Description

Simple

An anticoagulant drug or "blood thinner" used to prevent serious blood clots or heart complications due to blocked blood flow in certain patients who are at high risk.

Clinical

A low molecular weight heparin used for the prophylaxis of thrombotic events in certain patients and prevent acute cardiac ischemic events in patients with unstable angina and non-Q-wave myocardial infarction.

Overview

Dalteparin, a low molecular weight heparin (LMWH) prepared by nitrous acid degradation of unfractionated heparin of porcine intestinal mucosa origin, is an anticoagulant. It is composed of strongly acidic sulphated polysaccharide chains with an average molecular weight of 5000 and about 90% of the material within the range of 2000-9000. LMWHs have a more predictable response, a greater bioavailability, and a longer anti-Xa half life than unfractionated heparin. Dalteparin can also be safely used in most pregnant women. Low molecular weight heparins are less effective at inactivating factor IIa due to their shorter length compared to unfractionated heparin.

Pharmacology

Indication

Dalteparin is used as a prophylaxis for deep-vein thrombosis and pulmonary embolisms in patients undergoing general surgery (e.g., abdominal, gynecologic, urologic), and in patients with acute medical conditions (e.g. cancer, bed rest, heart failure, severe lung disease). It is also used in patients... Read more

Pharmacodynamic

Dalteparin has an antithrombin binding site that is essential for high affinity binding to the plasma protein antithrombin (ATIII). Anti-Xa activity of plasma is used as both as an estimate of clotting activity, and as a basis to determine dosage. Its use should be avoided in patients with a creatin... Read more

Mechanism of action

Dalteparin potentiates the activity of ATIII, inhibiting the formation of both factor Xa and thrombin. The main difference between dalteparin and unfractionated heparin (UH) is that dalteparin preferentially inactivates factor Xa. As a result, only a slight increase in clotting time [(i.e. activated... Read more

Absorption

Almost completely absorbed after subcutaneous (sc) doses, with a bioavialability of about 87%.

Protein binding

Less than unfractionated heparin, which is more than 90%.

Volume of distribution

3 litres

Clearance

Excreted via kidneys. The plasma clearance rate is 33 mL/min.

Half life

Terminal Half life:
Intravenous - 2 hours. Subcutaneous - 3-5hours

Route of elimination

After 4 hours, about 20% is seen in urine. Most of the remainder is found in the liver, gastrointestinal tract and kidney. The kidneys are the major site of dalteparin excretion (approximately 70% based on animal studies).

Toxicity

Overdosage: hemorrhagic complications.
Adverse Drug Reaction:
(common) osteopenia with extended use; mild, reversible non-immunological thrombocytopenia; transient elevation of liver transaminases; alopecia.
(uncommon): severe immunologically-mediated heparin-induced thrombocytopenia; anaphyla... Read more

Adverse Effects

Contraindications

  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: Active major bleeding
      • Drugbank Id: DBCOND0107388
      • Modification Of:
        • Condition Status: active
        • Base:
          • Name: Major Bleeding
          • Drugbank Id: DBCOND0039116
  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: History of thrombocytopenia caused by Heparin
      • Drugbank Id: DBCOND0108468
      • Combination Of:
        • Caused By:
            • Name: Heparin
            • Drugbank Id: DBCOND0054463
        • Included Conditions:
            • Name: History of thrombocytopenia
            • Drugbank Id: DBCOND0108003
  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: History of thrombocytopenia with thrombosis caused by Heparin
      • Drugbank Id: DBCOND0108470
      • Combination Of:
        • Caused By:
            • Name: Heparin
            • Drugbank Id: DBCOND0054463
        • Included Conditions:
            • Name: History of thrombocytopenia with thrombosis
            • Drugbank Id: DBCOND0108469
  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: Unstable Angina
      • Drugbank Id: DBCOND0030047
  • With Therapies:
      • Name: Epidural Anesthesia
      • Drugbank Id: DBCOND0032044
      • Name: Neuraxial anesthesia
      • Drugbank Id: DBCOND0104583
  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: Non-Q-wave myocardial infarction
      • Drugbank Id: DBCOND0023401
  • With Therapies:
      • Name: Epidural Anesthesia
      • Drugbank Id: DBCOND0032044
      • Name: Neuraxial anesthesia
      • Drugbank Id: DBCOND0104583
  • Route:
    • Subcutaneous
  • Regions: US
  • Patient Conditions:
      • Name: Prophylaxis of prolonged venous thromboembolism
      • Drugbank Id: DBCOND0108471
  • With Therapies:
      • Name: Epidural Anesthesia
      • Drugbank Id: DBCOND0032044
      • Name: Neuraxial anesthesia
      • Drugbank Id: DBCOND0104583
  • Route:
    • Subcutaneous
  • Hypersensitivity:
    • heparin
    • pork products
  • Regions: US

Food Interactions

  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include ginseng, ginkgo, ginger, and garlic.

Interactions

Type in a drug name to check for interaction with Dalteparin
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Dalteparin.
(R)-warfarin
The risk or severity of bleeding can be increased when Dalteparin is combined with (R)-warfarin.
(S)-Warfarin
The risk or severity of bleeding can be increased when Dalteparin is combined with (S)-Warfarin.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Dalteparin.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Dalteparin.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Dalteparin.
4-hydroxycoumarin
The risk or severity of bleeding can be increased when Dalteparin is combined with 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Dalteparin.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Dalteparin.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Dalteparin.
Abciximab
The risk or severity of bleeding can be increased when Abciximab is combined with Dalteparin.
Acebutolol
The risk or severity of hyperkalemia can be increased when Acebutolol is combined with Dalteparin.
Aceclofenac
The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Dalteparin.
Acemetacin
The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Dalteparin.
Acenocoumarol
The risk or severity of bleeding can be increased when Acenocoumarol is combined with Dalteparin.
Acetylsalicylic acid
Acetylsalicylic acid may increase the anticoagulant activities of Dalteparin.
Agmatine
The risk or severity of hyperkalemia can be increased when Dalteparin is combined with Agmatine.
Alaproclate
The risk or severity of hemorrhage can be increased when Alaproclate is combined with Dalteparin.
Albutrepenonacog alfa
The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Dalteparin.
Alclofenac
The risk or severity of bleeding and hemorrhage can be increased when Alclofenac is combined with Dalteparin.
13 References
  1. 1 . King DJ, Kelton JG: Heparin-associated thrombocytopenia. Ann Intern Med. 1984 Apr;100(4):535-40.PubMed: 6367579
  2. 2 . Bell WR, Royall RM: Heparin-associated thrombocytopenia: a comparison of three heparin preparations. N Engl J Med. 1980 Oct 16;303(16):902-7.PubMed: 6997743
  3. 3 . Ockelford PA, Patterson J, Johns AS: A double-blind randomized placebo controlled trial of thromboprophylaxis in major elective general surgery using once daily injections of a low molecular weight heparin fragment (Fragmin). Thromb Haemost. 1989 Dec 29;62(4):1046-9.PubMed: 2559484
  4. 4 . Hartl P, Brucke P, Dienstl E, Vinazzer H: Prophylaxis of thromboembolism in general surgery: comparison between standard heparin and Fragmin. Thromb Res. 1990 Feb 15;57(4):577-84.PubMed: 2158151
  5. 5 . Monreal M, Lafoz E, Salvador R, Roncales J, Navarro A: Adverse effects of three different forms of heparin therapy: thrombocytopenia, increased transaminases, and hyperkalaemia. Eur J Clin Pharmacol. 1989;37(4):415-8.PubMed: 2557219
  6. 6 . Holmer E, Soderberg K, Bergqvist D, Lindahl U: Heparin and its low molecular weight derivatives: anticoagulant and antithrombotic properties. Haemostasis. 1986;16 Suppl 2:1-7.PubMed: 3744129
  7. 7 . Malm K, Dahlback B, Arnljots B: Low-molecular-weight heparin (dalteparin) effectively prevents thrombosis in a rat model of deep arterial injury. Plast Reconstr Surg. 2003 Apr 15;111(5):1659-66.PubMed: 12655212
  8. 8 . Tincani E, Mannucci C, Casolari B, Turrini F, Crowther MA, Prisco D, Cenci AM, Bondi M: Safety of dalteparin for the prophylaxis of venous thromboembolism in elderly medical patients with renal insufficiency: a pilot study. Haematologica. 2006 Jul;91(7):976-9. Epub 2006 Jun 1.PubMed: 16757417
  9. 9 . Schmid P, Brodmann D, Fischer AG, Wuillemin WA: Study of bioaccumulation of dalteparin at a prophylactic dose in patients with various degrees of impaired renal function. J Thromb Haemost. 2009 Apr;7(4):552-8. doi: 10.1111/j.1538-7836.2009.03292.x. Epub 2009 Jan 19.PubMed: 19175499
  10. 10 . Abe W, Ikejima K, Lang T, Okumura K, Enomoto N, Kitamura T, Takei Y, Sato N: Low molecular weight heparin prevents hepatic fibrogenesis caused by carbon tetrachloride in the rat. J Hepatol. 2007 Feb;46(2):286-94. Epub 2006 Oct 25.PubMed: 17166617
  11. 11 . Frydman A: Low-molecular-weight heparins: an overview of their pharmacodynamics, pharmacokinetics and metabolism in humans. Haemostasis. 1996;26 Suppl 2:24-38.PubMed: 8707165
  12. 12 . Samama MM, Gerotziafas GT: Comparative pharmacokinetics of LMWHs. Semin Thromb Hemost. 2000;26 Suppl 1:31-8.PubMed: 11011804
  13. 13 . Rey E, Rivard GE: Prophylaxis and treatment of thromboembolic diseases during pregnancy with dalteparin. Int J Gynaecol Obstet. 2000 Oct;71(1):19-24.PubMed: 11044537