Identification

Name
Prothrombin
Accession Number
DB11311
Type
Biotech
Groups
Approved
Biologic Classification
Protein Based Therapies
Blood factors
Description

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.

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
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Beriplex P/n 1000Prothrombin (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 solutionIntravenousCsl Behring2013-11-21Not applicableCanada
Beriplex P/n 500Prothrombin (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 solutionIntravenousCsl Behring2011-07-28Not applicableCanada
KcentraProthrombin (1180 U/40mL) + Coagulation Factor IX Human (1020 U/40mL) + Coagulation factor VII human (700 U/40mL) + Coagulation factor X human (1520 U/40mL) + Protein C (1240 U/40mL) + Protein S human (920 U/40mL)KitCSL Behring GmbH2013-12-13Not applicableUs
KcentraProthrombin (590 U/20mL) + Coagulation Factor IX Human (510 U/20mL) + Coagulation factor VII human (350 U/20mL) + Coagulation factor X human (760 U/20mL) + Protein C (620 U/20mL) + Protein S human (460 U/20mL)KitCSL Behring GmbH2013-04-29Not applicableUs
OctaplexProthrombin (760 unit) + Coagulation Factor IX Human (500 unit) + Coagulation factor VII human (480 unit) + Coagulation factor X human (600 unit) + Protein C (620 unit) + Protein S human (640 unit)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2008-07-08Not applicableCanada
OctaplexProthrombin (1520 unit) + Coagulation Factor IX Human (1000 unit) + Coagulation factor VII human (960 unit) + Coagulation factor X human (1200 unit) + Protein C (1240 unit) + Protein S human (1280 unit)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2015-08-11Not applicableCanada
Categories
UNII
8FB1K07F16
CAS number
9001-26-7

Pharmacology

Indication

For use in the emergency reversal of coagulation factor deficiency in patients receiving vitamin K antagonist therapy. Prothrombin is administered as part of a cocktail containing several coagulation factors.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action
TargetActionsOrganism
AFibrinogen alpha chain
cleavage
Humans
AFibrinogen beta chain
cleavage
Humans
ACoagulation factor XIII A chain
agonist
Humans
ACarboxypeptidase B2
agonist
Humans
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe therapeutic efficacy of Prothrombin can be decreased when used in combination with (R)-warfarin.
(S)-WarfarinThe therapeutic efficacy of Prothrombin can be decreased when used in combination with (S)-Warfarin.
4-hydroxycoumarinThe therapeutic efficacy of Prothrombin can be decreased when used in combination with 4-hydroxycoumarin.
AbciximabThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Abciximab.
AcenocoumarolThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Acenocoumarol.
Acetylsalicylic acidThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Acetylsalicylic acid.
Alpha-1-proteinase inhibitorAlpha-1-proteinase inhibitor may increase the thrombogenic activities of Prothrombin.
AlteplaseThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Alteplase.
AmediplaseThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Amediplase.
Aminocaproic AcidThe risk or severity of adverse effects can be increased when Aminocaproic Acid is combined with Prothrombin.
Food Interactions
Not Available

References

General References
  1. 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. [PubMed:25535411]
External Links
PubChem Substance
347911184
Wikipedia
Prothrombin
FDA label
Download (638 KB)
MSDS
Download (77.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentThrombotic events1
3CompletedTreatmentAcute Major Bleeding / Disorders, Blood Coagulation1
3CompletedTreatmentReversal of Anticoagulant Treatment1
3CompletedTreatmentReversal of Coagulopathy1
3RecruitingTreatmentHeart Disease End Stage / Heart Failureļ¼ŒCongestive1
3RecruitingTreatmentSignificant Bleeding Risk1
4Enrolling by InvitationTreatmentBleeding / Blood Loss,Surgical / Cardiovascular Surgical Procedures / Fresh Frozen Plasma / Prothrombin Complex Concentrates1
4WithdrawnTreatmentPostpartum Haemorrhage (PPH)1
Not AvailableCompletedNot AvailableHemorrhage1
Not AvailableRecruitingNot AvailableHemorrhage1
Not AvailableWithdrawnTreatmentIntracranial Hemorrhage, Spontaneous / Intracranial Hemorrhage, Traumatic1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Powder, for solutionIntravenous
Kit
Kit; powder, for solutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Taxonomy

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

Targets

Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General Function
Structural molecule activity
Specific 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 ...
Gene Name
FGA
Uniprot ID
P02671
Uniprot Name
Fibrinogen alpha chain
Molecular Weight
94972.455 Da
References
  1. 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. [PubMed:25535411]
  2. UniProt: Fibrinogen Alpha Chain [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Cleavage
General Function
Structural molecule activity
Specific 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...
Gene Name
FGB
Uniprot ID
P02675
Uniprot Name
Fibrinogen beta chain
Molecular Weight
55927.9 Da
References
  1. 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. [PubMed:25535411]
  2. UniProt: Fibrinogen Beta Chain [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Protein-glutamine gamma-glutamyltransferase activity
Specific 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 fibr...
Gene Name
F13A1
Uniprot ID
P00488
Uniprot Name
Coagulation factor XIII A chain
Molecular Weight
83266.805 Da
References
  1. 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. [PubMed:25535411]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific 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...
Gene Name
CPB2
Uniprot ID
Q96IY4
Uniprot Name
Carboxypeptidase B2
Molecular Weight
48423.85 Da
References
  1. 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. [PubMed:25535411]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Serine-type endopeptidase activity
Specific 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.
Gene Name
F10
Uniprot ID
P00742
Uniprot Name
Coagulation factor X
Molecular Weight
54731.255 Da
References
  1. 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. [PubMed:25535411]

Drug created on December 03, 2015 09:52 / Updated on November 02, 2018 07:08