Actilyse (Alteplase) 50mg, vial 50ml

The composition and form of issue:

Powder dried for solution for infusion. 1 flask contains:

Alteplase 50 mg

excipients: L-arginine — 1742 mg phosphoric acid 536 mg Polysorbate 802 — <5 mg 

1 ml of the solution after dilution contains:

Alteplase 1 mg

excipients: L-arginine — to 34.84 mg of phosphoric acid of 10.72 mg Polysorbate 802 — <0.1 mg 

1 — the specific activity of alteplase 580 IU/mg. This corresponds to the second international who standard for TPA (tissue plasminogen activator). The specific activity of alteplase varies in different batches from 522 to 696 IU/mg. 

2 — in different batches, the amount of Polysorbate 80 may vary, but 1 ml of the dissolved drug should not be more than 0.1 mg 

3 — divorce in 50 ml of water for injection, pH of this solution: 7,3±0,5 

in sterile glass vials of 50 ml volume, complete with solvent (water for injection) in vials of 50 ml in the box 1 set.

Pharmacokinetics:

After the on/in the rapidly distributed. T1/2 alpha 4-5 minutes, i.e. 20 min in plasma is less than 10% of the initial quantity of the drug. T1/2 beta of remaining in the depot number — 40 min. is Metabolized mainly in the liver (Cl plasma 550-680 ml/min).

Description pharmacological action:

At/in the alteplaza relatively inactive in the blood. Is activated by binding to fibrin and induces the conversion of plasminogen to plasmin, promoting the dissolution of fibrin clot.

Dosage:

Manual.

Indications:

Acute myocardial infarction (first 6 to 12 hours), acute massive pulmonary embolism.

Contraindications:

Haemorrhagic diathesis, concomitant use of anticoagulants, internal bleeding (including recent), cerebrovascular disease (including 6-month history), tumors with a high risk of bleeding, aneurysms and malformations of vessels, intracranial or spinal surgical intervention during the 2 preceding months, hemorrhagic retinopathy, the period up to 10 days after severe trauma, traumatic open heart massage, extensive surgical operations, childbirth, and puncture of vessels with low pressure, including the subclavian and jugular veins, severe uncontrolled hypertension, bacterial endocarditis, pericarditis, acute pancreatitis, ulcers disease stomach and duodenal ulcers within 3 months after the exacerbation, liver failure, cirrhosis, portal hypertension, accompanied by varicose veins of the esophagus, active hepatitis.

Relative: minor injuries in recent medical history: biopsy, puncture of vessels to/m injection, heart massage, etc. conditions associated with risk of bleeding.

Application of pregnancy and breast-feeding:

Perhaps if the expected effect therapy outweighs the potential risk to the fetus (experience of pregnancy and breastfeeding is limited).

Side effects:

Bleeding: external (from the place puncture damaged receptacles nose, gums) and internal (gastrointestinal tract, urogenital tract, retroperitoneal space, Central nervous system, including intracranial (1%), parenchymatous organs) arrhythmias (with successful recanalization of coronary arteries in patients with acute myocardial infarction), is rarely — cholesterol or thrombotic embolism, incl. kidney renal failure, nausea, vomiting and reduction of AD (can be symptoms of myocardial infarction).

Drug interactions:

Bleeding risk increases with concurrent use of coumarin derivatives, antiplatelet agents, heparin and other drugs, oppressive blood clotting.

Method of application and dose:

Contents of bottle dissolved in water for injection to a concentration of 1 mg/ml (the resulting solution can be further diluted with sterile 0.9 percent saline solution until the minimum concentration 0.2 mg/ml).

Myocardial infarction in the period up to 6 h after the onset of symptoms patients with body weight more than 65 kg — 15 mg in bolus, then 50 mg as an infusion over 30 min and then 35 mg over 1 h, until the total dose 100 mg When assigning 6-12 hours of onset of symptoms 10 mg in bolus, then, in the form of infusions 50 mg during the first 60 min and then 10 mg every 30 minutes up to a total dose 100 mg over 3 h in patients with body weight less than 65 kg total dose should not exceed 1.5 mg/kg. Secondary therapy — appointment of acetylsalicylic acid (as soon as possible and within the first months after myocardial infarction) and heparin (24 hours or longer) recommended bolus dose of 5000 UNITS and then infuzionno in the regime of 1000 IU/h. the Treatment to control activated partial thromboplastin time (APTT), which should not exceed the original more than 1.5–2.5 times.

When pulmonary embolism: 10 mg IV bolus over 1-2 min, and 90 mg as an infusion over 2 h, until reaching a total dose of 100 mg. Total dose when body weight less than 65 kg should not exceed 1.5 mg/kg. adjunct therapy: if APTT after applying Actilyse above baseline is less than 2 times, should be prescribed heparin or continue treating them (under the control of the APTT, which should not exceed the original more than 1.5–2.5 times).

Overdose:

Symptoms: hemorrhagic complications: bleeding, external and internal (digestive tract, urinary organs, in the retroperitoneal space and the CNS).

Treatment. In most cases it is sufficient to await the physiological regeneration of these factors after cessation of therapy Actilyse, due to short T1/2 of the drug. For serious bleeding — the introduction of fresh frozen plasma or fresh whole blood, plasma-substituting solutions in case of need — purpose synthetic antifibrinolitikov.

Precautions:

Note that doses above 100 mg, increasing the risk of intracranial hemorrhage. The experience in children is limited. In the event of anaphylactic reaction, discontinue the infusion and start symptomatic therapy.

Special instructions:

Actilyse not mix with other drugs (not even with heparin) no General vial for infusions or in a common catheter.

Storage conditions:

The prepared solution in the refrigerator for up to 24 h at a temperature not exceeding 25 °C up to 8 h