Buy Actilyse vials 50 mg
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Actilyse [Alteplase]

Boehringer Ingelheim
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2019-09-19
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Clinical Pharmacology

Thrombolytic. Recombinant human tissue plasminogen activator, glycoprotein.
With the on / in the introduction of the drug is relatively inactive in the systemic circulation. Activated after binding to fibrin, inducing the conversion of plasminogen to plasmin, which leads to the dissolution of the fibrin clot.
The use of Actilyse reduces the release of the enzyme alpha-hydroxybutyrate dehydrogenase.
The use of Actilyse at a dose of 100 mg for 90 minutes together with iv injection of heparin in more than 40,000 patients with acute myocardial infarction (GUSTO study) resulted in a decrease in 30-day mortality (6.3%) compared with the use of streptokinase (1.5 million units for 60 min) simultaneously with sc or v / v heparin administration (7.3%). It was shown that after 60 min and 90 min of thrombolysis in patients receiving Actilise, a higher incidence of vascular patency in the infarction area was detected than with the use of streptokinase. 180 minutes after the start of therapy and later differences in the frequency of vascular patency is not observed.
When using Actilyse, there was a decrease in 30-day mortality after myocardial infarction compared with patients who did not receive thrombolytic therapy.
In patients treated with Actilyse, compared with patients who did not receive thrombolytic therapy, there was less significant damage to the overall function of the left ventricle of the heart and local wall mobility.
A placebo-controlled study (LATE) showed that the use of Actilyse at a dose of 100 mg for 3 hours in patients with myocardial infarction (in the case of initiation of therapy within 6-12 hours after the onset of symptoms) resulted in a decrease in 30-day mortality compared to placebo. The therapeutic effect in patients with confirmed myocardial infarction was also observed in cases where treatment began within 24 hours after the onset of symptoms.
In patients with acute massive embolism of the pulmonary artery, accompanied by unstable hemodynamics, the use of Actilyse leads to a rapid decrease in the size of a blood clot and a decrease in pressure in the pulmonary artery, however, there are no data on mortality.
In two studies conducted in the United States (NINDS A / B), which studied the effect of the drug on stroke (within the first 3 hours after the onset of symptoms), more frequent achievement of a favorable result (no disability of patients or minimal severity of these disorders) compared to placebo.
In the case of initiation of therapy at a later date, the effectiveness of the drug decreases, as was shown in two European studies and in an additional study conducted in the United States.
The results of a meta-analysis of all patients receiving therapy during the first 3 hours after the onset of a stroke confirmed the positive effect of alteplase.
Despite the increased risk of serious and even fatal intracranial hemorrhages, the likelihood of a favorable outcome of therapy compared with placebo was 14.9% (95% confidence intervals: 8.1% and 21.7%). These data do not allow a definite conclusion regarding the effect of therapy on mortality. The benefit / risk ratio in the case of alteplase within 3 hours after the onset of a stroke (taking into account the above warnings) can be generally considered favorable, although research data do not allow an unequivocal conclusion regarding the effect of therapy on mortality.
A meta-analysis of all available clinical data shows that alteplase is less effective in patients whose treatment begins 3-6 hours after the onset of symptoms, compared with therapy undertaken in the first 3 hours after the development of clinical manifestations. At the same time, the risk of complications of stroke therapy is higher in the first case, which leads to an unfavorable outcome of the benefit / risk ratio.
Due to the relative specificity for fibrin, the use of alteplase at a dose of 100 mg leads to a moderate decrease in the level of circulating fibrinogen (up to about 60% after 4 hours), which by 24 hours usually increases by more than 80%. Concentrations of plasminogen and alpha-2-antiplasmin decrease after 4 hours, respectively, to 20% and 35% of baseline levels, and after 24 hours they increase again to more than 80%. A significant and prolonged decrease in the level of circulating fibrinogen was observed only in a small number of patients.

Indications

- thrombolytic therapy of acute myocardial infarction in the first 6 hours after the development of symptoms (90-minute / accelerated / dosing regimen);
- thrombolytic therapy of acute myocardial infarction in the period from 6 to 12 hours after the development of symptoms (3-hour dosing regimen);
- thrombolytic therapy of acute massive pulmonary thromboembolism, accompanied by unstable hemodynamics, the diagnosis should be, if possible, confirmed objectively (for example, pulmonary angiography or non-invasive methods, for example, lung tomography). Clinical studies on mortality and long-term results of treatment of pulmonary embolism have not been conducted;
- thrombolytic therapy of acute ischemic stroke (shown only if administered within 3 hours after the onset of stroke symptoms, and if intracranial hemorrhage / hemorrhagic stroke / is excluded using appropriate imaging techniques, such as computed tomography of the brain).

Composition

1 fl. contains alteplaza 50 mg.

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Actilyse [Alteplase]

Dosage and Administration

Actilyse should be applied as early as possible from the onset of symptoms.
Withmyocardial infarction with a 90-minute (accelerated) dosing regimen for patients in whom treatment can be initiated within 6 h after the development of symptoms,the drug is administered at a dose of 15 mg i.v. in a jet, then 50 mg as an intravenous infusion for the first 30 minutes, followed by an infusion of 35 mg for 60 minutes until the maximum dose of 100 mg is reached.
In patients with a body weight of less than 65 kg, the dose of the drug should be calculated depending on the body weight. Initially, the drug is prescribed in a dose of 15 mg IV bolus, then 750 μg / kg body weight (maximum 50 mg) for 30 minutes IV a drip, followed by infusion of 500 μg / kg (maximum 35 mg) for 60 minutes .
Withmyocardial infarction with a 3-hour dosing regimen for patients in whom treatment can be initiated between 6 h and 12 h after the development of symptoms, the drug is prescribed at a dose of 10 mg IV bolus, then 50 mg as an intravenous infusion for the first hour, followed by an IV infusion of 10 mg for 30 minutes until the maximum dose of 100 mg is reached within 3 hours.
In patients with a body weight of less than 65 kg, the total dose should not exceed 1.5 mg / kg.
The recommended maximum dose of Actilyse in acute myocardial infarction is 100 mg.
Auxiliary therapy: Acetylsalicylic acid should be prescribed as soon as possible after the onset of thrombosis and continue to be taken during the first months after a myocardial infarction. The recommended dose is 100-300 mg / day. At the same time, heparin should be used for a period of 24 hours or more (with an accelerated dosing regimen of at least 48 hours). It is recommended to start with iv injection of heparin at a dose of 5000 U / h before starting thrombolytic therapy. Subsequently, heparin is administered infusionally at a rate of 1000 U / h. The dose of heparin should be adjusted depending on the results of repeated determination of the APTT (values ​​should be 1.5-2.5 times the initial level).
Withpulmonary embolism Actilyse is administered in a total dose of 100 mg for 2 hours. The greatest experience was obtained using the following dosing regimen: first, the drug is administered at a dose of 10 mg IV in a jet for 1-2 minutes, then 90 mg IV drip for 2 h. In patients with a body weight less than 65 kg, the total dose should not exceed 1.5 mg / kg body weight.
Auxiliary therapy: after the use of Actilyse, if the APTT is less than 2 times the initial level, heparin should be prescribed (or continued). Further infusion is also carried out under the control of APTT, which should not exceed the baseline level more than 1.5-2.5 times.
Withischemic stroke The recommended dose is 900 mcg / kg (maximum 90 mg), as an intravenous infusion for 60 minutes after the initial intravenous injection dose of 10% of the total dose. Therapy should be started as soon as possible after the onset of symptoms (preferably within 3 hours).
Auxiliary therapy: The safety and efficacy of the above treatment regimen, used in combination with heparin and acetylsalicylic acid in the first 24 hours after the onset of symptoms, are not well understood. In this regard, in the first 24 hours after the start of therapy, the use of acetylsalicylic acid or iv heparin should be avoided. If the use of heparin is required for other indications (for example, for the prevention of deep vein thrombosis), its dose should not exceed 10,000 IU per day, while the drug is injected s / c.

Adverse reactions

The most common side effect is bleeding, leading to a decrease in hematocrit and / or hemoglobin.
Bleeding associated with thrombolytic therapy can be divided into two main categories:
- external bleeding (as a rule, from puncture sites or damage to blood vessels);
- internal bleeding from the gastrointestinal tract, urinary tract, bleeding in the retroperitoneal space, bleeding in the brain or bleeding from parenchymal organs.
The data below is based on the results of clinical studies of Actilyse in 8299 patients with acute myocardial infarction.
A case of cholesterol crystal embolization that was not observed in a population of patients who participated in clinical trials is based on a separate report.
Compared to studies on myocardial infarction, the number of patients with pulmonary embolism and stroke who participated in clinical studies (within 0–3 hours from the onset of symptoms of these diseases) was very small. Therefore, the small numerical differences noted in comparison with the data obtained during myocardial infarction were most likely the result of a small sample size. In addition to 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 side effects of Actilise in the case of its use in pulmonary embolism and acute ischemic stroke, or with myocardial infarction.
Side effects noted when using for myocardial infarction
Often: reperfusion arrhythmias that can be life-threatening and require the use of conventional antiarrhythmic therapy.
Side effects noted when using for myocardial infarction and pulmonary embolism
Seldom: intracranial hemorrhage.
Side effects noted with acute ischemic stroke
Often: intracranial hemorrhage. The main adverse event was clinically significant intracranial hemorrhage (their incidence reached 10%). However, an increase in the frequency of complications or total mortality has not been established.
It was.
Side effects noted when using for myocardial infarction, pulmonary embolism and acute ischemic stroke
Often: external bleeding, usually from puncture sites or from damaged blood vessels, decreased blood pressure.
Often: gastrointestinal bleeding, nausea, vomiting (nausea and vomiting could also be symptoms of myocardial infarction), increased body temperature, bleeding from the urinary tract, nosebleeds, ecchymosis.
Infrequently: hemorrhages in the retroperitoneal space, bleeding from the gums, thromboembolism, which can be accompanied by the corresponding consequences of the affected internal organs. Anaphylactoid reactions were noted (usually mild, but in some cases can be life-threatening); rashes, urticaria, bronchospasm, angioedema, hypotension, shock or any other allergic reaction are possible. In the case of the development of these reactions should be applied generally accepted antiallergic therapy. It was established that a relatively large proportion of patients with similar reactions simultaneously used ACE inhibitors. Anaphylactic reactions (i.e. due to IgE) are unknown to Actilyse.
Seldom: transient formation of antibodies to Actilyse (in low titers), but the clinical significance of this phenomenon has not been established; cholesterol crystal embolization, which can lead to corresponding consequences on the part of the affected internal organs; bleeding from parenchymal organs.
Often it was necessary to have a blood transfusion.

- hemorrhagic diathesis;
- bleeding now or within the previous 6 months;
- simultaneous administration of oral anticoagulants (for example, warfarin; international normalized ratio> 1.3);
- diseases of the central nervous system in history (including neoplasms, aneurysm);
- surgery on the brain or spinal cord;
- intracranial (including subarachnoid) hemorrhage at present or in history;
- suspected hemorrhagic stroke;
- severe uncontrolled arterial hypertension;
- extensive surgery or severe injury during the previous 10 days (including any injury in combination with this acute myocardial infarction);
- recent traumatic brain injury;
- prolonged or traumatic cardiopulmonary resuscitation (more than 2 min), giving birth within the previous 10 days;
- recently produced puncture of incompressible blood vessels (for example, subclavian and jugular vein);
- hemorrhagic retinopathy (including diabetes mellitus), which may indicate visual impairment;
- other hemorrhagic diseases of the eye;
- bacterial endocarditis;
- pericarditis;
- acute pancreatitis;
- confirmed gastric ulcer and duodenal ulcer in the last 3 months;
- severe liver diseases, including liver failure, liver cirrhosis, portal hypertension (with esophageal varices), active hepatitis;
- artery aneurysm, congenital malformations of arteries and veins;
- neoplasms with an increased risk of bleeding;
- Hypersensitivity to the drug.
In the case of the use of the drug for the treatment of acute myocardial infarction and pulmonary embolism, in addition to the above contraindications, there is the following contraindication:
- A history of stroke.
In the case of the use of the drug for the treatment of acute ischemic stroke, in addition to the above contraindications, there are the following contraindications:
- the onset of symptoms of ischemic stroke more than 3 hours before the start of the infusion, or the lack of accurate information about the time of onset of the disease;
- rapid improvement in acute ischemic stroke or mild symptoms by the time of the start of the infusion;
- severe stroke, based on clinical data (for example, if NIHSS is> 25) and / or according to the results of appropriate imaging methods;
- convulsions at the beginning of a stroke;
- information about a stroke or a serious head injury during the previous 3 months;
- the occurrence of a previous stroke on the background of diabetes;
- use of heparin within 48 hours before the onset of the stroke, if at the given moment of time the activated partial thrombin time is increased (APTT);
- use of antiplatelet agents at the time of infusion and within 24 hours after infusion;
- platelet count less than 100 000 / mm3*;
- systolic blood pressure above 185 mm Hg. Art., or diastolic blood pressure above 110 mm Hg. Art., or it is necessary to use intensive therapy (IV the introduction of drugs) to reduce blood pressure to these boundaries;
- blood glucose level less than 50 mg / dl or more than 400 mg / dl.

Contraindications

The drug Actilyse is not indicated for the treatment of acute stroke in children and adolescents under the age of 18 years and in adults over the age of 80 years.

Drug interactions

There have been no special studies on the interaction of Actilize with other drugs commonly used in acute myocardial infarction.
The use of drugs that affect blood coagulation or alter platelet function, before, during or after initiating therapy, can increase the risk of bleeding.
The simultaneous use of ACE inhibitors may increase the risk of anaphylactoid reactions. These reactions were observed in a relatively large proportion of patients receiving ACE inhibitors.
Pharmaceutical Interaction
The drug Actilyse should not be mixed with other drugs (even with heparin), neither in the vial for infusion, nor in the general system for iv administration.

Pregnancy and Lactation

The clinical experience of using Actilyse during pregnancy and lactation is limited. The issue of isolating alteplazy with breast milk has not been studied.
If necessary, the use of the drug (diseases that directly threaten life) during pregnancy and lactation should assess the expected benefits of therapy for the mother and the potential risk to the fetus or infant.

Special instructions

In the following cases, when Actilyse is prescribed, the degree of perceived benefit and possible risk of bleeding should be carefully evaluated:
- a recent intramuscular injection or minor recent interventions, such as a biopsy, puncture of large vessels, heart massage during resuscitation;
- diseases (not mentioned in the list of contraindications) for which the risk of bleeding is increased.
In the treatment of acute myocardial infarction and acute pulmonary embolism, the drug should be used with caution:
- with systolic blood pressure above 160 mm Hg. v .;
- in old age, when the risk of intracranial hemorrhage may increase. Since in elderly patients the probability of a positive outcome of this treatment also increases, a careful evaluation of the benefit / risk ratio is necessary.
In the treatment of acute ischemic stroke, the drug should be used with caution, because the use of Actilyse in this category of patients (compared to the use of this drug for other indications) is accompanied by a markedly increased risk of intracranial hemorrhage, since the bleeding occurs mainly in the necrotic area.
This should especially be taken into account in the following cases:
- all conditions listed in the section "Contraindications", and in general, all conditions characterized by a high risk of bleeding;
- the presence of small asymptomatic cerebral vascular aneurysms;
- in patients who have previously been treated with acetylsalicylic acid or other antiplatelet agents, an increased risk of intracerebral hemorrhage is possible, especially if the use of Actilyse was started at a later date. Given the increased risk of cerebral hemorrhage, the dose of alteplase used should not exceed 900 mcg / kg (the maximum dose is 90 mg).
Treatment should not begin later than 3 hours after the onset of symptoms, due to an unfavorable benefit / risk ratio, due to the following circumstances:
- The positive effect of treatment decreases with late initiation of therapy;
- mortality increases mainly in patients who previously received acetylsalicylic acid;
- the risk of bleeding increases.
Treatment Actilyse should be carried out by a physician with experience in thrombolytic therapy and the ability to control its effectiveness. When using Actilyse, it is recommended to have available standard resuscitation equipment and appropriate medicines.
Bleeding is the most common complication of Actilyse therapy. The simultaneous use of heparin may contribute to the occurrence of bleeding. As Actilyse dissolves fibrin, bleeding from recent puncture sites may occur. Therefore, thrombolytic therapy requires careful monitoring of areas of possible bleeding (including the insertion of a catheter, arterial and venous punctures, incisions and injections). The use of hard catheters, intramuscular injections and unreasonable manipulations during the treatment of Actilyse should be avoided.
In the event of severe bleeding, especially cerebral, fibrinolytic therapy, as well as the use of heparin should be immediately discontinued. If heparin was used for 4 hours prior to the onset of bleeding, consideration should be given to the advisability of using protamine. In rare cases where the above conservative measures are ineffective, the use of blood products may be indicated. Transfusion administration of cryoprecipitate, fresh frozen plasma and platelets can be prescribed in accordance with clinical and laboratory parameters, which are determined again after each injection. Infusion of cryoprecipitate is preferably carried out to achieve a fibrinogen concentration of 1 g / l. You can consider the use of antifibrinolytic agents (for example, tranexamic acid), but no special studies have been conducted.
In acute myocardial infarction and pulmonary embolism, Actilise should not be used in a dose exceeding 100 mg, and in acute ischemic stroke in a dose of more than 90 mg, since increases the risk of intracranial hemorrhage.
After the end of treatment, stable formation of antibodies to the recombinant human tissue tissue activator plasminogen was not observed. Systematic experience re-use of Actilyse is not available. In case of anaphylactoid reaction, the infusion should be stopped and appropriate treatment should be prescribed. Regular monitoring of treatment tolerability is recommended, especially for patients who simultaneously receive ACE inhibitors.
In the treatment of acute myocardial infarction, the following precautions should also be kept in mind:
- coronary thrombolysis may lead to arrhythmias associated with reperfusion;
- Experience with the use of glycoprotein IIb / IIIa antagonists during the first 24 hours after the start of treatment is absent;
- the use of thrombolytic agents may increase the risk of thromboembolism in patients with thrombosis of the left heart, for example, with mitral stenosis or with atrial fibrillation.
In the treatment of acute stroke, the following precautions should be kept in mind.
Treatment should be carried out exclusively by an experienced doctor with skills and experience in providing intensive neurological care, in a specialized department, with the ability to conduct the full range of neuroimaging studies.
It is necessary to monitor blood pressure during treatment and within 24 hours after its completion. With an increase in systolic blood pressure above 180 mm Hg. Art. or diastolic blood pressure below 105 mm Hg. Art. recommended IV the use of antihypertensive drugs.
The therapeutic effect is reduced in patients who have had a previous stroke, or in the presence of uncontrolled diabetes. In such patients, the benefit / risk ratio is considered less favorable, although it still remains positive. In patients with a very small stroke, the risk exceeds the expected benefit, so the use of Actilyse is not recommended.
Patients with very severe stroke have an increased risk of intracranial bleeding and death. In these cases, Actilyse should not be used.
In patients with extensive cerebral infarctions, there is an increased risk of adverse outcome, including pronounced intracerebral hemorrhage and death. In such cases, the risk and benefit of therapy should be carefully weighed.
In stroke, the likelihood of a favorable outcome of treatment decreases with increasing age, as well as with increasing severity of stroke and with elevated levels of glucose in the blood. At the same time, the likelihood of a serious disability and death or serious intracranial hemorrhage increases, regardless of treatment. Actilyse should not be used in patients over 80 years of age, in the case of severe stroke (according to clinical data and / or according to imaging studies), and in cases where the initial blood glucose values ​​are less than 50 mg / dL or more than 400 mg / dL.
Reperfusion of the ischemic region can lead to swelling of the brain in the infarction area. Because of the increased risk of hemorrhage, the use of platelet aggregation inhibitors should not be started during the first 24 hours after thrombolysis with alteplase.
Use in Pediatrics
Currently, the experience of using Actilyse in children is limited.

Overdosage

Symptoms: despite the relative specificity for fibrin, overdose may have a clinically significant decrease in fibrinogen levels and blood coagulation factors.
Treatment: in most cases, a wait-and-see tactic is sufficient with a view to the physiological regeneration of these factors after the termination of the administration of Actilize.If severe bleeding occurs, transfusion of fresh frozen plasma or fresh whole blood is recommended, if necessary, synthetic antifibrinolytics can be prescribed.

  • Brand name: Actilyse
  • Active ingredient: Alteplaza
  • Dosage form: Lyophilized powder for solution for infusion.
  • Manufacturer: Boehringer Ingelheim
  • Country of Origin: Austria

Studies and clinical trials of Alteplase (Click to expand)

  1. Lesion-directed administration of alteplase with intracoronary heparin in patients with unstable angina and coronary thrombus undergoing angioplasty
  2. Efficiency of alteplase in the treatment of venous and arterial thrombosis in neonates
  3. Combined fibrinolysis using reduced-dose alteplase plus abciximab with immediate rescue angioplasty versus primary angioplasty with adjunct use of abciximab for the treatment of acute myocardial infarction: Asia-Pacific Acute Myocardial Infarction Trial (APAMIT) pilot study
  4. Facilitated primary coronary intervention with abciximab and very low dose of alteplase during off-hours compared with direct primary intervention during regular hours
  5. Stroke in a young patient treated by alteplase heralding an acquired thrombotic thrombocytopenic purpura
  6. Stability of alteplase in presence of cavitation
  7. Effects of liver blood flow on the pharmacokinetics of tissue-type plasminogen activator (alteplase) during thrombolysis in patients with acute myocardial infarction*
  8. Alteplase Use for Clotted Catheters
  9. Thrombolyse mit Alteplase 3 bis 4.5 Stunden nach akutem ischämischen Schlaganfall
  10. Behandlung einer schweren Lungenembolie bei Heparin-induzierter Thrombozytopenie Typ II (HIT II) mit Alteplase und Lepirudin
  11. Successful recanalization of an occluded coronary artery by percutaneous coronary intervention, systemic administration of tirofiban, a glycoprotein IIb/IIIa inhibitor, and intracoronary thrombolysis with alteplase
  12. Pilotstudie zur Wirksamkeit einer Kombinationstherapie einer reduzierten Dosis von Alteplase und dem Glykoprotein IIb/IIIa Antagonisten Tirofiban beim akuten Myokardinfarkt
  13. Spurious hyperphosphatemia in a patient with alteplase-locked central venous catheter
  14. Kathetergesteuerte intraarterielle Lysetherapie mit Alteplase bei peripheren Gefäß- und Bypassverschlüssen
  15. Intravenöse Thrombolyse mit Alteplase beim akuten ischämischen Schlaganfall
  16. Safety outcomes of Alteplase among acute ischemic stroke patients with special characteristics
  17. Effect of heparin, aspirin, or alteplase in reduction of myocardial ischemia in refractory unstable angina: Semeri GG, Gensini GF, Poggesi L, et al Lancet 335:615–618 Mar 1990
  18. Can we improve on front-loaded alteplase (r-TPA)?
  19. Alteplase (r-TPA) vs streptokinase
  20. Short and long alteplase dwells in dysfunctional hemodialysis catheters
  21. Thrombolysis With Alteplase: A Non-Invasive Treatment for Occluded Arteriovenous Fistulas and Grafts
  22. Effectiveness of Thrombolysis with Intravenous Alteplase for Acute Ischemic Stroke in Older Adults
  23. An Overview of the Patency and Stroke Rates Following Thrombolysis with Streptokinase, Alteplase, and Anistreplase Used to Treat an Acute Myocardial Infarction
  24. Trials of the European Working Party on Streptokinase and of the European Cooperative Study Group on Alteplase in Patients with Acute Myocardial Infarction

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