Trasylol^® 500 000 (Solution) Instructions for Use

Marketing Authorization Holder

Bayer HealthCare AG (Germany)

ATC Code

B02AB01 (Aprotinin)

Active Substance

Aprotinin (Rec.INN registered by WHO)

Dosage Form

Trasylol® 500 000

Solution for infusion 500 thousand IU/50 ml: vial 1 pc.

Dosage Form, Packaging, and Composition

50 ml – vials (1) – cardboard packs.

Clinical-Pharmacological Group

Hemostatic agent. Fibrinolysis inhibitor – polyvalent plasma proteinase inhibitor

Pharmacotherapeutic Group

Proteolysis inhibitor

Pharmacological Action

A polypeptide obtained from bovine lungs. It blocks the kallikrein-kinin system. It inhibits both the total proteolytic activity and the activity of individual proteolytic enzymes. It is a polyvalent protease inhibitor (including plasmin, kininogenases, trypsin, chymotrypsin, kallikrein, including those activating fibrinolysis).

It reduces the fibrinolytic activity of blood, inhibits fibrinolysis, and exerts a hemostatic effect in coagulopathies.

The activity of aprotinin is expressed in kallikrein inactivating units (KIU), in trypsin inactivating units of the European Pharmacopoeia (Ph.Eur.U), and in antitrypsin units (ATrU). 1 Ph.Eur.U corresponds to 1800 KIU. 1 ATrU corresponds to 1.33 KIU.

Pharmacokinetics

Aprotinin, being a polypeptide, is inactivated in the gastrointestinal tract. It is excreted in the urine as inactive breakdown products. The T_1/2 in the terminal phase is 7-10 hours.

Indications

Pancreatitis (acute, exacerbation of chronic), pancreatic necrosis. Performance of diagnostic studies and operations on the pancreas (prevention of enzymatic autolysis of the pancreas during operations on it and adjacent abdominal organs).

Prevention of acute nonspecific postoperative parotitis.

Bleeding against the background of hyperfibrinolysis: post-traumatic, postoperative (especially during operations on the prostate gland, lungs), before, after and during childbirth (including amniotic fluid embolism); polymenorrhea.

Angioneurotic edema.

Shock (toxic, traumatic, burn, hemorrhagic).

Extensive and deep traumatic tissue damage.

As an auxiliary therapy – coagulopathies characterized by secondary hyperfibrinolysis (in the initial phase, before the effect occurs after the use of heparin and replacement of coagulation factors); massive bleeding (during thrombolytic therapy), during extracorporeal circulation.

Prevention of postoperative pulmonary embolism and bleeding; fat embolism in polytrauma, especially in fractures of the lower extremities and skull bones.

ICD codes

Dosage Regimen

Administer intravenously only, as a short-term or prolonged infusion. Determine the dosage individually based on the clinical indication and patient condition.

For acute pancreatitis or pancreatic necrosis, administer an initial dose of 500,000 KIU intravenously. Follow with a maintenance dose of 50,000 KIU/hour by continuous infusion until clinical improvement is observed.

To prevent perioperative blood loss during major surgeries, such as cardiac procedures with cardiopulmonary bypass, administer a loading dose of 2 million KIU intravenously after anesthesia induction. Add 2 million KIU to the priming fluid of the cardiopulmonary bypass circuit. After the initial dose, infuse 500,000 KIU/hour for the duration of the surgery.

For the management of hyperfibrinolytic bleeding, administer a loading dose of 500,000 to 1 million KIU intravenously. Follow with a continuous infusion of 200,000 to 500,000 KIU/hour until hemostasis is achieved.

In the context of obstetric hemorrhage or amniotic fluid embolism, administer a single intravenous dose of 1 million KIU. Repeat dosing may be considered based on clinical response.

For all indications, do not exceed a total daily dose of 7 million KIU. Monitor patients closely for signs of allergic or anaphylactic reactions, especially upon re-exposure.

Adverse Reactions

From the cardiovascular system arterial hypotension and/or tachycardia.

Allergic reactions skin rash, urticaria, rhinitis, conjunctivitis, bronchospasm, myalgia, symptoms of anaphylactic reactions up to the development of anaphylactic shock (more often occur after repeated infusions of aprotinin).

From the CNS psychotic reactions, hallucinations, confusion.

From the digestive system with rapid administration – nausea, vomiting.

Local reactions with prolonged infusion – thrombophlebitis.

Contraindications

DIC syndrome (except for the coagulopathy phase), I and III trimesters of pregnancy, lactation period, hypersensitivity to aprotinin, hypersensitivity to bovine protein.

Use in Pregnancy and Lactation

Contraindicated in the I and III trimesters of pregnancy. Clinical data on the safety of aprotinin use in the II trimester of pregnancy and during lactation are lacking.

Use in Renal Impairment

Dose adjustment is not required for patients with impaired renal function.

Pediatric Use

Use is contraindicated in children and adolescents under 18 years of age.

Geriatric Use

No change in the dosage regimen is required for elderly patients (over 65 years of age).

Special Precautions

Before starting therapy, it is advisable to perform a skin test for individual patient sensitivity to aprotinin. If there is a history of allergic reactions, it is recommended to use histamine H₁-receptor blockers and corticosteroids before starting aprotinin therapy.

In hyperfibrinolysis and DIC syndrome, Aprotinin can be used only after elimination of all manifestations of DIC syndrome and against the background of the prophylactic action of heparin.

Use with caution in patients who have received muscle relaxants within the previous 2-3 days.

Drug Interactions

Adding aprotinin to heparinized blood causes an increase in whole blood clotting time.

When used concomitantly with rheomacrodex, the sensitizing effect is mutually enhanced.

When used concomitantly, Aprotinin, depending on the dose, inhibits the action of streptokinase, urokinase, alteplase.

Aprotinin is a weak inhibitor of serum pseudocholinesterase. When used concomitantly, this may contribute to a slowdown in the metabolism of suxamethonium chloride and an enhancement of muscle relaxation; there is a risk of apnea.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.