Alteplase (Alteplasum)
Regular monitoring of treatment tolerability is recommended, especially in patients receiving ACE inhibitors concomitantly. Therapy requires careful monitoring of areas of possible bleeding (including catheter insertion sites, arterial and venous punctures, incisions and injections). The use of rigid catheters, intramuscular injections and unnecessary manipulation should be avoided during treatment
In acute coronary syndrome, thrombolysis is advisable. It helps reduce mortality and is economically beneficial. There were no differences in survival after tissue plasminogen activator, streptokinase, and anisolated plasminogen-streptokinase complex; The duration and regimen of thrombolytic therapy are discussed. Additional treatment with anticoagulants and antiplatelet agents likely increases the effectiveness of thrombolytic therapy.
The earlier thrombolysis is performed, the more effective it is. That is why thrombolysis needs to be introduced into the daily practice of medical institutions. The risk of requiring resuscitation associated with thrombolysis should be taken into account.
In outpatient practice, urokinase (bolus administration of tenecteplase or reteplase) is considered the drug of choice; in inpatient settings, streptokinase is considered (except for cases where patients have received it previously). New drugs (alteplase) are more expensive and therefore cannot be first-line drugs. The approximate cost of a course of treatment for one patient using tissue thromboplastin activator inhibitor is $2900, using streptokinase - $400, anisolated plasminogen-streptokinase complex - $1900, urokinase - $775.
Heads and administrators of healthcare, hospital cardiologists should facilitate the implementation of thrombolysis by general practitioners.
Monitoring coagulogram (aPTT, fibrinogen, fibrin degradation products, thrombin, thrombin time), hematocrit, hemoglobin concentration, platelet count, electrocardiogram (for coronary artery thrombosis); for thrombosis of cerebral vessels - control of mental and neurological status (before the start of treatment and periodically while taking the drug). To evaluate treatment over time, one or more criteria are used; blood pressure, pulse and respiratory rate are determined regularly.
The risk of developing hemorrhagic complications increases when using doses of the drug exceeding 100 mg.
The potential risks and benefits of using alteplase should be weighed against recent minor injuries (biopsy, vascular puncture, intramuscular injections, cardiac massage) and in other conditions accompanied by a risk of bleeding, during pregnancy, during the first 10 days of the postpartum period (increased risk of bleeding) , during breastfeeding, in old age and in children.
Sodium heparin is discontinued before thrombolytic therapy; the next administration is possible after thrombolysis and the return of thrombin time and/or aPTT to double control values or lower (usually after 2-4 hours).
Instructions for use ACTILYSE
The most common adverse reaction associated with the use of Actilyse is bleeding (> 1:100, <1:
- 10 - massive bleeding;
- >1:10 - any bleeding), leading to a decrease in hematocrit and/or hemoglobin. Bleeding may occur in any part or cavity of the body and result in a life-threatening situation, temporary disability, or death.
Bleeding events associated with thrombolytic therapy can be divided into two main categories:
- external bleeding (usually from puncture sites or damage to blood vessels);
- internal bleeding in any part or cavity of the body.
The following neurological symptoms may be associated with intracranial bleeding:
- drowsiness, aphasia, hemiparesis, convulsions.
The incidence of fat embolism, which was not observed in patients participating in clinical trials, is based on spontaneous reporting.
Compared with studies in myocardial infarction, the number of patients with pulmonary embolism and cerebral infarction who participated in clinical trials (within the therapeutic window of 0-4.5 hours from the onset of symptoms of these diseases) was very small. Therefore, the small numerical differences noted when compared with data obtained in myocardial infarction were most likely a consequence of the small sample size. Apart from intracranial hemorrhage as a side effect in stroke and reperfusion arrhythmias as a side effect in myocardial infarction, there is no clinical reason to assume qualitative and quantitative differences in the spectrum of side effects of Actilyse when used in pulmonary embolism and acute cerebral infarction, or in myocardial infarction.
Immune system disorders:
anaphylactoid reactions, which are usually mild, but in some cases can be life-threatening;
- possible - rash, urticaria, bronchospasm, angioedema, hypotension, shock or any other allergic reactions.
- embolism, which can lead to corresponding consequences from the affected internal organs;
- bleeding from parenchymal organs, for example, hepatic bleeding and pulmonary hemorrhage.
- retroperitoneal bleeding (retroperitoneal hematoma);
- nausea;
- vomit.
- increase in body temperature.
If these reactions develop, conventional antiallergic therapy should be used. It was found that in a relatively large proportion of patients with such reactions, angiotensin-converting enzyme inhibitors were simultaneously used. Anaphylactoid reactions (due to IgE) are not known with Actilyse. In rare cases, transient formation of antibodies to Actilyse (in low titers) was observed, but the clinical significance of this phenomenon has not been established.
Visual disorders:
hemorrhage in the eyeball.
Cardiac disorders:
pericardial bleeding.
Vascular disorders:
bleeding (such as a hematoma);
Respiratory, thoracic and mediastinal disorders:
bleeding from the respiratory tract, such as pharyngeal bleeding, hemoptysis, nosebleeds.
Gastrointestinal disorders:
gastrointestinal bleeding, such as - stomach bleeding, bleeding from a stomach ulcer, bleeding from the rectum, hematemesis, melena, bleeding from the mouth, bleeding from the gums;
Skin and subcutaneous tissue disorders:
ecchymoses.
Renal and urinary tract disorders:
urogenital bleeding, such as hematuria, bleeding from the urinary tract.
General disorders and reactions at the injection site:
bleeding at the injection site, punctures, such as hematoma at the catheter site, bleeding at the catheter site.
Reactions identified during special studies:
decrease in blood pressure;
Damage, toxic effects and complications due to procedures associated with the use of the drug:
fat embolism, which can lead to corresponding consequences from the affected internal organs.
Other:
need for blood transfusion.
Side effects when used for myocardial infarction:
Cardiac disorders:
reperfusion arrhythmias - arrhythmia, extrasystole, atrial fibrillation, atrioventricular block from the first degree to complete block, bradycardia, tachycardia, ventricular arrhythmia, ventricular fibrillation, ventricular tachycardia, occur in close temporal connection with Actilyse therapy.
Reperfusion arrhythmias can lead to cardiac arrest, be life-threatening, and require the use of conventional antiarrhythmic therapy.
Side effects when used for myocardial infarction and pulmonary embolism:
Nervous system disorders:
intracranial hemorrhage, namely cerebral hemorrhage, cerebral hematoma, intracranial hematoma, subarachnoid hemorrhage.
Side effects when used for acute cerebral infarction:
Nervous system disorders:
intracranial hemorrhage, namely cerebral hemorrhage, cerebral hematoma, hemorrhagic transformation of stroke, intracranial hematoma, subarachnoid hemorrhage.
The main adverse event was clinically significant intracerebral hemorrhage (up to 10% of patients). However, this was not reflected in increased rates of mortality and permanent disability.
Note!
Description of the drug Actilyse Lyof. d/r-ra d/inf. 50mg fl. + solution fl. 50ml No. 1*** on this page is a simplified author’s version of the apteka911 website, created on the basis of the instructions for use.
Before purchasing or using the drug, you should consult your doctor and read the manufacturer's original instructions (attached to each package of the drug). Information about the drug is provided for informational purposes only and should not be used as a guide to self-medication. Only a doctor can decide to prescribe the drug, as well as determine the dose and methods of its use.
Compound
- active ingredient: alteplase;
- 1 bottle of lyophilisate for solution for infusion contains alteplase 50 mg;
- 1 bottle of solvent contains sterile water for injection 50 ml.
Alteplase is produced by recombinant DNA technology using Chinese hamster ovarian cells. The specific activity of the manufacturer's alteplase standard is 580,000 IU/mg, which was confirmed in comparison with the second WHO international standard for t-PA. The specific activity of alteplase is 522,000 - 696,000 IU/mg; other components: L-arginine, phosphoric acid, polysorbate 80.
Storage conditions
Store in original packaging at a temperature not exceeding 25 °C out of the reach of children.
Shelf life – 3 years.
The prepared solution can be stored at 2-8 C for 24 hours or for 8 hours at a temperature not exceeding 25 C.
If the medicine is not used immediately after reconstitution, the user is responsible for the period and storage conditions (no more than 24 hours at a temperature of 2-8 ° C).
Incompatibility. The resulting solution can be further diluted with sterile saline 0.9% (9 mg/ml) for injection to obtain a minimum concentration of 0.2 mg alteplase per 1 ml.
The resulting solution is not recommended to be diluted in water for injection or in infusion solutions based on carbohydrates, such as dextrose, due to the possible turbidity of the diluted solution.
ACTILYSE should not be mixed with other drugs in any infusion bottle or intravenous system (even with heparin).
Product description certified by the manufacturer Boehringer Ingelheim
.
Verified by
Likar Turumkulova Irina
Features of application
Use during pregnancy or breastfeeding
Pregnancy. The amount of data on the use of Actilyse during pregnancy is limited. Preclinical studies using alteplase at doses higher than those used in humans have shown fetal effects and/or embryotoxicity secondary to the known pharmacological activity of the drug. Alteplase is not considered teratogenic. In acute life-threatening illnesses, the benefit should be weighed against the potential risk.
Lactation. It is unknown whether alteplase passes into breast milk.
Children
Experience with the use of the drug Actilyse in children is limited. ACTILYSE is contraindicated for the treatment of acute ischemic stroke in children under 16 years of age. The dose for the treatment of acute ischemic stroke in children 16-17 years old corresponds to the dose for adults. For other indications, the use of the drug in children (under 18 years of age) is contraindicated.
There are no clinical data on the use of Actilyse in children in the treatment of acute massive pulmonary embolism.
There are no clinical data on the use of ACTILYSE in children in the treatment of myocardial infarction.
The ability to influence the reaction rate when driving vehicles or other mechanisms
Not applicable.
Overdose
If the maximum recommended dose is exceeded, the risk of intracranial bleeding increases.
Despite the relative fibrin specificity, after an overdose, a clinically significant decrease in fibrinogen and other components of blood coagulation is possible.
Treatment
In most cases, it is enough to wait for the physiological regeneration of these factors after completion of Actilyse therapy. However, if severe bleeding occurs, fresh frozen plasma infusion is recommended, and synthetic antifibrinolytics can be prescribed if necessary.
