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Health

Zygrys

, medical expert
Last reviewed: 03.07.2025
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Zigris is an antithrombotic enzyme drug.

Indications Zygrys

It is used to eliminate sepsis with concomitant multiple organ failure in acute form (with a high risk of death).

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Release form

Released as a lyophilisate for the preparation of infusion solutions, in glass vials with a volume of 5 or 20 mg. The package contains 1 vial with powder.

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Pharmacodynamics

Drotrecogin-α (in its active form) is an external element of activated protein type C (this component plays an important role in modulating the systemic response of the human body to the infectious process). Protein type C in its active form has an effect on antithrombotic properties, inhibiting factors Va, as well as VIIIa. Data obtained from in vitro tests demonstrate that protein group C has an indirect profibrinolytic effect, because it is able to inhibit the element IAP-1, and in addition to this, limit the production of thrombin-activated element, which inhibits the process of fibrinolysis.

In addition, in vitro studies have shown that protein C has anti-inflammatory properties that arise from the suppression of monocyte-bound tumor necrosis factors, as well as from blocking leukocyte adhesion processes to selectin and limiting the thrombin-induced inflammatory response within the vascular endothelium in the microcirculatory system.

The mechanism by which active drotrecogin-α reduces mortality in people with severe sepsis is not yet fully understood. In people with severe sepsis, drug infusions lasting either 48 or 96 hours caused dose-dependent reductions in D-dimer levels, as well as IL-6.

Compared with placebo, drotrecogin-α users showed a faster decrease in IAP-1, D-dimer, and also prothrombin F1.2 with thrombin-antithrombin, as well as IL-6. In addition, an accelerated increase in antithrombin with protein type C and stabilization of plasminogen levels were detected.

Taking into account the duration of the infusion procedure, it was found that the peak medicinal effects of the active component of the drug relative to D-dimer indicators were observed at the end of the 96th hour of the infusion (in the amount of 24 mcg/kg/hour).

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Pharmacokinetics

Drotrecogin-α together with intrinsic active protein C are inactivated by intrinsic plasma protease inhibitors. The level of protein C in the plasma of healthy individuals, as well as individuals with severe sepsis, is often below the minimum detectable concentration.

In patients with severe sepsis, drug infusion at a rate of 12-30 mcg/kg/hour quickly forms equilibrium values proportional to the infusion intensity. Average drug clearance values are 40 l/hour (range 27-52 l/hour). Average equilibrium values of 45 ng/ml (range 35-62 ng/ml) were observed 2 hours after the start of the infusion procedure.

In many patients, plasma drotrecogin-α levels decreased below the detectable threshold of 10 ng/mL within 2 hours of completion of the infusion. Drug clearance in people with severe sepsis is approximately 50% higher than in healthy individuals.

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Dosing and administration

The infusion is administered intravenously at a rate of 24 mcg/kg/hour. The entire infusion procedure should last for 96 hours.

An interrupted infusion should be resumed at the standard rate stated above. Dosage increases or bolus injections should not be used.

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Use Zygrys during pregnancy

There is no information about the likelihood of a negative effect of the drug on the fetus if used by pregnant women, and in addition, about the effect of Zigris on reproductive activity. The drug can be used during pregnancy only in cases where the likelihood of a beneficial effect on the woman exceeds the possibility of complications in the fetus.

There is no information about the possibility of penetration of the drug into breast milk or systemic absorption after penetration of the substance into the gastrointestinal tract. However, since many drugs are excreted with breast milk, and in addition, due to the high risk of adverse reactions in the infant, it is necessary to stop breastfeeding during the period of use of the drug.

Contraindications

Main contraindications:

  • presence of ongoing endogenous bleeding;
  • hemorrhagic stroke suffered within the previous 90 days;
  • surgery performed within the previous 60 days inside the skull or in the spinal cord area, or an existing severe TBI;
  • injuries that pose a high risk of life-threatening bleeding;
  • presence of an epidural catheter;
  • tumors inside the skull or symptoms of developing a hernia in the brain;
  • diagnosed hypersensitivity to drotrecogin-α.

There is no information on the efficacy and safety of using the drug in infants during the gestational period (up to 38 weeks), as well as in children and adolescents under 18 years of age.

Side effects Zygrys

The drug may cause side effects in the hematopoietic system: bleeding, which often occurs during the infusion process.

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Overdose

There is information about the development of poisoning due to the introduction of an excessively large dose of the drug. In many cases (with the introduction of a dose that is 60 times higher than the standard infusion), negative reactions were not noted. In other cases, the victims developed bleeding due to sepsis.

There is no information about the existence of antidotes. If the patient develops an overdose, it is necessary to immediately stop the infusion of the drug and carefully monitor the possible occurrence of bleeding, while performing symptomatic therapy in parallel.

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Interactions with other drugs

The interaction of the drug with other drugs has not been studied in patients with severe sepsis. Zigris should be used with caution in combination with other drugs that affect hemostasis processes.

When combined with unfractionated heparin (in small doses: <15,000 U/day), and in addition with low molecular weight heparin (for prevention - 2850 U/day), no negative impact on the properties of the drug and no increase in the risk of severe bleeding (this also includes bleeding in the central nervous system) was observed.

As a result of using heparin in small doses, the incidence of bleeding (not life-threatening) increased compared to placebo during the testing period (in the first 6 days). Small doses of heparin can be prescribed in combination with Zigris - as a means of preventing existing venous thrombosis. It is prohibited to interrupt the prophylactic use of heparin until medical indications allow it.

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Storage conditions

The lyophilisate should be kept in the refrigerator. It is necessary to avoid exposure to sunlight, and also to limit access to the medicine for small children. Temperature values are within 2-8°C.

Shelf life

Zigris can be used for a period of 3 years from the date of manufacture of the drug. In this case, the prepared solution can be stored in the refrigerator for a maximum of 24 hours (this includes the time spent on its preparation).

Attention!

To simplify the perception of information, this instruction for use of the drug "Zygrys" translated and presented in a special form on the basis of the official instructions for medical use of the drug. Before use read the annotation that came directly to medicines.

Description provided for informational purposes and is not a guide to self-healing. The need for this drug, the purpose of the treatment regimen, methods and dose of the drug is determined solely by the attending physician. Self-medication is dangerous for your health.

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