Косопт

General characteristics. Structure:

Active ingredients: 22,26 mg of a dorzolamid of a hydrochloride (equivalent of 20 mg of a dorzolamid), 6,83 mg of Timololum of a maleate (equivalent of 5 mg of Timololum).

Excipients: a benzalkoniya chloride (in the form of 50% of solution a chloride benzalkoniya), sodium citrate, Mannitolum, a gietelloza (hydroxyethylcellulose), 1M hydroxide sodium solution - q.s. to pH 5.6, water for and.

Pharmacological properties:

Pharmacodynamics. Protivoglaukomny drug of the combined structure. Contains two active components: the dorzolamida a hydrochloride and Timololum a maleate, each of which reduces the increased intraocular pressure due to decrease in secretion of intraocular liquid. Combined action of these substances as a part of drug leads to more expressed decrease in intraocular pressure.

Dorzolamida a hydrochloride is the selection inhibitor of a karboangidraza of the II type. The inhibition of a karboangidraza of a ciliary body leads to decrease in secretion of intraocular liquid, presumably due to reduction of formation of bicarbonate ions that in turn leads to delay of transport of sodium and liquid.

Timololum the maleate is non-selective beta adrenoblocker. Though the exact mechanism of action of Timololum of a maleate in decrease in intraocular pressure is still not installed, a number of researches showed preferential decrease in education, and also insignificant strengthening of outflow of liquid.

Pharmacokinetics. Dorzolamida hydrochloride. At topical administration дорзоламид gets into a system blood stream. At prolonged use дорзоламид collects in erythrocytes as a result of the selection linkng with karboangidrazy Iitipa, maintaining extremely low concentration of free drug in plasma. As a result of metabolism of a dorzolamid the only N is formed - the desetilny metabolite which it is less expressed blocks a karboangidraza of the II type in comparison with its initial form, however at the same time inhibits a karboangidraza of the I type - less active isoenzyme. The metabolite also collects in erythrocytes where communicates mainly with karboangidrazy the I type.
About 33% of a dorzolamid contact proteins of a blood plasma. Dorzolamid is brought with urine in not changed look and in the form of a metabolite. After drug phase-out дорзоламид it is not linearly washed away from erythrocytes that at first leads to bystry decrease in its concentration, and then elimination is slowed down. T1/2 makes about 4 months.

At reception of a dorzolamid inside, for the purpose of modeling of the maximum system influence during its topical administration, a stable state it was succeeded to reach in 13 weeks. At the same time in plasma free drug or its metabolites actually was not revealed. The inhibition of a karboangidraza of erythrocytes was insufficient to reach pharmacological effect on function of kidneys and breath. Similar pharmacokinetic results were observed at prolonged topical administration of a dorzolamid of a hydrochloride. Nevertheless, at some elderly patients with a renal failure (clearance of creatinine of 30-60 ml/min.) higher concentration of a metabolite in erythrocytes were revealed, however it had no clinical value.

Timololum maleate. At topical administration of Timololum the maleate gets into a system blood stream. Concentration of Timololum in plasma was studied at 6 patients at topical administration of eye drops of Timololum of a maleate of 0,5% twice a day. Average peak concentration after a morning dosage made 0,46 ng/ml, after a day dosage - 0,35 ng/ml. The hypotensive effect occurs in 20 minutes after instillation, reaches a maximum in 2 hours and not less than 24 hours proceed.

Indications to use:

Косопт it is used for treatment of povychenny intraocular pressure at an open angle glaucoma and at prsevdoeksfoliativny glaucoma at insufficient efficiency of monotherapy.

Route of administration and doses:

Косопт appoint on 1 drop in a conjunctival sac of the affected eye (or both eyes) 2 times/days. If Kosopt appoint as replacement of other ophthalmologic drug for treatment of glaucoma, the last should be cancelled a day before the beginning of therapy by Kosopt.

In case of sharing with other local ophthalmologic drug, Kosopt it is necessary to appoint with an interval not less than 10 min.

Rules of use of drug. Косопт represents sterile solution therefore patients have to be instructed as it is correct to use a bottle.

1. Before the first use of drug it is necessary to make sure that the protective strip outside of a bottle is not damaged. Not opened bottles can have a gap between a bottle and a cap.

2. It is necessary to remove a protective strip to open a cap.

3. To open a bottle, it is necessary to turn off a cap, turning it in the direction of pointers on an upper surface of a cap.

4. To incline the head back and to slightly delay a lower eyelid for emergence of space down between a century and an eye.

5. To turn a bottle, a big or index finger slightly to press in the place which is specially designated on a bottle so that one drop got into an eye. It is impossible to concern the surface of an eye or a century a bottle tip. At misuse, the bottle can be infected and become the reason of serious infectious injuries of an eye and the subsequent loss of sight.

6. To repeat points 4 and 5 for other eye if it is necessary.

7. To close a bottle a cap, having twirled it before dense contact with a bottle. It is not necessary to press a cover too strongly, otherwise it is possible to damage a bottle or a cover.

8. It is not necessary to increase an opening of specially developed dozatorny tip.

Features of use:

49% of patients in clinical trials were at the age of 65 years and are more senior, 13% of patients - at the age of 75 years and are more senior. The difference in efficiency and safety of drug in these age groups in comparison with younger patients was not. Nevertheless, it is not necessary to exclude possibilities of higher sensitivity to drug at some elderly patients.

Active agents of drug of Kosopt can be absorbed in a system blood stream. Timololum which is a part of drug is beta adrenoblocker, thus the side reactions known at system use of beta adrenoblockers can be noted at topical administration of drug, including an exacerbation of vasospastic stenocardia (Printsmetal's stenocardia), disturbances of peripheric and central circulation, arterial hypotension.

Adequate control of heart failure before an initiation of treatment by Kosopt is necessary. Patients with heavy pathology of heart in the anamnesis and symptoms of heart failure have to be under careful observation, it is necessary to watch ChSS at such patients.

At emergence of the first signs or symptoms of heart failure Kosopt's use should be stopped.

Messages on death as a result of a bronchospasm at patients with bronchial asthma and heart failure against the background of use of the eye drops containing Timololum a maleate are registered.

Researches of use of Kosopt for patients with a liver failure in this connection drug at such patients should be used with care were not conducted.

Use of system inhibitors of a karboangidraza can lead to disturbance of KShchR and be followed by an urolithiasis, especially at patients with an urolithiasis in the anamnesis. During Kosopt's use similar disturbances were not observed, messages on an urolithiasis were rare. Since karboangidraza inhibitor which at topical administration can be absorbed and get into a system blood stream, risk of development of an urolithiasis in patients with an urolithiasis in the anamnesis is Kosopt's part can raise at treatment by Kosopt.

Therapy by beta adrenoblockers can distort some symptoms of a hypoglycemia at patients with a diabetes mellitus or a hypoglycemia.

Beta adrenoblockers can smooth a current of a hyperthyroidism. The termination of reception of beta adrenoblockers can be the cause of an aggravation of symptoms.

In case of the forthcoming operative measure under the general anesthesia, it is necessary to cancel drug for 48 h before operation since Timololum strengthens action of muscle relaxants and the general anesthetics.

Preservative a benzalkoniya chloride which can be an origin of irritation of an eye is Kosopt's part. Lenses should be taken out before an instillation of drug and to wait within not less than 15 min. after an instillation before again to put on them. Benzalkoniya chloride is capable to decolour soft contact lenses.

Influence on ability to driving of motor transport and to control of mechanisms. At Kosopt's use development of side effects which at some patients can complicate driving or work with difficult mechanisms is possible.

At renal failures. Contraindication: renal failure of heavy degree (KK <30 ml/min.).

At abnormal liver functions. Researches of use of Kosopt for patients with a liver failure in this connection drug at such patients should be used with care were not conducted.

Use at advanced age. 49% of patients in clinical trials were at the age of 65 years and are more senior, 13% of patients - at the age of 75 years and are more senior. The difference in efficiency and safety of drug in these age groups in comparison with younger patients was not. Nevertheless, it is not necessary to exclude possibilities of higher sensitivity to drug at some elderly patients.

Use at children's age. It is contraindicated at children's and teenage age up to 18 years.

Side effects:

Косопт in general it is well transferred. In clinical trials of the side effects inherent it is exclusive to this combined drug, it was not observed. Side reactions were limited to already known side effects of a dorzolamid of a hydrochloride and/or Timololum of a maleate. In general system side effects were poorly expressed and did not lead to drug withdrawal.

In clinical trials of Kosopt it was appointed to 1035 patients. About 2.4% of patients drug was cancelled in connection with local side reactions from an eye. About 1.2% of patients drug was cancelled because of local side reactions as hypersensitivity or an allergy.

Side effects from an organ of sight were most often observed: burning sensation or an itch in an eye, distortion of taste, an erosion of a cornea, conjunctiva injection, a sight illegibility, dacryagogue.

Possible side effects of components of drug are included below.

Dorzolamida hydrochloride. From an organ of sight: an inflammation of a century, irritation and a peeling of a century, an iridocyclitis, a dot keratitis, the tranzitorny myopia (passing after drug withdrawal).

From a nervous system: headache, dizziness, paresthesias.

Allergic reactions: Quincke's disease, bronchospasm, small tortoiseshell, itch.

Others: adynamy/fatigue, nasal bleeding, irritation of a throat, dryness in a mouth, rash.

Timololum maleate (topical administration). From an organ of sight: conjunctivitis, blepharitis, keratitis, decrease in sensitivity of a cornea, dryness; the visual disturbances including changes of a refractivity of an eye (in some cases because of cancellation of miotik), a diplopia, a ptosis.

From cardiovascular system: a ring in ears, arrhythmia, hypotension, a faint, cardiovascular disturbances, disturbances of a rhythm, a cardiac standstill, hypostases, lameness, paresthesias, Reynaud's phenomenon, decrease in temperature of hands and legs.

From respiratory system: a bronchospasm (it is preferential at patients with the previous bronkhoobstruktivny pathology), cough.

Dermatological reactions: alopecia, psoriazopodobny rashes or exacerbation of psoriasis.

Allergic reactions: anaphylaxis, Quincke's disease, small tortoiseshell, local or generalized rashes.

From TsNS: dizziness; depression, sleeplessness, dreadful dreams, decrease in memory, increase of symptoms of a myasthenia.

From the alimentary system: diarrhea, dyspepsia, dryness in a mouth.

From an organism in general: headache, adynamy, fatigue, stethalgia, decrease in a libido, Peyroni's disease, system lupus erythematosus.

Interaction with other medicines:

Specific researches of interaction of drug of Kosopt with other medicines were not conducted.

Nevertheless, there is a possibility of strengthening of hypotensive effect and/or the expressed bradycardia at combined use of eye drops of Timololum of a maleate and system blockers of calcium channels, a catecholamine - the exhausting means, β-adrenoblockers, antiarrhytmic means (including Amiodaronum), glycosides of a foxglove, parasympathomimetics, opioid analgetics and MAO inhibitors.

The potentiated effect of system blockade of beta adrenoceptors (for example, reduction of ChSS, a depression) was reported when sharing Timololum and CYP2D6 inhibitors (for example, quinidine or selective serotonin reuptake inhibitors).

Thereof, the possibility of similar interaction needs to be taken into account at the patients receiving Kosopt.

In spite of the fact that at monotherapy by Kosopt the effect on a pupil is minimum or is absent, there are single descriptions of development of a mydriasis at combined use of Timololum of a maleate and adrenaline.

There is a probability of strengthening of the known system effects of inhibition of a karboangidraza at the combined use of local and system inhibitors of a karboangidraza. Since data on use of a similar combination are absent, combined use of Kosopt and system inhibitors, karboangidraza is not recommended.

Contraindications:

— bronchial asthma, bronchial asthma in the anamnesis, heavy HOBL;

— a sinus bradycardia, AV blockade of II and III degrees, the expressed heart failure, cardiogenic shock;

— renal failure of heavy degree (KK <30 ml/min.);

— dystrophic processes in a cornea;

— pregnancy;

— period of a lactation (breastfeeding);

— children's and teenage age up to 18 years (in connection with a lack of data on efficiency and safety);

— hypersensitivity to drug components.

Overdose:

Data on accidental or deliberate overdose of Kosopt are absent.

Symptoms: cases of unintentional overdose of the eye drops containing Timololum a maleate with development of system effects of overdose of the beta adrenoblockers accepted inside are described: dizziness, headache, short wind, bradycardia, bronchospasm, cardiac standstill.

The most expected symptoms of overdose of a dorzolamid are disturbance of electrolytic balance, development of acidosis, possible side effects from TsNS.

Treatment: carrying out a symptomatic and maintenance therapy. It is necessary to control the level of electrolytes (first of all sodium) and рН a blood plasma. In researches it is also shown that Timololum is not removed at dialysis.

Storage conditions:

Drug should be stored in protected from light, the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 2 years. After the first opening of a bottle it is not necessary to use drug more than 4 weeks.

Issue conditions:

According to the recipe

Packaging:

On 5 ml of solution in plastic bottles like Okumeter Plus. On 1 bottle in a cardboard pack.