Peringatan Keamanan

With regards to bovine thrombin, no cases of overdose have been reported so far T155. Bovine thrombin however, is capable of causing fatal severe bleeding or thrombosis FDA Label. This thrombosis may result from the development of antibodies against bovine thrombin FDA Label. Bleeding may result from the development of antibodies against bovine factor V FDA Label. These antibodies may subsequently cross-react with endogenous human factor V and lead to its deficiency FDA Label. Patients who are know or suspected to have antibodies to bovine thrombin and/or bovine factor V should not be re-exposed to the product FDA Label. Patients who are administered bovine thrombin should be monitored for abnormal coagulation laboratory values, bleeding, or indeed, thrombosis FDA Label.

LD50 values are available for rat and mouse models where rat subcutaneous LD50 > 40mg/kg, rat IP LD50 > 40mg/kg, and mouse subcutaneous LD50 > 50 mg/kg (in which the greater than symbol indicates that the toxicity endpoint being tested was not achievable at the highest dose used in the test) MSDS.

Regardless, the most common adverse reactions following administration of bovine thrombin include hypersensitivity, bleeding, anemia, post-operative wound infection, thromboembolic events, hypotension, pyrexia, tachycardia, and/or thrombocytopenia FDA Label.

Thrombin

DB11300

biotech approved investigational

Deskripsi

Also known as coagulation factor II, thrombin is a serine protease that plays a physiological role in regulating hemostasis and maintaining blood coagulation. Once converted from prothrombin, thrombin converts fibrinogen to fibrin, which, in combination with platelets from the blood, forms a clot.

Medical thrombin is a protein substance produced through a conversion reaction in which prothrombin of bovine origin is activated by tissue thromboplastin in the presence of calcium chloride. Thrombin requires no intermediate physiological agent for its action. It clots the fibrinogen of the blood directly. Failure to clot blood occurs in the rare case where the primary clotting defect is the absence of fibrinogen itself.

Bovine thrombin however, is capable of causing fatal severe bleeding or thrombosis FDA Label. This thrombosis may result from the development of antibodies against bovine thrombin FDA Label. Bleeding may result from the development of antibodies against bovine factor V FDA Label. These antibodies may subsequently cross-react with endogenous human factor V and lead to its deficiency FDA Label. Patients who are know or suspected to have antibodies to bovine thrombin and/or bovine factor V should not be re-exposed to the product FDA Label. Patients who are administered bovine thrombin should be monitored for abnormal coagulation laboratory values, bleeding, or indeed, thrombosis FDA Label.

A variety of human thrombin and recombinant thrombin (ie. thrombin alfa) products are available as alternatives to using bovine thrombin.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Unfortunately, little has been reported about the systemic pharmacokinetics of bovine thrombin preparations [T155].
Volume Distribusi Little has been reported about the systemic pharmacokinetics of bovine thrombin preparations [T155], but owing to its topical mode of application, systemic exposure or distribution to other organs and tissues is not expected.
Klirens (Clearance) Although little has been reported about the systemic pharmacokinetics of bovine thrombin preparations [T155], it is expected that they are generally rapidly neutralized by naturally circulating plasma inhibitors limiting its duration of action and preventing the active form from diffusing into the general circulation [L2079].

Absorpsi

Little has been reported about the systemic pharmacokinetics of bovine thrombin preparations T155, but owing to its topical mode of administration, it is expected that any kind of systemic absorption would be minimal.

Metabolisme

Although little has been reported about the systemic pharmacokinetics of bovine thrombin preparations T155, such products are expected to be metabolized in the same way as endogenous thrombin is. Endogenous thrombin does not circulate in the blood as a free, active molecule for very long L2079. After performing its function it is rapidly inactivated after formation of complexes with various circulating endogenous plasma inhibitors (like antithrombin III) L2079. This rapid inactivation prevents the active agent from diffusing into the general circulation. The complexes formed are then generally cleared and eliminated by the liver L2079.

Rute Eliminasi

Although little has been reported about the systemic pharmacokinetics of bovine thrombin preparations T155, they are expected to act in much the same way as endogenous thrombin does. Natural bodily thrombin is cleared by two primary separate pathways: (1) through rapid formation of thrombin inhibitor complexes, which are recognized by hepatic receptors and degraded, and (2) via direct binding to thrombomodulin on the endothelium, followed by internalization and degradation L2079. Specific thrombin inhibitors include ATIII, alpha-2M and heparin cofactor II L2079.

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Coagulation factor XI F11
Coagulation factor XIII A chain F13A1
Coagulation factor XIII B chain F13B
Fibrinogen alpha chain FGA
Fibrinogen beta chain FGB
Fibrinogen gamma chain FGG
Coagulation factor V F5
Coagulation factor VIII F8
Proteinase-activated receptor 1 F2R
Proteinase-activated receptor 4 F2RL3

Referensi & Sumber

Artikel (PubMed)
  • PMID: 17635715
    Crawley JT, Zanardelli S, Chion CK, Lane DA: The central role of thrombin in hemostasis. J Thromb Haemost. 2007 Jul;5 Suppl 1:95-101. doi: 10.1111/j.1538-7836.2007.02500.x.
Textbook
  • ISBN: 0781728452
    Richard C. Dart (2004). Medical Toxicology Third Edition (3rd ed.). Lippincott Williams & Wilkins.

Contoh Produk & Brand

Produk: 8 • International brands: 0
Produk
  • Thrombin-jmi
    Kit; Solution • 5000 [iU]/5mL • Topical • US • Approved
  • Thrombin-jmi
    Kit; Solution • 20000 [iU]/20mL • Topical • US • Approved
  • Thrombin-jmi
    Kit; Solution • 5000 [iU]/5mL • Topical • US • Approved
  • Thrombin-jmi
    Kit; Solution • 5000 [iU]/5mL • Topical • US • Approved
  • Thrombinar Pws 5000unit/vial
    Powder, for solution • 5000 unit / vial • Topical • Canada • Approved
  • Thrombostat 10000units
    Powder • 10000 unit / vial • Topical • Canada • Approved
  • Thrombostat 1000units
    Powder • 1000 unit / vial • Topical • Canada • Approved
  • Thrombostat 5000units
    Powder, for solution • 5000 unit / vial • Topical • Canada • Approved

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