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

Hemorrhages in the anterior chamber of the eye

Hemase® is used in ophthalmology to treat the following pathology:

• hyphema, hemophthalmus;
• retinal, subretinal and intraretinal hemorrhages;
• fibrinoid syndrome of various genesis;
• thrombosis of the central retinal vein and its branches;
• prevention of adhesions in post-operative period in anti-glaucoma surgeries.

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Active ingredient

Prourokinase

Composition

1 ampule with a capacity of 1 ml contains:

active ingredient:

recombinant prourokinase – 5000 ME.

Excipients: sodium chloride, dextran 40.

How to take, the dosage

The contents of 1 ampoule of “Hemase®” is diluted in 0.5 ml of 0.9% sodium chloride solution. The resulting solution contains a dose corresponding to 5000 ME. The drug is administered parabulbar or subconjunctival up to 10 injections per course. For irrigation of the anterior chamber in case of massive fibrin sweat into the anterior chamber or hyphema the lyophilized substance (5000 ME) is diluted in 1 ml of 0.9% sodium chloride solution, then 0.2 ml (1000 ME) or 0.1 ml (500 ME) of the obtained solution is taken and diluted to 0.5 ml of 0.9% sodium chloride solution.

For intravitreal injection 5000 ME of lyophilizate is diluted in 1 ml of 0.9% sodium chloride solution, 0.1 ml (500 ME) of the obtained solution is taken and diluted in 0.1-0.2 ml of 0.9% sodium chloride solution. The obtained amount (0.2-0.3 ml) is injected intravitreally once.

In case of hyphema and fibrinous effusion after cataract extraction subconjunctival or parabulbar injection of “Hemase®” is recommended as well as injection into the anterior chamber. At hemorrhages in the vitreous body, retina, occlusive lesions of retinal vessels and the optic nerve, the parabulbar injection of “Hemase®” is indicated. Intravitreal injection of the drug is possible in case of hemophthalms of various etiology and fibrinoid syndrome.

For prevention of adhesive process in postoperative period during antiglaucoma surgeries Gemase® is diluted in the ratio specified for subconjunctival injections and injected into the filtration pad in early postoperative period in the quantity of 1-3 injections (at the surgeon’s discretion).

Interaction

Combined use of the drug with proteolytic agents has shown that it is not advisable to combine the drug “Hemase®” with collalysin injections. Combination of Hemase® with other thrombolytics should be used with caution.

Combined use of solutions of Hemase® and emoxipine as well as Hemase® and dexamethasone is possible.

Special Instructions

The ability of the drug “Hemase®” to affect the reaction rate when driving motor transport or operating other mechanisms has not been noted.

But depending on the patient’s individual reaction to Gemase® , caution should be exercised when driving and operating machinery during treatment with the drug.

Contraindications

• individual hypersensitivity to the drug components;
• conditions with high risk of bleeding, including blood diseases (hemorrhagic diathesis);
• gastrointestinal bleeding;

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• bacterial endocarditis;
• active form of tuberculosis;
• proliferative diabetic retinopathy with gliosis of degree III – IV;
• arterial hypertension with diastolic blood pressure over 105 mmHg. systolic blood pressure.
• hypertensive crisis (due to the possible development of recurrence of intraocular hemorrhage)
• chronic renal insufficiency (serum creatinine over 0.02 g/l, urea over 0.5 g/l);
• severe hepatocellular insufficiency (blood albumin less than 3 g %);
• pregnancy and lactation period;
• age below 18 years.

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Side effects

There may be an allergic reaction, manifested by edema and hyperemia of the skin on the side of injection of the drug, allergic tenonitis (chemosis, conjunctival hyperemia, decreased mobility of the eyeball).

Overdose

There is no risk of systemic bleeding when administering Hemase® in doses of 5000 ME locally.

In case of overdose of the drug, which is unlikely when using the recommended doses (up to 5000 ME once), a recurrence of intraocular hemorrhage is possible. At a single injection of the drug in dose greater than 5000 ME the risk of allergic reactions, indicated in the side effects, increases.

At overdose of the drug and during surgical interventions against the background of treatment course with “Hemase®” to reduce the risk of hemorrhage the total administration of etamsilate in injections of 250-500 mg intramuscularly is recommended.

Pregnancy use

It is contraindicated in pregnancy.

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