For the treatment of diseases associated with a permanent or temporary increase in pressure inside the eyeball, leading to a decrease in visual acuity and atrophy of the corresponding nerve, the drug "Cosopt" is used. Analogs with a similar effect may be an alternative to this tool.
Description
The drug is available in the form of eye drops as a combined anti-glaucoma medication designed to reduce intraocular pressure by reducing the secretion of fluid in the body.
Being complex in formulation, Kosopt drops contain two active ingredients. One of them, dorzolamide hydrochloride, is present in an amount of 22.26 mg per 1 ml, which is equivalent to 20 mg of dorzolamide base. The second active component is timolol maleate in an amount of 6.83 mg per 1 ml, which equates to 5 mg of timolol base. To create a stable solution, additional substances are used that ensure the storage of the drug during the stated storage period. These include: 50% benzalkonium chloride solution, sodium citrate, mannitol, hydroxyethyl cellulose, sodium hydroxide solution, distilled water for injection.
The drug "Cosopt", eye drops, is a transparent, colorless or almost colorless, slightly viscous liquid. Available in 5 ml plastic bottles.
Mechanism of action
The antiglaucoma effect is based on the action of two active components: dorzolamide hydrochloride and timolol maleate. Each of them reduces the secretion of intraocular fluid, which leads to normalization of increased intraocular pressure. And the instruction characterizes the result of their joint action as part of the Cosopt preparation (eye drops) as a more pronounced decrease in this parameter.
The effect of dorzolamide hydrochloride is based on the selective inhibition of type II carbonic anhydrase. Slowing down the work of this enzyme of the ciliary body reduces the secretion of intraocular fluid, which is associated with a decrease in the formation of bicarbonate ions and a slowdown in the transport of sodium and water ions.
During local administration of dorzolamide, hydrochloride enters the general circulatory system. Long-term use of this compound leads to the accumulation of its molecules in red blood cells. This is due to the selective binding of carbonic anhydrase of the second type with dorzolamide hydrochloride, which leads to a decrease in the plasma content of the drug in free form. A metabolite of dorzolamide is an N-desethyl derivative, in which the ability to block carbonic anhydrase of the second type is less pronounced, when compared with the action of the original form, but inhibition of carbonic anhydrase of the first type is possible. The accumulation of the metabolite also occurs in red blood cells, in a bound form with carbonic anhydrase of the first type.
Up to 33% of dorzolamide molecules bind to blood albumin. Excretion of the active substance and its metabolite is carried out with urine. Cancellation of the drug leads to nonlinear excretion of dorzolamide from red blood cells. At the beginning of treatment, a rapid decrease in its content is observed, after which the removal of the active substance from red blood cells is reduced. The half-life of dorzolamide after instillation of the drug "Cosopt" instructions for use sets at least 4 months.
Features of the action of active substances
Timolol maleate exhibits the properties of a non-selective beta-blocker. Its role in reducing pressure inside the eye is associated with a decrease in production and increased excretion of fluid from the intraocular space.
Local administration of timolol maleate in the composition of Cosopt drops leads to the penetration of this substance into the general blood flow system. The hypotensive effect of timolol begins 20 minutes after administration of the drug, its maximum effect occurs after 120 minutes and lasts for 1 day.
Indications for use
The main indication for the use of the drug "Cosopt" (eye drops) is open-angle and pseudoexfoliation glaucoma with signs of increased pressure inside the eye when the outflow of intraocular fluid is impaired. The action of the medication is aimed at removing it and reducing the production of moisture, which, accumulating in the chambers of the eye, presses on the optic nerve, leading to its gradual atrophy.
How to use
The drug "Cosopt" instructions for use prescribes to instill 1 drop into the area of the conjunctival sac of the sick eye or for prevention in both eyes 2 times a day.
When the appointment of this medication is carried out in order to replace the previously used drops for glaucoma, they need to stop being used for 1 day, and only then can a new treatment be possible. The Kosopt solution is administered no earlier than 10 minutes after the use of other local ophthalmic preparations.
The use of this tool requires patients to follow special instructions when working with a sterile solution. The vial of the drug "Cosopt" (eye drops), the instruction advises to check the integrity of the protective strip before opening.
Unopened vials have gaps between the cap and the vial. To open the cap, remove the strip to protect it from opening.
To open the bottle, the cap is unscrewed in the direction indicated by the index arrow located on the cap.
Before direct application of the drug, the patient throws back his head, pulls the edge of the lower eyelid, so that there is a space between the inner surface of the eyelid and the eyeball.
Next, the bottle is turned over, with the help of the thumb and forefinger, it is necessary to gently press on the place specially marked on the surface of the bubble so that only one drop of the solution comes out into the sore eye. Do not touch the neck of the vial on the surface of the eyeball or eyelid. Improper use of the vial causes infection of the eye with various pathogens, which entails serious consequences with further loss of vision.
If both eyes are sick, the above manipulation is carried out in the same order with the other.
After use, screw the cap tightly onto the bottle, but do not press the cap tightly so as not to damage the shape of the thread. The hole at the tip of the spout has a diameter that allows you to dose the solution when instilled, so you should not expand it.
Adverse reactions
The drug "Cosopt" (eye drops) has good tolerance, side effects are described extremely rarely. When studying a medication during a clinical trial, undesirable reactions inherent only to this combination were not recorded, however, already known side effects from dorzolamide hydrochloride and timolol maleate were noted, but these manifestations were weak and did not require discontinuation of the drug.
The drug "Cosopt" was studied in clinical trials on 1035 volunteers. For 2.4% of patients, eye drops had to be canceled due to point adverse reactions that appeared on the organs of vision. The treatment of 1.2% of the volunteers who had local unwanted effects associated with hypersensitivity and allergies was not possible.
The most frequent manifestations were directly related to the organs of vision. They were expressed by a burning sensation in the eye area, corneal erosion, blurred vision, and lacrimation.
The instructions for use attached to the Cosopt preparation (eye drops) include a description of possible adverse reactions of the body to the active components of the drug solution, which can penetrate into the general bloodstream.
The effect of dorzolamide hydrochloride on the organs of vision can be manifested by inflammation of the eyelid, irritation and peeling of the skin on the eyelid, iridocyclitis, pinpoint keratitis, transient myopia. All these changes pass some time after the withdrawal of treatment with this drug.
The effect of dorzolamide hydrochloride on the nervous system is noted for headache, dizziness, sensitivity disorder with numbness of the extremities, tingling sensation and goosebumps, fatigue and asthenic syndrome.
An allergic reaction may occur in the form of angioedema of the face, limbs, urticaria, itching, spasm in the bronchi, irritation of the pharyngeal mucosa, and dry mouth.
The undesirable effect of dorzolamide hydrochloride may manifest as nosebleeds.
With the introduction of the drug “Cosopt”, adverse reactions from the effects of timolol maleate on the organs of vision can be manifested by inflammation in the mucous membrane and cornea of the eye, inflammatory process of the ciliary edge of the eyelid, decreased susceptibility of the cornea, dry mucous membrane, visual acuity disorders, refractive errors of the lens of the eye, bifurcation of the visible picture omission of the upper eyelid.
The active substance of the drug timolol maleate, being a beta-blocker, can cause adverse reactions inherent in this group of substances.
The effect on the cardiovascular system is characterized by tinnitus, disturbance of the rhythm of the heart muscle and blood circulation, increased pressure, exacerbation of angina pectoris of vasospastic nature, fainting, cardiac arrest, swelling of the tissues, lameness, sensitivity disorder with numbness of the limbs, tingling sensation and goosebumps, signs of Raynaud, cold arms and legs.
Local administration of timolol maleate causes coughing and bronchospasm, especially in people with bronchial obstruction.
Skin changes caused by the action of thymol are associated with hair loss, psoriasis-like rashes, or exacerbation of psoriasis lesions.
Allergic reactions are associated with the appearance of anaphylactic shock, angioedema, urticaria, localized or generalized skin rashes.
Timolol maleate affects the central nervous system with manifestations of dizziness, depression, sleep disturbances, memory loss, rapid fatigue of striated muscles.
The substance has an effect on the digestive system that causes diarrhea, malabsorption, and drying of the oral mucosa.
Features of use
Prescribing drops "Cosopt", the doctor must make sure in advance that there is no insufficiency of the heart muscle. Patients with severe myocardial pathology in the past and signs of insufficiency at the moment during treatment with such a medication should be periodically observed by a cardiologist and monitor the heart rate. Deterioration of the state of the heart requires immediate withdrawal of the drug.
There are cases of death from bronchial spasm caused by timolol maleate drops "Cosopt" in patients with bronchial asthma and heart failure.
The effect of the drug on people with liver failure has not been studied, therefore caution is needed in the treatment of antiglaucoma agents.
Imbalance in the acid-base balance is caused by the use of carbonic anhydrase enzyme inhibitors, which leads to urolithiasis, which often develops in patients with urolithiasis in the past.
In the treatment with beta-blockers of people with diabetes mellitus or hypoglycemia, some symptoms characteristic of hypoglycemia are distorted.
Reception of beta-blockers smoothes the symptoms of hyperthyroidism, and the withdrawal of this drug can worsen the condition.
Before the upcoming surgery using general anesthesia, eye drops are canceled two days before the prescribed procedure to reduce the effect of timolol on muscle relaxants and general anesthetics.
The composition of Cosopt drops contains benzalkonium chloride, which acts as a preservative, which can cause irritation of the mucous membrane of the eyes. When using contact lenses together with the drug, they must be removed in advance and put on 15 minutes after the solution is administered. Benzalkonium chloride may discolour soft contact lenses.
Side effects of using the drug make it difficult to drive a car or operate complex mechanisms.
Interactions
Calcium channel blockers, beta-blockers, antiarrhythmic drugs, digitalis glycosides, catecholamine-depleting drugs, parasympathomimetics, opioid analgesics and monoamine oxidase inhibitors in combination with eye drops based on timolol maleate show a hypotensive effect and cause a greater degree of bradycardia.
Systemic beta-adrenergic blockade, associated with a decrease in heart rate, was observed during the interaction of timolol maleate with quinidine or a selective inhibitor that affects the reuptake of serotonin.
The interaction of timolol maleate with adrenaline can cause the patient's pupils to dilate.
Analogs
The manufacturer of the original Kosopt drops is the Dutch company Merck Sharp and Dome B.V., in the laboratories of which a special solution for the eye was created from two active substances (dorzolamide hydrochloride and timolol maleate) and auxiliary components. This tool has been widely used in the treatment of glaucoma.
Romanian pharmaceutical company K.O. Rompharm Company S.RL. ” An analogue of Cosopt was developed, repeating the qualitative and quantitative composition of the active components of the original. Both drugs are made in the form of eye drops with the exact content of dorzolamide hydrochloride in an amount of 22.26 mg and 6.84 mg of timolol maleate, but there is a slight difference in the auxiliary components. An analogue of Cosopt under the trade name Dorzopt Plus is produced. The action of the original drug and generic is aimed at reducing intraocular pressure in invitation, which means they are interchangeable, and if one of them is not available for sale, you can buy a drug available in the pharmacy.
Another analogue of Kosopt eye drops is produced by the Croatian company Jadran Galennaya Laboratory d.d. called "Dorzotimol." The composition of this generic also contains dorzolamide hydrochloride in an amount of 22.26 mg and 6.84 mg of timolol maleate, in addition, their additional components coincide. According to the pharmacotherapeutic effect, the preparations are similar, therefore, a generic may be an alternative to Cosopt drops. Instructions for use analogues unites in one pharmaceutical group - "antiglaucoma drugs". Indications, method of use, dosage, adverse reactions and overdose (symptoms) in all three medicines should be the same. The manufacturer can add its own nuances to the manual for the use of eye drops.
The drug "Cosopt" (eye drops) analogues can be both combined and single drugs, have in its composition either dorzolamide hydrochloride or timolol maleate. In the case of combined analogues, the second active substance is not part of the original drug and this causes differences in their effectiveness, side effects and interactions with other medicines.
The monopreparation Timolol in the form of eye drops of 0.25% and 0.5% is an analogue of Cosopt based on timolol maleate produced by the Indian company Genome Biotek Pvt. Ltd. " As part of a 1 ml solution of this product contains timolol maleate (equivalent to timolol) 2.5 mg and 5 mg.
Another Indian counterpart is Okamed, eye drops in two doses - 0.25% and 0.5% each. The manufacturer of this tool is Promed Exports Pvt. Ltd. ", India. The composition of 1 ml of Okamed solution, like Timolol, contains the active substance timolol maleate 2.5 and 5 mg (equivalent to timolol).
The German analogue of Kosopt eye drops is the Arutimol medication, in two doses - 0.25% and 0.5%, which is produced by the Chauven Anchorfarm GmbH. The drops, as in the previous synonyms, contain timolol maleate 2.5 mg and 5 mg (equivalent to timolol).
In 2008, the Russian analogue Timolol-AKOS, produced by the pharmaceutical plant Synthesis OJSC, appeared on the market of the Russian Federation, similar to the drug Cosopt. Available in the form of transparent, colorless eye drops 0.25%. The composition of this tool includes 2.5 mg of timolol (in the form of maleate).
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