Peringatan Keamanan

The onset and severity of the symptoms are dependent on the individual's sensitivity to oral anticoagulants, the severity of the overdosage, and the duration of treatment. Bleeding is the major sign of toxicity with oral anticoagulant drugs. The most frequent symptoms observed are: cutaneous bleeding (80%), haematuria (with renal colic) (52%), haematomas, gastrointestinal bleeding, haematemesis, uterine bleeding, epistaxis, gingival bleeding and bleeding into the joints. Further symptoms include tachycardia, hypotension, peripheral circulatory disorders due to loss of blood, nausea, vomiting, diarrhoea and abdominal pains.

Acenocoumarol

DB01418

small molecule approved investigational

Deskripsi

Acenocoumarol is a coumarin derivative used as an anticoagulant. Coumarin derivatives inhibit the reduction of vitamin K by vitamin K reductase. This prevents carboxylation of vitamin K-dependent clotting factors, II, VII, IX and X, and interferes with coagulation.A188739 Hematocrit, hemoglobin, international normalized ratio and liver panel should be monitored. Patients on acenocoumarol are prohibited from giving blood.

Struktur Molekul 2D

Berat 353.3255
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 8 to 11 hours.
Volume Distribusi The volume of distribution at steady-state appeared to be significantly dose dependent: 78 ml/kg for doses < or = 20 microg/kg and 88 ml/kg for doses > 20 microg/kg respectively
Klirens (Clearance) -

Absorpsi

Rapidly absorbed orally with greater than 60% bioavailability. Peak plasma levels are attained 1 to 3 hours following oral administration.

Metabolisme

Extensively metabolized in the liver via oxidation forming two hydroxy metabolites and keto reduction producing two alcohol metabolites. Reduction of the nitro group produces an amino metabolite which is further transformed to an acetoamido metabolite. Metabolites do not appear to be pharmacologically active.

Rute Eliminasi

Mostly via the kidney as metabolites

Farmakogenomik

5 Varian
CYP2C9 (rs1799853)

The presence of this polymorphism in CYP2C9 is associated with reduction in acenocoumarol metabolism.

CYP2C9 (rs1057910)

The presence of this polymorphism in CYP2C9 is associated with reduction in acenocoumarol metabolism.

CYP2C9 (rs1799853)

Patients with this polymorphism in CYP2C9 may be at a higher risk of developing drug-related hemorrhage or thrombosis when treated with acenocoumarol.

CYP2C9 (rs1057910)

Patients with this polymorphism in CYP2C9 may be at a higher risk of developing drug-related hemorrhage or thrombosis when treated with acenocoumarol.

VKORC1 (rs9934438)

The presence of this single nucleotide polymorphism in VKORC1 is associated with reduction in acenocoumarol metabolism and increased risk of drug-related hemorrhage.

Interaksi Makanan

3 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Ensure consistent Vitamin K intake. Changes in vitamin K intake may impact coagulation. Foods containing vitamin K include spinach, kale, and swiss chard.
  • 3. Exercise caution with St. John's Wort.

Interaksi Obat

1749 Data
Apixaban Apixaban may increase the anticoagulant activities of Acenocoumarol.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Acenocoumarol.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Acenocoumarol.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Acenocoumarol is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Taurocholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Acenocoumarol is combined with Hyodeoxycholic Acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Acenocoumarol.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Acenocoumarol.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Acenocoumarol is combined with Obinutuzumab.
Rivaroxaban Acenocoumarol may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Acenocoumarol is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Acenocoumarol.
Tipranavir The risk or severity of bleeding and hemorrhage can be increased when Tipranavir is combined with Acenocoumarol.
Urokinase Urokinase may increase the anticoagulant activities of Acenocoumarol.
Vitamin E Vitamin E may increase the anticoagulant activities of Acenocoumarol.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Acenocoumarol.
Modafinil The metabolism of Acenocoumarol can be increased when combined with Modafinil.
Armodafinil The metabolism of Acenocoumarol can be increased when combined with Armodafinil.
Peginterferon alfa-2b The serum concentration of Acenocoumarol can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Acenocoumarol can be decreased when it is combined with Leflunomide.
Dabrafenib The serum concentration of Acenocoumarol can be decreased when it is combined with Dabrafenib.
Luliconazole The serum concentration of Acenocoumarol can be increased when it is combined with Luliconazole.
Metreleptin The metabolism of Acenocoumarol can be increased when combined with Metreleptin.
Mirtazapine Mirtazapine may increase the anticoagulant activities of Acenocoumarol.
Sorafenib The risk or severity of bleeding can be increased when Sorafenib is combined with Acenocoumarol.
Gemcitabine The therapeutic efficacy of Acenocoumarol can be increased when used in combination with Gemcitabine.
Trilostane Trilostane may increase the anticoagulant activities of Acenocoumarol.
Ciclesonide Ciclesonide may increase the anticoagulant activities of Acenocoumarol.
Aldosterone Aldosterone may increase the anticoagulant activities of Acenocoumarol.
Fluprednidene Fluprednidene may increase the anticoagulant activities of Acenocoumarol.
Tixocortol Tixocortol may increase the anticoagulant activities of Acenocoumarol.
Fluprednisolone Fluprednisolone may increase the anticoagulant activities of Acenocoumarol.
Meprednisone Meprednisone may increase the anticoagulant activities of Acenocoumarol.
Melengestrol Melengestrol may increase the anticoagulant activities of Acenocoumarol.
Deflazacort Deflazacort may increase the anticoagulant activities of Acenocoumarol.
Cortivazol Cortivazol may increase the anticoagulant activities of Acenocoumarol.
Prednylidene Prednylidene may increase the anticoagulant activities of Acenocoumarol.
Fluocortin Fluocortin may increase the anticoagulant activities of Acenocoumarol.
Fluperolone Fluperolone may increase the anticoagulant activities of Acenocoumarol.
Cloprednol Cloprednol may increase the anticoagulant activities of Acenocoumarol.
Fluclorolone Fluclorolone may increase the anticoagulant activities of Acenocoumarol.
Mometasone furoate Mometasone furoate may increase the anticoagulant activities of Acenocoumarol.
Hydrocortisone cypionate Hydrocortisone cypionate may increase the anticoagulant activities of Acenocoumarol.
Prednisolone phosphate Prednisolone phosphate may increase the anticoagulant activities of Acenocoumarol.
Prednisolone hemisuccinate Prednisolone hemisuccinate may increase the anticoagulant activities of Acenocoumarol.
Methylprednisolone hemisuccinate Methylprednisolone hemisuccinate may increase the anticoagulant activities of Acenocoumarol.
Prednisone acetate Prednisone acetate may increase the anticoagulant activities of Acenocoumarol.
Clocortolone acetate Clocortolone acetate may increase the anticoagulant activities of Acenocoumarol.
Melengestrol acetate Melengestrol acetate may increase the anticoagulant activities of Acenocoumarol.
Betamethasone phosphate Betamethasone phosphate may increase the anticoagulant activities of Acenocoumarol.
Cortisone Cortisone may increase the anticoagulant activities of Acenocoumarol.
Paramethasone Paramethasone may increase the anticoagulant activities of Acenocoumarol.
Fluticasone furoate Fluticasone furoate may increase the anticoagulant activities of Acenocoumarol.
Fluticasone Fluticasone may increase the anticoagulant activities of Acenocoumarol.
Fludrocortisone Fludrocortisone may increase the anticoagulant activities of Acenocoumarol.
Prednisone Prednisone may increase the anticoagulant activities of Acenocoumarol.
Clobetasol propionate Clobetasol propionate may increase the anticoagulant activities of Acenocoumarol.
Fluocinonide Fluocinonide may increase the anticoagulant activities of Acenocoumarol.
Hydrocortisone butyrate Hydrocortisone butyrate may increase the anticoagulant activities of Acenocoumarol.
Desoximetasone Desoximetasone may increase the anticoagulant activities of Acenocoumarol.
Mometasone Mometasone may increase the anticoagulant activities of Acenocoumarol.
Fluocortolone Fluocortolone may increase the anticoagulant activities of Acenocoumarol.
Prednisolone acetate Prednisolone acetate may increase the anticoagulant activities of Acenocoumarol.
Fluorometholone Fluorometholone may increase the anticoagulant activities of Acenocoumarol.
Difluocortolone Difluocortolone may increase the anticoagulant activities of Acenocoumarol.
Flumethasone Flumethasone may increase the anticoagulant activities of Acenocoumarol.
Methylprednisolone aceponate Methylprednisolone aceponate may increase the anticoagulant activities of Acenocoumarol.
Ritonavir The serum concentration of Acenocoumarol can be decreased when it is combined with Ritonavir.
Erlotinib The serum concentration of Acenocoumarol can be increased when it is combined with Erlotinib.
Tigecycline The serum concentration of Acenocoumarol can be increased when it is combined with Tigecycline.
Imatinib Imatinib may increase the anticoagulant activities of Acenocoumarol.
Trazodone Trazodone may decrease the anticoagulant activities of Acenocoumarol.
Allopurinol The risk or severity of bleeding can be increased when Allopurinol is combined with Acenocoumarol.
Methylene blue The serum concentration of Acenocoumarol can be increased when it is combined with Methylene blue.
Viloxazine The metabolism of Acenocoumarol can be decreased when combined with Viloxazine.
Azelastine The metabolism of Acenocoumarol can be decreased when combined with Azelastine.
Aldesleukin The serum concentration of Acenocoumarol can be increased when it is combined with Aldesleukin.
Fluvoxamine The serum concentration of Acenocoumarol can be increased when it is combined with Fluvoxamine.
Fluconazole The serum concentration of Acenocoumarol can be increased when it is combined with Fluconazole.
Citalopram The risk or severity of bleeding can be increased when Acenocoumarol is combined with Citalopram.
Lovastatin The risk or severity of bleeding can be increased when Lovastatin is combined with Acenocoumarol.
Ziprasidone The serum concentration of Acenocoumarol can be increased when it is combined with Ziprasidone.
Cabergoline The serum concentration of Acenocoumarol can be increased when it is combined with Cabergoline.
Diethylstilbestrol The serum concentration of Acenocoumarol can be increased when it is combined with Diethylstilbestrol.
Isradipine The serum concentration of Acenocoumarol can be increased when it is combined with Isradipine.
Valproic acid The serum concentration of Acenocoumarol can be increased when it is combined with Valproic acid.
Dihydroergotamine The serum concentration of Acenocoumarol can be increased when it is combined with Dihydroergotamine.
Diltiazem The serum concentration of Acenocoumarol can be increased when it is combined with Diltiazem.
Methylergometrine The serum concentration of Acenocoumarol can be increased when it is combined with Methylergometrine.
Mefloquine The serum concentration of Acenocoumarol can be increased when it is combined with Mefloquine.

Target Protein

Vitamin K epoxide reductase complex subunit 1 VKORC1

Referensi & Sumber

Synthesis reference: Stoll, W. and Litvan, F.; U.S. Patent 2,648,682; August 11,1953; assigned to J.R. Geigy A.G., Switzerland.
Artikel (PubMed)
  • PMID: 15613922
    Cesar JM, Garcia-Avello A, Navarro JL, Herraez MV: Aging and oral anticoagulant therapy using acenocoumarol. Blood Coagul Fibrinolysis. 2004 Oct;15(8):673-6.
  • PMID: 15724697
    Lengyel M: Warfarin or acenocoumarol is better in the anticoagulant treatment of chronic atrial fibrillation?. Orv Hetil. 2004 Dec 26;145(52):2619-21.
  • PMID: 16372822
    Ufer M: Comparative pharmacokinetics of vitamin K antagonists: warfarin, phenprocoumon and acenocoumarol. Clin Pharmacokinet. 2005;44(12):1227-46.
  • PMID: 16611310
    Montes R, Ruiz de Gaona E, Martinez-Gonzalez MA, Alberca I, Hermida J: The c.-1639G > A polymorphism of the VKORC1 gene is a major determinant of the response to acenocoumarol in anticoagulated patients. Br J Haematol. 2006 Apr;133(2):183-7.
  • PMID: 9684795
    Girard P, Nony P, Erhardtsen E, Delair S, Ffrench P, Dechavanne M, Boissel JP: Population pharmacokinetics of recombinant factor VIIa in volunteers anticoagulated with acenocoumarol. Thromb Haemost. 1998 Jul;80(1):109-13.
  • PMID: 18495950
    Danziger J: Vitamin K-dependent proteins, warfarin, and vascular calcification. Clin J Am Soc Nephrol. 2008 Sep;3(5):1504-10. doi: 10.2215/CJN.00770208. Epub 2008 May 21.

Contoh Produk & Brand

Produk: 3 • International brands: 2
Produk
  • Sintrom
    Tablet • 4 mg • Oral • Canada • Approved
  • Sintrom
    Tablet • 1 mg • Oral • Canada • Approved
  • Truemed Group LLC
    Tablet • 4 mg/1 • Oral • US
International Brands
  • Ascumar — Star
  • Mini-sintrom

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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