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Identification
- Summary
Antithrombin III human is an alpha-2-glycoprotein used to prevent thromboembolisms in patients with hereditary antithrombin III deficiency.
- Brand Names
- Thrombate III
- Generic Name
- Antithrombin III human
- DrugBank Accession Number
- DB11598
- Background
A plasma alpha 2 glycoprotein that accounts for the major antithrombin activity of normal plasma and also inhibits several other enzymes. It is a member of the serpin superfamily.
- Type
- Biotech
- Groups
- Approved
- Biologic Classification
- Protein Based Therapies
Thrombolytic agents - Protein Chemical Formula
- Not Available
- Protein Average Weight
- Not Available
- Sequences
- Not Available
- Synonyms
- Antithrombin III
- Antithrombin III (human)
- Antithrombin III (human) concentrate IV
- Antithrombin III human
- Antithrombin III human plasma-derived
- Antithrombin III, human
- Antithrombin III,human
- Antitrombina III
- AT-III
- Heparin cofactor B
- External IDs
- ORG 10849
Pharmacology
- Indication
Antithrombin III human is a human antithrombin (AT) indicated in patients with hereditary antithrombin deficiency for the treatment and prevention of thromboembolism and prevention of peri-operative and peri-partum thromboembolism
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Hereditary antithrombin iii deficiency •••••••••••• - Contraindications & Blackbox Warnings
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Hereditary AT deficiency causes an increased risk of venous thromboembolism (VTE). During high-risk situations such as surgery or trauma or for pregnant women, during the peri-partum period, the risk of development of VTEs as compared to the normal population in these situations is increased by a factor 10 to 50. In hereditary antithrombin deficient patients ATryn restores (normalize) plasma AT activity levels during peri-operative and peri-partum periods.
- Mechanism of action
Antithrombin, an alpha2-glycoprotein of molecular weight 58,000, is normally present in human plasma at a concentration of approximately 12.5 mg/dL and is the major plasma inhibitor of thrombin. Inactivation of thrombin by AT occurs by formation of a covalent bond resulting in an inactive 1:1 stoichiometric complex between the two, involving an interaction of the active serine of thrombin and an arginine reactive site on AT. AT is also capable of inactivating other components of the coagulation cascade including factors IXa, Xa, XIa, and XIIa, as well as plasmin. The neutralization rate of serine proteases by AT proceeds slowly in the absence of heparin, but is greatly accelerated in the presence of heparin. As the therapeutic antithrombotic effect of heparin is mediated by AT, heparin in vivo is ineffective in the absence or near absence of AT. After administration, Antithrombin III human temporarily replaces the missing AT in patients with hereditary antithrombin deficiency.
Target Actions Organism UAntithrombin-III agonistHumans - Absorption
Therapeutic target plasma concentrations in patients with congenital antithrombin III deficiency range from 80–120% of values in healthy adults. At plasma concentrations ≤70% of normal, increased thrombin generation. Supraphysiologic plasma concentrations (e.g., 150–200% of normal) have increased bleeding risk in patients with sepsis and disseminated intravascular coagulation, not known whether supraphysiologic concentrations increase bleeding risk in patients with congenital antithrombin III deficiency.
- Volume of distribution
Distributed into plasma (39%), extravascular space (49%), and vascular endothelial cells (11%).
- Protein binding
Not Available
- Metabolism
<5% metabolized to low molecular weight breakdown products.
- Route of elimination
Complexes of antithrombin III with thrombin or other proteinases cleared principally by liver and excreted in urine.
- Half-life
2.5 - 3.8 hs
- Clearance
Not Available
- Adverse Effects
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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 softwareAbacavir Abacavir may decrease the excretion rate of Antithrombin III human which could result in a higher serum level. Abciximab The risk or severity of bleeding can be increased when Abciximab is combined with Antithrombin III human. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Antithrombin III human. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Antithrombin III human is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Antithrombin III human. - Food Interactions
- Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
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.- International/Other Brands
- Thrombotrol-VF (CSL Behring)
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Antithrombin III Nf Kit; Powder, for solution 1100 unit / vial Intravenous Takeda 1999-07-05 Not applicable Canada 
Antithrombin III Nf Kit; Powder, for solution 550 unit / vial Intravenous Takeda 1999-07-05 Not applicable Canada Thrombate III Injection, powder, lyophilized, for solution; Kit 50 [iU]/1mL Intravenous GRIFOLS USA, LLC 1991-12-30 2017-06-22 US 
Thrombate III Powder, for solution 500 unit / vial Intravenous Grifols Therapeutics Llc Not applicable Not applicable Canada Thrombate III Injection, powder, lyophilized, for solution; Kit 50 [iU]/1mL Intravenous GRIFOLS USA, LLC 1991-12-30 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Antithrombin III Immuno Antithrombin III human (1650 unit / kit) + Water (30 mL / kit) Powder, for solution Intravenous Baxter Ag 1999-07-05 2011-10-07 Canada Thrombate III Antithrombin III human (50 [iU]/1mL) + Water (1 mL/1mL) Injection, powder, lyophilized, for solution; Kit Intravenous GRIFOLS USA, LLC 1991-12-30 Not applicable US
Categories
- ATC Codes
- B01AB02 — Antithrombin iii
- Drug Categories
- Alpha-Globulins
- Amino Acids, Peptides, and Proteins
- Anticoagulants
- Antithrombin III
- Antithrombin III, agonists
- Antithrombin Proteins
- Biological Factors
- Blood and Blood Forming Organs
- Blood Coagulation Factor Inhibitors
- Blood Proteins
- Carbohydrates
- Drugs that are Mainly Renally Excreted
- Enzyme Inhibitors
- Globulins
- Glycosaminoglycans
- Hematologic Agents
- Oligosaccharides
- Peptides
- Polysaccharides
- Proteins
- Serum Globulins
- 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
- T0LTO7L82X
- CAS number
- 9000-94-6
References
- General References
- Cavenagh JD, Colvin BT: Guidelines for the management of thrombophilia. Department of Haematology, The Royal London Hospital, Whitechapel, London, UK. Postgrad Med J. 1996 Feb;72(844):87-94. [Article]
- Menache D, Grossman BJ, Jackson CM: Antithrombin III: physiology, deficiency, and replacement therapy. Transfusion. 1992 Jul-Aug;32(6):580-8. [Article]
- Aibiki M, Fukuoka N, Nishiyama T, Maekawa S, Shirakawa Y: Differences in antithrombin III activities by administration method in critical patients with disseminated intravascular coagulation: a pharmacokinetic study. Shock. 2007 Aug;28(2):141-7. [Article]
- Collen D, Schetz J, de Cock F, Holmer E, Verstraete M: Metabolism of antithrombin III (heparin cofactor) in man: effects of venous thrombosis and of heparin administration. Eur J Clin Invest. 1977 Feb;7(1):27-35. [Article]
- FDA label [Link]
- External Links
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 Coronavirus Disease 2019 (COVID‑19) 1 somestatus stop reason just information to hide Not Available Completed Not Available Liver Transplantation and Antithrombin 1 somestatus stop reason just information to hide Not Available Completed Prevention Complication of Transplanted Liver 1 somestatus stop reason just information to hide 4 Unknown Status Supportive Care Acute Coronary Syndrome (ACS) / Aortic Valve Insufficiency / Mitral Valve Insufficiency / Mitral Valve Stenosis / Valve Stenoses, Aortic 1 somestatus stop reason just information to hide 4 Withdrawn Supportive Care Hereditary antithrombin III deficiency 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder, for solution Parenteral 1000 UI/20ML Powder, for solution Parenteral 500 UI/10ML Injection, powder, lyophilized, for solution Intravenous 1000 IU/20ml Injection, powder, lyophilized, for solution Intravenous 500 IU/10ml Injection, powder, for solution Parenteral 50 I.E./ml Powder, for solution Intravenous Kit; powder, for solution Intravenous 1100 unit / vial Kit; powder, for solution Intravenous 550 unit / vial Powder, for solution Injection, powder, for solution Intravenous 1000 IU/20ML Injection, powder, for solution Intravenous 500 IU/10ML Powder, for solution Parenteral 1500 UI/30ML Solution Parenteral 500.000 UI Injection, powder, lyophilized, for solution Intravenous 1000 IU Powder, for solution Parenteral 2000 UI/40ML Powder, for solution Parenteral 1500 U.I./30ML Injection, powder, for solution Parenteral Solution Parenteral 500 UI Injection, powder, for solution Intravenous 1000 UI/20ML Injection, powder, for solution Intravenous 2000 UI/40ML Powder, for solution Intravenous 500 IU/10ML Injection, powder, for solution Intravenous 1000 IU Injection, powder, for solution Intravenous 500 IU Injection, powder, for solution 500 IU Injection, powder, lyophilized, for solution Intravenous 500 iu Solution Parenteral 1000.000 UI Injection, powder, lyophilized, for solution; kit Intravenous Injection, powder, lyophilized, for solution; kit Intravenous 50 [iU]/1mL Powder, for solution Intravenous 1000 unit / vial Powder, for solution Intravenous 500 unit / vial - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Agonist
- General Function
- Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade (PubMed:15140129, PubMed:15853774). AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa (PubMed:15140129). Its inhibitory activity is greatly enhanced in the presence of heparin
- Specific Function
- heparin binding
- Gene Name
- SERPINC1
- Uniprot ID
- P01008
- Uniprot Name
- Antithrombin-III
- Molecular Weight
- 52601.935 Da
References
- Menache D, Grossman BJ, Jackson CM: Antithrombin III: physiology, deficiency, and replacement therapy. Transfusion. 1992 Jul-Aug;32(6):580-8. [Article]
Drug created at May 20, 2016 20:36 / Updated at October 07, 2024 13:57