Dorzopt Plus eye drops 20 mg + 5 mg 1 ml dropper bottle 5 ml
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Active ingredients
Dorzolamide
Release form
Drops
Composition
1 ml contains: dorzolamide hydrochloride 22.26 mg, which corresponds to the content of dorzolamide 20 mg, timolol maleate 6.84 mg, which corresponds to the content of timolol 5 mg. Additional substances: hyethyllose - 1 mg, citric acid monohydrate - 4 mg, sodium hydroxide solution 1M - 0.066 ml, mannitol - 20 mg, benzalkonium chloride - 0.075 mg, sodium hydroxide solution 1M / acid hydrochloric solution 1M - to pH 5.6 ± 0.1, purified water - up to 1 ml.
Pharmacological effect
Antiglaucoma drug contains two active ingredients: dorzolamide and timolol, each of which reduces the increased intraocular pressure by reducing the secretion of intraocular fluid. The combined effect of these substances in the composition of the combined drug Dorzopt Plus leads to a more pronounced decrease in intraocular pressure. Dorzolamide Selective type II carbonic anhydrase inhibitor. Inhibition of ciliary body carbonic anhydrase leads to a decrease in the secretion of intraocular fluid, presumably due to a decrease in the formation of bicarbonate ions, which in turn leads to a slowdown in the transport of sodium and intraocular fluid. Timolol Non-selective beta-adrenergic blocker. Although the exact mechanism of the action of timolol in reducing intraocular pressure has not yet been established, a number of studies have shown a predominant reduction in the formation of intraocular fluid, as well as a slight increase in its outflow. The intraocular pressure decreases 20 minutes after instillation, reaches a maximum after 2 hours and lasts no less 24 h
Pharmacokinetics
Dorzolamide Penetrates into the eye mainly through the cornea (to a lesser extent through the sclera or limb). Systemic absorption is low. After entering the blood, it penetrates rapidly into red blood cells containing a significant amount of carbonic anhydrase II. Communication with plasma proteins - 33%. It is transformed into an N-dezetilirovanny metabolite, less active in relation to carbonic anhydrase II, but capable of blocking a significant amount of carbonic anhydrase II. Communication with plasma proteins -33%. It is transformed into an N-dezetilirovanny metabolite, less active in relation to carbonic anhydrase II, but capable of blocking carbonic anhydrase I.With prolonged use cumulates in erythrocytes. It is excreted by the kidneys in unchanged form and in the form of metabolites. After the abolition of the rapid phase of elimination is replaced by a slow, due to the gradual release of dorzolamide from erythrocytes, with a half-life (T1 / 2) of about 4 months. Timolol When topically administered, timolol penetrates the systemic circulation. Plasma timolol concentration was studied in 6 patients with topical application of timolol in the form of 0.5% eye drops 2 times / day. The average maximum concentration (Cmax) after morning use was 0.46 ng / ml, after applying during the day it was 0.35 ng / ml.
Indications
Increased intraocular pressure with: Open-angle glaucoma. Pseudo-excoliative glaucoma.
Contraindications
Bronchial asthma, incl. in history. Severe chronic obstructive pulmonary disease. Sinus bradycardia. AV-block II and III degree. Severe heart failure. Cardiogenic shock. Hypersensitivity to any component of the drug. Chronic renal failure (creatinine clearance less than 30 ml / min). Degenerative effects in the cornea.
Precautionary measures
Before using Dorzopt Plus, it is necessary to ensure adequate monitoring of the cardiovascular system. Patients with a history of severe heart disease and signs of heart failure should be carefully monitored. Dorzopt Plus contains the preservative benzalkonium chloride, which can be deposited in soft contact lenses and have a damaging effect on the eye tissue. Therefore, patients who wear soft contact lenses should remove them before using drops and install them back no earlier than 20 minutes after instillation. Patients with diabetes are prescribed with caution, because beta-blockers can mask the symptoms of acute hypoglycemia. Before a planned surgical operation the drug should be gradually discontinued 48 hours before general anesthesia, since beta-blockers enhance the action of muscle relaxants and agents for general anesthesia. The effect on the ability to drive av otransporta and management mechanisms In the period of treatment should refrain from driving motor vehicles and activities potentially hazardous activities that require high concentration and speed of psychomotor reactions
Use during pregnancy and lactation
The drug Dorzopt Plus is contraindicated for use during pregnancy and lactation (breastfeeding)
Dosage and administration
Instill 1 drop in the conjunctival sac 2 times a day. The duration of treatment is determined by the doctor depending on the patient’s clinical condition. If several local ophthalmic drugs are used in the treatment, they should be administered at 10-minute intervals.
Side effects
Dorzolamide On the part of the organ of vision: inflammation of the eyelid, lacrimation, irritation and desquamation of the eyelid, iridocyclitis, point keratitis, transient myopia (passing after drug withdrawal). From the central nervous system (CNS) and peripheral nervous system: headache, asthenia / fatigue, paresthesias. Allergic reactions: angioedema, bronchospasm, urticaria, pruritus. Others: nosebleeds, pharynx irritation, dry mouth, rash. Timolol On the part of the organ of vision: conjunctivitis, blepharitis, keratitis, decreased sensitivity of the cornea, dry eye syndrome; visual disturbances, including changes in the refractive ability of the eye (in some cases due to the abolition of miotics), diplopia, ptosis. On the side of the central nervous system and the peripheral nervous system: tinnitus, headache, asthenia, fatigue, tincture; depression, insomnia, nightmares, memory loss, increase in symptoms of myasthenia. On the part of the cardiovascular system: arrhythmia, lowering blood pressure, fainting, rhythm disturbances, cardiac arrest, edema, Raynaud's syndrome, lowering the temperature of the arms and legs. On the part of the respiratory system : bronchospasm (mainly in patients with previous broncho-obstructive pathology), cough, chest pain. Dermatological reactions: alopecia, psoriasis-like rash or exacerbation of psoriasis. Allergic reactions: anaphylaxis, angioneuro matic edema, urticaria, local or generalized syp.So the digestive system: diarrhea, dyspepsia, dry rtu.Prochie: reduced libido, Peyronie's disease, systemic lupus erythematosus (SLE).
Overdose
Symptoms of unintentional overdose of timolol in the form of eye drops with the development of systemic effects of beta-adrenergic blockers for systemic use: dizziness, headache, shortness of breath, bradycardia, bronchospasm, cardiac arrest. The most expected symptoms of dorzolamide overdose are an electrolyte imbalance, heart failure. asthenia / fatigue, paresthesia. Treatment: carry out symptomatic and supportive therapy.Control of the level of electrolytes (especially K +) and the level of blood pH. In studies it was also shown that timolol is not eliminated during dialysis
Interaction with other drugs
Combination with antiglaucoma drugs (β-blockers, Pilocarpine, Dipivefrin, Carbachol) causes an increase in the effect of Dorzolamide. With Acetazolamide, the risk of systemic side effects increases. With high doses of Acetylsalicylic acid, the toxicity is likely to increase
special instructions
Dorsopt Plus, like other ophthalmic preparations for local use, can penetrate into the systemic circulation. Since timolol is a beta-blocker in the drug, adverse reactions that develop with systemic use of beta-blockers can be observed when Dorzopt Plus is used topically. Reactions from the cardiovascular and respiratory systems Before starting the use of Dorzopt Plus, it is necessary to ensure adequate control cardiovascular conditions. Patients with a history of cardiovascular disease, including heart failure, should be carefully monitored. following observation of signs of worsening of these diseases (heart rate and blood pressure control). There have been reports of cases of heart failure with a fatal outcome with timolol in the form of eye drops. When the first signs or symptoms of heart failure appear, Dorzopt Plus should be stopped. Patients with I degree heart block, beta-blockers should be prescribed with caution because of their ability to slow impulse conduction. There have been reports of cases of bronchospasm with a fatal outcome in patients with asthma while using timolol in the form of eye drops. In patients with mild to moderate COPD, Dorzopt Plus should be used with caution and only if the perceived benefit of treatment outweighs the potential risk. The drug should be used with caution in patients with severe peripheral circulatory disorders (severe forms of the disease or Raynaud's syndrome) .Diabetes mellitus The drug should be used with caution in patients with spontaneous hypoglycemia or in patients with diabetes mellitus (especially with a labile course) while using insulin or oral hypoglycemic drugs, since beta-blockers may mask some of the symptoms of hypoglycemia. Hyperthyroidism Beta-blockers may mask some clinical hyperthyroidism (for example, tachycardia). If hyperthyroidism is suspected, patients should be closely monitored. It is necessary to avoid abrupt withdrawal of beta-blockers due to the risk of a thyrotoxic crisis. Anesthesia in Surgery The need to cancel beta-blockers in the event of an impending extensive surgical intervention has not been proven. The effects of beta-adrenergic blockers during surgery can be eliminated, if necessary, by applying sufficient doses of adrenomimetics. Liver dysfunction Study of the use of Dorsopt Plus in patients with hepatic insufficiency was not performed, so the drug in these patients should be used with caution. Allergy and hypersensitivity reactions Like other ophthalmic drugs for local use, the drug Dorzopt Plus can penetrate into the systemic circulation. Dorzolamide is a sulfanilamide. Adverse reactions identified with the systemic use of sulfonamides may be observed when the drug is applied topically (Stevens-Johnson syndrome and toxic epidermal necrolysis). If there are signs of serious hypersensitivity reactions, the drug should be stopped. When treating beta-adrenergic blockers in patients with atopy or severe anaphylactic reactions to various allergens in the history, the response may be enhanced if they re-contact with these allergens. In this group of patients, the use of epinephrine in the standard therapeutic dose for the relief of allergic reactions may be ineffective. Concomitant Therapy When using Dorsopt Plus in patients taking systemic beta-blockers, it is necessary to take into account the possible mutual enhancement of the pharmacological action of the drugs, both with respect to the known systemic effects of beta-blockers, and with respect to the reduction of intraocular pressure.The combined use of the drug Dorzopt Plus with other beta-blockers is not recommended. Termination of therapyIf the need to cancel the topical application of timolol, as in the case of withdrawal of systemic beta-blockers, termination of therapy in patients with IHD should be carried out gradually. Corneal abnormalities Beta-blockers used in ophthalmology can cause dry eye mucosa. In patients with corneal disorders, the drug should be used with caution. Patients with a low number of endothelial cells have an increased risk of corneal edema. Urolithiasis The use of systemic carbonic anhydrase inhibitors can disrupt acid-base balance and can be accompanied by urolithiasis, especially in patients with urolithiasis in history. when applied topically, it can be absorbed and enter the systemic circulation, therefore the risk of urolithiasis in patients with urolithiasis A history of drug treatment with Dorzopt Plus may increase. The use in elderly patients In clinical studies, the difference in efficacy and safety of the dorzolamide + timolol combination in patients over 65 years of age compared with younger patients has not been identified. However, one should not exclude the possibility of a higher sensitivity to the drug in some elderly patients. The use of contact lenses Dorzopt Plus contains the preservative benzalkonium chloride, which can be a cause of eye irritation. Therefore, patients before using the drug should remove soft contact lenses and install them back no earlier than 15 minutes after instillation of the drug. Benzalkonium chloride can discolor soft contact lenses. Effect on the ability to drive vehicles and mechanismsDuring the use of the drug Dorzopt Plus, it is necessary to refrain from driving vehicles and mechanisms and practicing potentially hazardous activities that require high concentration of attention and quickness of psychomotor reactions