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After administration of tenecteplase observed dose-α2-antiplasmin consumption (plasmin inhibitor in the liquid phase) with a consequent increase in systemic plasmin concentration that the intended effect of plasminogen activation. In comparative studies in patients who received the maximum dose tenecteplase (10,000 U, eq. 50 mg) decreased fibrinogen concentrations less than 15% and a plasminogen concentration of less than 25%, and dianabol cycle use of alteplase decreased the concentration of fibrinogen and plasminogen approximately 50%. After 30 days after the start of Metalize antibodies were not detected for tenecteplase.
Angiographic data show that a single intravenous administration of tenecteplase promotes recanalization of the artery due to thrombosis which developed acute myocardial infarction. This effect is dose-dependent. The use of tenecteplase reduces mortality from myocardial infarction (6.2% after 30 days). When applying the frequency of bleeding tenecteplase (except intracranial) was 26.4% (lower than with alteplase – 28.9%). Therefore, the need for transfusion therapy using tenecteplase significantly lower (4.3% tenecteplase group and 5.5% in alteplase group). The frequency of intracranial haemorrhage was 0.93% in the tenecteplase and 0.94% in the alteplase group. In cases where treatment was started later than 6 hours after the appearance of symptoms of myocardial infarction, use of tenecteplase (versus alteplase) has advantages in terms of 30-day mortality (4.3% in the group tenecteplase and 9.6% in the alteplase), stroke rate (0.4% and 3.3%, respectively) and the frequency of intracranial hemorrhage (1.7%, and 0%, respectively).

Pharmacokinetics
tenecteplase output from the bloodstream by binding to receptors in liver and degradation with the formation of small peptides. After a single injection of tenecteplase in patients with acute myocardial infarction observed biphasic elimination of tenecteplase antigen from blood plasma. When using the drug at therapeutic doses, depending on the nature of excretion of the administered dose tenecteplase not observed. The initial half-life is 24 ± 5,5 min. (mean +/- standard deviation), that is 5 times the half-life of natural tissue plasminogen activator. The final half-life is 129 ± 87 min; plasma clearance – 119 ± 49 ml / min.

With increased body mass observed a moderate increase in the plasma clearance with increasing age marked decrease in this indicator. In women, plasma clearance parameters are generally lower than in men, which may be explained by a lower body weight of women.

Tenecteplase is excreted in the bile, so it is assumed that the renal function does not alter the pharmacokinetics METALIZE. pharmacokinetic study with abnormal liver function have not been conducted.

Indications
Thrombolytic therapy of acute myocardial infarction (AMI).

Contraindications

  • diseases accompanied by significant bleeding within the last 6 months, hemorrhagic diathesis;
  • concomitant use of oral anticoagulants (international standardized index> 1.3);
  • central nervous system (CNS) in history (neoplasm, aneurysm, surgery on the brain and spinal cord);
  • severe uncontrolled hypertension;
  • major surgery, biopsy of parenchymal organ, or significant trauma within the past 2 months (including injury combined with acute myocardial infarction at the moment), recently transferred head injuries;
  • prolonged or traumatic cardiopulmonary resuscitation (> 2 minutes) within the past 2 weeks;
  • severe hepatic dysfunction, including hepatic failure, cirrhosis, portal hypertension (including with esophageal varices..) and active hepatitis;
  • Diabetic haemorrhagic retinopathy or other haemorrhagic diseases of the eye;
  • gastric ulcer or duodenal ulcer in the acute stage;
  • artery dianabol cycle aneurysm or the presence of arterial / venous vascular malformations;
  • neoplasm with increased bleeding risk;
  • Acute pericarditis and / or subacute bacterial endocarditis;
  • acute pancreatitis;
  • sensitivity to the active ingredient (tenecteplase), or to any other component of the preparation.

Precautions
In the following cases, the appointment METALIZE should carefully assess the extent of the expected benefits and the possible risk of bleeding:

  • systolic blood pressure> 160 mm Hg;
  • stroke or transient ischemic attack in history;
  • recently transferred bleeding from the gastrointestinal or urogenital tract (within the past 10 days);
  • recently made an intramuscular injection (within the past 2 days);
  • advanced age (over 75 years);
  • low body weight <60 kg;
  • cerebrovascular diseases

Pregnancy and lactation
Experience with METALIZE in pregnant women available. No data on the excretion of tenecteplase in breast milk. It is necessary to correlate the degree of possible risks and anticipated benefits in the appointment of the drug in the case dianabol cycle of AMI during pregnancy and lactation. anabolic steroids online shop

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