Peringatan Keamanan

In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced thrombocytopenia (HIT syndrome). Platelet counts usually do not fall until between days 5 and 12 of heparin therapy. HIT is caused by an immunological reaction that makes platelets form clots within the blood vessels, thereby using up coagulation factors. It can progress to thrombotic complications such as arterial thrombosis, gangrene, stroke, myocardial infarction and disseminated intravascular coagulation. Symptoms of overdose may show excessive prolongation of aPTT or by bleeding, which may be internal or external, major or minor. Therapeutic doses of heparin give for at least 4 months have been associated with osteoporosis and spontaneous vertebral fractures. Osteoporosis may be reversible once heparin is discontinued. Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100–400 mg/kg daily) of benzyl alcohol in these neonates. Its use is principally associated with the use of bacteriostatic 0.9% sodium chloride intravascular flush or endotracheal tube lavage solutions.

Heparin

DB01109

small molecule approved investigational

Deskripsi

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 antithrombin III (ATIII) and greatly accelerates the rate at which ATIII inactivates coagulation enzymes thrombin (factor IIa) and factor Xa. UH is different from low molecular weight heparin (LMWH) in the following ways: the average molecular weight of LMWH is about 4.5 kDa whereas it is 15 kDa for UH; UH requires continuous infusions; activated partial prothrombin time (aPTT) monitoring is required when using UH; and UH has a higher risk of bleeding and higher risk of osteoporosis in long term use. Unfractionated heparin is more specific than LMWH for thrombin. Furthermore, the effects of UH can typically be reversed by using protamine sulfate.

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The plasma half-life is dose-dependent, and it ranges from 0.5 to 2 h.[L47396] For the purpose of choosing a protamine dose, heparin can be assumed to have a half-life of about 30 minutes after intravenous injection.[L47396] The plasma half-life of heparin increases from about 30 min after an IV bolus of 25 units/kg to 60 minutes with a 100 unit/kg dose or to about 150 minutes with a 400 unit/kg dose.[A1870]
Volume Distribusi The volume of distribution is 0.07 L/kg.[L47396] Although heparin does not distribute into adipose tissues, clinicians should use actual body weight in obese patients to account for extra vasculature.[A1874]
Klirens (Clearance) The clearance in adults receiving a bolus dose of 75 units/kg and preterm newborns receiving a bolus dose of 100 units/kg were calculated to be 0.43 ml/kg/min and 1.49 ml/kg/min respectively.[A1876]

Absorpsi

Heparin is not absorbed through the gastrointestinal tract and is therefore administered via a parenteral route. Peak plasma concentration and the onset of action are achieved immediately after intravenous administration.L47396 Plasma heparin concentrations may be increased and activated partial thromboplastin times (aPTTs) may be more prolonged in geriatric adults (older than 60 years of age) compared with younger adults.L47396

Metabolisme

Heparin does not undergo enzymatic degradation.L47396

Rute Eliminasi

Heparin undergoes biphasic clearance, a) rapid saturable clearance (zero-order process due to binding to proteins, endothelial cells, and macrophages), and b) slower first-order elimination. Low doses of heparin are cleared mostly by a saturable, rapid, zero-order process. Slower first-order elimination usually occurs with very high doses of heparin and is dependent on renal function.L47396 High-molecular-weight moieties are cleared more rapidly than lower molecular-weight moieties.A1870

Interaksi Makanan

2 Data
  • 1. Administer calcium supplement. This drug decreases calcium levels.
  • 2. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

898 Data
Apixaban Apixaban may increase the anticoagulant activities of Heparin.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Heparin.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Heparin.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Heparin is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Taurocholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Heparin is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Heparin is combined with Hyodeoxycholic Acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Heparin.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Heparin.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Heparin is combined with Obinutuzumab.
Rivaroxaban Heparin may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Heparin is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Heparin.
Tipranavir The risk or severity of bleeding and hemorrhage can be increased when Tipranavir is combined with Heparin.
Urokinase Urokinase may increase the anticoagulant activities of Heparin.
Vitamin E Vitamin E may increase the anticoagulant activities of Heparin.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Heparin.
Trandolaprilat The risk or severity of hyperkalemia can be increased when Trandolaprilat is combined with Heparin.
Moexiprilat The risk or severity of hyperkalemia can be increased when Moexiprilat is combined with Heparin.
Cilazaprilat The risk or severity of hyperkalemia can be increased when Cilazaprilat is combined with Heparin.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Heparin.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Heparin.
Quinine The therapeutic efficacy of Heparin can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Heparin can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Heparin.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Heparin.
Nitroglycerin Nitroglycerin may decrease the anticoagulant activities of Heparin.
Corticorelin ovine triflutate The risk or severity of hypotension and sinus node depression can be increased when Heparin is combined with Corticorelin ovine triflutate.
Oritavancin The therapeutic efficacy of Heparin can be decreased when used in combination with Oritavancin.
Streptokinase Streptokinase may increase the anticoagulant activities of Heparin.
Telavancin The therapeutic efficacy of Heparin can be decreased when used in combination with Telavancin.
Palifermin The serum concentration of Palifermin can be increased when it is combined with Heparin.
Pentoxifylline The therapeutic efficacy of Heparin can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate Pentosan polysulfate may increase the anticoagulant activities of Heparin.
Levocarnitine The therapeutic efficacy of Heparin can be increased when used in combination with Levocarnitine.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Heparin.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Heparin.
Zeranol Zeranol may decrease the anticoagulant activities of Heparin.
Equol Equol may decrease the anticoagulant activities of Heparin.
Methallenestril Methallenestril may decrease the anticoagulant activities of Heparin.
Epimestrol Epimestrol may decrease the anticoagulant activities of Heparin.
Moxestrol Moxestrol may decrease the anticoagulant activities of Heparin.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Heparin.
Biochanin A Biochanin A may decrease the anticoagulant activities of Heparin.
Formononetin Formononetin may decrease the anticoagulant activities of Heparin.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Heparin.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Heparin.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Heparin.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Heparin.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Heparin.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Heparin.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Heparin.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Heparin.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Heparin.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Heparin.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Heparin.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Heparin.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Heparin.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Heparin.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Heparin.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Heparin.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Heparin.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Heparin.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Heparin.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Heparin.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Heparin.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Heparin.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Heparin.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Heparin.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Heparin.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Heparin.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Heparin.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Heparin.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Heparin.
Olsalazine The risk or severity of bleeding can be increased when Heparin is combined with Olsalazine.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Heparin.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Heparin.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Heparin.
Choline magnesium trisalicylate The risk or severity of bleeding and hemorrhage can be increased when Choline magnesium trisalicylate is combined with Heparin.
Antrafenine The risk or severity of bleeding and hemorrhage can be increased when Antrafenine is combined with Heparin.
Aminophenazone The risk or severity of bleeding and hemorrhage can be increased when Aminophenazone is combined with Heparin.
Antipyrine The risk or severity of bleeding and hemorrhage can be increased when Antipyrine is combined with Heparin.
Tiaprofenic acid The risk or severity of bleeding and hemorrhage can be increased when Tiaprofenic acid is combined with Heparin.
Etoricoxib The risk or severity of bleeding and hemorrhage can be increased when Etoricoxib is combined with Heparin.
Taxifolin The risk or severity of bleeding and hemorrhage can be increased when Taxifolin is combined with Heparin.
Oxyphenbutazone The risk or severity of bleeding and hemorrhage can be increased when Oxyphenbutazone is combined with Heparin.
Licofelone The risk or severity of bleeding and hemorrhage can be increased when Licofelone is combined with Heparin.
Benoxaprofen The risk or severity of bleeding and hemorrhage can be increased when Benoxaprofen is combined with Heparin.
Metamizole The risk or severity of hyperkalemia can be increased when Heparin is combined with Metamizole.
Zomepirac The risk or severity of bleeding and hemorrhage can be increased when Zomepirac is combined with Heparin.

Target Protein

Antithrombin-III SERPINC1
Coagulation factor X F10
P-selectin SELP
Fibroblast growth factor receptor 4 FGFR4
Fibroblast growth factor 4 FGF4
Fibroblast growth factor 19 FGF19
Fibroblast growth factor receptor 1 FGFR1
Fibroblast growth factor 1 FGF1
Fibroblast growth factor receptor 2 FGFR2
Fibroblast growth factor 2 FGF2
Platelet factor 4 PF4
Hepatocyte growth factor HGF

Referensi & Sumber

Synthesis reference: Fernando Fussi, Gianfranco Fedeli, "Oligo-heteropolysaccharides having a heparin-like activity method for their preparation and pharmaceutical compositions based thereon." U.S. Patent US4757057, issued June, 1952.
Artikel (PubMed)
  • PMID: 10549711
    Linhardt RJ, Gunay NS: Production and chemical processing of low molecular weight heparins. Semin Thromb Hemost. 1999;25 Suppl 3:5-16.
  • PMID: 2331699
    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.
  • PMID: 8352752
    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.
  • PMID: 15383472
    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.
  • PMID: 10201371
    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.
  • PMID: 11760916
    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.
  • PMID: 7254945
    McDonald MM, Jacobson LJ, Hay WW Jr, Hathaway WE: Heparin clearance in the newborn. Pediatr Res. 1981 Jul;15(7):1015-8.
  • PMID: 6889041
    Authors unspecified: Benzyl alcohol: toxic agent in neonatal units. Pediatrics. 1983 Sep;72(3):356-8.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 282 • International brands: 8
Produk
  • Calcilean Inj 20000unit/0.8ml
    Liquid • 20000 unit / .8 mL • Subcutaneous • Canada • Approved
  • Calciparine Inj 20000iu/amp
    Liquid • 20000 unit / amp • Subcutaneous • Canada • Approved
  • Calciparine Inj 5000iu
    Liquid • 5000 unit / syr • Subcutaneous • Canada • Approved
  • Defencath
    Solution • - • Intraluminal • US • Approved
  • Defencath
    Solution • - • Intraluminal • US • Approved
  • Hep-Lock
    Solution • 10 [USP'U]/1mL • Intravenous • US • Approved
  • Hep-Lock
    Solution • 10 [USP'U]/1mL • Intravenous • US • Approved
  • Hep-Lock
    Solution • 10 [USP'U]/1mL • Intravenous • US • Approved
Menampilkan 8 dari 282 produk.
International Brands
  • Calcilean
  • Calciparine
  • Hepalean
  • Heparin LEO
  • Liquaemin
  • Liquemin
  • Multiparin
  • Novoheparin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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