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Suspected adverse reactions reported for Lepirudin
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Data from the MHRA Yellow Card scheme. A reported reaction does not necessarily mean the medicine caused it. Contains public sector information licensed under the Open Government Licence v3.0.
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Suspected adverse reactions reported for Lepirudin
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1 branded products available
WHO defined daily dose (DDD)
250 mg
Not a recommended dose. The DDD is the assumed average maintenance dose per day for a drug used for its main indication in adults. It is a statistical measure used for research and comparison purposes only.
Source: WHO Collaborating Centre for Drug Statistics Methodology, distributed via the NHS dm+d supplementary BNF/ATC mapping files (NHSBSA). Contains public sector information licensed under the Open Government Licence v3.0.
Therapeutically similar medicines
Similarity is based on WHO Anatomical Therapeutic Chemical (ATC) classification and on a factual NHS dm+d therapeutic-grouping code prefix. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
NHS prescribing volume and spending trends
Check stock at pharmacies and supply information
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Search for this medicine at major UK pharmacy chains. These links open the retailer's own website — results depend on their current online catalogue.
Supply & safety information
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Pharmacy links redirect to the retailer's own search and do not represent real-time stock levels. Shortage and safety information sourced from MHRA drug safety updates (gov.uk, Crown Copyright under OGL v3.0).
Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF code shown is the factual mapping value distributed by NHS Business Services Authority (NHSBSA) in the dm+d supplementary file under OGL v3.0; it is not affiliated with, nor licensed from, the publishers of the British National Formulary. ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Academic studies and reviews for this medicine's active substance
Showing the 50 most relevant studies.
Reviews & meta-analyses: 8 · Randomised trials: 3 · 1999–2025
Showing the 50 most relevant studies, sorted by most relevant.
A. Greinacher, P. Eichler, N. Lubenow, et al.
Blood, 2000
- Anticoagulants
- Clinical Trials as Topic
- Heparin
The Lancet, 1999
- Electrocardiography
- Angina, Unstable
- Cardiovascular Diseases
Zhengwu Sun, Xiaoyan Lan, Shen Li, et al.
International Journal of Hematology, 2017
- Arginine
- Heparin
- Hirudins
M. Beiderlinden, P. Werner, Astrid Bahlmann, et al.
BMC Anesthesiology, 2018
- Blood Coagulation Tests
- Anticoagulants
- Arginine
T. Mollnes, O. Brekke, M. Fung, et al.
Blood, 2002
- Phagocytosis
- Respiratory Burst
- Blood Cells
A. Greinacher, H. Völpel, U. Janssens, et al.
Circulation, 1999
- Anticoagulants
- Germany
- Hemorrhage
Andreas Greinacher, Uwe Janssens, Günther Berg, et al.
Circulation, 1999
- Amputation, Surgical
- Anticoagulants
- Autoimmune Diseases
N. Lubenow, P. Eichler, T. Lietz, et al.
Journal of Thrombosis and Haemostasis, 2005
- Amputation, Surgical
- Anticoagulants
- Hemorrhage
Andreas Greinacher, Norbert Lübenow, Petra Eichler
Circulation, 2003
- Anaphylaxis
- Anticoagulants
- Cardiovascular Diseases
P. Eichler, H. Friesen, N. Lubenow, et al.
Blood, 2000
- Partial Thromboplastin Time
- Amputation, Surgical
- Antibodies
Sources: aggregated from Europe PMC (EMBL-EBI), OpenAlex, Crossref, PubMed and other open scholarly databases. Retracted articles are excluded. Study information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
153 found
Half-life
10 minutes
Mechanism
Lepirudin is a direct thrombin inhibitor used as an anticoagulant in patients for whom heparin is contraindicated.
Food interactions
1 warning
Human targets
1 target
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
0.4 mg/k
Half-life
10 minutes
Protein binding
3%
[L41539]
Volume of distribution
12.2 L
Metabolism
[L41539][L41544]…
Elimination
48.3%
Clearance
164 mL/min
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Lepirudin is used as an anticoagulant in patients with heparin-induced thrombocytopenia (HIT), an immune reaction associated with a high risk of thromboembolic complications.[A3][L41539] HIT is caused by the expression of immunoglobulin G (IgG) antibodies that bind to the complex formed by heparin and platelet factor 4. This activates endothelial cells and platelets and enhances the formation of thrombi.[A246609] Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.[L41574]
[L41539]
Lepirudin is also indicated for anticoagulation in patients with heparin-induced thrombocytopenia (HIT) and associated thromboembolic disease in order to prevent further thromboembolic complications.
[L41539]
Known interactions with other medications. Always consult a healthcare professional.
Showing 50 of 654 interactions
[L41539]
The acute toxicity of lepirudin administered subcutaneously was also evaluated in mice (1-1250 mg/kg) and rats (1-500 mg/kg), and no toxicity was detected.
[L41539]
One rat (100 mg/kg) died of rapid blood loss after the subcutaneous administration of lepirudin. Reactions to local injections such as hemorrhages, hematomas and/or nodules were detected in mice and rats given subcutaneous doses of lepirudin equal or higher than 500 mg/kg and 10 mg/kg, respectively.
[L41539]
Chronic toxicity was evaluated in rats and monkeys given lepirudin for up to 3 months. Most of the effects observed were due to the antithrombotic action of lepirudin.
After 3 months, hemosiderin deposits in the spleen and moderate sinus histiocytosis in the lymph node were observed in rats. In monkeys, external and internal hemorrhages and hematomas were detected.
[L41539]
Lepidurin was reported as not mutagenic.
[L41539]
Relative overdose may occur in patients with renal impairment, therefore, bolus dose and rate of infusion must be reduced in case of known or suspected renal insufficiency.
[L41539]
Excessively high activated partial thromboplastin time (aPTT) values suggest an overdose and a risk of bleeding. Lepirudin has no known antidote.
In case of life-threatening bleeding and if excessive plasma levels of lepirudin are suspected: 1)stop the administration of lepirudin immediately, 2) determine aPTT and coagulation parameters, 3) determine hemoglobin, and prepare for a transfusion, 4) follow the treatment guidelines for patients with shock.
[L41539]
Hemofiltration or hemodialysis may be useful in case of overdose, based in single case reports and animal data.
[L41539]
Lepirudin binds to the catalytic and substrate-binding sites of thrombin, forming a stable, irreversible and non-covalent complex.[A246609] This blocks the protease activity of thrombin and inhibits the coagulation process. Each molecule of lepirudin binds to a single molecule of thrombin,[L41539] and unlike [heparin], it is able to inhibit thrombin in both its clot-bound or free states.[A246609]
The pharmacodynamic effect of lepirudin was evaluated by measuring an increase in aPTT. No saturable effect was observed at the highest tested dose (0.5 mg/kg, IV bolus).[L41539] Thrombin time was considered an unsuitable routine test for lepirudin monitoring due to the high values detected (200 seconds) even at low doses.[L41539] The concomitant use of thrombolytic therapy and lepirudin is not recommended due to the high risk of bleeding that may be life-threatening. In patients with a risk of bleeding, a physician should weigh the risks of lepirudin administration against its benefits. There is also an especially high risk of bleeding in patients who weigh less than 50 kg, and a lower dosage is required. Patients with renal impairment have a higher risk of hemorrhagic adverse events.[L41539]
How the body processes this drug — absorption, distribution, metabolism, and elimination
[L41539]
When 0.1, 0.15 and 0.2 mg/kg of lepirudin was administered as a single intravenous infusion over 6 hours in healthy male volunteers, lepirudin had a corresponding Cmax of 111, 203, and 2446 ng/mL and a corresponding AUC of 612, 1184, and 1446 ng•h/mL.
[L41544]
Bioavailability is 100% following injection. Also, it has been reported that following subcutaneous (sc) administration, the bioavailability of lepirudin is almost 100%.
[A246609]
[L41539]
Lepirudin has a first-order elimination kinetic; plasma concentration increases proportionally as the lepirudin intravenous dose is increased. Elimination half-life values of up to 2 days were detected in patients with marked renal insufficiency (creatinine clearance < 15 mL/min).
[L41539]
[L41539]
[L41539]
The distribution of lepirudin is mainly restricted to extracellular fluids.
[L41539]
[L41539][L41544]
The C-terminal cleavage of lepirudin aminoacids (aminoacids 1 to 65) produces four metabolites with anti-thrombotic activity: M1 (aminoacids 1 to 64), M2 (aminoacids 1 to 63), M3 (aminoacids 1 to 62), and M4 (aminoacids 1 to 61).
[L41544]
[L41544]
[L41539]
This is possibly due to the lower creatinine clearance in elderly patients.
In renally impaired subjects (n=16, creatinine clearance < 80 mL/min), clearance was 61 mL/min, and in heparin-induced thrombocytopenia patients (n=73), it was 114 mL/min.
[L41539]
Proteins and enzymes this drug interacts with in the body
PMID:2019570 PMID:21976677
Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL8/CXCL8, in endothelial cells PMID:30568593 PMID:9780208
Involved compounds
ATC B01AE02
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Lepirudin
Additional database identifiers
Drugs Product Database (DPD)
11916
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3535
GenAtlas
F2
GeneCards
F2
GenBank Gene Database
M17262
GenBank Protein Database
339641
Guide to Pharmacology
2362
UniProt Accession
THRB_HUMAN
DrugBank citations
If you use DrugBank data in your research, please cite the following publications:
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Structured knowledge from the free knowledge base
ATC classifications (Wikidata)
Linked open data from Wikidata (Q3271949), a free and open knowledge base operated by the Wikimedia Foundation. Data is available under the Creative Commons CC0 1.0 Public Domain Dedication.