Bemiparin
Identification
- Summary
Bemiparin is an ultra-low molecular weight heparin (ultra-LMWH) used to prevent thromboembolism following surgery and extracorporeal clotting during dialysis.
- Generic Name
- Bemiparin
- DrugBank Accession Number
- DB09258
- Background
Bemiparin is an antithrombotic and belongs to the group of drugs known as the low molecular weight heparins (LMWH). Like semuloparin, bemiparin is classified as an ultra-LMH because of its low mean molecular mass of 3600 daltons, which is a unique property of this class 1. These heparins have lower anti-thrombin activity than the traditional low molecular weight heparins and act mainly on factor-Xa, reducing the risk of bleeding due to selectivity for this specific clotting factor. Interestingly, current research is underway for the potential benefit of bemiparin in the treatment of tumors and diabetic foot ulcers 12,1.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Not Available
Pharmacology
- Indication
Bemiparin is indicated in the following cases: To prevent blood clots in the veins after general abdominal surgery in patients with a moderate risk of venous thromboembolism; in the prevention of the thromboembolic disease in non-surgical patients; prevention of clotting in the extracorporeal circuit during hemodialysis; to prevent blood clots in the veins after a major orthopedic surgery in patients with high risk of venous thromboembolism; secondary prevention of venous thromboembolism; recurrence in patients with deep vein thrombosis; transient prevention and treatment of deep vein thrombosis (DVT) 8.
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- Associated Therapies
- Contraindications & Blackbox Warnings
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- Pharmacodynamics
Bemiparin is an anticoagulant classified under the broad category of low molecular weight heparins. In humans, bemiparin has been proven to possess antithrombotic activity and, at therapeutic doses, does not significantly prolong global clotting laboratory tests 9.
- Mechanism of action
This drug is a second-generation low molecular weight heparin (LMWH). It has a very low mean molecular weight (3600 Dalton), a long half-life (5.3 hrs) and a large anti-Xa: anti-IIa ratio (8:1)8. The mechanism of action of bemiparin is inhibition of factor Xa, which is a necessary step in the clotting cascade. Factor-Xa is necessary for the propagation of a thrombus. Combined with various co-factors that bind to activated platelets, Factor-Xa increases coagulation by converting prothrombin to thrombin 11. Activated Factor-X, bound as part of the prothrombinase complex on the external surface of activated platelets, converts significant amounts of prothrombin to thrombin, promoting the so-called ‘thrombin burst’, referring to a burst of thrombin release 11.
A secondary but less potent mechanism of action of this drug is binding to antithrombin III and activated factor II (Factor IIa), which further prevents the propagation of thrombi 14.
Due to its excellent pharmacological profile-the second-generation LMWH with the lowest molecular weight, the longest half-life and the highest anti-Factor Xa/anti-Factor IIa activity ratio-it can be safely used in special categories of patients (children, elderly, patients with renal impairment and congestive heart failure). Several studies demonstrated its safety and efficacy, while cost analyses show the economic benefits of bemiparin treatment as compared to other heparins 1,2.
Target Actions Organism ACoagulation factor X antagonistHumans UAntithrombin-III antagonistHumans UHeparin cofactor 2 antagonistHumans - Absorption
Hemiparin sodium is rapidly absorbed following its subcutaneous dose of injection, and the bioavailability is estimated to be 96% 7.
- Volume of distribution
5.1 L 4.
- Protein binding
There are currently no data available with regards to plasma protein binding, metabolism and excretion of bemiparin in humans 9.
- Metabolism
In a study of healthy volunteers, bemiparin 3500 IU achieved more anti-Xa activity than enoxaparin 4000 IU, measured by the area under the curve. The peak of anti-Xa activity was reached at 3h post-administration, and there were anti-Xa measurable levels up to 16 h after subcutaneous injection 6.
- Route of elimination
This drug is eliminated by the renal and hepatic routes. Elimination is prolonged in those with renal or hepatic impairment 10.
- Half-life
Bemiparin, when administered in the dose range of 2,500 IU to 12,500 (therapeutic dosing), it has an approximate half-life of 5-6 hours 7.
- Clearance
Elimination occurs in a linear fashion, with a mean clearance time of over 7 h and total clearance of 0.9 L/h 4.
- Adverse Effects
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- Toxicity
Bemiparin, like other drugs in its class, may suppress adrenal secretion of aldosterone, leading to elevated potassium (hyperkalemia). This may occur more frequently in patients with conditions such as diabetes mellitus, chronic renal failure, metabolic acidosis, an increased plasma potassium, and those ingesting potassium sparing drugs. There is a linear relationship between duration of therapy and adverse effects, but this is usually reversible with cessation of treatment. Serum electrolytes should be measured in at-risk patients before starting bemiparin, and these patients should be monitored regularly thereafter particularly if treatment is prolonged beyond 1 week.
In rare cases, mild transient thrombocytopenia (HIT type I) at the beginning of therapy with heparin with platelet counts between 100,000/mm3 and 150,000/mm3 due to temporary platelet activation has been noted in clinical studies.
On rare occasions, antibody-mediated severe thrombocytopenia (HIT type II) with platelet counts clearly below 100,000/mm3 has been observed (see section 4.8). This effect usually occurs within 5-21 days after the initiation of treatment, although in patients with a history of heparin-induced thrombocytopenia this may occur more rapidly.
Platelet count studies are recommended before the administration of bemiparin, on the first day of therapy and then every 3-4 days, in addition to repeating platelet studies at the end of therapy. Treatment must be discontinued immediately and an alternate therapy initiated if significant reductions in platelet counts are observed ( 30% decrease and above) 7.
As with other heparin products, cases of cutaneous necrosis, often preceded by purpura or painful erythematous, ecchymose-like lesions have been reported with bemiparin. In these cases, treatment should cease immediately 7.
Overdosage after subcutaneous or other routes of administration of bemiparin may lead to hemorrhagic complications. Neutralization can be obtained by slow intravenous of a suitable dose of the antidote protamine sulphate 8.
- 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 risk or severity of bleeding can be increased when Abciximab is combined with Bemiparin. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Bemiparin. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Bemiparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Bemiparin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Bemiparin. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Bemiparin. Albutrepenonacog alfa The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Bemiparin. Alclofenac The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Bemiparin. Aldesleukin The risk or severity of bleeding can be increased when Bemiparin is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Bemiparin is combined with Alemtuzumab. Identify potential medication risksEasily compare up to 40 drugs with our drug interaction checker.Get severity rating, description, and management advice.Learn more - 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.
- Product Ingredients
Ingredient UNII CAS InChI Key Bemiparin sodium P59JKU02CE Not Available Not applicable - International/Other Brands
- Badyket / Heporax / Hibor / Zibor
Categories
- ATC Codes
- B01AB12 — Bemiparin
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Humans
Chemical Identifiers
- UNII
- PUE0TO3XDR
- CAS number
- 91449-79-5
- InChI Key
- Not Available
- InChI
- Not Available
- IUPAC Name
- Not Available
- SMILES
- Not Available
References
- General References
- Chapman TM, Goa KL: Bemiparin: a review of its use in the prevention of venous thromboembolism and treatment of deep vein thrombosis. Drugs. 2003;63(21):2357-77. [Article]
- Planes A: Review of bemiparin sodium--a new second-generation low molecular weight heparin and its applications in venous thromboembolism. Expert Opin Pharmacother. 2003 Sep;4(9):1551-61. [Article]
- Jeske WP, Hoppensteadt D, Gray A, Walenga JM, Cunanan J, Myers L, Fareed J, Bayol A, Rigal H, Viskov C: A common standard is inappropriate for determining the potency of ultra low molecular weight heparins such as semuloparin and bemiparin. Thromb Res. 2011 Oct;128(4):361-7. doi: 10.1016/j.thromres.2011.03.001. Epub 2011 Apr 2. [Article]
- Sanchez-Ferrer CF: Bemiparin: pharmacological profile. Drugs. 2010 Dec 14;70 Suppl 2:19-23. doi: 10.2165/1158581-S0-000000000-00000. [Article]
- Hoffman M, Monroe DM: Coagulation 2006: a modern view of hemostasis. Hematol Oncol Clin North Am. 2007 Feb;21(1):1-11. doi: 10.1016/j.hoc.2006.11.004. [Article]
- Antonijoan RM, Rico S, Martinez-Gonzalez J, Borrell M, Valcarcel D, Fontcuberta J, Barbanoj MJ: Comparative pharmacodynamic time-course of bemiparin and enoxaparin in healthy volunteers. Int J Clin Pharmacol Ther. 2009 Dec;47(12):726-32. [Article]
- Irish Medicines Board: Bemiparin [Link]
- Hibor-Bemiparin Sodium [Link]
- Zibor 2,500 IU Solution for Injection [Link]
- Injectable drugs guide [Link]
- Thrombosis Advisors- Factor Xa inhibitor [Link]
- Anti-tumor effects of bemiparin in HepG2 and MIA PaCa-2 cells [Link]
- Bemiparin, an effective and safe low molecular weight heparin: a review [Link]
- Bemiparin sodium [Link]
- External Links
- PubChem Substance
- 347910422
- 280611
- Wikipedia
- Bemiparin_sodium
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Treatment Acute Gastrointestinal Bleeding 1 4 Recruiting Treatment Infertility 1 3 Completed Prevention Cancer / Venous Thromboembolism 1 3 Completed Treatment Deep Vein Thrombosis 1 3 Completed Treatment Diabetic Foot Ulcers (DFUs) 1 3 Terminated Prevention Cancer / Thrombosis 1 3 Terminated Treatment Long-term Oral Anticoagulant Therapy 1 3 Terminated Treatment Neoplasm / Venous Thromboembolism 1 3 Unknown Status Prevention Cirrhosis and Coagulation 1 3 Unknown Status Prevention Coronavirus Disease 2019 (COVID‑19) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Parenteral 10000 IU/0.4mL Injection Intravenous 10000 iu/0.4ml Injection, solution Parenteral 2500 IU/0.2mL Injection Intravenous 2500 iu/0.2ml Injection, solution Parenteral 3500 IU/0.2mL Injection Intravenous 3500 iu/0.2ml Injection, solution Parenteral 5000 IU/0.2mL Injection Intravenous 5000 iu/0.2ml Injection, solution Parenteral 7500 IU/0.3mL Injection Intravenous 7500 iu/0.3ml Solution Subcutaneous 10000 IU Solution Subcutaneous 3500 IU Solution Subcutaneous 5000 IU Solution Subcutaneous 7500 IU Solution Subcutaneous 2500 IU Injection, solution Parenteral 2500 UI/0.2ML Injection, solution Parenteral 25000 UI/ML Injection, solution Parenteral 3500 UI/0.2ML Injection, solution Subcutaneous 0.2 ml Injection, solution Subcutaneous 25000 IE - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) >228 https://www.trc-canada.com/prod-img/MSDS/H245800MSDS.pdf - Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
Targets

- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Antagonist
- 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
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Most important serine protease inhibitor in plasma that regulates the blood coagulation cascade. AT-III inhibits thrombin, matriptase-3/TMPRSS7, as well as factors IXa, Xa and XIa. Its inhibitory a...
- Gene Name
- SERPINC1
- Uniprot ID
- P01008
- Uniprot Name
- Antithrombin-III
- Molecular Weight
- 52601.935 Da
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Antagonist
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Thrombin inhibitor activated by the glycosaminoglycans, heparin or dermatan sulfate. In the presence of the latter, HC-II becomes the predominant thrombin inhibitor in place of antithrombin III (AT...
- Gene Name
- SERPIND1
- Uniprot ID
- P05546
- Uniprot Name
- Heparin cofactor 2
- Molecular Weight
- 57070.16 Da
Drug created at October 26, 2015 16:50 / Updated at May 07, 2021 21:40