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Composition:


active ingredient: ulinastatin;


4 ml of the solution contains ulinastatin 100000 IU;


excipients: m-cresol, sucrose, disodium hydrogen phosphate dihydrate, twin 80, phosphoric acid.


Dosage form. Solution for injection.


Basic physical and chemical properties: transparent colorless solution.


Pharmacotherapeutic group.


Proteinase inhibitors. The ATX code is B02AB.


Pharmacological properties.


Pharmacodynamics.


Ulinastatin is a polyvalent Kunitz-type serine protease inhibitor found in human urine and blood. Ulinastatin inhibits inflammatory markers trypsin, pancreatic elastase, polymorphonuclear, leukocyte elastase, and endotoxin-stimulated TNF-alpha and interleukin 1,8 and 6. Ulinastatin reduces the increase in neutrophil elastase release, thus slowing the growth of pro-inflammatory cytokines, and also inhibits the secretion of pro-inflammatory cytokines IL-1, IL-6, IL-8, IL-10, IL-11, TNF, N.O., PAF. It inhibits coagulation and fibrinolysis and promotes microperfusion. It has the property of stabilizing the lysosomal membrane and reducing the production of free oxygen radicals.


Ulinastatin inhibits the activity of various hydrolases and increases the release of inflammatory mediators and improves microcirculation and tissue perfusion. It is an effective drug in the treatment of acute pancreatitis, chronic recurrent pancreatitis. Ulinastatin blocks the development of Systemic Inflammatory Response Syndrome (SIRS) and protects the function of important organs. Various serine proteases such as trypsin, thrombin, chymotrypsin, kallikrein, plasmin, elastase, cathepsin, and factors Xa, Xia, and Xlla are suppressed by ulinastatin. Ulinistatin has a localized anti-inflammatory effect and suppresses the proteolytic effect of trypsin on a number of tissues, primarily pancreatic tissues. Ulinastatin is a serine proteinase inhibitor that reduces the inflammatory response resulting from acute pancreatitis. Ulinastatin prevents organ damage by inhibiting the activity of these proteases. The drug also shows protective effects of the body during the postoperative period.


In clinical practice, the drug is used in the treatment of acute sepsis, chronic recurrent pancreatitis. Ulinastatin mainly inhibits inflammatory proteases, including trypsin, chymotrypsin, plasmin, cathepsin G, and white blood cell elastase, as well as proteases in the coagulation cascade. As with other serine protease inhibitors, ulinastatin, according to available data, in addition to blocking the protease pathway in vitro, also has anti-inflammatory properties. Ulinastatin inhibits increased production of pro-inflammatory molecules such as prostaglandin H2 synthase-2, thromboxane B2, interleukin (IL)-8, and lipopolysaccharide-induced tumor necrosis factor in vitro.


In order to assess the protective effect and mechanism of action, ulinastatin was studied in animals with experimental acute pancreatitis caused by the maximum allowable dose of cerulin (5 mcg/kg/h for 3.5 hours). Ulinastatin at a dose of 10,000 units/kg/hour was administered by three continuous intravenous infusion methods: (1) 2 hours before and during the cerulin infusion, (2) only during the cerulin infusion, and (3) starting 1 hour after the start of the cerulin infusion and continuing for 3.5 hours. In protocol 1 and 2, ulinastatin was significantly more protective than in protocol 3. In protocol 1, ulinastatin was highly protective in all parameters tested (serum amylase levels, pancreatic and amylase water content, distribution of lysosomal enzymes, Cellular and lysosomal resistance). These results suggest that administration of ulinastatin before and during intravenous cerulin infusion may stop the pathogenesis and development of pancreatitis by inhibiting the chain reaction of activation of pancreatic enzymes closely related to the redistribution of lysosomal enzymes and lysosomal resistance.


Pharmacokinetics.


After intravenous administration of 300,000 IU/10 ml in the blood of a healthy person, the concentration decreases linearly after 3 hours. The Half-Life is approximately 40 minutes. 6 hours after administration, 24% of ulinastatin is found in the urine.


The Half-Life of ulinastatin for 0-3 hours after injection was 33 minutes, and for the next 4 hours, the half-life was 2 hours.


The distribution of ulinastatin was studied after injection to animals by measuring radioactivity in promptly removed organs. 15 minutes after the injection, 44% of radioactivity was detected in the kidneys and 9% in the liver, which indicates that the kidneys are the main site of ulinastatin metabolism.


Clinical characteristics.


Indications.


Treatment of acute pancreatic inflammation (pancreatitis), chronic pancreatitis in the acute stage, after endoscopic retrograde cholangiopancreatography (IFCHG).


Contraindications.


Hypersensitivity to the active substance or to any of the components of the drug.


Interactions with other drugs and other types of interactions.


Not investigated.


Application features.


Use during pregnancy or lactation.


During pregnancy or lactation, the drug is not used.


Ability to influence the reaction rate when driving vehicles or other mechanisms.


Unknown.


Dosage and administration.


Restore the contents of the vial in 100 ml of 5% glucose or 100 ml of 0.9% sodium chloride solution.


In acute inflammation of the pancreas, 1-2 vials (200,000 IU) of the drug are administered by intravenous infusion for 1 hour 2-3 times a day for 3-5 days.


In case of exacerbation of chronic pancreatitis, after endoscopic retrograde cholangiopancreatography, 1-2 vials (100,000-200,000 IU) of the drug are administered by intravenous infusion for 1 hour 1-3 times a day for 3-5 days.


The dose is adjusted depending on the age of patients and the severity of symptoms.


Overdose.


Cases of overdose have not been described.


There is no specific antidote.


Adverse reactions.


From the digestive tract: nausea, vomiting, diarrhea.


Laboratory parameters: changes in the parameters of aspartate transaminase, alanine transaminase; a decrease in the number of white blood cells.


General disorders and reactions at the injection site: fever; redness, itching, pain at the injection site, allergic reactions.


Expiration date. 2 years.


Storage conditions.


Store at a temperature of 2 to 8 °C in a dark place. Do not freeze.


Keep out of reach of children.


Incompatibility.


The drug should not be mixed with other medicinal products.


Use only the solvents specified in the section"dosage and administration".

Tags: Ulinastatin