Gemase lyophilisate for preparation of injection solution 5000ME, 1ml No. 5

The drug 'GemazaЃ' is used in ophthalmology to treat the following pathology:

• hyphema, hemophthalmus;

• preretinal, subretinal and intraretinal hemorrhages;

• fibrinoid syndrome of various origins;

• occlusion of the central retinal artery and its branches;

• thrombosis of the central retinal vein and its branches;

• prevention of adhesions in the postoperative period during antiglaucomatous operations;

The content of 1 ampoule of the drug 'GemazaЃ' is diluted in 0.5 ml of 0.9% sodium chloride solution. The resulting solution contains a dose corresponding to 5000 IU. The drug is administered parabulbar or subconjunctivally up to 10 injections per course. To flush the anterior chamber of the eye with massive effusion of fibrin into the anterior chamber or hyphema, the lyophilized substance (5000 IU) is diluted in 1 ml of 0.9% sodium chloride solution, after which 0.2 ml (1000 IU) or 0.1 ml (500 ME) of the resulting solution and diluted to 0.5 ml with 0.9% sodium chloride solution.
For intravitreal administration, 5000 IU of the lyophilisate is diluted in 1 ml of 0.9% sodium chloride solution, 0.1 ml (500 IU) of the resulting solution is taken and diluted with 0.1-0.2 ml of 0.9% sodium chloride solution. The resulting volume (0.2-0.3 ml) is injected intravitreally once.
In the presence of hyphema and fibrin effusion after cataract extraction, subconjunctival or parabulbar administration of GemazaЃ is recommended, as well as introduction into the anterior chamber. In case of hemorrhages in the vitreous body, retina, occlusive lesions of the vessels of the retina and optic nerve, parabulbar administration of the drug 'GemazaЃ' is indicated. With hemophthalmia of various etiology and fibrinoid syndrome, intravitreal administration of the drug is possible.
For the prevention of adhesions in the postoperative period during antiglaucomatous operations, the drug 'GemazaЃ' is diluted in the ratio indicated for subconjunctival injections, and injected into the filtration pad in the early postoperative period in the amount of 1-3 injections (at the discretion of the surgeon).

1 ampoule with a capacity of 1 ml or 2 ml contains

The active substance is recombinant prourokinase - 5000 ME.
Excipients: sodium chloride, dextran 40.

• individual hypersensitivity to the components of the drug;

• conditions with a high risk of bleeding, including blood diseases (hemorrhagic diathesis);

• gastrointestinal bleeding;

• bacterial endocarditis;

• active form of tuberculosis;

• proliferative diabetic retinopathy with grade III - IV gliosis;

• arterial hypertension with diastolic blood pressure more than 105 mm Hg. Art .;

• hypertensive crisis (due to the possible development of recurrence of intraocular hemorrhage);

• chronic renal failure (serum creatinine level more than 0.02 g / l, urea more than 0.5 g / l);

• severe hepatocellular insufficiency (blood albumin less than 3 g%);

• pregnancy and lactation;

• age up to 18 years.

Trade name: GEMAZAЃ

INN or grouping name: prourokinase.

Dosage form:

lyophilisate for preparation of solution for injection.

Description: amorphous powder or white, odorless porous mass.

Composition:
1 ampoule with a capacity of 1 ml or 2 ml contains

The active substance is recombinant prourokinase - 5000 ME.
Excipients: sodium chloride, dextran 40.

Pharmacological group: fibrinolytic agent.

ATX code: B01AD

Pharmacological properties
Fibrinolytic is a recombinant urokinase-type plasminogen activator. It is a recombinant prourokinase (RPK) and catalyzes the conversion of plasminogen to plasmin, which is able to lyse fibrin clots. The specificity of the action of RPU is based on the fact that it predominantly activates fibrin-bound plasminogen, which has a different conformation compared to plasminogen circulating in the bloodstream, into plasmin, and in the area of ??the fibrin clot is not sensitive to specific inhibitors present in the blood plasma. The single-stranded RPU molecule under the influence of plasmin is converted into a double-stranded molecule, which, in contrast to the single-stranded pro-form, is much more active against fibrin-bound plasminogen. A 'chain reaction' of interaction between RPU and fibrin-bound plasminogen is formed,as a result of which the fibrin clot is destroyed. Specific enzymatic activity of the 'GemazaЃ' preparation is from 4500 to 5500 ME in an ampoule.
Pharmacokinetics
With local periocular administration, the maximum concentration of the drug 'GemazaЃ' in the tissues of the eye is reached by 1-2 hours, the concentration of the drug gradually decreases, after 12-24 hours the drug is found in trace amounts. The maximum concentration of the drug is determined in the intraocular structures during intraocular administration. The half-life of the drug is 4-6 hours. Since the dose for topical application is small (up to 5000 IU), no blood concentrations that are significant for the systemic action of the drug are created.

Indications for use
The drug 'GemazaЃ' is used in ophthalmology for the treatment of the following pathology:

• hyphema, hemophthalmus;

• preretinal, subretinal and intraretinal hemorrhages;

• fibrinoid syndrome of various origins;

• occlusion of the central retinal artery and its branches;

• thrombosis of the central retinal vein and its branches;

• prevention of adhesions in the postoperative period during antiglaucomatous operations;

Contraindications

• individual hypersensitivity to the components of the drug;

• conditions with a high risk of bleeding, including blood diseases (hemorrhagic diathesis);

• gastrointestinal bleeding;

• bacterial endocarditis;

• active form of tuberculosis;

• proliferative diabetic retinopathy with grade III - IV gliosis;

• arterial hypertension with diastolic blood pressure more than 105 mm Hg. Art .;

• hypertensive crisis (due to the possible development of recurrence of intraocular hemorrhage);

• chronic renal failure (serum creatinine level more than 0.02 g / l, urea more than 0.5 g / l);

• severe hepatocellular insufficiency (blood albumin less than 3 g%);

• pregnancy and lactation;

• age up to 18 years.

Dosage and administration The content of 1 ampoule of the drug 'GemazaЃ' is diluted in 0.5 ml of 0.9% sodium chloride solution. The resulting solution contains a dose corresponding to 5000 IU. The drug is administered parabulbar or subconjunctivally up to 10 injections per course. To flush the anterior chamber of the eye with massive effusion of fibrin into the anterior chamber or hyphema, the lyophilized substance (5000 IU) is diluted in 1 ml of 0.9% sodium chloride solution, after which 0.2 ml (1000 IU) or 0.1 ml (500 ME) of the resulting solution and diluted to 0.5 ml with 0.9% sodium chloride solution.
For intravitreal administration, 5000 IU of the lyophilisate is diluted in 1 ml of 0.9% sodium chloride solution, 0.1 ml (500 IU) of the resulting solution is taken and diluted with 0.1-0.2 ml of 0.9% sodium chloride solution. The resulting volume (0.2-0.3 ml) is injected intravitreally once.
In the presence of hyphema and fibrin effusion after cataract extraction, subconjunctival or parabulbar administration of GemazaЃ is recommended, as well as introduction into the anterior chamber. In case of hemorrhages in the vitreous body, retina, occlusive lesions of the vessels of the retina and optic nerve, parabulbar administration of the drug 'GemazaЃ' is indicated. With hemophthalmia of various etiology and fibrinoid syndrome, intravitreal administration of the drug is possible.
For the prevention of adhesions in the postoperative period during antiglaucomatous operations, the drug 'GemazaЃ' is diluted in the ratio indicated for subconjunctival injections, and injected into the filter pad in the early postoperative period in the amount of 1-3 injections (at the discretion of the surgeon).

Side effect
There may be an allergic reaction, expressed in edema and hyperemia of the skin of the face on the side of administration of the drug, the phenomena of allergic tenonitis (chemosis, conjunctival hyperemia, decreased mobility of the eyeball).

Interaction with other drugs The
combined use of the drug with proteolytic agents has shown that it is inappropriate to combine the drug 'GemazaЃ' with collalizin injections. The combination of GemazaЃ with other thrombolytics should be used with caution. Combined use of solutions of the drug 'GemazaЃ' and emoxipin, as well as the drug 'GemazaЃ' and dexamethasone is possible.

Drug overdose
With local administration of the drug 'GemazaЃ' in doses of 5000 IU, there is no risk of systemic bleeding.
In case of an overdose of the drug, which is unlikely when using the recommended doses (up to 5000 IU once), a recurrence of intraocular hemorrhage is possible. With a single administration of the drug in a dose exceeding 5000 IU, the risk of allergic reactions indicated in the side effects increases.
In case of an overdose of the drug and during surgical interventions against the background of a course of treatment with GemazaЃ, to reduce the risk of hemorrhage, the general use of etamsylate in injections of 250-500 mg intramuscularly is recommended.

Special instructions
The ability of the drug 'GemazaЃ' to influence the reaction rate when driving vehicles or other mechanisms has not been noted. But depending on the individual patient's reaction to the drug 'GemazaЃ' during the course of treatment with the drug, care should be taken when driving a car and operating mechanisms.

Release form
Lyophilisate for preparation of solution for injection 5000 ME. In neutral glass ampoules with a capacity of 1 ml or 2 ml. 5 ampoules in a blister strip with or without foil. 1 blister strip packaging together with instructions for use in a cardboard box.

Storage conditions:

In a dark place, out of the reach of children, at a temperature of 2 to 20 ? C.

Shelf life:

4 years. Do not use after the expiration date printed on the package.

Terms of dispensing from pharmacies:

On prescription.