Aprotinin ( Eng. Aprotinin , CAS code 9087-70-1, gross formula C 284 H 432 N 84 O 79 S 7 ) - a drug , an antienzyme preparation obtained from cattle organs (lungs, etc.), polyvalent protease inhibitor .
| Aprotinin | |
|---|---|
| Aprotinin | |
 | |
| Active substance | |
| Cas | |
| Drugbank | |
| Single chain polypeptide containing 58 amino acids. [one] | |
| Classification | |
| Farmakol. Group | Fibrinolysis Inhibitors Enzymes and antiferments . [one] |
| ATX | |
| ICD-10 | |
| Dosage Forms | |
| concentrate for solution for infusion, lyophilisate for solution for infusion [2] | |
| Other names | |
| Aprotex, Aprotinin, Vero-Narkap, Gordoks, Ingiprol, Ingitril, Contrikal, Trasilol 500000 [2] , Traskolan | |
Aprotinin activity is expressed in various units: KIE - kallikrein inactivating units; Ph.Eur.U - trypsin inactivating units of the European Pharmacopoeia, 1 Ph.Eur.U corresponds to 1800 KIE; АТРЕ - antitrypsin units, 1 АТРЕ corresponds to 1.33 KIE; ED - units of action of the enzyme according to the State Pharmacopoeia of the USSR. [one]
The developer of the drug aprotinin is positioned as a tool for the treatment of pancreatitis and pancreatic necrosis . However, at this time, the indications for the use of aprotinin and its analogues are significantly changed. So, it is excluded from recommendations for the treatment of acute (and especially chronic) pancreatitis as it has not confirmed its effectiveness according to the criteria of evidence-based medicine not only in the West (USA and Europe), but also in Russia. However, it is allowed in Russia for use in relation to such indications as:
- withdrawal syndrome with opium addiction;
- treatment of opiate withdrawal symptoms both independently and as part of complex therapy;
- painful symptoms, including “intolerable pain”, muscle pain, sinusopathy, chills, hyperthermia, sweating, anorexia, insomnia, dysphoria, hypochondria. [3]
- Trade name - Aptotex (lat. Aptotex).
Pharmacological action
Polyvalent protease inhibitor, has antiproteolytic, antifibrinolytic and hemostatic effects. Inactivates the most important proteases (trypsin, chymotrypsin, kininogenase, kallikrein, including activating fibrinolysis). It inhibits both total proteolytic activity and the activity of individual proteolytic enzymes.
The presence of antiprotease activity determines the effectiveness of aprotinin in lesions of the pancreas and other conditions, accompanied by a high content of kallikrein and other proteases in plasma and tissues.
Reduces the fibrinolytic activity of blood, inhibits fibrinolysis and has a hemostatic effect in coagulopathies.
The blockade of the kallikrein-kinin system allows it to be used for the prevention and treatment of various forms of shock. [2]
Inactivates the most important proteinases of blood plasma and tissues involved in the formation of withdrawal symptoms in opium addiction. The increased formation of kinins (bradykinin in plasma and kallikrein in tissues), the release of leukocyte elastase, neutrophil proteinases, anti-inflammatory cytokines that cause microcirculatory disorders, vasodilation, and increased vascular permeability are an important pathophysiological mechanism accompanying the onset of pain syndrome with opioid. The mechanism of action of aprotinin in opiate withdrawal syndrome is associated, to the greatest extent, with the effect of peptide molecules on the catabolism system, which leads to relief or weakening of vegetative and algic (pain) manifestations of opiate withdrawal syndrome. [3]
Pharmacokinetics
After iv administration, it is rapidly distributed in the extracellular space, and accumulates in the liver for a short time.
Inactivated in the digestive tract, part is destroyed in the liver. T1 / 2 - 150 min, terminal - 7-10 hours. It is excreted by the kidneys - 5-6 hours in the form of inactive decay products. [2]
Dosage Forms
- solution for infusion of 10 thousand KIE / ml ("Trasilol" 500,000 ");
- solution for infusion 10 thousand KIU / ml ("Contriven", PrJSC Biofarm);
- concentrate for the preparation of a solution for intravenous administration of 10 thousand KIE / ml ("Gordoks");
- concentrate for the preparation of a solution for infusion 10 thousand KIU / ml (Ingiprol);
- lyophilisate for the preparation of a solution for intravenous administration of 30 thousand ATre (Vero-Narcap);
- lyophilisate for the preparation of a solution for intravenous and intracavitary administration of 10 thousand ATPE ("Contrical");
- lyophilisate for the preparation of a solution for infusion of 10 thousand ATPE, 100 thousand ATPE ("Aprotex");
- lyophilisate for preparation of solution for infusion of 15 PIECES ("Ingitril"). [2]
A comparison conducted by objective methods (determining the amount of aprotinin on an HPLC and trypsin activity) shows that 1 amp. 15 units of ingitrile is equal to 1 amp. 10,000 ATPE contrikala . [one]
Notes
- ↑ 1 2 3 4 5 Aprotinin . Register of medicines . ReLeS.ru (05/12/2002). Date of treatment April 7, 2008. Archived March 11, 2012.
- ↑ 1 2 3 4 5 Search the database of drugs, search options: INN - Aprotinin , the flags “Search in the register of registered drugs” , “Search TKFS” , “Show drug forms” unspecified . The circulation of drugs . Federal State Institution “Scientific Center for Expertise of Medical Application Tools” of the Russian Healthcare Supervision Service of the Russian Federation (03/27/2008) - A typical clinical and pharmacological article is a by-law and is not protected by copyright in accordance with part four of the Civil Code of the Russian Federation No. 230-FZ of December 18, 2006. Date of treatment April 7, 2008. Archived August 22, 2011.
Links
- Vero-drug addict. Register of medicines. Registration certificate number: LS-000693. Registration date: 04/20/2011.