Dorzopt Plus (Dorzopt Plus)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceDorzolamide + TimololDorzolamide + Timolol
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  • Dorzopt Plus
    drops d / eye 
    ROMFARMA, OOO     Russia
  • Kosopt
    drops d / eye 
    Santen, AO     Finland
    • Dosage form: & nbspeye drops
    Composition:

    In 1 ml of the drug contains:

    active substances: dorzolamide hydrochloride (22.26 mg) in terms of dorzolamide 20 mg, timolol maleate (6.84 mg) in terms of timolol 5 mg;

    Excipients: hyetylose 1.0 mg, citric acid monohydrate 4.0 mg, 1 M sodium hydroxide solution 0.066 ml, mannitol 20.0 mg, benzalkonium chloride 0.075 mg, 1 M sodium hydroxide solution / 1 M hydrochloric acid solution to pH 5.6 ± 0.1, water purified to 1 ml.

    Description:Transparent, colorless or almost colorless, slightly viscous solution.
    Pharmacotherapeutic group:antiglaucoma
    ATX: & nbsp

    S.01.E.X   Other antiglaucoma drugs

    Pharmacodynamics:

    The antiglaucoma preparation contains two active components: dorzolamide and timolol, each of which reduces the increased intraocular pressure by decreasing the secretion of the aqueous humor. Joint action of these substances in the combined preparation Dorzopt Plus leads to a more pronounced decrease in intraocular pressure.

    Dorzolamide - selective inhibitor of carbonic anhydrase type II.Inhibition of the carbonic anhydrase of the ciliary body leads to a decrease in the secretion of the aqueous humor, presumably due to a decrease in the formation bicarbonate ions, which in turn leads to a slowdown in the transport of sodium and intraocular fluid.

    Timolol non-selective beta-blocker. Although the exact mechanism of action of timolol in reducing intraocular pressure has not yet been established, a number of studies have shown a predominant decrease in the formation of intraocular fluid, as well as a slight increase in its outflow.

    Decrease in intraocular pressure occurs 20 minutes after instillation, reaches a maximum after 2 hours and lasts at least 24 hours.

    Pharmacokinetics:

    Dorzolamide

    It penetrates the eye mainly through the cornea (to a lesser extent through the sclera or limbus). Systemic absorption is low. After entering the blood quickly penetrates into the red blood cells containing a significant amount of carbonic anhydrase II. The connection with plasma proteins is 33%. It is transformed into N-Desetylated metabolite, less active with respect to carbonic anhydrase II, but capable of blocking carbonic anhydrase I.With prolonged use cumulates in red blood cells. It is excreted by the kidneys in the unmodified form and in the form of metabolites. After withdrawal, the fast phase of withdrawal is replaced by a slow one, caused by the gradual release of dorzolamide from erythrocytes, with a half-life (T1/2) about 4 months.

    Timolol

    When topical, timolol penetrates the systemic circulation. The concentration of timolol in plasma was studied in 6 patients with topical administration of timolol in the form of 0.5% eye drops 2 times / day. The mean maximum concentration (CmOh ) after morning use was 0.46 ng / ml, after application in the afternoon - 0.35 ng / ml.

    Indications:

    Increased intraocular pressure with:

    - open-angle glaucoma;

    - pseudoexfoliation glaucoma.

    Contraindications:Bronchial asthma (including in the anamnesis); severe chronic obstructive pulmonary disease (COPD); sinus bradycardia; AV-blockade II and III degree; severe heart failure; cardiogenic shock; renal failure of severe degree (creatine kinase (CC) less than 30 ml / min); dystrophic processes in the cornea; pregnancy; lactation (breastfeeding); children and adolescence up to 18 years (t.efficiency and safety are not well understood); hypersensitivity to the components of the drug.
    Carefully:

    Hepatic insufficiency, advanced age, diabetes mellitus.

    Pregnancy and lactation:The drug Dorzopt Plus is contraindicated in pregnancy and during lactation (breastfeeding).
    Dosing and Administration:

    Bury 1 drop in the conjunctival sac 2 times a day.

    If several local ophthalmic drugs (LS) are used in the treatment, the administration of drugs should occur at an interval of 10 minutes.

    The duration of treatment is determined by the physician depending on the clinical the patient's condition.

    Side effects:

    Dorzolamide

    From the side of the organ of vision: inflammation of the eyelids, lacrimation, irritation and peeling of the eyelid, iridocyclitis, spot keratitis, transient myopia (passing after drug discontinuation).

    From the central nervous system (CNS) and the peripheral nervous system: headache, asthenia / fatigue, paresthesia.

    Allergic reactions: angioedema, bronchospasm, urticaria, itching.

    Other: nosebleeds, irritation of the pharynx, dry mouth, rash.

    Timolol

    From the side of the organ of vision: conjunctivitis, blepharitis, keratitis, decreased corneal sensitivity, dry eye syndrome; visual disturbances, including changes in the refractive power of the eye (in some cases because of the cancellation of miotics), diplopia, ptosis.

    From the side of the central nervous system and peripheral nervous system: ringing in the ears of paresthesia, headache, asthenia, fatigue, dizziness; depression, insomnia, nightmares, memory loss, increased myasthenia symptoms.

    From the cardiovascular system: arrhythmia, lowering blood pressure, fainting, rhythm disturbances, cardiac arrest, swelling, Raynaud's syndrome, lowering the temperature of the hands and feet.

    From the respiratory system: bronchospasm (mainly in patients with previous bronchial obstructive pathology), cough, chest pain.

    Dermatological reactions: alopecia, psoriasis-like rash or exacerbation of psoriasis.

    Allergic reactions: anaphylaxis, angioedema, urticaria, localized or generalized rash.

    From the digestive system: diarrhea, dyspepsia, dry mouth.

    Other: decreased libido, Peyronie's disease, systemic lupus erythematosus (SLE).

    Overdose:

    Symptoms unintentional overdose of timolol in the form of eye drops with the development of systemic effects of beta-adrenoblocker overdose for systemic application: dizziness, headache, dyspnea, bradycardia, bronchospasm, cardiac arrest.

    The most anticipated symptoms of an overdose of dorzolamide are a violation of the electrolyte balance, the development of acidosis, headache, asthenia / fatigue, paresthesia.

    Treatment: conduct symptomatic and supportive therapy. It is necessary to control the concentration of electrolytes (primarily sodium) and the pH of the blood plasma. In studies it is also shown that timolol not output during dialysis.

    Interaction:

    There were no studies of Dorsopt Plus interaction with other drugs.

    Nevertheless, it is possible to intensify the hypotensive effect and / or develop a pronounced bradycardia when the ophthalmic solution of timolol is used together with the blockers of the "slow" calcium channels, sympatholytics, beta-blockers, antiarrhythmics (including amiodarone), cardiac glycosides, parasympathomimetics, opioid analgesics and monoamine oxidase inhibitors.

    With the simultaneous use of timolol and isoenzyme inhibitors CYP2D6 (e.g., quinidine or selective inhibitors of inverse, serotonin uptake) has been reported on the potentiated effect of systemic beta-adrenergic blockade (eg, reduction in heart rate, depression).

    Despite the fact that the Dorsopt Plus inhibitor of carbonic anhydrase dorzolamide It is used locally, it can penetrate into the systemic bloodstream. In clinical studies of the use of an ophthalmic solution of dorzolamide, acid-base balance disorders were not detected. Nevertheless, with systemic use of carbonic anhydrase inhibitors, these disorders are known, and in some cases they can affect the interaction with other drugs (for example, enhance toxic reactions when using salicylates in high doses). There is a possibility of enhancing the known systemic effects of inhibiting carbonic anhydrase in the combined use of local and systemic inhibitors of carbonic anhydrase. Since there is no data on the use of such a combination, the combined use of Dorzopt Plus and systemic inhibitors of carbonic anhydrase is not recommended.

    Special instructions:

    Before using Dorsopt Plus, you need to ensure adequate control of the cardiovascular system. Patients with a history of severe cardiac disease and signs of heart failure should be closely monitored.

    Dorzopt Plus contains a preservative benzalkonium chloride, Which can precipitate in soft contact lenses and have a damaging effect on the eye tissue. Therefore, patients wearing soft contact lenses should be removed before applying drops and set back no earlier than 20 minutes after instillation.

    Caution is prescribed to patients with diabetes mellitus, since beta-blockers may mask the symptoms of acute hypoglycemia.

    Before a planned surgical procedure, you should gradually cancel the drug 48 hours before the general anesthesia, since beta-blockers increase the effect of muscle relaxants and means for general anesthesia.

    Effect on the ability to drive transp. cf. and fur:During the period of treatment it is necessary to refrain from driving motor vehicles and practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
    Form release / dosage:Eye drops, 20 mg / ml + 5 mg / ml.
    Packaging:

    To 5 ml of solution in a white or transparent polymer bottle-dropper closed with a polymer lid with a safety ring.

    One bottle-dropper along with instructions for use in a cardboard pack.

    Storage conditions:

    In a dry, the dark place at a temperature of no higher than 25 ° C.

    Out of reach of children
    Shelf life:

    2 years. After opening the bottle, drops should be used within 4 weeks.

    Do not use after the expiration date indicated on the package.

    Terms of leave from pharmacies:On prescription
    Registration number:LP-000580
    Date of registration:08.09.2011
    Date of cancellation:2016-09-08
    The owner of the registration certificate:ROMFARMA, OOO ROMFARMA, OOO Russia
    Manufacturer: & nbsp
    Representation: & nbspРомфарма ОООРомфарма ООО
    Information update date: & nbsp20.01.2016
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