Kosopt eye drops 20mg ml + 5mg ml bottle
Condition: New product
1000 Items
Rating:
Be the first to write a review!
More info
Active ingredients
Dorzolamide + timolol
Release form
Drops
Composition
1 ml contains dorzolamide hydrochloride 22.26 mg, which corresponds to a content of dorzolamide base 20 mg, timolol maleate 6.83 mg, which corresponds to a content of timolol base 5 mg. Excipients: benzalkonium chloride (in the form of a 50% solution of benzalkonium chloride) - 0.075 mg (0.15 mg), sodium citrate - 2.94 mg, mannitol - 16 mg, gietelloza (hydroxyethylcellulose) - 4.75 mg, 1M sodium hydroxide solution - q.s. to pH 5.6, water d / and - q.s. to 1 ml.
Pharmacological effect
The antiglaucoma drug contains two active ingredients: dorzolamide hydrochloride and timolol maleate, 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 Kosopt leads to a more pronounced decrease in intraocular pressure. Dorzolamide hydrochloride is a selective type II carbonic anhydrase inhibitor. Inhibition of ciliary body carbonic anhydrase leads to a decrease in the secretion of intraocular fluid, presumably by reducing the formation of bicarbonate ions, which in turn leads to a slowdown in the transport of sodium and fluid. Timolola maleate is a non-selective beta-blocker. Although the exact mechanism of the action of timolol maleate in reducing intraocular pressure has not yet been established, a number of studies have shown a predominant decrease in the formation, as well as a slight increase in fluid outflow
Pharmacokinetics
Dorzolamide hydrochlorideDorzolamide, when applied topically, penetrates the systemic circulation. With prolonged use, dorzolamide accumulates in erythrocytes as a result of selective binding to type II carbonic anhydrase, maintaining extremely low concentrations of free drug in plasma. As a result of the metabolism of dorzolamide, a single N-desethyl metabolite is formed, which less clearly blocks type II carbonic anhydrase compared to the original substance, but at the same time inhibits type I carbonic anhydrase (a less active isoenzyme). The metabolite also accumulates in erythrocytes, where it binds mainly to type I carbonic anhydrase. About 33% of dorzolamide is bound to plasma proteins.Dorzolamide is excreted in the urine unchanged and as a metabolite. After stopping the use of the drug, dorzolamide is non-linearly washed out of red blood cells, which first leads to a rapid decrease in its concentration, and then elimination slows down. T1 / 2 is about 4 months. When receiving dorzolamide inside, in order to simulate the maximum systemic effects during its local application, an equilibrium state was achieved after 13 weeks. In addition, no free drug or its metabolites were actually detected in the plasma. Inhibition of erythrocyte carbonic anhydrase was insufficient to achieve a pharmacological effect on kidney function and respiration. Similar pharmacokinetic results were observed with long-term topical application of dorzolamide hydrochloride. However, in some elderly patients with renal insufficiency (creatinine clearance 30–60 ml / min), higher concentrations of the metabolite in erythrocytes were detected, but this did not have clinical significance. Timolol maleate With topical application of timolol maleate penetrates the systemic circulation. Plasma timolol concentration was studied in 6 patients with topical application of timolol maleate in the form of 0.5% eye drops 2 times / day. The average Cmax after morning use was 0.46 ng / ml, after applying during the day it was 0.35 ng / ml. The reduction in intraocular pressure occurs 20 minutes after instillation, reaches a maximum after 2 hours and lasts at least 24 hours.
Indications
For the treatment of elevated intraocular pressure in: open-angle glaucoma, pseudoexfoliative glaucoma
Contraindications
Bronchial asthma, history of bronchial asthma, severe COPD, sinus bradycardia, AV and II and III degree blockade, severe heart failure, cardiogenic shock, severe renal failure (CC <30 ml / min), dystrophic processes in the cornea; - pregnancy; - lactation period (breastfeeding); - children and adolescents under 18 years of age (due to lack of data on efficacy and safety); - hypersensitivity to the components of the drug.
Use during pregnancy and lactation
Contraindicated
Dosage and administration
Kosopt is prescribed 1 drop in the conjunctival sac of the affected eye (or both eyes) 2 times / day. If Kosopt is prescribed as a substitute for another ophthalmologic drug for the treatment of glaucoma, the latter should be canceled the day before Kosotherapy begins. other local ophthalmologic preparation, Kosopt should be appointed with an interval of not less than 10 min.
Side effects
Kosopt is generally well tolerated. In clinical studies of side effects, peculiar exclusively to this combination drug, was not observed. Adverse reactions were limited by the known side effects of dorzolamide hydrochloride and / or timolol maleate. In general, systemic side effects were mild and did not lead to discontinuation of the drug. In clinical studies, Kosopt was prescribed to 1035 patients. In about 2.4% of patients, the drug was discontinued due to local adverse reactions from the eye. Approximately 1.2% of patients had the drug canceled due to local adverse reactions such as hypersensitivity or allergy. The most common adverse effects were: burning sensation or itching in the eye, taste distortion, corneal erosion, conjunctival injection, blurred vision, tearing. The following are possible side effects of the components of the drug. Dorzolamide hydrochloride On the part of the organ of vision: inflammation of the eyelid, irritation and flaking of the eyelid, iridocyclitis, point keratitis, transient myopia (passing through After drug withdrawal. From the nervous system: headache, dizziness, paresthesias. Allergic reactions: angioedema, bronchospasm, urticaria, pruritus. Others: asthenia / fatigue, nasal bleeding, irritation of the pharynx, dry mouth, rash. Timolol male local application) On the part of the organ of vision: conjunctivitis, blepharitis, keratitis, reduced sensitivity of the cornea, dryness; visual disturbances, including changes in the refractive ability of the eye (in some cases due to the abolition of miotics), diplopia, ptosis. On the part of the cardiovascular system: tinnitus, arrhythmia, hypotension, syncope, cardiovascular disorders, rhythm disturbances, cardiac arrest , edema, lameness, paresthesia, Raynaud's phenomenon,lowering the temperature of the hands and feet. From the side of the respiratory system: bronchospasm (mainly in patients with previous broncho-obstructive pathology), cough. Dermatological reactions: alopecia, psoriasis-like rashes or exacerbation of psoriasis. Allergic reactions: anaphylaxis, angiouroedema, anaphylaxis; From the side of the central nervous system: dizziness; depression, insomnia, nightmares, memory loss, increase in symptoms of myasthenia. From the digestive system: diarrhea, dyspepsia, dry mouth. On the whole body: headache, asthenia, fatigue, chest pain, decreased libido, Peyronie's disease, systemic lupus erythematosus
Overdose
There are no data on accidental or deliberate overdose of Kosopt. Symptoms: cases of inadvertent overdose of eye drops containing timolol maleate are described, with the development of systemic effects of beta-adrenergic blockers taken orally: dizziness, headache, shortness of breath, bradycardia, bronchospasm, and cardiac arrest. symptoms of dorzolamide overdose are electrolyte imbalance, the development of acidosis, possible side effects from the CNS. Treatment: symptomatic th and maintenance therapy. The level of electrolytes (primarily sodium) and the pH of the blood plasma should be monitored. Studies have also shown that timolol is not removed during dialysis.
Interaction with other drugs
Specific studies of the interaction of the drug Kosopt with other drugs have not been carried out. However, there is a possibility of enhancing the hypotensive effect and / or severe bradycardia with the combined use of timolol maleate eye drops and systemic calcium channel blockers, catecholamine-depleting agents, β-blockers, antiarrhythmic agents (including amiodarone), digitalis glycosides, parasympathomimetics, opioid analgesics and MAO inhibitors. Potentiated effect of systemic block beta-adrenoreceptor dyes (for example, a decrease in heart rate, depression) have been reported with the combined use of timolol and CYP2D6 inhibitors (for example, quinidine or selective serotonin reuptake inhibitors). Consequently,the possibility of such interaction should be taken into account in patients receiving Kosopt. Despite the fact that when Kosotherapy monotherapy is used, the effect on the pupil is minimal or absent, there are few descriptions of the development of mydriasis when co-administration of timolol maleate and adrenaline exists. combined use of local and systemic carbonic anhydrase inhibitors. Since data on the use of such a combination are not available, the combined use of Kosopt and systemic inhibitors, carbonic anhydrase is not recommended
special instructions
49% of patients in clinical studies were aged 65 years and older, 13% of patients aged 75 years and older. There were no differences in the efficacy and safety of the drug in these age groups compared with younger patients. However, one should not exclude the possibility of a higher sensitivity to the drug in some elderly patients. The active substances of the drug Kosopt can be absorbed into the systemic circulation. Timolol, which is part of the preparation, is a beta-blocker, thus adverse reactions, known for the systemic use of beta-blockers, may be noted when the preparation is used topically, including exacerbation of vasospastic angina pectoris (Prinzmetal stenocardia), disturbances of the peripheral and central blood circulation, arterial hypotension. Adequate control of heart failure is necessary before starting treatment Kosopt. Patients with a history of severe heart disease and signs of heart failure should be carefully monitored, they should be monitored for heart rate in such patients. When the first signs or symptoms of heart failure appear, use of Kosopt should be stopped. Deaths due to bronchospasm in patients with bronchial asthma have been reported and heart failure on the background of the use of eye drops containing timolol maleate. No studies have been conducted on the use of Kosopt in patients in hepatic insufficiency, and therefore the drug in these patients should be used with caution. The use of systemic carbonic anhydrase inhibitors can lead to a violation of KCHR and accompanied by urolithiasis, especially in patients with urolithiasis in history. During the use of Kosopt such violations were not observed, reports of urolithiasis were rare. SinceKosopta contains a carbonic anhydrase inhibitor, which, when applied topically, can be absorbed and enter the systemic circulation, the history of urolithiasis in patients with urolithiasis and an increase in the history of Kosopt can increase. or hypoglycemia. Beta-blockers can smooth the course of hyperthyroidism. Discontinuation of beta-blockers may cause deterioration. In the case of an upcoming surgery under general anesthesia, it is necessary to cancel the drug 48 hours before the operation, because timolol enhances the action of muscle relaxants and general anesthetics. The composition of Kosopt includes benzalkonium chloride preservative, which can cause eye irritation. Lenses should be removed before instillation of the drug and wait at least 15 minutes after instillation before putting them on again. Benzalkonium chloride can discolour soft contact lenses. Effects on the ability to drive vehicles and control mechanisms. When using Kosopt, side effects may occur that in some patients may make it difficult to drive or work with complex mechanisms.