Prothrombin

Identification

Summary

Prothrombin is a coagulation factor used for emergency reversal of vitamin K antagonist therapy.

Brand Names
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

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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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

Adverse Effects
Medicalerrors
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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.
DrugInteraction
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.
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.
Aminocaproic acidThe risk or severity of adverse effects can be increased when Aminocaproic acid is combined with Prothrombin.
AncrodThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Ancrod.
AnistreplaseThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Anistreplase.
Antithrombin AlfaThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Antithrombin Alfa.
Antithrombin III humanThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Antithrombin III human.
ApixabanThe therapeutic efficacy of Prothrombin can be decreased when used in combination with Apixaban.
Interactions
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Food Interactions
No interactions found.

Products

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Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
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 flag
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 flag
COFACT 250 IU/10 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETProthrombin (245 IU) + Coagulation Factor IX Human (250 IU) + Coagulation factor VII human (135 IU) + Coagulation factor X human (245 IU) + Protein C (250 IU) + Protein S human (45 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
COFACT 500 IU/20 ML IV ENJEKSIYON IÇIN TOZ IÇEREN FLAKON, 1 ADETProthrombin (490 IU) + Coagulation Factor IX Human (500 IU) + Coagulation factor VII human (270 IU) + Coagulation factor X human (490 IU) + Protein C (500 IU) + Protein S human (90 IU)InjectionIntravenousCENTURION İLAÇ SAN. VE TİC. A.Ş.2020-08-14Not applicableTurkey flag
Feiba Vh Immuno Anti InhibitorProthrombin + Antihemophilic factor human (4 unit) + Coagulation factor VII human + Coagulation factor X human + Factor IX Complex (Human)Powder, for solutionIntravenousOsterreichisches Institut Fur Haemoderivate Ges M.B.H.1986-12-311998-08-13Canada flag
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)KitIntravenousCSL Behring GmbH2013-12-13Not applicableUS flag
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)KitIntravenousCSL Behring GmbH2013-04-29Not applicableUS flag
OctaplexProthrombin (760 unit / vial) + Coagulation Factor IX Human (500 unit / vial) + Coagulation factor VII human (480 unit / vial) + Coagulation factor X human (600 unit / vial) + Protein C (620 unit / vial) + Protein S human (640 unit / vial)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2008-07-08Not applicableCanada flag
OctaplexProthrombin (1520 unit / vial) + Coagulation Factor IX Human (1000 unit / vial) + Coagulation factor VII human (960 unit / vial) + Coagulation factor X human (1200 unit / vial) + Protein C (1240 unit / vial) + Protein S human (1280 unit / vial)Kit; Powder, for solutionIntravenousOctapharma Pharmazeutika Produktionsges M B H2015-08-11Not applicableCanada flag

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

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. [Article]
PubChem Substance
347911184
RxNav
1441689
Wikipedia
Thrombin
FDA label
Download (638 KB)
MSDS
Download (77.5 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentHemophilia A1
4Enrolling by InvitationTreatmentBleeding / Blood Loss,Surgical / Cardiovascular Surgical Procedures / Fresh Frozen Plasma / Prothrombin Complex Concentrates1
4RecruitingTreatmentCoagulation Disorders / Massive Hemorrhage / Traumatic haemorrhage1
4WithdrawnTreatmentPostpartum Haemorrhage (PPH)1
3CompletedTreatmentAcute Major Bleeding / Disorders, Blood Coagulation1
3CompletedTreatmentCardiovascular Disease (CVD)1
3CompletedTreatmentReversal of Anticoagulant Treatment1
3CompletedTreatmentReversal of Coagulopathy1
3Not Yet RecruitingTreatmentAcute Major Bleeding1
3RecruitingTreatmentCongestive Heart Failure (CHF) / Heart Disease End Stage1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Injection, powder, for solutionParenteral
InjectionIntravenous
KitIntravenous
Powder, for solutionParenteral
Kit; powder, for solutionIntravenous
Injection, powder, for solutionIntravenous
Powder, for solutionIntravenous
SolutionIntravenous
Prices
Not Available
Patents
Not Available

Properties

State
Liquid
Experimental Properties
Not Available

Targets

Drugtargets
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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. [Article]
  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. [Article]
  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. [Article]
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. [Article]

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. [Article]

Drug created on December 03, 2015 16:52 / Updated on May 21, 2021 10:21