Kosopt eye drops bottle 5ml

Dosage form

drops

Active ingredient

Eye drops in the form of a clear, colorless or almost colorless, slightly viscous liquid, contain: dorzolamide hydrochloride 226 mg, which corresponds to the content of dorzolamide 20 mg in 1 ml, Timolol maleate 683 mg, which corresponds to the content of timolol 5 mg in 1 ml.

Excipients: benzalkonium chloride, sodium citrate, mannitol, gietelloza (hydroxyethyl cellulose), sodium hydroxide, in d / and.

Packaging

5 ml - plastic bottles of the "Okumer plus" type (1) - packs cardboard.

Mechanism of action

Kosopt - 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 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 the outflow of fluid.

Indications and usage

For the treatment of increased intraocular pressure in:
- Open-angle glaucoma.
- Pseudoexfoliative glaucoma.

Contraindications

- Bronchial asthma (including a history).
- Severe COPD.
- Sinus bradycardia.
- AV blockade II and III degree.
- Severe heart failure.
- Cardiogenic shock.
- Renal failure severe (CK (creatinine clearance) less than 30 ml / min).
- Dystrophic processes in the cornea.
- Pregnancy.
- Lactation (breastfeeding).
- Children and adolescents up to 18 years (becauseefficiency and safety are not well understood).
- Hypersensitivity to the drug.

Pregnancy and Breastfeeding

The drug is contraindicated for use during pregnancy and lactation (breastfeeding).

Dosage and administration

The drug is prescribed 1 drop in the conjunctival sac of the affected eye (or in 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 abolished the day before the use of Kosopt. In case of combined use with other eye drops, Kosopt should be administered at intervals of at least 10 minutes. Kosopt is a sterile solution, so patients should be instructed how to properly use the bottle.

Instructions for use:
Before using the drug for the first time, make sure that the protective strip on the outside of the vial is intact. For unopened vials, there may be a gap between the bottle and the cap.
Remove the protective strip in order to open the cap.
To open the bottle, you must unscrew the cap, turning it in the direction of the directional arrows on the top surface of the cap.
Bend the head back and slightly pull the lower eyelid down to create space between the eyelid and the eye.
Flip the bottle, with a thumb or index finger, lightly press in a place marked on the bottle so that one drop falls into the eye. Do not touch the surface of the eye or eyelid with the tip of the bottle. If used improperly, the vial can become infected and cause serious infectious damage to the eye and subsequent loss of vision.
Repeat steps 4 and 5 for each eye, if the drug should be instilled into both eyes.
Close the bottle cap, twisting it until tight contact with the bottle. Do not press the cap too hard, otherwise the bottle or cap may be damaged.
Do not enlarge the opening of a specially designed metering tip.

Adverse reactions

The drug 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 already known side effects of dorzolamide hydrochloride and / or timolol maleate. In general, systemic side effects were mild and did not lead to drug withdrawal. In clinical studies Kosopt was prescribed to 1035 patients. In approximately 2.4% of patients, the drug was canceled due to local adverse reactions from the organ of vision. In approximately 1.2% of patients, the drug was canceled due to local adverse hypersensitivity reactions or allergies.

Among the most frequent side effects were a burning sensation or itching in the eye, taste distortion, corneal erosion, conjunctival injection, blurred vision, tearing.

The following adverse events were noted during the post-marketing observation period: dyspnea, respiratory failure, contact dermatitis, bradycardia, AV-blockade, choroidal detachment of the eye, nausea, described the development of edema and irreversible corneal destruction in patients with chronic corneal defects and / or undergoing intraocular surgery.

The following possible side effects of the drug components are known:

Special senses: eyelid inflammation, eyelid irritation and desquamation, iridocyclitis, punctate keratitis, transient myopia (passing after drug withdrawal).

Nervous system: headache, asthenia / fatigue, paresthesias.

Allergic reactions: angioedema, bronchospasm, urticaria, pruritus.

Other: epistaxis, pharyngeal irritation, dry mouth, rash.

Special senses: conjunctivitis, blepharitis, keratitis, decreased corneal sensitivity, dryness, visual disturbances, including changes in the refractive ability of the eye (in some cases due to the abolition of miotics), diplopia, ptosis.

Nervous system: paresthesia tinnitus, headache, asthenia, fatigue, dizziness, depression, insomnia, nightmares, memory loss, increased symptoms of myasthenia.

Cardiovascular: arrhythmia, hypotension, syncope, cardiovascular disorders, rhythm disturbances, cardiac arrest, edema, Raynaud's syndrome, a decrease in the temperature of the arms and legs.

Respiratory: bronchospasm (mainly in patients with previous broncho-obstructive pathology), cough, chest pain.

Dermatologic: alopecia, psoriasis-like rashes or exacerbation of psoriasis.

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

Gastrointestinal: diarrhea, dyspepsia, dry mouth.

Other: decreased libido, Peyronie's disease, SLE.

With systemic use:
Cardiovascular: pain in the extremities, decreased tolerance to physical exertion, AV-blockade 2 and 3 degrees, sinoauricular blockade, pulmonary edema, worsening of peripheral circulation disorders, worsening of angina, vasodilation.

Dermatologic: scabies, increased sweating, exfoliative dermatitis.

From the side of the central nervous system: dizziness, weakness, decreased concentration, increased drowsiness.

Other: vomiting, hyperglycemia, hypoglycemia, nonthrombocytopenic purpura, wheezing, arthralgia, impotence, urination disorders.

Clinically significant changes in the systemic application of timolol maleate were extremely rare. A slight increase in the amount of residual nitrogen, the content of potassium, uric acid and plasma triglycerides is described; a slight decrease in hemoglobin, hematocrit, cholesterol, HDL, however, these changes did not progress and were not clinically manifested.

The use of beta-blockers may cause exacerbation of pseudoparalytic myasthenia.

There have been no studies on the use of Kosopt in patients with liver failure, and therefore the drug in such patients should be used with caution.

In clinical studies of Kosopt, 49% of patients were 65 years old and older, 13% of patients were 75 years old 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. Like other ophthalmic drugs for local use, 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 topical application of the drug Kosopt, including exacerbation of vasospastic angina pectoris (Prinzmetal stenocardia), impaired peripheral and central blood circulation, arterial hypotension. Before starting the drug Kosopt necessary to ensure adequate control of heart failure. Patients with a history of severe heart disease and signs of heart failure should be carefully monitored (it is necessary to monitor the heart rate in these patients). There have been reports of death from bronchospasm in patients with asthma and heart failure with the use of eye drops containing timolol maleate. There have been no studies on the use of Kosopt in patients with liver failure, and therefore the drug in these patients should be used with caution. The use of systemic inhibitors of carbonic anhydrase can lead to a violation of CSF and is 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. The risk of urolithiasis in patients with urolithiasis in history can be increased with the use of Kosopt, since It contains a carbonic anhydrase inhibitor, which, when applied topically, can be absorbed and enter the systemic circulation. Therapy with beta-blockers may distort some of the symptoms of hypoglycemia in patients with diabetes or hypoglycemia. Beta-blockers can smooth the course of hyperthyroidism. Discontinuation of beta-blockers may cause deterioration. When the first signs or symptoms of heart failure appear, Kosopt should be discontinued. In case of an upcoming surgery using general anesthesia, it is necessary to cancel the drug 48 hours before the operation, since timolol enhances the action of muscle relaxants and general anesthetics. Kosopta contains benzalkonium chloride preservative, which can cause eye irritation.Contact lenses before instillation of the drug should be removed and installed again no earlier than 15 minutes after instillation. Benzalkoniya chloride can discolor soft contact lenses.

With the use of Kosopt possible the development of side effects that in some patients may hinder driving or work with complex mechanisms.

Specific studies of the interaction Kosopt with other drugs was not conducted. Nevertheless, it is possible to enhance the hypotensive effect and / or the development of bradycardia during concomitant use ophthalmic solution of timolol maleate and Calcium channel blockers, catecholamine-depleting agents, beta-blockers, antiarrhythmics (including amiodarone), digitalis glycosides, parasympathomimetics, opioid analgesics and MAO inhibitors.

With the combined use of timolol and inhibitors of CYP2D6 (for example, quinidine or selective serotonin reuptake inhibitors), the potentiated effect of systemic blockade of beta-adrenergic receptors (for example, a decrease in the frequency of heart rate, depression) has been reported.

Despite the fact that the doprolamide carbonic anhydrase inhibitor, which is part of Kosopta, is used topically, it can penetrate the systemic circulation. In clinical studies, the use of dorzolamide hydrochloride ophthalmic solution did not reveal any disorders of CSR. However, 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). The possibility of such an interaction must be considered in patients receiving Kosopt.

Systemic beta-blockers may enhance the hypoglycemic effect of antidiabetic drugs and hypertension, which is the effect of the withdrawal of clonidine (clonidine).

Despite the fact that with Kosotherapy monotherapy, the effect on the pupil is minimal or absent, there are isolated descriptions of the development of mydriasis with the combined use of timolol maleate and adrenaline.

There is a possibility of enhancing the known systemic effects of inhibition of carbonic anhydrase with the combined use of local and systemic inhibitors of carbonic anhydrase. Since data on the use of such a combination are not available, the combined use of Kosopt and systemic carbonic anhydrase inhibitors is not recommended.

There are no data on accidental or deliberate overdose of Kosopt.

Cases of unintentional overdose of timolol maleate in the form of eye drops with the development of systemic effects of beta-blockers for systemic use are described: dizziness, headache, shortness of breath, bradycardia, bronchospasm, cardiac arrest.

The most anticipated symptoms of dorzolamide overdose are electrolyte imbalance, the development of acidosis, and possible side effects from the central nervous system.

Treatment: Conduct symptomatic and supportive 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 eliminated during dialysis.

The drug should be stored out of the reach of children, protected from light at a temperature not higher than 25 ° C. After the first opening of the vial, Kosopt should not be used for longer than 4 weeks.

2 years.