Nadroparin

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.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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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.

TargetActionsOrganism
AAntithrombin-III
potentiator
Humans
UP-selectin
inhibitor
Humans
UProto-oncogene c-Fos
inhibitor
Humans
UMyc proto-oncogene protein
inhibitor
Humans
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
Adverseeffects
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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.
DrugInteraction
AbciximabThe risk or severity of bleeding can be increased when Abciximab is combined with Nadroparin.
AcebutololThe risk or severity of hyperkalemia can be increased when Acebutolol is combined with Nadroparin.
AceclofenacThe risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Nadroparin.
AcemetacinThe risk or severity of bleeding and hemorrhage can be increased when Nadroparin is combined with Acemetacin.
AcenocoumarolThe risk or severity of bleeding can be increased when Acenocoumarol is combined with Nadroparin.
Acetylsalicylic acidAcetylsalicylic acid may increase the anticoagulant activities of Nadroparin.
Albutrepenonacog alfaThe therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Nadroparin.
AlclofenacThe risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Nadroparin.
AldesleukinThe risk or severity of bleeding can be increased when Nadroparin is combined with Aldesleukin.
AlemtuzumabThe risk or severity of bleeding can be increased when Nadroparin is combined with Alemtuzumab.
Interactions
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Food Interactions
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Nadroparin calciumLIA7Z4002P37270-89-6Not applicable
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FraxiparineSolution9500 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1998-02-05Not applicableCanada flag
FraxiparineSolution9500 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1998-02-05Not applicableCanada flag
FraxiparineSolution9500 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1998-02-05Not applicableCanada flag
FraxiparineSolution9500 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1998-02-05Not applicableCanada flag
FraxiparineSolution9500 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1998-02-05Not applicableCanada flag
Fraxiparine ForteSolution19000 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1999-06-22Not applicableCanada flag
Fraxiparine ForteSolution19000 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1999-06-22Not applicableCanada flag
Fraxiparine ForteSolution19000 unit / mLIntravenous; SubcutaneousAspen Pharmacare Canada Inc.1999-06-22Not applicableCanada flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
FRAXIPARINE 2850 IU/0.3 ML 2 ENJEKTORNadroparin calcium (2850 IU)SolutionSubcutaneousVLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ.2020-08-14Not applicableTurkey flag
FRAXIPARINE 3800 IU/0.4 ML 2 ENJEKTORNadroparin calcium (3800 IU)SolutionSubcutaneousVLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ.2020-08-14Not applicableTurkey flag
FRAXIPARINE 5700 IU/0.6 ML 2 ENJEKTORNadroparin calcium (5700 IU)SolutionSubcutaneousVLD DANIŞMANLIK TIBBİ ÜRÜNLER VE TANITIM HİZMETLERİ LTD. ŞTİ.2020-08-14Not applicableTurkey flag

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
  1. 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]
  2. Frydman A: Low-molecular-weight heparins: an overview of their pharmacodynamics, pharmacokinetics and metabolism in humans. Haemostasis. 1996;26 Suppl 2:24-38. [Article]
  3. 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]
  4. 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]
  5. 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]
  6. 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]
  7. Breddin HK: Prophylaxis and treatment of deep-vein thrombosis. Semin Thromb Hemost. 2000;26 Suppl 1:47-52. [Article]
  8. Haas SK: Venous thromboembolic risk and its prevention in hospitalized medical patients. Semin Thromb Hemost. 2002 Dec;28(6):577-84. [Article]
  9. 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]
  10. 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]
  11. 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]
  12. 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]
PubChem Substance
347910374
RxNav
67031
Wikipedia
Nadroparin_calcium

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedPreventionCritically Ill Patients1
4CompletedTreatmentAcute Renal Failure (ARF)1
4CompletedTreatmentCirrhosis of the Liver / High Blood Pressure (Hypertension) / Status;Splenectomy / Venous Thrombosis (Disorder)1
4CompletedTreatmentCirrhosis of the Liver / Thrombosis Portal Vein1
4CompletedTreatmentPulmonary Embolism / Thromboembolism / Thrombotic events / Vascular Diseases1
4RecruitingPreventionCirrhosis of the Liver / High Blood Pressure (Hypertension) / Status;Splenectomy / Venous Thrombosis (Disorder)1
4RecruitingPreventionCirrhosis of the Liver / Portal Hypertension / Status;Splenectomy / Venous Thrombosis (Disorder)1
4RecruitingPreventionCoronavirus Disease 2019 (COVID‑19) / COVID / Deep Vein Thrombosis / Pulmonary Embolism / Thrombotic events1
4RecruitingPreventionDeep Vein Thrombosis / Pulmonary Embolism1
4Unknown StatusPreventionBypass Complications / Obesity, Morbid / Thromboembolism1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
InjectionParenteral
Injection, solutionParenteral0.3 ML
Injection, solutionParenteral0.4 ML
Injection, solutionParenteral0.6 ML
Injection, solutionParenteral0.8 ML
Injection, solutionParenteral1.0 ML
Injection, solutionParenteral
Injection, solutionParenteral2850 IU
Injection, solutionParenteral3800 IU
Injection, solutionParenteral5700 IU
Injection, solutionParenteral7600 IU
Injection
SolutionIntravenous; Subcutaneous9500 unit / mL
SolutionHemodialysis; Intravenous; Subcutaneous1900 IU
Injection, solutionParenteral0.2 ML
SolutionHemodialysis; Intravenous; Subcutaneous
InjectionSubcutaneous
SolutionHemodialysis; Intravenous; Subcutaneous3800 IU
SolutionHemodialysis; Intravenous; Subcutaneous5700 IU
SolutionSubcutaneous
Injection, solutionParenteral9500 IU
Injection, solutionParenteral1 ML
SolutionIntravenous; Subcutaneous19000 unit / mL
SolutionSubcutaneous19000 IU
Injection, solutionParenteral19.000 I.E.
Injection, solutionParenteral11400 IU/0.6ml
Injection, solutionParenteral15200 IU/0.8ml
Injection, solutionParenteral19000 IU/ml
Injection, solutionParenteral2.85 IU/0.3ml
Injection, solutionParenteral3800 IU/0.4ml
Injection, solutionParenteral5700 IU/0.6ml
Injection, solutionParenteral7600 IU/0.8ml
Injection, solutionParenteral9500 IU/ml
Solution9500 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

Targets

Drugtargets2
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insights and accelerate drug research.
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Use our structured and evidence-based datasets to unlock new insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Potentiator
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
References
  1. 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]
  2. 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
Sialic acid binding
Specific 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 ligan...
Gene Name
SELP
Uniprot ID
P16109
Uniprot Name
P-selectin
Molecular Weight
90833.105 Da
References
  1. 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]
  2. 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
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific 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 s...
Gene Name
FOS
Uniprot ID
P01100
Uniprot Name
Proto-oncogene c-Fos
Molecular Weight
40694.855 Da
References
  1. 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]
  2. 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
Transcriptional activator activity, rna polymerase ii core promoter proximal region sequence-specific binding
Specific Function
Transcription factor that binds DNA in a non-specific manner, yet also specifically recognizes the core sequence 5'-CAC[GA]TG-3'. Activates the transcription of growth-related genes.
Gene Name
MYC
Uniprot ID
P01106
Uniprot Name
Myc proto-oncogene protein
Molecular Weight
48803.55 Da
References
  1. 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]
  2. 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 on June 15, 2011 05:17 / Updated on September 18, 2021 03:33