Peringatan Keamanan

Subcutaneous administration of a single dose at 3800 anti-Xa units/kg, which is 20.5 times the recommended dose for humans based on body surface area, was found to be lethal to female rats. Lethal effects were seen in male rats when administering a single subcutaneous dose at 15200 anti-Xa units/kg, which is approximately 82 times the recommended human dose based on body surface area FDA Label. In rats, the symptoms of acute toxicity following intravenous administration included respiratory depression, prostration and twitching FDA Label.

Accidental overdosage of danaparoid may lead to severe bleeding complications. While protamine sulfate may partially neutralize the anti-Xa actions of danaparoid, there is no evidence that it is capable of reducing severe non-surgical bleeding during treatment of danaparoid. In case of serious bleeding, danaparoid should be discontinued and blood transfusions should be administered if necessary. Withdrawal of danaparoid is expected to restore the coagulation balance without rebound phenomenon FDA Label.

There is no evidence of danaparoid to have a potential to induce carcinogenesis, mutagenesis and impairment of fertility FDA Label.

Danaparoid

DB06754

small molecule approved withdrawn

Deskripsi

Danaparoid is a low-molecular-weight heparinoid with an average molecular weight of 5500 Daltons consisting of a mixture of glycosaminoglycans A32565. The active constituents are heparan, dermatan and DB09301 T28, and they are isolated from the porcine intestinal mucosa FDA Label. Danaparoid possesses a potent antithrombic activity that works by inhibiting activated factor X (Factor Xa) and activated factor II (Factor IIa). It is chemically distinct from heparin by containing different protein binding properties, thus has lower cross-reactivity in heparin-intolerant patients. Danaproid is used in the treatment of heparin-induced thrombocytopenia (HIT) as an off-label indication and prevention of post-operative deep venous thrombosis (DVT). While it was initially approved by the FDA as Orgaran™, danaparoid was withdrawn by Organon International on August 14, 2002, due to a shortage in drug substance by the manufacturer. The use of Orgaran™ was discontinued in the United States however it is available in several other countries including European countries and Japan. Danaparoid sodium is the common salt form in therapeutic preparations and is typically administered subcutaneously.

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) Pharmacokinetic studies on danaparoid are based on the kinetics of its anticoagulant activities, which are mostly anti factor Xa and anti factor IIa activities. The elimination half-life ranges from 19.2 to 24.5 hours during anti-Xa activity and ranges from 1.8 to 4.3 hours during anti-IIa activity [A32564].
Volume Distribusi Pharmacokinetic studies on danaparoid are based on the kinetics of its anticoagulant activities, which are mostly anti factor Xa and anti factor IIa activities. The volumes of distribution of anti-Xa and anti-IIa activities are 9.1 L and 7.3-9.0 L, respectively [A32564].
Klirens (Clearance) Pharmacokinetic studies on danaparoid are based on the kinetics of its anticoagulant activities, which are mostly anti factor Xa and anti factor IIa activities. Total plasma clearance is about 0.36 L/h during anti-Xa activity, which may be accelerated with higher body surface area [FDA Label]. Total plasma clearance during anti-IIa activity ranges from 2.3 to 3 L [A32564].

Absorpsi

Pharmacokinetic studies on danaparoid are based on the kinetics of its anticoagulant activities, which are mostly antifactor Xa and antifactor IIa activities. The bioavailability of danaparoid is 100% following subcutaneous administration FDA Label. Following administration of single subcutaneous doses of 750, 1500, 2250, and 3250 anti-Xa units of danaparoid, the peak plasma anti-Xa activities were 102.4, 206.1, 283.9, and 403.4 mU/mL, respectively FDA Label. The time to reach maximum anti-Xa activity is approximately 2-5 hours FDA Label.

Metabolisme

There is no evidence of hepatic metabolism and danaparoid is unlikely to undergo cellular metabolism A32564.

Rute Eliminasi

Renal excretion is the main route of elimination, accounting for approximately 40-50% of the total clearance of antifactor Xa activity following intravenous administration of danaparoid A32564. Therefore in patients with severe renal impairment, the elimination half-life of anti-Xa activity may be prolonged FDA Label.

Interaksi Makanan

2 Data
  • 1. Avoid excessive or chronic alcohol consumption. Ingesting alcohol increases the risk of bleeding.
  • 2. Avoid herbs and supplements with anticoagulant/antiplatelet activity. These may increase the risk of bleeding. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

860 Data
Apixaban Apixaban may increase the anticoagulant activities of Danaparoid.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Danaparoid.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Danaparoid.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Danaparoid is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Taurocholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Danaparoid is combined with Hyodeoxycholic Acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Danaparoid.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Danaparoid.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Danaparoid is combined with Obinutuzumab.
Rivaroxaban Danaparoid may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Danaparoid is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Danaparoid.
Tipranavir The risk or severity of bleeding and hemorrhage can be increased when Tipranavir is combined with Danaparoid.
Urokinase Urokinase may increase the anticoagulant activities of Danaparoid.
Vitamin E Vitamin E may increase the anticoagulant activities of Danaparoid.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Danaparoid.
Trandolaprilat The risk or severity of hyperkalemia can be increased when Trandolaprilat is combined with Danaparoid.
Moexiprilat The risk or severity of hyperkalemia can be increased when Moexiprilat is combined with Danaparoid.
Cilazaprilat The risk or severity of hyperkalemia can be increased when Cilazaprilat is combined with Danaparoid.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Danaparoid.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Danaparoid.
Quinine The therapeutic efficacy of Danaparoid can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Danaparoid can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Danaparoid.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Danaparoid.
Corticorelin ovine triflutate The risk or severity of hypotension and sinus node depression can be increased when Danaparoid is combined with Corticorelin ovine triflutate.
Oritavancin The therapeutic efficacy of Danaparoid can be decreased when used in combination with Oritavancin.
Streptokinase Streptokinase may increase the anticoagulant activities of Danaparoid.
Telavancin The therapeutic efficacy of Danaparoid can be decreased when used in combination with Telavancin.
Palifermin The serum concentration of Palifermin can be increased when it is combined with Danaparoid.
Pentoxifylline The therapeutic efficacy of Danaparoid can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate Pentosan polysulfate may increase the anticoagulant activities of Danaparoid.
Levocarnitine The therapeutic efficacy of Danaparoid can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Danaparoid.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Danaparoid.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Danaparoid.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Danaparoid.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Danaparoid.
Quinestrol Quinestrol may decrease the anticoagulant activities of Danaparoid.
Hexestrol Hexestrol may decrease the anticoagulant activities of Danaparoid.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Danaparoid.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Danaparoid.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Danaparoid.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Danaparoid.
Zeranol Zeranol may decrease the anticoagulant activities of Danaparoid.
Equol Equol may decrease the anticoagulant activities of Danaparoid.
Methallenestril Methallenestril may decrease the anticoagulant activities of Danaparoid.
Epimestrol Epimestrol may decrease the anticoagulant activities of Danaparoid.
Moxestrol Moxestrol may decrease the anticoagulant activities of Danaparoid.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Danaparoid.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Danaparoid.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Danaparoid.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Danaparoid.
Biochanin A Biochanin A may decrease the anticoagulant activities of Danaparoid.
Formononetin Formononetin may decrease the anticoagulant activities of Danaparoid.
Estriol Estriol may decrease the anticoagulant activities of Danaparoid.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Danaparoid.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Danaparoid.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Danaparoid.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Danaparoid.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Danaparoid.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Danaparoid.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Danaparoid.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Danaparoid.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Danaparoid.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Danaparoid.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Danaparoid.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Danaparoid.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Danaparoid.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Danaparoid.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Danaparoid.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Danaparoid.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Danaparoid.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Danaparoid.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Danaparoid.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Danaparoid.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Danaparoid.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Danaparoid.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Danaparoid.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Danaparoid.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Danaparoid.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Danaparoid.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Danaparoid.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Danaparoid.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Danaparoid.
Olsalazine The risk or severity of bleeding can be increased when Danaparoid is combined with Olsalazine.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Danaparoid.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Danaparoid.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Danaparoid.

Target Protein

Antithrombin-III SERPINC1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12890149
    Kodityal S, Manhas AH, Udden M, Rice L: Danaparoid for heparin-induced thrombocytopenia: an analysis of treatment failures. Eur J Haematol. 2003 Aug;71(2):109-13.
  • PMID: 12381232
    Ibbotson T, Perry CM: Danaparoid: a review of its use in thromboembolic and coagulation disorders. Drugs. 2002;62(15):2283-314.
  • PMID: 9421696
    Wilde MI, Markham A: Danaparoid. A review of its pharmacology and clinical use in the management of heparin-induced thrombocytopenia. Drugs. 1997 Dec;54(6):903-24.
  • PMID: 17131147
    Liu J, Pedersen LC: Anticoagulant heparan sulfate: structural specificity and biosynthesis. Appl Microbiol Biotechnol. 2007 Feb;74(2):263-72. doi: 10.1007/s00253-006-0722-x. Epub 2006 Nov 28.
Textbook
  • ISBN: 978-0-7020-3471-8
    24. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 299-300). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Orgaran
    Solution • 750 unit / 0.6 mL • Intravenous; Subcutaneous • Canada • Approved

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul