Peringatan Keamanan

Excessive bleeding. Overdosages should be treated using activated charcoal and supportive measures such as mechanical compression and hemodynamic support. If bleeding is not controlled, the following procoagulants can be administered: activated prothrombin complex concentrate, prothrombin complex concentrate and recombinant factor VIIa. There is also a higher chance of post procedural hemorrhage compared to enoxaparin (1.55% vs. 1.39% respectively).

Rivaroxaban

DB06228

small molecule approved

Deskripsi

Rivaroxaban is an anticoagulant and the first orally active direct factor Xa inhibitor. Unlike warfarin, routine lab monitoring of INR is not necessary. However there is no antidote available in the event of a major bleed. Only the 10 mg tablet can be taken without regard to food. The 15 mg and 20 mg tablet should be taken with food. FDA approved on July 1, 2011.

Struktur Molekul 2D

Berat 435.881
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The terminal half life is 5-9 hours in adults and 11-13 hours in the elderly.
Volume Distribusi The steady state Vd is 50 L
Klirens (Clearance) Systemic clearance is approximately 10 L/h, so rivaroxaban is considered a drug with low clearance. Renal clearance is ~3-4 L/h.

Absorpsi

Following oral administration, rivaroxaban is rapidly absorbed and reaches peak plasma concentration in 2-4 hours. Bioavailability of the 10 mg dose is >80%. However, the 15-20 mg dose have a lower bioavailability if taken in the fasted state and consequently should be taken with food.

Metabolisme

Approximately two-thirds of the dose is metabolized. It is metabolized by CYP3A4, CYP3A5, CYP2J2 and CYP-independant mechanisms

Rute Eliminasi

Approximately two-thirds of rivaroxaban is excreted into urine (via active tubular secretion in which approximately 36% as unchanged drug and 30% as inactive metabolism). The remaining third of the administered dose is excreted via feces in which 7% is in the form of unchanged drug and 21% as inactive metabolites.

Interaksi Makanan

4 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Avoid St. John's Wort. Co-administration will decrease levels of this medication.
  • 3. Take with food. Rivaroxaban 15-20mg dose should be taken with food as food significantly impacts the bioavailability at that dose.
  • 4. Take with or without food. Rivaroxaban 10mg dose can be taken with or without food as it does not significantly impact the bioavailability at that dose.

Interaksi Obat

1488 Data
Apixaban Apixaban may increase the anticoagulant activities of Rivaroxaban.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Rivaroxaban.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Rivaroxaban.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Rivaroxaban is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Taurocholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Rivaroxaban is combined with Hyodeoxycholic Acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Rivaroxaban.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Rivaroxaban.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Rivaroxaban is combined with Obinutuzumab.
Lepirudin Lepirudin may increase the anticoagulant activities of Rivaroxaban.
Bivalirudin Bivalirudin may increase the anticoagulant activities of Rivaroxaban.
Alteplase Alteplase may increase the anticoagulant activities of Rivaroxaban.
Urokinase Urokinase may increase the anticoagulant activities of Rivaroxaban.
Reteplase Reteplase may increase the anticoagulant activities of Rivaroxaban.
Anistreplase Anistreplase may increase the anticoagulant activities of Rivaroxaban.
Tenecteplase Tenecteplase may increase the anticoagulant activities of Rivaroxaban.
Abciximab Abciximab may increase the anticoagulant activities of Rivaroxaban.
Drotrecogin alfa Drotrecogin alfa may increase the anticoagulant activities of Rivaroxaban.
Streptokinase Streptokinase may increase the anticoagulant activities of Rivaroxaban.
Dicoumarol Dicoumarol may increase the anticoagulant activities of Rivaroxaban.
Argatroban Argatroban may increase the anticoagulant activities of Rivaroxaban.
Ardeparin Ardeparin may increase the anticoagulant activities of Rivaroxaban.
Phenindione Phenindione may increase the anticoagulant activities of Rivaroxaban.
Fondaparinux Fondaparinux may increase the anticoagulant activities of Rivaroxaban.
Warfarin Warfarin may increase the anticoagulant activities of Rivaroxaban.
Pentosan polysulfate Pentosan polysulfate may increase the anticoagulant activities of Rivaroxaban.
Phenprocoumon Phenprocoumon may increase the anticoagulant activities of Rivaroxaban.
Dipyridamole Dipyridamole may increase the anticoagulant activities of Rivaroxaban.
Heparin Heparin may increase the anticoagulant activities of Rivaroxaban.
Enoxaparin Enoxaparin may increase the anticoagulant activities of Rivaroxaban.
Epoprostenol Epoprostenol may increase the anticoagulant activities of Rivaroxaban.
Acenocoumarol Acenocoumarol may increase the anticoagulant activities of Rivaroxaban.
4-hydroxycoumarin 4-hydroxycoumarin may increase the anticoagulant activities of Rivaroxaban.
Coumarin Coumarin may increase the anticoagulant activities of Rivaroxaban.
Ximelagatran Ximelagatran may increase the anticoagulant activities of Rivaroxaban.
Desmoteplase Desmoteplase may increase the anticoagulant activities of Rivaroxaban.
Defibrotide Defibrotide may increase the anticoagulant activities of Rivaroxaban.
Ancrod Ancrod may increase the anticoagulant activities of Rivaroxaban.
Beraprost Beraprost may increase the anticoagulant activities of Rivaroxaban.
Prasugrel Prasugrel may increase the anticoagulant activities of Rivaroxaban.
Sulodexide Sulodexide may increase the anticoagulant activities of Rivaroxaban.
Semuloparin Semuloparin may increase the anticoagulant activities of Rivaroxaban.
Idraparinux Idraparinux may increase the anticoagulant activities of Rivaroxaban.
Cangrelor Cangrelor may increase the anticoagulant activities of Rivaroxaban.
Astaxanthin Astaxanthin may increase the anticoagulant activities of Rivaroxaban.
Otamixaban Otamixaban may increase the anticoagulant activities of Rivaroxaban.
Amediplase Amediplase may increase the anticoagulant activities of Rivaroxaban.
Danaparoid Danaparoid may increase the anticoagulant activities of Rivaroxaban.
Dalteparin Dalteparin may increase the anticoagulant activities of Rivaroxaban.
Tinzaparin Tinzaparin may increase the anticoagulant activities of Rivaroxaban.
(R)-warfarin (R)-warfarin may increase the anticoagulant activities of Rivaroxaban.
Ethyl biscoumacetate Ethyl biscoumacetate may increase the anticoagulant activities of Rivaroxaban.
Nadroparin Nadroparin may increase the anticoagulant activities of Rivaroxaban.
Triflusal Triflusal may increase the anticoagulant activities of Rivaroxaban.
Ticagrelor Ticagrelor may increase the anticoagulant activities of Rivaroxaban.
Ditazole Ditazole may increase the anticoagulant activities of Rivaroxaban.
Vorapaxar Vorapaxar may increase the anticoagulant activities of Rivaroxaban.
Potassium citrate Potassium citrate may increase the excretion rate of Rivaroxaban which could result in a lower serum level and potentially a reduction in efficacy.
Sodium citrate Sodium citrate may increase the anticoagulant activities of Rivaroxaban.
Dextran Dextran may increase the anticoagulant activities of Rivaroxaban.
Bemiparin Bemiparin may increase the anticoagulant activities of Rivaroxaban.
Parnaparin Parnaparin may increase the anticoagulant activities of Rivaroxaban.
Desirudin Desirudin may increase the anticoagulant activities of Rivaroxaban.
Antithrombin Alfa Antithrombin Alfa may increase the anticoagulant activities of Rivaroxaban.
Protein C Protein C may increase the anticoagulant activities of Rivaroxaban.
Antithrombin III human Antithrombin III human may increase the anticoagulant activities of Rivaroxaban.
Letaxaban Letaxaban may increase the anticoagulant activities of Rivaroxaban.
Darexaban Darexaban may increase the anticoagulant activities of Rivaroxaban.
Betrixaban Betrixaban may increase the anticoagulant activities of Rivaroxaban.
Nafamostat Nafamostat may increase the anticoagulant activities of Rivaroxaban.
Monteplase Monteplase may increase the anticoagulant activities of Rivaroxaban.
Gabexate Gabexate may increase the anticoagulant activities of Rivaroxaban.
Fluindione Fluindione may increase the anticoagulant activities of Rivaroxaban.
Protein S human Protein S human may increase the anticoagulant activities of Rivaroxaban.
Brinase Brinase may increase the anticoagulant activities of Rivaroxaban.
Clorindione Clorindione may increase the anticoagulant activities of Rivaroxaban.
Diphenadione Diphenadione may increase the anticoagulant activities of Rivaroxaban.
Tioclomarol Tioclomarol may increase the anticoagulant activities of Rivaroxaban.
Melagatran Melagatran may increase the anticoagulant activities of Rivaroxaban.
Saruplase Saruplase may increase the anticoagulant activities of Rivaroxaban.
(S)-Warfarin (S)-Warfarin may increase the anticoagulant activities of Rivaroxaban.
Tocopherylquinone Tocopherylquinone may increase the anticoagulant activities of Rivaroxaban.
Dabigatran Dabigatran may increase the anticoagulant activities of Rivaroxaban.
Edetic acid Edetic acid may increase the anticoagulant activities of Rivaroxaban.
Troxerutin Troxerutin may increase the anticoagulant activities of Rivaroxaban.
Reviparin Reviparin may increase the anticoagulant activities of Rivaroxaban.
Dermatan sulfate Dermatan sulfate may increase the anticoagulant activities of Rivaroxaban.
SR-123781A SR-123781A may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Rivaroxaban is combined with Sugammadex.

Target Protein

Coagulation factor X F10

Referensi & Sumber

Synthesis reference: Prabhudas BODHURI, Gamini Weeratunga, "PROCESSES FOR THE PREPARATION OF RIVAROXABAN AND INTERMEDIATES THEREOF." U.S. Patent US20100273790, issued October 28, 2010.
Artikel (PubMed)
  • PMID: 18491993
    Piccini JP, Patel MR, Mahaffey KW, Fox KA, Califf RM: Rivaroxaban, an oral direct factor Xa inhibitor. Expert Opin Investig Drugs. 2008 Jun;17(6):925-37. doi: 10.1517/13543784.17.6.925 .
  • PMID: 18473863
    Alban S: Pharmacological strategies for inhibition of thrombin activity. Curr Pharm Des. 2008;14(12):1152-75.
  • PMID: 19846028
    Stevenson M, Scope A, Holmes M, Rees A, Kaltenthaler E: Rivaroxaban for the prevention of venous thromboembolism: a single technology appraisal. Health Technol Assess. 2009 Oct;13 Suppl 3:43-8. doi: 10.3310/hta13suppl3/07.
  • PMID: 19696978
    Imberti D, Dall'Asta C, Pierfranceschi MG: Oral factor Xa inhibitors for thromboprophylaxis in major orthopedic surgery: a review. Intern Emerg Med. 2009 Dec;4(6):471-7. doi: 10.1007/s11739-009-0293-9.
  • PMID: 21554163
    Alexander D, Jeremias A: Rivaroxaban in the contemporary treatment of acute coronary syndromes. Expert Opin Investig Drugs. 2011 Jun;20(6):849-57. doi: 10.1517/13543784.2011.580274. Epub 2011 May 10.
  • PMID: 23645472
    Cabral KP: Pharmacology of the new target-specific oral anticoagulants. J Thromb Thrombolysis. 2013 Aug;36(2):133-40. doi: 10.1007/s11239-013-0929-5.

Contoh Produk & Brand

Produk: 263 • International brands: 0
Produk
  • Ach-rivaroxaban
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ach-rivaroxaban
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Ach-rivaroxaban
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Ach-rivaroxaban
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Ag-rivaroxaban
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ag-rivaroxaban
    Tablet • 15 mg • Oral • Canada • Generic • Approved
  • Ag-rivaroxaban
    Tablet • 20 mg • Oral • Canada • Generic • Approved
  • Apo-rivaroxaban
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 263 produk.

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