Aktilize - Instructions For Use, Indications, Doses, Analogues

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Aktilize

Instructions for use:

1. 1. Release form and composition
2. 2. Indications for use
3. 3. Contraindications
4. 4. Method of application and dosage
5. 5. Side effects
6. 6. Special instructions
7. 7. Drug interactions
8. 8. Analogs
9. 9. Terms and conditions of storage
10. 10. Terms of dispensing from pharmacies

Prices in online pharmacies:

from 23 987 rub.

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Aktilize - thrombolytic, recombinant human tissue plasminogen activator; a glycoprotein that directly activates the conversion of plasminogen to plasmin.

Release form and composition

Dosage form - lyophilisate for preparation of solution for infusion: white or pale yellow mass (50 mg of lyophilisate and 50 ml of solvent in colorless glass vials, in a cardboard box 1 vial with lyophilizate complete with 1 vial of solvent).

1 bottle of Aktilize contains:

• Active ingredient: alteplase - 50 mg (in 1 ml of the finished solution 1 mg);
• Auxiliary components: L-arginine, polysorbate 80, phosphoric acid, gentamicin (residual traces after the production process).

Solvent: water for injection - 50 ml.

Indications for use

The use of Aktilize is indicated in the thrombolytic therapy of the following diseases / conditions:

• Acute myocardial infarction;
• Massive thromboembolism of the pulmonary artery, accompanied by unstable hemodynamics;
• Acute period of ischemic stroke.

Contraindications

• The period of pregnancy and breastfeeding;
• Children and adolescents up to 18 years old;
• Hypersensitivity to the components of the drug.

Contraindications for patients with an increased risk of bleeding:

• Hemorrhagic diathesis;
• Extensive bleeding, including in the previous 6 months;
• History of aneurysm, neoplasms, and other pathologies of the central nervous system, including surgery on the brain or spinal cord;
• Suspected hemorrhagic stroke;
• Intracranial (including subarachnoid) hemorrhage, including a history;
• Severe uncontrolled arterial hypertension;
• Concomitant therapy with warfarin and other oral anticoagulants;
• Severe trauma, major surgical intervention in the period of the previous ten days, including any injury sustained against the background of developing myocardial infarction;
• Recent puncture of incompressible blood vessels (including the subclavian or jugular vein)
• Traumatic or prolonged (more than 2 minutes) cardiopulmonary resuscitation;
• Traumatic brain injury, suffered recently;
• Childbirth within the previous 10 days;
• Severe liver pathologies such as liver cirrhosis, liver failure, active hepatitis, portal hypertension (including esophageal varices);
• Acute pancreatitis;
• Pericarditis, bacterial endocarditis;
• Peptic ulcer and duodenal ulcer diagnosed within the last 3 months;
• Neoplasms with a risk of bleeding;
• Defects in the development of veins and arteries, arterial aneurysms.

Additional contraindications for the use of Aktilize in acute myocardial infarction and pulmonary embolism:

• A history of hemorrhagic or unknown stroke;
• Transient ischemic attacks or ischemic stroke within the last 6 months (not including the first 4.5 hours of the current acute ischemic stroke).

In addition to the above contraindications, in acute ischemic stroke, Actilize cannot be used in the following cases:

• Weak severity of symptoms of acute ischemic stroke at the beginning of the infusion or rapid improvement in the patient's condition;
• Lack of accurate data on the time of onset of the disease, a period of more than 4.5 hours from the moment of the first symptoms of ischemic stroke to the start of the infusion;
• Severe, clinically proven stroke, for example, if the NIHSS (National Institutes of Health Stroke Severity Scale) score is greater than 25, or the corresponding CT scan or nuclear magnetic resonance is obtained;
• Serious head injury or stroke in the previous three months;
• Convulsions at the onset of a stroke;
• The appearance of a previous stroke in diabetes mellitus;
• Taking heparin within 48 hours before the first symptoms of a stroke, with increased activated partial thromboplastin time (APTT) at a given time;
• The number of platelets is less than 100,000 per μl;
• Systolic blood pressure (BP) above 185 mm Hg. or diastolic blood pressure above 110 mm Hg, or, if necessary, the use of intensive antihypertensive therapy (intravenous administration of drugs) to reduce the pressure to these limits;
• The concentration of glucose in the blood is below 3 or above 20 mmol / L.

With caution, only on the basis of a preliminary assessment of the degree of the expected benefit from therapy and the risk of bleeding, Aktilize should be prescribed to patients after a recent minor intervention with a needle during biopsy or puncture of large vessels, heart massage during resuscitation performed by intramuscular (i / m) injection; for any diseases (not listed in the list of contraindications) associated with an increased risk of bleeding; in the case of simultaneous administration of oral anticoagulants, the use of the drug is indicated only if the anticoagulant activity according to laboratory studies is not clinically significant.

In acute myocardial infarction and acute pulmonary embolism, additional caution should be exercised when treating patients with systolic blood pressure above 160 mm Hg. Art. and elderly patients, as they may have an increased risk of intracranial hemorrhage.

Since the likelihood of a positive clinical effect of this therapy in elderly patients is quite high, despite the indicated negative side effects, it is necessary to carefully compare the intended benefits and risks.

In acute ischemic stroke, the use of Aktilize is accompanied by an increased threat of intracranial hemorrhage, since it predominantly occurs in the necrotic area. In this connection, it is required to additionally take into account the presence of the following features in patients:

• Pathologies associated with a high risk of bleeding;
• Minor asymptomatic cerebral aneurysms;
• Delay in initiation of therapy;
• Previous therapy with acetylsalicylic acid or other antiplatelet agents / drugs increase the risk of intracerebral hemorrhage, especially at a later start of treatment (the dose of alteplase should be no more than 0.9 mg per 1 kg of patient weight per day);
• Older age is more than 80 years, the risk of cerebral hemorrhage increases and the overall benefit of therapy decreases.

It is impossible to start treatment with alteplase 4.5 hours after the onset of symptoms of the disease, since this leads to a decrease in the positive effect, an increase in mortality against the background of preliminary therapy with acetylsalicylic acid and the risk of bleeding.

Method of administration and dosage

The lyophilisate is intended for the preparation of a solution for infusion by dissolving the contents of 1 bottle (50 mg) of the drug in 1 bottle (50 ml) of solvent.

Mix until complete dissolution should be done carefully, avoiding strong agitation in order to avoid the formation of foam. The liquid should have a clear, colorless, pale yellow structure without any particles.

For additional dilution, 0.9% sodium chloride solution can be used.

The minimum concentration of alteplase in the solution for infusion should be 0.2 mg / ml.

The initially obtained solution cannot be further diluted with a carbohydrate-based infusion solution or water for injection, as well as mixed with other drugs in the intravenous administration system.

The use of Aktilize should be started when the first symptoms of the disease appear.

Recommended dosage regimen:

• Myocardial infarction, with treatment started within 6 hours after the onset of symptoms: an accelerated therapy regimen - intravenous jet at a dose of 15 mg, then infusion for 30 minutes at a dose of 50 mg, in the next 60 minutes - 35 mg, the total maximum dose is 100 mg. Patients weighing up to 65 kg: intravenous jet - 15 mg, then intravenous drip - at the rate of 0.75 mg per 1 kg of body weight (no more than 50 mg) for 30 minutes, in the next 60 minutes the patient is administered a dose of 0.5 mg per 1 kg (no more than 35 mg);
• Myocardial infarction, when starting treatment between 6 and 12 hours after the onset of symptoms: a three-hour dosing regimen - 10 mg intravenous stream, then 50 mg intravenously drip for 60 minutes, then 10 mg every next 30 minutes until a maximum total dose of 100 mg is reached. For patients weighing up to 65 kg, the dose is prescribed at the rate of 1.5 mg per 1 kg of patient weight;
• Pulmonary embolism: first, within 1-2 minutes intravenous stream - 10 mg, then intravenous drip for 120 minutes - 90 mg, total dose 100 mg. With a patient weighing up to 65 kg - no more than 1.5 mg per 1 kg;
• The acute period of ischemic stroke (during the first 4.5 hours, treatment should be started as soon as possible after the onset of the first symptoms): at the rate of 0.9 mg per 1 kg of the patient's weight (no more than 90 mg), of which 10% - in / in a stream, then the rest of the drug is injected / in drip for 60 minutes. The earlier treatment is started in the specified period of time, the more likely a favorable treatment result is.

Antithrombotic adjuvant therapy is indicated for patients with ST-segment elevation myocardial infarction according to international recommendations.

After the administration of Aktilize, auxiliary therapy for pulmonary embolism in the form of infusion of heparin may be required for patients if the APTT is less than 2 times higher than congenital adrenal hyperplasia (ANH).

During the first 24 hours after starting treatment for ischemic stroke, adjuvant therapy with acetylsalicylic acid or intravenous heparin should be avoided.

Side effects

The most common side effect of using Actilize for myocardial infarction, pulmonary embolism or acute ischemic stroke is bleeding, leading to a decrease in hemoglobin. It can occur in any cavity or part of the body and cause a life-threatening situation, even fatal.

Bleeding can be external (from the nose, puncture sites, damage to blood vessels) and internal (bleeding in any cavity or part of the body).

The neurological symptoms of intracranial bleeding include drowsiness, aphasia, hemiparesis, convulsions.

In addition, the use of the drug for myocardial infarction, pulmonary embolism or the acute period of ischemic stroke can cause the following undesirable phenomena:

• Immune system: anaphylactoid reactions; possibly - lowering blood pressure, bronchospasm, urticaria, angioedema, rash, other hypersensitivity reactions, shock;
• Cardiovascular system: bleeding (in the form of a hematoma), pericardial bleeding, embolism, bleeding into the parenchymal organs (intrahepatic bleeding, pulmonary bleeding);
• Nervous system: intracranial hemorrhage - cerebral hematoma, cerebral hemorrhage, hemorrhagic stroke, intracranial hematoma, hemorrhagic transformation of stroke, subarachnoid hemorrhage;
• Organ of vision: retinal hemorrhage;
• Digestive system: nausea, vomiting, bleeding from the gums, bloody vomiting, bleeding from the mouth, bleeding from a stomach ulcer, stomach bleeding, bleeding from the rectum, melena, retroperitoneal bleeding (retroperitoneal hematoma);
• Respiratory system: hemoptysis, bleeding from the throat or nose;
• Urinary system: bleeding from the urinary tract, hematuria;
• Dermatological reactions: ecchymosis;
• Local reactions: bleeding at the injection site, hematoma, bleeding at the puncture site;
• Others: an increase in body temperature, a decrease in blood pressure, fat embolism, the need for transfusions.

In the treatment of myocardial infarction, it is possible to develop additional undesirable effects from the cardiovascular system - reperfusion arrhythmias: tachycardia, extrasystole, arrhythmia, atrial fibrillation, bradycardia, atrioventricular (AV) block from I degree to complete blockade, ventricular arrhythmia, ventricular tibachycardia, cardiac arrest, death.

special instructions

The use of Aktilize should be carried out in a hospital setting, in the presence of standard resuscitation equipment and appropriate medications, under the supervision of a physician with experience in conducting thrombolytic therapy.

Infusion must be accompanied by regular monitoring of the tolerance of treatment, especially with the simultaneous use of angiotensin-converting enzyme (ACE) inhibitors. With the development of an anaphylactoid reaction, the administration of the drug is stopped.

Since bleeding is a frequent complication of therapy, it is necessary to avoid the use of intramuscular injections, rigid catheters, unreasonable manipulations during the treatment period and carefully monitor the areas of possible bleeding.

The occurrence of bleeding can be facilitated by the simultaneous use of heparin. If bleeding develops while taking heparin within the next 4 hours, the patient should be prescribed protamine.

With cerebral and other severe bleeding, fibrinolytic therapy and the use of heparin should be canceled. In the absence of a clinical effect from conservative measures to stop bleeding, therapy with blood preparations (cryoprecipitate, freshly frozen plasma and platelets) is indicated.

The diagnosis of pulmonary embolism requires objective confirmation by pulmonary angiography or pulmonary tomography.

It has been clinically proven that in acute myocardial infarction, the use of Actilize helps to reduce mortality in the first 30 days of illness.

In the treatment of acute myocardial infarction, the risk of bleeding is increased by concomitant therapy with antagonists of glycoprotein IIb / IIIa, thromboembolism is increased by the use of thrombolytic agents in patients with left heart thrombosis. Reperfusion arrhythmias can be caused by coronary thrombolysis.

Treatment of ischemic stroke in the acute period should be started only after excluding intracranial bleeding using computed tomography or magnetic resonance imaging of the brain.

In acute ischemic stroke, the clinical effect of therapy is lower in patients with previous stroke with concomitant uncontrolled diabetes mellitus.

It is not recommended to use Aktilize for stroke with mild severity, since the potential risk from using the drug is higher than the expected benefit.

Due to the high risk of intracranial hemorrhage and death, it is not recommended to use alteplase in severe stroke.

Resumption of blood flow to the ischemic area can cause cerebral edema in the infarction area. Due to the high risk of hemorrhage, antiplatelet agents should not be started within 24 hours after alteplase application.

Drug interactions

Medicines that alter platelet function or affect blood clotting can increase the risk of bleeding.

The risk of developing anaphylactoid reactions increases with the simultaneous use of ACE inhibitors with alteplase.

Analogs

Alteplaza is an analogue of Aktilize.

Terms and conditions of storage

Store in a dark place at temperatures up to 25 ° C. Keep out of the reach of children.

The shelf life is 3 years.

In the refrigerator, at a temperature of 2-8 ° C, the solution ready for infusion can be saved for 24 hours; at temperatures up to 25 ° C - no more than 8 hours.

Terms of dispensing from pharmacies

Dispensed by prescription.

Aktilize: prices in online pharmacies

Drug name Price Pharmacy

Actilise 50 mg lyophilisate for preparation of solution for infusion complete with solvent 50 ml 1 pc. RUB 23987 Buy

Actilise lyoph. d / inf. 50mg 50ml n1 RUB 27393 Buy

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!