Peringatan Keamanan

Animal studies have shown an increased risk of maternal bleeding during pregnancy but no increase in fetal malformations or fetal or maternal deathsLabel. It is unknown if this animal data also translates to humans so apixaban should only be used in pregnancy if the benefits outweigh the risksLabel. It is not know whether apixaban is safe and effective in labor and during birth, though animal studies have shown an increased rate of maternal bleedingLabel. Animal studies in rats show apixaban excreted in milk, though it is not know if this also applies to humansLabel. Nursing mothers should either stop breastfeeding or stop taking apixaban depending on the risk and benefit of each optionLabel. Studies to determine safety and effectiveness in pediatric patients have yet to be performedLabel. Studies that involved geriatric patients (at least 75 years old) saw no difference in safety or effectiveness compared to younger patients, though geriatric patients at an especially advanced age may be more susceptible to adverse effectsLabel. Dosage adjustments for patients with end stage renal disease(ESRD) are based on estimates of pharmacokinetic principles and not clinical studyLabel. Patients with ESRD may experience pharmacodynamics similar to those seen in well controlled studies but it may not lead to the same clinical effectsLabel. Dosage adjustments are not necessary in mild hepatic impairmentLabel. In moderate hepatic impairment patients may already experience abnormalities in coagulation and so no dose recommendations are possibleLabel. Apixaban is not recommended for patients with severe hepatic impairmentLabel.

Apixaban

DB06605

small molecule approved

Deskripsi

Apixaban is an oral, direct, and highly selective factor Xa (FXa) inhibitor of both free and bound FXa, as well as prothrombinase, independent of antithrombin III for the prevention and treatment of thromboembolic diseasesLabel,A6897. It is marketed under the name EliquisLabel,L6043. Apixaban was approved by the FDA on December 28, 2012L6043.

Struktur Molekul 2D

Berat 459.4971
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 12.7±8.55h[Label,A177565,A6897].
Volume Distribusi Approximately 21L[Label].
Klirens (Clearance) 3.3L/h[Label] though other studies report 4876mL/h[A177565].

Absorpsi

Apixaban is approximately 50% bioavailableLabel though other studies report 43-46% oral bioavailabilityA177565.

Metabolisme

50% of the orally administered dose is excreted as the unchanged parent compound, however 25% of the dose is excreted as O-demethyl apixaban sulfateLabel,A177565. All apixaban metabolites account for approximately 32% of the excreted dose though the structure of all metabolites are not well definedA177565. Apixaban is mainly metabolized by cytochrome p450(CYP)3A4 and to a lesser extent by CYP1A2, CYP2C8, CYP2C9, CYP2C19, and CYP2J2Label.

Rute Eliminasi

56% of an orally administered dose is recovered in the feces and 24.5-28.8% of the dose is recovered in the urinelabel,A177565,A6897. 83-88% of the dose recovered in the urine was the unchanged parent compoundA177565.

Interaksi Makanan

4 Data
  • 1. Avoid grapefruit products.
  • 2. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 3. Avoid St. John's Wort. St. John's Wort will decrease levels of this medication.
  • 4. Take with or without food.

Interaksi Obat

1253 Data
Lepirudin Apixaban may increase the anticoagulant activities of Lepirudin.
Bivalirudin Apixaban may increase the anticoagulant activities of Bivalirudin.
Alteplase Apixaban may increase the anticoagulant activities of Alteplase.
Urokinase Apixaban may increase the anticoagulant activities of Urokinase.
Reteplase Apixaban may increase the anticoagulant activities of Reteplase.
Anistreplase Apixaban may increase the anticoagulant activities of Anistreplase.
Tenecteplase Apixaban may increase the anticoagulant activities of Tenecteplase.
Abciximab Apixaban may increase the anticoagulant activities of Abciximab.
Drotrecogin alfa Apixaban may increase the anticoagulant activities of Drotrecogin alfa.
Streptokinase Apixaban may increase the anticoagulant activities of Streptokinase.
Dicoumarol Apixaban may increase the anticoagulant activities of Dicoumarol.
Argatroban Apixaban may increase the anticoagulant activities of Argatroban.
Ardeparin Apixaban may increase the anticoagulant activities of Ardeparin.
Phenindione Apixaban may increase the anticoagulant activities of Phenindione.
Fondaparinux Apixaban may increase the anticoagulant activities of Fondaparinux.
Warfarin Apixaban may increase the anticoagulant activities of Warfarin.
Pentosan polysulfate Apixaban may increase the anticoagulant activities of Pentosan polysulfate.
Phenprocoumon Apixaban may increase the anticoagulant activities of Phenprocoumon.
Dipyridamole Apixaban may increase the anticoagulant activities of Dipyridamole.
Heparin Apixaban may increase the anticoagulant activities of Heparin.
Enoxaparin Apixaban may increase the anticoagulant activities of Enoxaparin.
Epoprostenol Apixaban may increase the anticoagulant activities of Epoprostenol.
Acenocoumarol Apixaban may increase the anticoagulant activities of Acenocoumarol.
4-hydroxycoumarin Apixaban may increase the anticoagulant activities of 4-hydroxycoumarin.
Coumarin Apixaban may increase the anticoagulant activities of Coumarin.
Ximelagatran Apixaban may increase the anticoagulant activities of Ximelagatran.
Desmoteplase Apixaban may increase the anticoagulant activities of Desmoteplase.
Defibrotide Apixaban may increase the anticoagulant activities of Defibrotide.
Ancrod Apixaban may increase the anticoagulant activities of Ancrod.
Beraprost Apixaban may increase the anticoagulant activities of Beraprost.
Prasugrel Apixaban may increase the anticoagulant activities of Prasugrel.
Rivaroxaban Apixaban may increase the anticoagulant activities of Rivaroxaban.
Sulodexide Apixaban may increase the anticoagulant activities of Sulodexide.
Semuloparin Apixaban may increase the anticoagulant activities of Semuloparin.
Idraparinux Apixaban may increase the anticoagulant activities of Idraparinux.
Cangrelor Apixaban may increase the anticoagulant activities of Cangrelor.
Astaxanthin Apixaban may increase the anticoagulant activities of Astaxanthin.
Otamixaban Apixaban may increase the anticoagulant activities of Otamixaban.
Amediplase Apixaban may increase the anticoagulant activities of Amediplase.
Dabigatran etexilate Apixaban may increase the anticoagulant activities of Dabigatran etexilate.
Danaparoid Apixaban may increase the anticoagulant activities of Danaparoid.
Dalteparin Apixaban may increase the anticoagulant activities of Dalteparin.
Tinzaparin Apixaban may increase the anticoagulant activities of Tinzaparin.
(R)-warfarin Apixaban may increase the anticoagulant activities of (R)-warfarin.
Ethyl biscoumacetate Apixaban may increase the anticoagulant activities of Ethyl biscoumacetate.
Nadroparin Apixaban may increase the anticoagulant activities of Nadroparin.
Triflusal Apixaban may increase the anticoagulant activities of Triflusal.
Ticagrelor Apixaban may increase the anticoagulant activities of Ticagrelor.
Ditazole Apixaban may increase the anticoagulant activities of Ditazole.
Vorapaxar Apixaban may increase the anticoagulant activities of Vorapaxar.
Edoxaban Apixaban may increase the anticoagulant activities of Edoxaban.
Sodium citrate Apixaban may increase the anticoagulant activities of Sodium citrate.
Dextran Apixaban may increase the anticoagulant activities of Dextran.
Bemiparin Apixaban may increase the anticoagulant activities of Bemiparin.
Parnaparin Apixaban may increase the anticoagulant activities of Parnaparin.
Desirudin Apixaban may increase the anticoagulant activities of Desirudin.
Antithrombin Alfa Apixaban may increase the anticoagulant activities of Antithrombin Alfa.
Protein C Apixaban may increase the anticoagulant activities of Protein C.
Antithrombin III human Apixaban may increase the anticoagulant activities of Antithrombin III human.
Letaxaban Apixaban may increase the anticoagulant activities of Letaxaban.
Darexaban Apixaban may increase the anticoagulant activities of Darexaban.
Betrixaban Apixaban may increase the anticoagulant activities of Betrixaban.
Nafamostat Apixaban may increase the anticoagulant activities of Nafamostat.
Monteplase Apixaban may increase the anticoagulant activities of Monteplase.
Gabexate Apixaban may increase the anticoagulant activities of Gabexate.
Fluindione Apixaban may increase the anticoagulant activities of Fluindione.
Protein S human Apixaban may increase the anticoagulant activities of Protein S human.
Brinase Apixaban may increase the anticoagulant activities of Brinase.
Clorindione Apixaban may increase the anticoagulant activities of Clorindione.
Diphenadione Apixaban may increase the anticoagulant activities of Diphenadione.
Tioclomarol Apixaban may increase the anticoagulant activities of Tioclomarol.
Melagatran Apixaban may increase the anticoagulant activities of Melagatran.
Saruplase Apixaban may increase the anticoagulant activities of Saruplase.
(S)-Warfarin Apixaban may increase the anticoagulant activities of (S)-Warfarin.
Tocopherylquinone Apixaban may increase the anticoagulant activities of Tocopherylquinone.
Dabigatran Apixaban may increase the anticoagulant activities of Dabigatran.
Edetic acid Apixaban may increase the anticoagulant activities of Edetic acid.
Troxerutin Apixaban may increase the anticoagulant activities of Troxerutin.
Reviparin Apixaban may increase the anticoagulant activities of Reviparin.
Dermatan sulfate Apixaban may increase the anticoagulant activities of Dermatan sulfate.
SR-123781A Apixaban may increase the anticoagulant activities of SR-123781A.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Apixaban.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Apixaban is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Taurocholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Apixaban is combined with Hyodeoxycholic Acid.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Apixaban.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Apixaban is combined with Obinutuzumab.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Apixaban is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Apixaban.

Target Protein

Coagulation factor X F10

Referensi & Sumber

Artikel (PubMed)
  • PMID: 18832478
    Raghavan N, Frost CE, Yu Z, He K, Zhang H, Humphreys WG, Pinto D, Chen S, Bonacorsi S, Wong PC, Zhang D: Apixaban metabolism and pharmacokinetics after oral administration to humans. Drug Metab Dispos. 2009 Jan;37(1):74-81. doi: 10.1124/dmd.108.023143. Epub 2008 Oct 2.
  • PMID: 21870978
    Granger CB, Alexander JH, McMurray JJ, Lopes RD, Hylek EM, Hanna M, Al-Khalidi HR, Ansell J, Atar D, Avezum A, Bahit MC, Diaz R, Easton JD, Ezekowitz JA, Flaker G, Garcia D, Geraldes M, Gersh BJ, Golitsyn S, Goto S, Hermosillo AG, Hohnloser SH, Horowitz J, Mohan P, Jansky P, Lewis BS, Lopez-Sendon JL, Pais P, Parkhomenko A, Verheugt FW, Zhu J, Wallentin L: Apixaban versus warfarin in patients with atrial fibrillation. N Engl J Med. 2011 Sep 15;365(11):981-92. doi: 10.1056/NEJMoa1107039. Epub 2011 Aug 27.

Contoh Produk & Brand

Produk: 129 • International brands: 0
Produk
  • Ach-apixaban
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Ach-apixaban
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Ag-apixaban
    Tablet • 2.5 mg • Oral • Canada • Generic • Approved
  • Ag-apixaban
    Tablet • 5 mg • Oral • Canada • Generic • Approved
  • Apixaban
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Apixaban
    Tablet • 2.5 mg • Oral • Canada • Approved
  • Apixaban
    Tablet • 5 mg • Oral • Canada • Approved
  • Apixaban
    Tablet • 5 mg • Oral • Canada • Approved
Menampilkan 8 dari 129 produk.

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