Aktilize

The actilysis has thrombolytic properties.

Indications Aktilize

It is used for the restoration of bloody processes inside the vessels with the help of lysis of the thrombus - during a myocardial infarction having a sharp shape.

It is also used in PE, accompanied by a hemodynamic disorder.

Can be administered in the acute phase of an ischemic stroke.

Release form

The drug is sold in the form of an infusion lyophilizate, inside sterile bottles of glass, having a capacity of 50 ml. The box also contains a solvent - in bottles with a volume of 50 ml.

Pharmacodynamics

The drug has a thrombolytic effect and acts as a tissue activator element of plasminogen (it is a glycoprotein that helps modify a drug substance in plasmin). As a result, the anticoagulant and fibrinolytic effect develops.

The fibrinolytic activity of the drug is limited to the thrombus region, and it does not affect the other hemostasis processes (fibrinogen is not destroyed, and systemic fibrinolysis is also activated). Due to this, the probability of bleeding does not increase, and hypofibrinogenemia also does not develop.

If the acute stage of pulmonary embolism develops, against which background hemodynamic disorders are noted, the use of Aktiliset leads to a short-term reduction in the size of the thrombus, and in addition to stabilizing the pressure within the artery of the lung and to maintaining a physiologically adequate right ventricular function.

Pharmacokinetics

The drug is excreted rather quickly from the circulatory system. The half-life is approximately 5 minutes, so after 20 minutes, only about 10% of the baseline remains in the blood. Remains of alteplase, distributed inside liquids with tissues, are excreted for 40 minutes. The process of biotransformation of the drug is carried out in the liver.

Dosing and administration

Production of the infusion liquid: the lyophilizate from the vial is diluted in a sterile liquid that is contained in the second flacon from the bundle, to a concentration of 1 mg / ml. After this, this liquid can be diluted using saline. Medication is given in / in the method. The size of the portion is selected taking into account the condition and weight of the patient, as well as the nature of the disease.

During the acute phase of the infarction (the period of the first 6 hours), people with a weight above 65 kg should inject 15 mg of the medication intravenously; After this, 50 mg is administered through infusion (for 0.5 hours), as well as another 35 mg (60 minutes) until a portion of 0.1 g is reached. After 6-12 hours after the appearance of manifestations of the disease by the jet method, 10 mg of the substance are intravenously administered; After this, infusion of 50 mg LS and later 10 mg (with 30-minute intervals) is applied throughout the 1-hour period until a total dosage of 0.1 g for a 3-hour period is obtained.

Persons weighing less than 65 kg should be injected with a maximum of 1.5 mg / kg of drug substance. Together with Aktilise, aspirin and heparin are also administered. During the use of the drug, it is required to monitor the APTT values.

During therapy with PE, medication is administered by a jet method intravenously - in a dose of 10 mg, for 1-2 minutes, then at a dosage of 90 mg for 120 minutes, until a total dose of 0.1 g is obtained. People with a weight below 65 kg is allowed to use a maximum of 1.5 mg / kg of medicament.

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Use Aktilize during pregnancy

In pregnancy or lactation, the medication should be used with great care.

Contraindications

Among the contraindications:

• presence of strong sensitivity with respect to the drug;
• neoplasms affecting the central nervous system;
• hemorrhagic form of diathesis;
• surgical procedures in the spinal cord;
• pericarditis;
• diseases in which there is a disorder of cerebral circulation (hemorrhagic form of stroke, as well as hemorrhage inside the skull);
• vascular aneurysm;
• pancreatitis;
• retinopathy, which has a hemorrhagic character;
• obstetric labor or general surgical operations;
• a pronounced increase in blood pressure;
• bacterial genesis of endocarditis;
• exacerbated ulcer;
• hepatic cirrhosis;
• Varicose veins affecting the venous vessels in the esophagus;
• insufficiency of hepatic activity;
• portal hypertension;
• hepatitis.

Caution is required when prescribing drugs to elderly people, as well as individuals with conditions in which there is a high risk of bleeding (biopsies or punctures in the vascular region, as well as intramuscular injections).

Side effects Aktilize

The use of medication sometimes leads to such side effects:

• local external bleeding in the area of damaged vessels, and also from the nose, gums, or zone of puncture;
• internal bleeding (urogenital system, gastrointestinal tract, and parenchymal organs);
• arrhythmia;
• occasionally there is vomiting, a decrease in blood pressure, nausea and thromboembolism.

[1]

Overdose

When poisoning, there are complications of hemorrhagic nature - internal or external bleeding.

Interactions with other drugs

The use of medication together with other agents that affect the activity of platelets or blood loss, increases the likelihood of bleeding.

The combination of actilize with ACE inhibits the possibility of anaphylactic symptoms.

Infusion fluid of the drug should not be mixed within the same container with other medicinal products.

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Storage conditions

The actilysis should be kept at temperature values within the range of 25 ° C. Ready fluid infusion can be left in the refrigerator for a maximum of 24 hours.

Shelf life

The actilysis can be used within 36 months from the production of the therapeutic agent.

Application for children

Use with caution in pediatrics.

Analogues

The analogue of the drug is Alteplase.

Reviews

Aktilise receives mostly positive feedback from medical specialists. The drug has many advantages, the main one of which is its fibrin-specificity. The lack of antibody production with respect to the drug makes it possible to apply it repeatedly; It is also noted that it only occasionally leads to a decrease in blood pressure values.

The use of actilease in case of a heart attack (with the rapid onset of therapy - during the first 6 hours) significantly reduces the death rate from this disease. Along with this, the introduction of the drug often helps to avoid the development of cardiogenic shock, which is a serious complication of the occurred myocardial infarction.