The pharmacological equipoise results properties of fibrinolytic agents – recombinant urokinase-type plasminogen activator. It represents recombinant prourokinase (PAR) and catalyzes the conversion of plasminogen to plasmin, which is capable of lysing fibrin clots. Specificity of action is based on the PAR, it preferably activates fibrin-bound plasminogen, having a different conformation compared with circulating circulating plasminogen, plasmin, fibrin and clot in the field is not sensitive to specific inhibitors present in blood plasma. PAR-stranded molecule under the influence of plasmin converted into double-stranded molecule, which, unlike the single-stranded form about a much more active against fibrin-bound plasminogen. Formed a “chain reaction” PAR interaction with fibrin-bound plasminogen, resulting in a fibrin clot breaks. The specific enzyme activity “Gemaza drug » from 4500 to 5500 ME in a vial. Pharmacokinetics The local periocular administration of the maximum concentration of the drug “Gemaza » in the eye tissues is achieved in 1-2 hour, the concentration of the drug gradually decreases, the drug is found in 12-24 hours in trace quantities. The maximum concentration of the drug is determined to intraocular structures when administered intraocularly. The half-life is 4-6 hours. Since the dose is small for local application (5000 ME), is created in the blood concentration, significant systemic action of the drug.
The drug “Gemaza ® » is used in ophthalmology for the treatment of the following pathologies:
- hyphema, hemophthalmus;
- preretinal, subretinal hemorrhage and intraretinalnye;
- fibrinoid syndrome of different genesis;
- 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 when antiglaukomatoznyh operations;
- Individual hypersensitivity to the drug;
- state with a high risk of bleeding, including blood diseases (hemorrhagic diathesis);
- gastrointestinal bleeding;
- bacterial endocarditis;
- active form of tuberculosis;
- proliferative diabetic retinopathy with gliosis grade III – IV;
- hypertension with diastolic blood pressure greater than 105 mm Hg. Article .;
- hypertensive crisis (in connection with the possible development of recurrent intraocular hemorrhage);
- chronic renal impairment (serum equipoise results creatinine of more than 0.02 g / l, urea 0.5 g / l);
- severe hepatocellular impairment (blood albumin of less than 3% d);
- Pregnancy and lactation;
age 18 years.
Dosing and Administration
The contents of one ampoule “Gemaza drug ® » is diluted in 0.5 mL of 0.9% sodium chloride solution. The resulting solution contains a dose corresponding to 5,000 ME. The drug is injected or parabulbarno subkonyunktivalno to 10 injections per course. For washing the anterior chamber with massive effusion of fibrin in the anterior chamber or lyophilized substance hyphema (5000 ME) diluted in 1 ml of 0.9% sodium chloride solution and then 0.2 ml is taken (1000 ME) or 0.1 ml (500 ME) and the resulting solution is diluted to 0.5 ml of 0.9% sodium chloride solution.
For intravitreal ME 5000 lyophilizate is reconstituted with 1 ml of 0.9% sodium chloride, 0.1 ml is taken (500 ME) and the resulting solution is diluted 0.1-0.2 mL of 0.9% sodium chloride solution. This volume (0.2-0.3 mL) was injected intravitreally once.
In the presence of hyphema and fibrin effusion after cataract extraction is recommended subconjunctival or parabulbarnom a “drug Gemaza ® », and the introduction into the anterior chamber. When vitreous hemorrhage, retinal vascular occlusive lesions of the retina and optic nerve shows parabulbarnom a “drug Gemaza ® ». When hemophthalmus different etiology and fibrinoid syndrome may intravitreal injection of the drug.
For the prevention of adhesions in the postoperative period at antiglaukomatoznyh drug operations “Gemaza ® » is diluted specified for subconjunctival injection, and injected into the filter pad in the early postoperative period in the amount of 1-3 injection (at the discretion of the surgeon).
There may be an allergic reaction, which is expressed in the swelling and redness of the skin on the face of the administration of the drug, allergic phenomena tenonita (chemosis, conjunctival hyperemia, decreased mobility of the eyeball).
Interaction with other medicinal products
Co-administration of the preparation with proteolytic agents found that the drug combination “Gemaza ® » with equipoise results injections kollalizina inappropriate. Combination drug “Gemaza ® » with other thrombolytic agents used with caution. Perhaps the combined use solutions “Gemaza drug ® » and emoxipine and preparation “Gemaza ® » and dexamethasone.
Overdose of drug
When the local administration of the drug “Gemaza ® » 5000 ME doses the risk of systemic bleeding is absent.
In case of overdose of the drug, that when using the recommended doses (up to 5000 single ME) is unlikely to relapse of intraocular hemorrhage. With a single administration of the equipoise results drug at a dose exceeding 5,000 ME, increases the risk of allergic reactions, listed in the side effects.
In case of overdose of the drug and during surgical interventions on the background of the course of treatment “Gemaza ® » to reduce the bleeding risk is recommended that the general application etamzilata injections 250 -500 mg intramuscularly.
The ability of the drug “Gemaza ® » to influence the rate of reaction when driving or operating other mechanisms are not marked. But depending on the individual patient response to the drug “Gemaza ® » during the course of treatment must be careful when driving and management mechanisms.
Valium for 5000 ME solution for injection. The neutral glass ampoules capacity of 1 ml or 2 ml. 5 vials in blisters with foil or without foil. 1 blisters together with instructions for use in paper cartons.
In the dark, place inaccessible to children at temperature from 2 to 20 ° C.