Study of the pharmacokinetics of non-immunogenic staphylokinase in patients with acute myocardial infarction and acute ischemic stroke

The aim. To investigate the pharmacokinetic parameters of non-immunogenic staphylokinase (Fortelyzin®, SuperGene LLC, Russia) in patients with acute myocardial infarction with ST-segment elevation (STEMI) on the electrocardiogram and in patients with ischemic stroke.

Materials and methods. The clinical study was conducted in 50 patients with STEMI after a single intravenous administration of non-immunogenic staphylokinase at a dose of 15 mg and in 50 patients with ischemic stroke after a single intravenous administration of the drug at a dose of 10 mg. The main pharmacokinetic parameters were determined: half-life, initial concentration, volume of distribution, clearance, and area under the pharmacokinetic curve.

Results. As a result of the study of the pharmacokinetics of non-immunogenic staphylokinase, it was found that after a single intravenous administration of the drug at a dose of 15 mg, the initial concentration was 7.1 ± 2.7 μg/mL, the half-life was 5.77 ± 0.72 min, the clearance was 0.33 ± 0.04 l/min, and the area under the pharmacokinetic curve (AUC_0-t) was 42.9 ± 3.2 μg/mL*min. After administration of the drug at a dose of 10 mg, the initial concentration was 2.8 ± 0.3 μg/ml, the half-life was 5.11 ± 0.56 min, the clearance was 0.35 ± 0.06 l/min, and the area under the pharmacokinetic curve (AUC_0-t) was 28.5 ± 3.6 μg/mL*min. The terminal half-life was 32 min in both dosage regimens.

Conclusion. It was found that non-immunogenic staphylokinase is characterized by a short half-life and high clearance, which ensures the safety of the drug in clinical practice. The peculiarities of the pharmacodynamics of non-immunogenic staphylokinase, associated with its interaction with plasmin in the thrombus and subsequent recirculation of released drug molecules, allow it to be used in low doses, regardless of the patient’s body weight, despite the short half-life.

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