Identification
- Summary
Tinzaparin is a low molecular weight heparin used for the treatment of acute symptomatic deep vein thrombosis with or without pulmonary embolism when administered in conjunction with warfarin.
- Brand Names
- Innohep
- Generic Name
- Tinzaparin
- DrugBank Accession Number
- DB06822
- Background
Tinzaparin is a low molecular weight heparin (LMWH), produced by enzymatic depolymerization of unfractionated heparin from porcine intestinal mucosa. It is a heterogeneous mixture of with an average molecular weight between 5500 and 7500 daltons. Tinzaparin is composed of molecules with and without a special site for high affinity binding to antithrombin III (ATIII). This complex greatly accelerates the inhibition of factor Xa. It is an anticoagulant and considered an antithrombotic. Tinzaparin must be given either subcutaneously or parenterally. LMWHs are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Tinzaparin sodium
- Tinzaparina
Pharmacology
- Indication
Tinzaparin is used for the prevention of postoperative venous thromboembolism in patients undergoing orthopedic surgery and in patients undergoing general surgery who are at high risk of developing postoperative venous thromboembolism. It is also used for the treatment of deep vein thrombosis and/or pulmonary embolism. It is indicated for use in preventing clot formation in indwelling intravenous lines for hemodialysis.
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Tinzaparin, like other LMWHs, have a higher anti-Xa activity than anti-IIa activity. The anti-Xa activity of tinzaparin is 2.0 +/- 0.5 times greater than its to anti-IIa activity. Heparin exhibits approximately equal inhibitory activity against Xa and IIa. Tinzaparin is an anticoagulant that blocks the formation of thrombi. Like all LMWHs, tinzaparin only causes activated partial thromboplastin time (aPTT) prolongation at higher doses and routine monitoring is not recommended. However, anti-factor Xa levels may be monitored in some conditions such as pregnancy and renal dysfunction. Its use should be avoided in patients with a creatinine clearance less than 20 mL/min. In these patients, unfractionated heparin should be used. Tinzaparin can be used in patients who have a creatinine clearance between 20-30 mL/min, giving it the highest safety threshold for use in renal failure patients compared to all the LMWHs.
- Mechanism of action
Tinzaparin binds to the plasma protein antithrombin III, forming a complex with then accelerates the inhibition of factor Xa. Its affinity for factor Xa is 2-4 times greater than that of unbound ATIII. The inactivation of factor Xa in turn will exponentially generation of thrombin (factor IIa) molecules, which is needed to activate fibrinogen to fibrin. The coagulation cascade is inhibited because fibrin cannot be formed in the presence of tinzaparin. Like all LMWH, it cannot be given intramuscularly due to increased risk of hematoma.
Target Actions Organism AAntithrombin-III potentiatorHumans UIntegrin alpha-4 inhibitorHumans UStromal cell-derived factor 1 binderHumans - Absorption
Subcutaneous injection - about 90% when measured as anti-Xa activity versus 67% for anti-IIa activity.
- Volume of distribution
Anti-Xa activity is 4 L. Anti-IIa activity is 10.9 L
- Protein binding
Low protein binding compared to unfractionated heparin.
- Metabolism
Sulfation and polymerization occurs in the liver.
- Route of elimination
Linear elimination through kidneys
- Half-life
Anti-Xa activity is 82 minutes. Anti-IIa activity is 71 minutes.
- Clearance
Clearance is dose-dependant. The clearance of tinzaparin based on anti-Xa activity ranged from 1.14 to 2.04 L/hr
- Adverse Effects
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Osteoporosis with increasing duration of use, bleeding, alopecia, heparin induced thrombocytopenia (HIT). All of these adverse drug reactions occur less with LMWH compared to unfractionated heparin. Tinzaparin showed no toxic effects at doses up to 5 mg/kg in mice, rats, or dogs in standard acute, subacute, and chronic toxicity studies.
- 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 Tinzaparin. Acebutolol The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Tinzaparin. Aceclofenac The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Tinzaparin. Acemetacin The risk or severity of bleeding and hemorrhage can be increased when Tinzaparin is combined with Acemetacin. Acenocoumarol The risk or severity of bleeding can be increased when Acenocoumarol is combined with Tinzaparin. Acetylsalicylic acid Acetylsalicylic acid may increase the anticoagulant activities of Tinzaparin. Albutrepenonacog alfa The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Tinzaparin. Alclofenac The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Tinzaparin. Aldesleukin The risk or severity of bleeding can be increased when Tinzaparin is combined with Aldesleukin. Alemtuzumab The risk or severity of bleeding can be increased when Tinzaparin is combined with Alemtuzumab. 
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- 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.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Innohep Injection, solution 20000 [iU]/1mL Subcutaneous Leo Pharma 2010-07-01 2013-08-01 US 
Innohep Solution 10000 unit / mL Subcutaneous Leo Pharma 2011-09-09 Not applicable Canada 
Innohep Solution 12000 unit / 0.6 mL Subcutaneous Leo Pharma 2014-09-30 Not applicable Canada Innohep Solution 20000 unit / mL Subcutaneous Leo Pharma 1997-02-28 Not applicable Canada Innohep Solution 20000 unit / mL Subcutaneous Leo Pharma 2011-09-16 Not applicable Canada Innohep Injection 20000 [iU]/1mL Subcutaneous Celgene 2008-04-14 Not applicable US Innohep Solution 20000 unit / mL Subcutaneous Leo Pharma 1997-09-23 Not applicable Canada Innohep Solution 8000 unit / 0.4 mL Subcutaneous Leo Pharma 2014-09-30 Not applicable Canada Innohep Solution 10000 unit / mL Subcutaneous Leo Pharma 1995-12-31 Not applicable Canada Innohep Solution 10000 unit / mL Subcutaneous Leo Pharma 2011-12-10 Not applicable Canada
Categories
- ATC Codes
- B01AB10 — Tinzaparin
- Drug Categories
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 7UQ7X4Y489
- CAS number
- 9041-08-1
References
- General References
- Friedel HA, Balfour JA: Tinzaparin. A review of its pharmacology and clinical potential in the prevention and treatment of thromboembolic disorders. Drugs. 1994 Oct;48(4):638-60. [Article]
- Simonneau G, Sors H, Charbonnier B, Page Y, Laaban JP, Azarian R, Laurent M, Hirsch JL, Ferrari E, Bosson JL, Mottier D, Beau B: A comparison of low-molecular-weight heparin with unfractionated heparin for acute pulmonary embolism. The THESEE Study Group. Tinzaparine ou Heparine Standard: Evaluations dans l'Embolie Pulmonaire. N Engl J Med. 1997 Sep 4;337(10):663-9. [Article]
- Planes A, Samama MM, Lensing AW, Buller HR, Barre J, Vochelle N, Beau B: Prevention of deep vein thrombosis after hip replacement--comparison between two low-molecular heparins, tinzaparin and enoxaparin. Thromb Haemost. 1999 Jan;81(1):22-5. [Article]
- Cheer SM, Dunn CJ, Foster R: Tinzaparin sodium: a review of its pharmacology and clinical use in the prophylaxis and treatment of thromboembolic disease. Drugs. 2004;64(13):1479-502. [Article]
- Hoy SM, Scott LJ, Plosker GL: Tinzaparin sodium: a review of its use in the prevention and treatment of deep vein thrombosis and pulmonary embolism, and in the prevention of clotting in the extracorporeal circuit during haemodialysis. Drugs. 2010 Jul 9;70(10):1319-47. doi: 10.2165/11203710-000000000-00000. [Article]
- Hedner U: Development of tinzaparin: a heparinase-digested low-molecular-weight heparin. Semin Thromb Hemost. 2000;26 Suppl 1:23-9. [Article]
- Pautas E, Siguret V, d'Urso M, Laurent M, Gaussem P, Fevrier M, Durand-Gasselin B: [Monitoring of tinzaparin in a ten day treatment dose in elderly patients]. Rev Med Interne. 2001 Feb;22(2):120-6. [Article]
- Pineo GF, Hull RD: Tinzaparin in the treatment of venous thromboembolism. Expert Opin Pharmacother. 2003 Dec;4(12):2355-62. [Article]
- Fossler MJ, Barrett JS, Hainer JW, Riddle JG, Ostergaard P, van der Elst E, Sprogel P: Pharmacodynamics of intravenous and subcutaneous tinzaparin and heparin in healthy volunteers. Am J Health Syst Pharm. 2001 Sep 1;58(17):1614-21. [Article]
- Cambus JP, Saivin S, Heilmann JJ, Caplain H, Boneu B, Houin G: The pharmacodynamics of tinzaparin in healthy volunteers. Br J Haematol. 2002 Mar;116(3):649-52. [Article]
- External Links
- KEGG Drug
- D06398
- PubChem Substance
- 347910373
- 104466
- Wikipedia
- Tinzaparin_sodium
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Coronavirus Disease 2019 (COVID‑19) 1 4 Completed Not Available Venous Thromboembolism 1 4 Completed Prevention Coronavirus Disease 2019 (COVID‑19) / COVID / Deep Vein Thrombosis / Pulmonary Embolism / Thrombosis 1 4 Completed Prevention Deep Vein Thrombosis / Pulmonary Embolism 1 4 Completed Prevention Renal Failure, Chronic Renal Failure 1 4 Completed Treatment Acute Pulmonary Embolism (PE) 1 4 Completed Treatment Arterial Occlusion 1 4 Completed Treatment Deep Vein Thrombosis 1 4 Completed Treatment Intrauterine Growth Retardation (IUGR) 1 4 Completed Treatment Thromboembolism / Thrombosis / Venous Thrombosis (Disorder) 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection Subcutaneous 20000 [iU]/1mL Injection, solution Injection, solution Parenteral 10000 UI/0.5ML Injection, solution Parenteral 12000 UI/0.6ML Injection, solution Parenteral 14000 UI/0.7ML Injection, solution Parenteral 16000 UI/0.8ML Injection, solution Parenteral 18000 UI/0.9ML Injection, solution Parenteral 2500 UI/0.25ML Injection, solution Parenteral 3500 UI/0.35ML Injection, solution Parenteral 4500 UI/0.45ML Injection, solution Parenteral 8000 UI/0.4ML Injection, solution Subcutaneous 20000 [iU]/1mL Solution 20000 IU/1mL Solution Subcutaneous 10000 unit / mL Solution Subcutaneous 12000 unit / 0.6 mL Solution Subcutaneous 16000 unit / 0.8 mL Solution Subcutaneous 20000 unit / mL Solution Subcutaneous 8000 unit / 0.4 mL Suspension 10000 IU/1mL Injection, solution 20000 IU/1mL Injection, solution Parenteral Injection, solution Parenteral 10.000 IE/0.5ML Injection Subcutaneous Injection, solution Parenteral 12.000 IE/0.6ML Injection, solution Subcutaneous 14000 IU/0.7mL Injection, solution Parenteral 14.000 IE/0.7ML Injection, solution Parenteral 16.000 IE/0.8ML Injection, solution Parenteral 18.000 IE/0.9ML Injection Subcutaneous 18000 iu/0.9ml Injection, solution Parenteral 20000 IU Injection, solution Parenteral 0.35 ML Injection, solution Parenteral 4500 IU Injection, solution Parenteral 8.000 IE/0.4ML Injection, solution Parenteral 8000 IE/0.4ML Liquid Subcutaneous 11700 unit / mL Injection Subcutaneous 10,000 axa iu/ml Injection, solution Subcutaneous 10000 IU/0.5mL Injection, solution Subcutaneous 10000 IU/mL Injection Subcutaneous 14,000 IU Injection Subcutaneous 20000 axa iu/ml Injection Subcutaneous 3500 axa iu/0.35 ml Injection, solution Subcutaneous 3500 IU/0.35mL Injection Subcutaneous 4,500 IU Injection, solution Subcutaneous 4500 IU/0.45mL Solution Parenteral 2500 IU Solution Parenteral 3500 IU Injection Parenteral 10 IU Solution Parenteral 20000 IU Liquid Subcutaneous 10000 unit / mL - 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
- 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
- Bisio A, Vecchietti D, Citterio L, Guerrini M, Raman R, Bertini S, Eisele G, Naggi A, Sasisekharan R, Torri G: Structural features of low-molecular-weight heparins affecting their affinity to antithrombin. Thromb Haemost. 2009 Nov;102(5):865-73. doi: 10.1160/TH09-02-0081. [Article]
- Florian-Kujawski M, Hoppensteadt D, Maddineni J, Ziegler H, Fareed J: Differential regulation of thrombin activatable fibrinolytic inhibitor by low molecular weight heparins. Pharmacologic implications. Int Angiol. 2004 Dec;23(4):346-54. [Article]
- Morris TA, Jacobson A, Marsh JJ, Lane JR: Pharmacokinetics of UH and LMWH are similar with respect to antithrombin activity. Thromb Res. 2005;115(1-2):45-51. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Metal ion binding
- Specific Function
- Integrins alpha-4/beta-1 (VLA-4) and alpha-4/beta-7 are receptors for fibronectin. They recognize one or more domains within the alternatively spliced CS-1 and CS-5 regions of fibronectin. They are...
- Gene Name
- ITGA4
- Uniprot ID
- P13612
- Uniprot Name
- Integrin alpha-4
- Molecular Weight
- 114898.745 Da
References
- Schlesinger M, Simonis D, Schmitz P, Fritzsche J, Bendas G: Binding between heparin and the integrin VLA-4. Thromb Haemost. 2009 Nov;102(5):816-22. doi: 10.1160/TH09-01-0061. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Not Available
- Specific Function
- Not Available
- Gene Name
- CXCL12
- Uniprot ID
- P48061
- Uniprot Name
- Stromal cell-derived factor 1
- Molecular Weight
- 10665.75 Da
References
- Koo CY, Sen YP, Bay BH, Yip GW: Targeting heparan sulfate proteoglycans in breast cancer treatment. Recent Pat Anticancer Drug Discov. 2008 Nov;3(3):151-8. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Zinc ion binding
- Specific Function
- Cleaves aggrecan, a cartilage proteoglycan, and may be involved in its turnover. May play an important role in the destruction of aggrecan in arthritic diseases. Could also be a critical factor in ...
- Gene Name
- ADAMTS4
- Uniprot ID
- O75173
- Uniprot Name
- A disintegrin and metalloproteinase with thrombospondin motifs 4
- Molecular Weight
- 90196.02 Da
References
- Mousa SA: Effect of low molecular weight heparin and different heparin molecular weight fractions on the activity of the matrix-degrading enzyme aggrecanase: structure-function relationship. J Cell Biochem. 2005 May 1;95(1):95-8. [Article]
Drug created at September 14, 2010 16:21 / Updated at September 25, 2023 18:32