia, crust on the edges of the eyelids; systemic reactions - dizziness, hypertension, dyspnea, chest pain, dry mouth, dyspepsia, nausea, diarrhea, back pain, pharyngitis, alopecia, allergic reactions, urticaria.

    Asopt® is a sulfonamide. As with local administration, the drug is systemically absorbed, side reactions, characteristic of sulfonamides, may occur. Rarely, but there may be deaths caused by severe reactions to sulfanilamides, including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatonecrosis, agranulocytosis, aplastic anemia and other hematopoiesis.

    Overdose:

    There is no information about symptoms of overdose in topical application.

    When taking the drug orally, electrolyte imbalance, the development of the acidosis state, and disorders of the nervous system may occur. It is necessary to control the level of electrolytes (especially potassium) and the pH of the blood.

    Interaction:

    It is not recommended simultaneous use with oral inhibitors of carbonic anhydrase, since there is a possibility of increasing systemic adverse reactions.

    Salicylates in high doses increase the risk of systemic side effects.

    If necessary, it can be used in combination with other local ophthalmic preparations. In this case, the interval between their use should be at least 10 minutes.

    Special instructions:

    Vial before use shake.

    The bottle must be closed after each use.

    Do not touch the tip of the pipette with any surfaces.

    The drug contains a preservative benzalkonium chloride, which can be absorbed by contact lenses. Before using the drug, the lens should be removed and installed back no earlier than 15-20 minutes after instillation of the drug.

    Effect on the ability to drive transp. cf. and fur:If the patient is temporarily reduced visually after using the drug, it is not recommended to drive the car and engage in activities that require increased attention and response before recovery.
    Form release / dosage:

    Eye drops 1%.

    Packaging:

    5 ml per bottle-dropper "Droptainer ™" from low density polyethylene.

    1 bottle with instructions for use in a cardboard box.

    Storage conditions:Store at 4-30 ° C.

    Keep out of the reach of children.

    Shelf life:

    2 years.

    Use within 4 weeks after opening the vial.

    Do not use after the expiry date printed on the package!

    Terms of leave from pharmacies:On prescription
    Registration number:П N013601 / 01
    Date of registration:06.11.2007
    The owner of the registration certificate:Novartis Pharma AGNovartis Pharma AG Switzerland
    Manufacturer: & nbsp
    Representation: & nbspNOVARTIS PHARMA LLCNOVARTIS PHARMA LLC
    Information update date: & nbsp22.06.2017
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