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1 ml of drug of Kosopt includes 5 mg of Timololum and 20 mg of a dorzolamid.
Additional substances: sodium hydroxide solution, sodium citrate, chloride benzalkoniya, gietelloza, Mannitolum, water.
Transparent colourless liquid of slightly viscous consistence.
5 ml of liquid in a plastic bottle "Okumeter Plus ", 1 such bottle in a pack from a cardboard.
Pharmacodynamics and pharmacokinetics
Eye drops of Kosopt contain 2 operating components: the maleate of Timololum and a hydrochloride of a dorzolamid, each of which lowers the increased intraocular pressure as a result of reduction of release of intraocular liquid. Simultaneous effect of these substances as a part of means leads to stronger pressure decline in an eye.
The hydrochloride of a dorzolamid is a selective blocker of a karboangidraza of the second type. Oppression of a karboangidraza of fabrics of a ciliary body causes reduction of release of intraocular liquid as it is supposed, due to decrease in number of bicarbonate ions what provokes braking of transport of liquid and ions of sodium.
The maleate of Timololum is neizberatelny beta adrenoblocker. In spite of the fact that the mechanism of its action which consequence reduction of intraocular pressure is up to the end is not studied, a number of researches revealed decrease in education and strengthening of release of liquid.
Pharmacokinetics of a hydrochloride of a dorzolamid
At local use reaches a system blood-groove. At long use it is capable to collect in erythrocytes because of the selection reaction with karboangidrazy the second type, maintaining very low concentration of untied drug in plasma. After transformation the only metabolite of N – desetilny type which oppresses to a karboangidraz of the second type in comparison with its initial form more poorly is formed, but at the same time oppresses less active karboangidraza of the first type. The specified metabolite also collects in red blood cells where communicates generally with karboangidrazy the first type.
About a third of a dose contacts blood proteins. It is evacuated with urine in an original form and in the form of derivative. Time of semi-removal makes about 4 months.
Timololum maleate pharmacokinetics
When using locally Timololum maleate easily reaches a system blood-groove. The hypotensive effect is registered 20 minutes later after an instillation, reaches the maximum force 2 hours later and not less days last.
Indications to use
The increased intraocular pressure at pseudo-exfoliative and open-angle forms of glaucoma.
- sinus bradycardia, dekompensirovanny heart failure, AV blockade 2-3 degrees, cardiogenic shock;
- bronchial asthma (including in the anamnesis), a severe form of a chronic obstructive pulmonary disease;
- the expressed renal failure;
- pregnancy and lactation;
- dystrophic processes in cornea fabrics;
- hypersensitivity to medicine components;
- age less than 18 years.
In general drug is well transferred, and system side reactions (at their emergence) are expressed poorly and do not demand drug withdrawal. Most often side effects from an eye came to light: distortion of sense of taste, a burning sensation and an itch in the place of an instillation, injection of a conjunctiva, a cornea erosion, dacryagogue, a sight illegibility.
At conduct of clinical trials at 2,4% of patients of Kosopt it was cancelled because of by-effects from an eye. At 1,2% of patients medicine was cancelled in connection with development of an allergy.
Side effects after use of a hydrochloride of a dorzolamid
- Reactions from an eye: dot keratitis, irritation of a century, iridocyclitis, inflammation of a century, tranzitorny myopia.
- Reactions from nervous activity: dizziness, paresthesias, headache.
- Allergic reactions: bronchospasm, Quincke's edema, itch, urticaria.
- Other reactions: nasal bleeding, an adynamy, dryness in a mouth, irritation of a throat, rash.
Side effects after use of a maleate of Timololum
- Reactions from an eye: keratitis, conjunctivitis, reduction of sensitivity of a cornea, blepharitis, dryness, deterioration in sight, ptosis, diplopia.
- Reactions from blood circulation: cordial disturbances, arrhythmia, a ring in ears, a syncope, disturbances of a rhythm, hypotension, Reynaud's phenomenon, hypostases, a cardiac standstill, paresthesias, lameness, fall of temperature of extremities.
- Reactions from breath: cough, bronchospasm.
- Dermatological reactions: psoriazopodobny rashes, alopecia, exacerbation of psoriasis.
- Allergic reactions: a Quincke's edema, an anaphylaxis, urticaria, rashes on a body.
- Reactions from nervous activity: depression, dizziness, dreadful dreams, sleeplessness, increase of a myasthenia, decrease in memory.
- Reactions from digestion: dyspepsia, diarrhea, dryness in a mouth.
- General reactions: Peyroni's illness, adynamy, headache, fatigue, decrease libido, stethalgia, system lupus erythematosus.
Kosopt, application instruction (Way and dosage)
Drug is appointed to dig in on 1 drop for an eyelid of the affected eye (or an eye) twice a day.
If Kosopt use as replacement of other ophthalmologic means for therapy of glaucoma, then the last needs to be cancelled in one day prior to treatment by Kosopt.
In case of simultaneous use with other ophthalmologic drug of topical administration, Kosopt dig in with an interval of 10 minutes.
Rules of use of drug
Kosopt is a sterile solution therefore patients have to be informed on following instructions for use by a bottle:
- before the first use it is necessary to make sure that the safety strip which is outside of a bottle is kept; at not opened bottles the gap between a cap and a body of a bottle is possible;
- the protective strip should be removed for simplification of opening of a cap;
- the cap is turned off, turning it towards the pointers located from above a cap;
- the head needs to be inclined back and it is a little shifted a lower eyelid for an exposure mucous eyes;
- then in the designated place slightly squeeze the turned bottle that 1 drop got into a conjunctival sac;
- it is forbidden to concern tissues of an eye or a century a bottle dropper as at the same time the bottle is capable to be infected and in an effect to become the reason of infectious complications of an eye and the subsequent deterioration in sight;
- the bottle is closed a cap, it is dense it having twirled (at the same time it is not necessary to press too strongly a cover in order to avoid damage of a bottle);
- it is forbidden to increase an opening of a dozatorny tip.
Overdose signs: a bronchospasm, a headache, dizziness, bradycardia, short wind, a stop of cordial activity, development of acidosis, frustration of electrolytic balance, various reactions from a nervous system.
Overdose treatment: symptomatic and supporting, and also control of content of electrolytes and acidity of plasma. Timololum is not removed when carrying out a dialysis.
The probability of strengthening of hypotensive action and bradycardia at simultaneous use with system blockers of channels of calcium, β-adrenoblockers is not excluded, a catecholamine - the exhausting drugs, antiarrhytmic means, parasympathomimetics, foxglove glycosides, opioid analgetics and blockers of monoaminoxidase.
The effect of generalized blockade β - adrenoceptors (decrease in pulse rate, a depression) was registered at simultaneous use with CYP2D6 inhibitors (selective blockers of serotonin reuptake and other means).
At monotherapy by Kosopt the mydriasis is minimum, however cases of development of a mydriasis at a simultaneous instillation of Timololum and adrenaline are described.
There is a risk of strengthening of system effects of blocking of a karboangidraza at combined use of system and local inhibitors of enzyme of a karboangidraza therefore Kosopt's combination and system blockers of a karboangidraza is prohibited.
Terms of sale
According to the recipe.
To store in the dark at the room temperature. To protect from children. After opening of a bottle to use within 30 days.
Period of validity
The difference in efficiency of drug at young and elderly patients is absent, however it is not necessary to exclude detection of bigger sensitivity to Kosopt at some elderly patients.
Active components of Kosopt are capable to be soaked up in a system blood stream. As a result the side reactions arising at system reception of beta adrenoblockers can be noted even at local use of drug (including an exacerbation of stenocardia of Printsmetal, a circulatory disturbance, arterial hypotonia).
Control of a course of heart failure prior to therapy is recommended by drug. Patients with a serious illness of heart and signs of insufficiency of cordial activity have to be under continuous supervision.
At identification of the first symptoms of heart failure Kosopt's use should be stopped.
Messages on death as a result of a bronchospasm at the persons having heart failure and bronchial asthma against use of eye drops with Timololum in structure are registered.
At patients with insufficiency works of a liver Kosopt's use should be carried out with care.
Use of system blockers of a karboangidraza can provoke disturbance of acid-base balance and development of an urolithiasis, especially at persons with an urolithiasis.
Treatment by beta adrenoblockers is capable to distort a number of symptoms of a hypoglycemia at patients with a diabetes mellitus. Beta adrenoblockers can also smooth clinic of a hyperthyroidism, and the termination of their use can be the cause of an exacerbation of this disease.
In case of the planned operative measure with use of the general anesthesia, it is necessary to cancel Kosopt for the 48th hour prior to operation as Timololum strengthens effects of the general anesthetics and muscle relaxants.
Preservative chloride a benzalkoniya which can be the reason of irritation of an eye is a part of drops. Also this substance is capable to decolour contact lenses of soft type therefore before an instillation they need to be deleted.
At Kosopt's use emergence of side reactions which at a number of patients can complicate management of motor transport is possible.
Coincidence on the ATH code of the 4th level:
Kosopt's analogs: Dorzopt Plus, Dorzotimol, Mardoziya, Rozaky, Azarga, Ganfort.
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