Nadroparin
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Identification
- Summary
Nadroparin is a low molecular weight heparin used for the prophylaxis of thrombotic events and deep vein thrombosis, and prevent unstable angina and non-Q-wave myocardial infarction.
- Brand Names
- Fraxiparine
- Generic Name
- Nadroparin
- DrugBank Accession Number
- DB08813
- Background
Nadroparin is a low molecular weight heparin (LMWH) which, when bound to antithrombin III (ATIII), accelerates the inactivation of factor II and factor Xa. Nadroparin halts the coagulation pathway by inhibiting the activation of thrombin (factor IIa) by factor Xa. The amplification of the fibrin clotting cascade is stopped once factors Xa and IIa are inactivated. It is derived from porcine sources and has a mean molecular size of 5000 daltons. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Synonyms
- Nadroparina
- Nadroparine
Pharmacology
- Indication
Nadroparin is used for prophylaxis of thromboembolic disorders and general surgery in orthopedic surgery, treatment of deep vein thrombosis, prevention of clotting during hemodialysis and treatment of unstable angina and non-Q wave myocardial infarction.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prophylaxis of Clotting •••••••••••• Treatment of Dvt •••••••••••• Prophylaxis of Pulmonary embolism •••••••••••• Used in combination for prophylaxis of Thromboembolic events Combination Product in combination with: Water (DB09145) •••••••••••• ••••••••• •••• •••••••• Used in combination for prophylaxis of Thromboembolic events Combination Product in combination with: Water (DB09145) •••••••••••• ••••••••• •••• •••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Nadroparin is a low molecular weight heparin that is composed of a heterogeneous mixture of sulfated polysaccaride glycosaminoglycan chains. Th mean molecular weight is approximately 4300 daltons. The ratio of anti-Xa activity to anti-IIa is 3.5:1 whereas it is about 1:1 for heparin. Its use should be avoided in patients with a creatinine clearance less than 40mL/min. In these patients, unfractionated heparin should only be used. As for monitoring, active partial thromboplastin time (aPTT) will only increase at high doses of low molecular weight heparins (LMWH). Therefore, monitoring aPTT is not recommended. However, anti-Xa activity can be measured to monitor the efficacy of the LMWH.
- Mechanism of action
The mechanism of action for nadroparin is similar to all other LMWHs. Like all LMWHs, nadroparin has a pentasaccharide sequence which binds to ATIII, which potentiates the action of ATIII. This complex greatly accelerates the inactivation of factor Xa and factor IIa. As a result, the coagulation cascade is inhibited.
Target Actions Organism AAntithrombin-III potentiatorHumans UP-selectin inhibitorHumans UProtein c-Fos inhibitorHumans UMyc proto-oncogene protein inhibitorHumans - Absorption
Absorption is linear. The bioavailability of nadroparin after subcutaneous administration is about 89%.
- Volume of distribution
3.59L
- Protein binding
Much lower compared to heparin, which has over 90% protein bound.
- Metabolism
Nadroparin is metabolized in the liver.
- Route of elimination
Nadroparin is eliminated via the kidneys through non-saturable mechanisms.
- Half-life
In healthy patients, the half life is between 3.5hrs to 11.2hrs following subcutaneous administration.
- Clearance
The clearance of nadroparin is 21.4 +/- 7.0mL/min
- Adverse Effects
- Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.
- Toxicity
Osteopenia with extended use, skin necrosis, thrombocytosis, severe immunologically-mediated thrombocytopenia, eosinophilia (rare), calcinosis rarely occurs at the injection site, severe bleeding, transient elevation of liver transaminases.
- 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 Nadroparin. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Nadroparin. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Nadroparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Nadroparin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Nadroparin. - 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 Nadroparin calcium LIA7Z4002P 37270-89-6 Not applicable - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fraxiparine Solution 9500 unit / mL Intravenous; Subcutaneous Aspen Pharmacare Canada Inc. 1998-02-05 Not applicable Canada Fraxiparine Solution 9500 unit / mL Intravenous; Subcutaneous Aspen Pharmacare Canada Inc. 1998-02-05 Not applicable Canada Fraxiparine Solution 9500 unit / mL Intravenous; Subcutaneous Aspen Pharmacare Canada Inc. 1998-02-05 Not applicable Canada Fraxiparine Solution 9500 unit / mL Intravenous; Subcutaneous Aspen Pharmacare Canada Inc. 1998-02-05 Not applicable Canada Fraxiparine Solution 9500 unit / mL Intravenous; Subcutaneous Aspen Pharmacare Canada Inc. 1998-02-05 Not applicable Canada - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image FRAXIPARINE 2850 IU/0.3 ML 2 ENJEKTOR Nadroparin calcium (2850 IU) Solution Subcutaneous VLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ. 2020-08-14 2022-10-14 Turkey FRAXIPARINE 3800 IU/0.4 ML 2 ENJEKTOR Nadroparin calcium (3800 IU) Solution Subcutaneous VLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ. 2020-08-14 2022-10-14 Turkey FRAXIPARINE 5700 IU/0.6 ML 2 ENJEKTOR Nadroparin calcium (5700 IU) Solution Subcutaneous VLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ. 2020-08-14 2022-10-14 Turkey
Categories
- ATC Codes
- B01AB06 — Nadroparin
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 1K5KDI46KZ
- CAS number
- Not Available
References
- General References
- Collignon F, Frydman A, Caplain H, Ozoux ML, Le Roux Y, Bouthier J, Thebault JJ: Comparison of the pharmacokinetic profiles of three low molecular mass heparins--dalteparin, enoxaparin and nadroparin--administered subcutaneously in healthy volunteers (doses for prevention of thromboembolism). Thromb Haemost. 1995 Apr;73(4):630-40. [Article]
- Frydman A: Low-molecular-weight heparins: an overview of their pharmacodynamics, pharmacokinetics and metabolism in humans. Haemostasis. 1996;26 Suppl 2:24-38. [Article]
- Lai KN, Wang AY, Ho K, Szeto CC, Li M, Wong LK, Yu AW: Use of low-dose low molecular weight heparin in hemodialysis. Am J Kidney Dis. 1996 Nov;28(5):721-6. [Article]
- Boneu B, Navarro C, Cambus JP, Caplain H, d'Azemar P, Necciari J, Duret JP, Gaud C, Sie P: Pharmacodynamics and tolerance of two nadroparin formulations (10,250 and 20,500 anti Xa IU x ml(-1)) delivered for 10 days at therapeutic dose. Thromb Haemost. 1998 Feb;79(2):338-41. [Article]
- Laporte S, Mismetti P, Piquet P, Doubine S, Touchot A, Decousus H: Population pharmacokinetic of nadroparin calcium (Fraxiparine) in children hospitalised for open heart surgery. Eur J Pharm Sci. 1999 May;8(2):119-25. [Article]
- Ng HJ, Lee LH: Heparin-induced thrombocytopenia: acknowledging its presence in low-molecular weight heparin therapy. Int J Hematol. 2003 Feb;77(2):185-7. [Article]
- Breddin HK: Prophylaxis and treatment of deep-vein thrombosis. Semin Thromb Hemost. 2000;26 Suppl 1:47-52. [Article]
- Haas SK: Venous thromboembolic risk and its prevention in hospitalized medical patients. Semin Thromb Hemost. 2002 Dec;28(6):577-84. [Article]
- Davis R, Faulds D: Nadroparin calcium. A review of its pharmacology and clinical use in the prevention and treatment of thromboembolic disorders. Drugs Aging. 1997 Apr;10(4):299-322. [Article]
- Iaremchuk AIa, Zotov AS, Cheshuk VE, Anikuc'ko NF, Zakhartseva LM, Diatel MV, Kravchenko AV, Lobanova OE, Sidorchuk OI: [Clinical effectiveness of nadroparin calcium in the surgical treatment of breast cancer]. Vopr Onkol. 2003;49(2):205-8. [Article]
- Vitale FV, Rotondo S, Sessa E, Antonelli G, Colina P, Parisi A, Giamo V, Ferrau F: Successful administration of a low dose of calcium nadroparin in patients suffering from pulmonary embolism and brain metastases: a report of two cases. J Oncol Pharm Pract. 2011 Jun;17(2):141-4. doi: 10.1177/1078155209353465. Epub 2009 Dec 16. [Article]
- Agnelli G, Gussoni G, Bianchini C, Verso M, Mandala M, Cavanna L, Barni S, Labianca R, Buzzi F, Scambia G, Passalacqua R, Ricci S, Gasparini G, Lorusso V, Bonizzoni E, Tonato M: Nadroparin for the prevention of thromboembolic events in ambulatory patients with metastatic or locally advanced solid cancer receiving chemotherapy: a randomised, placebo-controlled, double-blind study. Lancet Oncol. 2009 Oct;10(10):943-9. doi: 10.1016/S1470-2045(09)70232-3. Epub 2009 Aug 31. [Article]
- External Links
- PubChem Substance
- 347910374
- 67031
- Wikipedia
- Nadroparin_calcium
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 Anticoagulants and Bleeding Disorders / Coronavirus Disease 2019 (COVID‑19) / Mechanical Ventilation / Nadroparin / Thrombosis 1 somestatus stop reason just information to hide Not Available Completed Not Available Unsuspected Pulmonary Embolism 1 somestatus stop reason just information to hide Not Available Completed Prevention Deep Vein Thrombosis / Pulmonary Embolism 2 somestatus stop reason just information to hide Not Available Completed Prevention Esophageal Neoplasms / Lung Neoplasm / Venous Thromboembolism 1 somestatus stop reason just information to hide Not Available Not Yet Recruiting Treatment Portal Vein Thrombosis 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Parenteral Injection, solution Parenteral 0.3 ML Injection, solution Parenteral 0.4 ML Injection, solution Parenteral 0.6 ML Injection, solution Parenteral 0.8 ML Injection, solution Parenteral 1.0 ML Injection, solution Parenteral Injection, solution Parenteral 11400 UI/0.6ML Injection, solution Parenteral 15200 UI/0.8ML Injection, solution Parenteral 19000 UI/1ML Injection, solution Parenteral 2850 UI/0.3ML Injection, solution Parenteral 3800 UI/0.4ML Injection, solution Parenteral 5700 UI/0.6ML Injection, solution Parenteral 7600 UI/0.8ML Injection, solution Parenteral 9500 UI/1ML Injection, solution Parenteral 2850 IU Injection, solution Parenteral 3800 IU Injection, solution Parenteral 5700 IU Injection, solution Parenteral 7600 IU Injection 2850 IU/0.3ml Solution Intravenous; Subcutaneous 9500 unit / mL Solution Hemodialysis; Intravenous; Subcutaneous 1900 IU Injection, solution Parenteral 0.2 ML Solution Hemodialysis; Intravenous; Subcutaneous Injection Subcutaneous Solution Hemodialysis; Intravenous; Subcutaneous 3800 IU Solution Hemodialysis; Intravenous; Subcutaneous 5700 IU Solution Subcutaneous 7600 IU Injection, solution Parenteral 9500 IU Solution Subcutaneous 9500 IU Injection, solution Parenteral 1 ML Solution Subcutaneous 2850 IU Solution Subcutaneous 3800 IU Solution Subcutaneous 5700 IU Solution Intravenous; Subcutaneous 19000 unit / mL Injection Subcutaneous 19000 IU AXA/mL Injection Subcutaneous 1900 IU AXA/0.2 mL Injection Subcutaneous 2850 IU AXA/0.3ml Injection Subcutaneous 3800 IU AXA/0.4ml Injection Subcutaneous 5700 IU AXA/0.6ml Injection Subcutaneous 7600 IU AXA/0.8 mL Injection Subcutaneous 9500 IU AXA/1.0 mL Injection Intravenous; Subcutaneous 9500 IU AXA/mL Solution Subcutaneous 11400 iu Solution Subcutaneous 15200 iu Injection, solution Parenteral 19.000 I.E. Solution Subcutaneous 19000 iu Injection, solution Parenteral 11400 IU/0.6ml Injection, solution Parenteral 15200 IU/0.8ml Injection, solution Parenteral 19000 IU/ml Injection, solution Parenteral 2.85 IU/0.3ml Injection, solution Parenteral 2.850 UI/0.3ML Injection, solution Parenteral 3800 IU/0.4ml Injection, solution Parenteral 5700 IU/0.6ml Injection, solution Parenteral 7600 IU/0.8ml Injection, solution Parenteral 9500 IU/ml Solution 9500 IU/1ml - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
- Not Available
- Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Potentiator
- 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
- Davis R, Faulds D: Nadroparin calcium. A review of its pharmacology and clinical use in the prevention and treatment of thromboembolic disorders. Drugs Aging. 1997 Apr;10(4):299-322. [Article]
- Frydman A: Low-molecular-weight heparins: an overview of their pharmacodynamics, pharmacokinetics and metabolism in humans. Haemostasis. 1996;26 Suppl 2:24-38. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Ca(2+)-dependent receptor for myeloid cells that binds to carbohydrates on neutrophils and monocytes. Mediates the interaction of activated endothelial cells or platelets with leukocytes. The ligand recognized is sialyl-Lewis X. Mediates rapid rolling of leukocyte rolling over vascular surfaces during the initial steps in inflammation through interaction with SELPLG. Mediates cell-cell interactions and cell adhesion via the interaction with integrin alpha-IIb/beta3 (ITGA2B:ITGB3) and integrin alpha-V/beta-3 (ITGAV:ITGB3) (PubMed:37184585)
- Specific Function
- calcium ion binding
- Gene Name
- SELP
- Uniprot ID
- P16109
- Uniprot Name
- P-selectin
- Molecular Weight
- 90819.085 Da
References
- Simonis D, Christ K, Alban S, Bendas G: Affinity and kinetics of different heparins binding to P- and L-selectin. Semin Thromb Hemost. 2007 Jul;33(5):534-9. [Article]
- Ludwig RJ, Alban S, Bistrian R, Boehncke WH, Kaufmann R, Henschler R, Gille J: The ability of different forms of heparins to suppress P-selectin function in vitro correlates to their inhibitory capacity on bloodborne metastasis in vivo. Thromb Haemost. 2006 Mar;95(3):535-40. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Nuclear phosphoprotein which forms a tight but non-covalently linked complex with the JUN/AP-1 transcription factor. In the heterodimer, FOS and JUN/AP-1 basic regions each seems to interact with symmetrical DNA half sites. On TGF-beta activation, forms a multimeric SMAD3/SMAD4/JUN/FOS complex at the AP1/SMAD-binding site to regulate TGF-beta-mediated signaling. Has a critical function in regulating the development of cells destined to form and maintain the skeleton. It is thought to have an important role in signal transduction, cell proliferation and differentiation. In growing cells, activates phospholipid synthesis, possibly by activating CDS1 and PI4K2A. This activity requires Tyr-dephosphorylation and association with the endoplasmic reticulum
- Specific Function
- chromatin binding
- Gene Name
- FOS
- Uniprot ID
- P01100
- Uniprot Name
- Protein c-Fos
- Molecular Weight
- 40694.855 Da
References
- Nagy Z, Turcsik V, Blasko G: The effect of LMWH (Nadroparin) on tumor progression. Pathol Oncol Res. 2009 Dec;15(4):689-92. doi: 10.1007/s12253-009-9204-7. [Article]
- Sustar V, Jansa R, Frank M, Hagerstrand H, Krzan M, Iglic A, Kralj-Iglic V: Suppression of membrane microvesiculation--a possible anticoagulant and anti-tumor progression effect of heparin. Blood Cells Mol Dis. 2009 May-Jun;42(3):223-7. doi: 10.1016/j.bcmd.2009.01.012. Epub 2009 Mar 3. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transcription factor that binds DNA in a non-specific manner, yet also specifically recognizes the core sequence 5'-CAC[GA]TG-3' (PubMed:24940000, PubMed:25956029). Activates the transcription of growth-related genes (PubMed:24940000, PubMed:25956029). Binds to the VEGFA promoter, promoting VEGFA production and subsequent sprouting angiogenesis (PubMed:24940000, PubMed:25956029). Regulator of somatic reprogramming, controls self-renewal of embryonic stem cells (By similarity). Functions with TAF6L to activate target gene expression through RNA polymerase II pause release (By similarity). Positively regulates transcription of HNRNPA1, HNRNPA2 and PTBP1 which in turn regulate splicing of pyruvate kinase PKM by binding repressively to sequences flanking PKM exon 9, inhibiting exon 9 inclusion and resulting in exon 10 inclusion and production of the PKM M2 isoform (PubMed:20010808)
- Specific Function
- core promoter sequence-specific DNA binding
- Gene Name
- MYC
- Uniprot ID
- P01106
- Uniprot Name
- Myc proto-oncogene protein
- Molecular Weight
- 50564.535 Da
References
- Nagy Z, Turcsik V, Blasko G: The effect of LMWH (Nadroparin) on tumor progression. Pathol Oncol Res. 2009 Dec;15(4):689-92. doi: 10.1007/s12253-009-9204-7. [Article]
- Sustar V, Jansa R, Frank M, Hagerstrand H, Krzan M, Iglic A, Kralj-Iglic V: Suppression of membrane microvesiculation--a possible anticoagulant and anti-tumor progression effect of heparin. Blood Cells Mol Dis. 2009 May-Jun;42(3):223-7. doi: 10.1016/j.bcmd.2009.01.012. Epub 2009 Mar 3. [Article]
Drug created at June 15, 2011 05:17 / Updated at October 03, 2024 07:19