Heparin


Description

Unfractionated heparin (UH) is a heterogenous preparation of anionic, sulfated glycosaminoglycan polymers with weights ranging from 3000 to 30,000 Da. It is a naturally occurring anticoagulant released from mast cells. It binds reversibly to antithro...

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Pharmacology

Indication

Unfractionated heparin is indicated for prophylaxis and treatment of venous thrombosis and its exten... Read more

Pharmacodynamic

Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glu... Read more

Mechanism of action

Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa... Read more

Absorption

Heparin must be given parenterally as it is not absorbed through the gastrointestinal mucosa. It is... Read more

Protein binding

Very high, mostly to low-density lipoproteins. It is also extensively bound by globulins and fibrino... Read more

Volume of distribution

40-70 mL/min (approximately the same as blood volume)Although heparin does not distribute into adipo... Read more

Clearance

Adult Clearance = 0.43 ml/kg/min25-28 weeks gestation = 1.49 ml/kg/min

Half life

1.5 hours.

The plasma half-life of heparin increases from about 60 minutes with a 100 unit/kg do...
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Route of elimination

The drug appears to be removed mainly by the reticuloendothelial system. A small fraction of unchang... Read more

Toxicity

In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced... Read more


Adverse Effects

Effect Regions Age Groups Incidences Evidence Type
Thrombocytopenia US
  • Kind: experimental
    • Percent: 0-30%
  • Varying Reports
    Local irritation US
    Varying Reports
    Erythema US
    Varying Reports
    Ovarian hemorrhage US
    Varying Reports
    Retroperitoneal hemorrhage US
    Varying Reports
    Adrenal hemorrhage US
    Varying Reports
    Fever US
    Varying Reports
    Chills US
    Varying Reports
    Asthma US
    Varying Reports
    Urticaria US
    Varying Reports
    Hematoma US
    Varying Reports
    Mild Pain US
    Varying Reports
    Hypersensitivity Reaction US
    Varying Reports
    Ulceration US
    Varying Reports
    Itching and burning at the plantar site of feet US
    Varying Reports
    Anaphylactoid reactions US
    Varying Reports
    Lacrimation US
    Varying Reports
    Rhinitis US
    Varying Reports
    Nausea and vomiting US
    Varying Reports
    Headache US
    Varying Reports
    Suppression of aldosterone synthesis US
    Varying Reports
    Delayed transient alopecia US
    Varying Reports
    Priapism US
    Varying Reports
    Osteoporosis US
    Varying Reports
    Episodes of painful, ischemic, and cyanosed limbs US
    Varying Reports
    Cutaneous necrosis US
    Varying Reports
    Rebound hyperlipemia US
    Varying Reports
    Elevations of aminotransferase levels US
    Varying Reports

    Contraindications

    • Regions: US
    • Patient Conditions:
        • Name: Uncontrollable active bleeding state
        • Drugbank Id: DBCOND0108200
    • Regions: US
    • Patient Conditions:
        • Name: Inability to perform blood coagulation tests
        • Drugbank Id: DBCOND0108199
    • Hypersensitivity:
      • false
    • Regions: US
    • Regions: US
    • Patient Conditions:
        • Name: Severe Thrombocytopenia
        • Drugbank Id: DBCOND0043521
        • Modification Of:
          • Base:
            • Name: Thrombocytopenia
            • Drugbank Id: DBCOND0006608
          • Severity:
            • Includes:
              • severe

    Food Interactions

    • Adequate calcium intake is recommended, needs increased with long term use, supplement recommended.
    • Many herbs with anticoagulant properties (e.g. ginger, garlic, ginseng, green tea, evening primrose) may increase the risk of bleeding in patients on anticoagulant therapy such as heparin

    Interactions

    Type in a drug name to check for interaction with Heparin

    (1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Heparin.
    The risk or severity of bleeding can be increased when Heparin is combined with (R)-warfarin.
    The risk or severity of bleeding can be increased when Heparin is combined with (S)-Warfarin.
    1-Testosterone may increase the anticoagulant activities of Heparin.
    18-methyl-19-nortestosterone may increase the anticoagulant activities of Heparin.
    3,5-Diiodotyrosine may increase the anticoagulant activities of Heparin.
    The risk or severity of bleeding can be increased when Heparin is combined with 4-hydroxycoumarin.
    4-Hydroxytestosterone may increase the anticoagulant activities of Heparin.
    The therapeutic efficacy of Heparin can be decreased when used in combination with 5-fluorouridine.
    5beta-dihydrotestosterone may increase the anticoagulant activities of Heparin.
    The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Heparin.
    The risk or severity of bleeding can be increased when Abciximab is combined with Heparin.
    The risk or severity of hyperkalemia can be increased when Heparin is combined with Acebutolol.
    The risk or severity of bleeding and hemorrhage can be increased when Aceclofenac is combined with Heparin.
    The risk or severity of bleeding and hemorrhage can be increased when Acemetacin is combined with Heparin.
    The risk or severity of bleeding can be increased when Heparin is combined with Acenocoumarol.
    Acetylsalicylic acid may increase the anticoagulant activities of Heparin.
    The risk or severity of hyperkalemia can be increased when Heparin is combined with Agmatine.
    The risk or severity of hemorrhage can be increased when Alaproclate is combined with Heparin.
    The therapeutic efficacy of Albutrepenonacog alfa can be decreased when used in combination with Heparin.

    References

    • 1 . Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16. [PubMed: 10549711]
    • 2 . Ferro DR, Provasoli A, Ragazzi M, Casu B, Torri G, Bossennec V, Perly B, Sinay P, Petitou M, Choay J: Conformer populations of L-iduronic acid residues in glycosaminoglycan sequences. Carbohydr Res. 1990 Jan 15;195(2):157-67. [PubMed: 2331699]
    • 3 . Mulloy B, Forster MJ, Jones C, Davies DB: N.m.r. and molecular-modelling studies of the solution conformation of heparin. Biochem J. 1993 Aug 1;293 ( Pt 3):849-58. [PubMed: 8352752]
    • 4 . Hirsh J, Raschke R: Heparin and low-molecular-weight heparin: the Seventh ACCP Conference on Antithrombotic and Thrombolytic Therapy. Chest. 2004 Sep;126(3 Suppl):188S-203S. [PubMed: 15383472]
    • 5 . Petitou M, Herault JP, Bernat A, Driguez PA, Duchaussoy P, Lormeau JC, Herbert JM: Synthesis of thrombin-inhibiting heparin mimetics without side effects. Nature. 1999 Apr 1;398(6726):417-22. [PubMed: 10201371]
    • 6 . Spruill WJ, Wade WE, Huckaby WG, Leslie RB: Achievement of anticoagulation by using a weight-based heparin dosing protocol for obese and nonobese patients. Am J Health Syst Pharm. 2001 Nov 15;58(22):2143-6. [PubMed: 11760916]
    • 7 . McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8. [PubMed: 7254945]
    • 8 . Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8. [PubMed: 6889041]
    • 9 . Authors unspecified: Benzyl alcohol may be toxic to newborns. FDA Drug Bull. 1982 Aug;12(2):10-1. [PubMed: 7188569]
    • 10 . Authors unspecified: Neonatal deaths associated with use of benzyl alcohol--United States. MMWR Morb Mortal Wkly Rep. 1982 Jun 11;31(22):290-1. [PubMed: 6810084]

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