Peringatan Keamanan

Hepatotoxicity (liver damage) was reported during trials.

Ximelagatran

DB04898

small molecule approved investigational withdrawn

Deskripsi

Ximelagatran is an anticoagulant intended to become a replacement for warfarin by overcoming the dietary restrictions, drug interaction, and monitoring issues associated with the former. In 2006, its manufacturer AstraZeneca announced that it would not attempt to market ximelagatran after reports of hepatotoxicity (liver damage) during trials, and to discontinue its distribution in countries where the drug had been approved.

Struktur Molekul 2D

Berat 473.5652
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 3-5 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Rapidly absorbed by the small intestine with an oral bioavailability of 20%.

Metabolisme

Ximelagatran is a prodrug, and hence, it requires in vivo conversion to the active agent, melagatran. The activation of ximelagatran is produced in the liver and many other tissues mainly by reactions of dealkylation and dehydroxylation.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Interaksi Obat

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

Target Protein

Prothrombin F2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 12871538
    Eriksson H, Wahlander K, Gustafsson D, Welin LT, Frison L, Schulman S: A randomized, controlled, dose-guiding study of the oral direct thrombin inhibitor ximelagatran compared with standard therapy for the treatment of acute deep vein thrombosis: THRIVE I. J Thromb Haemost. 2003 Jan;1(1):41-7.
  • PMID: 15339877
    Weitz JI: New anticoagulants for treatment of venous thromboembolism. Circulation. 2004 Aug 31;110(9 Suppl 1):I19-26.
  • PMID: 14585938
    Francis CW, Berkowitz SD, Comp PC, Lieberman JR, Ginsberg JS, Paiement G, Peters GR, Roth AW, McElhattan J, Colwell CW Jr: Comparison of ximelagatran with warfarin for the prevention of venous thromboembolism after total knee replacement. N Engl J Med. 2003 Oct 30;349(18):1703-12.
  • PMID: 17516699
    Bergqvist D, Solhaug JH, Holmdahl L, Eriksson UG, Andersson M, Boberg B, Ogren M: Pharmacokinetics, preliminary efficacy and safety of subcutaneous melagatran and oral ximelagatran : a multicentre study of thromboprophylaxis in elective abdominal surgery. Clin Drug Investig. 2004;24(3):127-36.
  • PMID: 17636192
    Koscielny J, Kiesewetter H, Jorg I, Harenberg J: Ximelagatran for treatment and prophylaxis of recurrent events in deep vein thrombosis. Clin Appl Thromb Hemost. 2007 Jul;13(3):299-307.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Exanta
  • Exarta

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