Prothrombin
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Identification
- Summary
Prothrombin is a coagulation factor used for emergency reversal of vitamin K antagonist therapy.
- Brand Names
- Balfaxar, Beriplex, Kcentra, Octaplex
- Generic Name
- Prothrombin
- DrugBank Accession Number
- DB11311
- Background
Prothrombin Complex Concentrate (Human), is indicated for the urgent reversal of acquired coagulation factor deficiency induced by Vitamin K antagonist (VKA, e.g., warfarin) therapy in adult patients with acute major bleeding.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Blood factors - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
>sp|P00734|THRB_HUMAN Prothrombin OS=Homo sapiens GN=F2 PE=1 SV=2 MAHVRGLQLPGCLALAALCSLVHSQHVFLAPQQARSLLQRVRRANTFLEEVRKGNLEREC VEETCSYEEAFEALESSTATDVFWAKYTACETARTPRDKLAACLEGNCAEGLGTNYRGHV NITRSGIECQLWRSRYPHKPEINSTTHPGADLQENFCRNPDSSTTGPWCYTTDPTVRRQE CSIPVCGQDQVTVAMTPRSEGSSVNLSPPLEQCVPDRGQQYQGRLAVTTHGLPCLAWASA QAKALSKHQDFNSAVQLVENFCRNPDGDEEGVWCYVAGKPGDFGYCDLNYCEEAVEEETG DGLDEDSDRAIEGRTATSEYQTFFNPRTFGSGEADCGLRPLFEKKSLEDKTERELLESYI DGRIVEGSDAEIGMSPWQVMLFRKSPQELLCGASLISDRWVLTAAHCLLYPPWDKNFTEN DLLVRIGKHSRTRYERNIEKISMLEKIYIHPRYNWRENLDRDIALMKLKKPVAFSDYIHP VCLPDRETAASLLQAGYKGRVTGWGNLKETWTANVGKGQPSVLQVVNLPIVERPVCKDST RIRITDNMFCAGYKPDEGKRGDACEGDSGGPFVMKSPFNNRWYQMGIVSWGEGCDRDGKY GFYTHVFRLKKWIQKVIDQFGE
Download FASTA Format- Synonyms
- Coagulation factor II (human)
- Coagulation factor II human
- Factor II
- Factor II (prothrombin)
- Human coagulation factor II
Pharmacology
- Indication
Prothrombin is administered as part of a cocktail containing several coagulation factors.
Along with other blood coagulation factors, it is used to reverse acquired coagulation factor deficiency induced by Vitamin K antagonist (VKA, e.g., warfarin) therapy in adult patients with a need for an urgent surgery/invasive procedure.2
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination for prophylaxis of Bleeding Combination Product in combination with: Protein C (DB11312), Coagulation Factor IX (Recombinant) (DB00100), Protein S human (DB13149), Coagulation factor X human (DB13148), Coagulation factor VII human (DB13150) •••••••••••• •••••••••••••• •••••••••• ••••••• ••• •••••••• Used in combination to treat Vitamin k antagonist induced major bleeding Regimen in combination with: Coagulation Factor IX Human (DB13152), Protein C (DB11312), Coagulation factor VII human (DB13150), Protein S human (DB13149), Coagulation factor X human (DB13148), Prothrombin (DB11311) •••••••••••• - Contraindications & Blackbox Warnings
- Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API
- Pharmacodynamics
Not Available
- Mechanism of action
Target Actions Organism AFibrinogen alpha chain cleavageHumans AFibrinogen beta chain cleavageHumans ACoagulation factor XIII A chain agonistHumans ACarboxypeptidase B2 agonistHumans - Absorption
Not Available
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
- Not Available
- Route of elimination
Not Available
- Half-life
Approximately 60h 1.
- Clearance
Not Available
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The therapeutic efficacy of Prothrombin can be decreased when used in combination with Abciximab. Acenocoumarol The therapeutic efficacy of Prothrombin can be decreased when used in combination with Acenocoumarol. Alpha-1-proteinase inhibitor Alpha-1-proteinase inhibitor may increase the thrombogenic activities of Prothrombin. Alteplase The therapeutic efficacy of Prothrombin can be decreased when used in combination with Alteplase. Aminocaproic acid The risk or severity of adverse effects can be increased when Aminocaproic acid is combined with Prothrombin. - Food Interactions
- No interactions found.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Balfaxar Prothrombin (26 [iU]/1mL) + Coagulation Factor IX Human (25.5 [iU]/1mL) + Coagulation factor VII human (16.5 [iU]/1mL) + Coagulation factor X human (24 [iU]/1mL) + Protein C (22 [iU]/1mL) + Protein S human (22 [iU]/1mL) Powder, for solution Intravenous Octapharma Italy S.P.A. 2023-11-30 Not applicable US Beriplex P/n 1000 Prothrombin (1600 unit) + Coagulation Factor IX Human (1240 unit) + Coagulation factor VII human (1000 unit) + Coagulation factor X human (2040 unit) + Protein C (1640 unit) + Protein S human (1360 unit) Powder, for solution Intravenous Csl Behring 2013-11-21 Not applicable Canada Beriplex P/N 1000 I.E. Pulver und Lösungsmittel zur Herstellung einer Injektionslösung Prothrombin (1360 IE) + Coagulation Factor IX Human (1020 IE) + Coagulation factor VII human (700 IE) + Coagulation factor X human (1640 IE) + Protein C (1200 I.E.) + Protein S human (1000 IE) Injection, powder, for solution Parenteral Csl Behring 2013-04-16 Not applicable Austria Beriplex P/N 250 I.E. Pulver und Lösungsmittel zur Herstellung einer Injektionslösung Prothrombin (340 I.E.) + Coagulation Factor IX Human (255 IE) + Coagulation factor VII human (175 IE) + Coagulation factor X human (410 IE) + Protein C (300 IE) + Protein S human (250 IE) Injection, powder, for solution Parenteral Csl Behring 2008-02-27 Not applicable Austria Beriplex P/n 500 Prothrombin (800 unit) + Coagulation Factor IX Human (620 unit) + Coagulation factor VII human (500 unit) + Coagulation factor X human (1020 unit) + Protein C (820 unit) + Protein S human (680 unit) Powder, for solution Intravenous Csl Behring 2011-07-28 Not applicable Canada
Categories
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 8FB1K07F16
- CAS number
- 9001-26-7
References
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Congenital FVII Deficiency / Congenital Hematological Disorder 1 somestatus stop reason just information to hide Not Available Completed Not Available Factor VII Deficiency 1 somestatus stop reason just information to hide Not Available Completed Not Available Hemorrhage 2 somestatus stop reason just information to hide Not Available Completed Treatment Acquired Fibrinogen Deficiency / Fibrinogenolysis; Hemorrhage / Massive Hemorrhage / Postpartum Haemorrhage (PPH) / Transfusion Related Complications 1 somestatus stop reason just information to hide Not Available Not Yet Recruiting Not Available High Bleeding Risk / Vitamin K-Dependent Coagulation Defect 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Intravenous Powder, for solution Intravenous Injection, powder, lyophilized, for solution; kit Intravenous Powder, for solution Parenteral Kit; powder, for solution Intravenous Injection, powder, for solution Intravenous drip 520 IU/vial Injection, powder, for solution Parenteral Injection, powder, for solution Intravenous Solution Intravenous - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Liquid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Cleavage
- General Function
- Cleaved by the protease thrombin to yield monomers which, together with fibrinogen beta (FGB) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However, subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets via an ITGB3-dependent pathway. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the immune response via both innate and T-cell mediated pathways
- Specific Function
- extracellular matrix structural constituent
- Gene Name
- FGA
- Uniprot ID
- P02671
- Uniprot Name
- Fibrinogen alpha chain
- Molecular Weight
- 94972.455 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Cleavage
- General Function
- Cleaved by the protease thrombin to yield monomers which, together with fibrinogen alpha (FGA) and fibrinogen gamma (FGG), polymerize to form an insoluble fibrin matrix. Fibrin has a major function in hemostasis as one of the primary components of blood clots. In addition, functions during the early stages of wound repair to stabilize the lesion and guide cell migration during re-epithelialization. Was originally thought to be essential for platelet aggregation, based on in vitro studies using anticoagulated blood. However subsequent studies have shown that it is not absolutely required for thrombus formation in vivo. Enhances expression of SELP in activated platelets. Maternal fibrinogen is essential for successful pregnancy. Fibrin deposition is also associated with infection, where it protects against IFNG-mediated hemorrhage. May also facilitate the antibacterial immune response via both innate and T-cell mediated pathways
- Specific Function
- extracellular matrix structural constituent
- Gene Name
- FGB
- Uniprot ID
- P02675
- Uniprot Name
- Fibrinogen beta chain
- Molecular Weight
- 55927.9 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Factor XIII is activated by thrombin and calcium ion to a transglutaminase that catalyzes the formation of gamma-glutamyl-epsilon-lysine cross-links between fibrin chains, thus stabilizing the fibrin clot. Also cross-link alpha-2-plasmin inhibitor, or fibronectin, to the alpha chains of fibrin
- Specific Function
- metal ion binding
- Gene Name
- F13A1
- Uniprot ID
- P00488
- Uniprot Name
- Coagulation factor XIII A chain
- Molecular Weight
- 83267.785 Da
References
- Palta S, Saroa R, Palta A: Overview of the coagulation system. Indian J Anaesth. 2014 Sep;58(5):515-23. doi: 10.4103/0019-5049.144643. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Cleaves C-terminal arginine or lysine residues from biologically active peptides such as kinins or anaphylatoxins in the circulation thereby regulating their activities. Down-regulates fibrinolysis by removing C-terminal lysine residues from fibrin that has already been partially degraded by plasmin
- Specific Function
- metallocarboxypeptidase activity
- Gene Name
- CPB2
- Uniprot ID
- Q96IY4
- Uniprot Name
- Carboxypeptidase B2
- Molecular Weight
- 48423.85 Da
References
- Palta S, Saroa R, Palta A: Overview of the coagulation system. Indian J Anaesth. 2014 Sep;58(5):515-23. doi: 10.4103/0019-5049.144643. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Factor Xa is a vitamin K-dependent glycoprotein that converts prothrombin to thrombin in the presence of factor Va, calcium and phospholipid during blood clotting. Factor Xa activates pro-inflammatory signaling pathways in a protease-activated receptor (PAR)-dependent manner (PubMed:24041930, PubMed:30568593, PubMed:34831181). Up-regulates expression of protease-activated receptors (PARs) F2R, F2RL1 and F2RL2 in dermal microvascular endothelial cells (PubMed:35738824). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL6, in cardiac fibroblasts and umbilical vein endothelial cells in PAR-1 (F2R)-dependent manner (PubMed:30568593, PubMed:34831181). Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2, IL6, TNF-alpha/TNF, IL-1beta/IL1B, IL8/CXCL8 and IL18, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Induces expression of adhesion molecules, such as ICAM1, VCAM1 and SELE, in endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824, PubMed:9780208). Increases expression of phosphorylated ERK1/2 in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Triggers activation of the transcription factor NF-kappa-B in dermal microvascular endothelial cells and atrial tissues (PubMed:24041930, PubMed:35738824). Up-regulates expression of plasminogen activator inhibitor 1 (SERPINE1) in atrial tissues (PubMed:24041930)
- Specific Function
- calcium ion binding
- Gene Name
- F10
- Uniprot ID
- P00742
- Uniprot Name
- Coagulation factor X
- Molecular Weight
- 54731.255 Da
References
- Palta S, Saroa R, Palta A: Overview of the coagulation system. Indian J Anaesth. 2014 Sep;58(5):515-23. doi: 10.4103/0019-5049.144643. [Article]
Drug created at December 03, 2015 16:52 / Updated at April 22, 2024 18:19