Hemase, lyophilizate 5 ths.me 5 pcs

Pharmacological group: fibrinolytic agent.

ATX code: B01AD

Pharmacological properties

Fibrinolytic is a recombinant urokinase-type plasminogen activator. It is a recombinant prourokinase (RPU) and catalyzes the conversion of plasminogen into plasmin, which is capable of lysing fibrin clots. The specificity of RPU action is based on the fact that it preferentially activates fibrin-bound plasminogen, which has a different conformation compared with circulating plasminogen in the bloodstream, into plasmin, and is not sensitive to the specific inhibitors present in plasma in the fibrin clot.

The single-chain RPU molecule under the influence of plasmin is converted into a double-chain molecule, which, unlike the single-chain pro-forma, is significantly more active against fibrin-linked plasminogen. A “chain reaction” of interaction between RPU and fibrin-linked plasminogen is formed, as a result of which the fibrin clot is destroyed. The specific enzymatic activity of Hemase® is 4500 to 5500 ME per ampoule.

Pharmacokinetics

In local periocular administration the maximum concentration of the drug “Hemase®” in the eye tissues is reached by 1-2 hours, the drug concentration gradually decreases, after 12-24 hours the drug is found in trace amounts. Maximum drug concentration is determined in the intraocular structures during intraocular administration. The half-life of the drug is 4-6 hours. Since the dose for topical administration is small (up to 5000 ME), no blood concentrations significant for the systemic action of the drug are produced.

Indications

The drug “Gemaza®” is used in ophthalmology to treat the following pathologies:

hyphema, hemophthalmos;
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.

Pharmacological effect

Pharmacological group: fibrinolytic agent.

ATX code: B01AD

Pharmacological properties

Fibrinolytic is a recombinant urokinase-type plasminogen activator. It is a recombinant prourokinase (RPU) and catalyzes the conversion of plasminogen to plasmin, which is capable of lysing fibrin clots. The specificity of the action of RPU is based on the fact that it preferentially 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 it is not sensitive to specific inhibitors present in the blood plasma.

The single-chain RPU molecule, under the influence of plasmin, is converted into a double-chain molecule, which, in contrast to the single-chain 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. The specific enzymatic activity of the drug “Gemaza®” is from 4500 to 5500 IU per ampoule.

Pharmacokinetics

With local periocular administration, the maximum concentration of the drug “Gemaza®” in the eye tissues is reached in 1-2 hours, the concentration of the drug gradually decreases, after 12-24 hours the drug is detected 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 use is small (up to 5000 IU), concentrations in the blood that are significant for the systemic effect of the drug are not created.

Special instructions

The ability of the drug “Gemaza®” to influence the reaction rate when driving vehicles or other mechanisms has not been noted.

But depending on the patient’s individual reaction to the drug “Gemaza®”, during the course of treatment with the drug, care should be taken when driving a car and operating machinery.

Active ingredient

Prourokinase

Composition

1 ampoule with a capacity of 1 ml contains:

active substance:

recombinant prourokinase – 5000 IU.

Excipients: sodium chloride, dextran 40.

Pregnancy

Contraindicated during pregnancy.

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 gliosis grade III – IV;
arterial hypertension with diastolic blood pressure more than 105 mm Hg. Art.;
hypertensive crisis (due to the possible development of relapse of intraocular hemorrhage);
chronic renal failure (serum creatinine level more than 0.02 g/l, urea level more than 0.5 g/l);
severe hepatocellular failure (blood albumin less than 3 g%);
pregnancy and lactation;
age up to 18 years.

Side Effects

An allergic reaction may occur, expressed in swelling and hyperemia of the skin of the face on the side of the drug administration, phenomena of allergic tenonitis (chemosis, conjunctival hyperemia, decreased mobility of the eyeball).

Interaction

The combined use of the drug with proteolytic agents showed that combining the drug “Gemaza®” with injections of collalysin is inappropriate. Use the combination of the drug “Gemaza®” with other thrombolytics with caution.

The combined use of solutions of the drug “Gemaza®” and emoxypine, as well as the drug “Gemaza®” and dexamethasone is possible.

Overdose

With local administration of the drug “Gemaza®” 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 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 overdose of the drug and during surgical interventions during the course of treatment with Gemaza®, to reduce the risk of hemorrhage, the general use of ethamsylate in injections of 250-500 mg intramuscularly is recommended.

Storage conditions

In a place protected from light, out of reach of children, at a temperature of 2 to 20°C.

Shelf life

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

Manufacturer

Federal State Budgetary Institution National Medical Research Center of Cardiology, Russia