Peringatan Keamanan

Excessive bleeding

Argatroban

DB00278

small molecule approved investigational

Deskripsi

Argatroban is a direct, selective thrombin inhibitor. The American College of Cardiologists (ACC) recommend using bivalirudin or argatroban in patients who have had, or at risk for, heparin induced thrombocytopenia (HIT) and are undergoing percutaneous coronary intervention. Argatroban is a non-heparin anticoagulant shown to both normalize platelet count in patients with HIT and prevent the formation of thrombi. Parental anticoagulants must be stopped and a baseline activated partial thromboplastin time must be obtained prior to administering argatroban.

Struktur Molekul 2D

Berat 508.64
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 39 and 51 minutes
Volume Distribusi * 174 mL/kg * 12.18 L [70-kg adult]
Klirens (Clearance) * 5.1 L/kg/hr [infusion doses up to 40 mcg/kg/min]

Absorpsi

Bioavailability is 100% (intravenous).

Metabolisme

Liver via hydroxylation and aromatization of the 3-methyltetrahydroquinoline ring. Age and gender do not substantially affect the pharmacodynamic or pharmacokinetic profile of argatroban.

Rute Eliminasi

Argatroban is excreted primarily in the feces (65%), presumably through biliary secretion; 22% is eliminated via urine.

Interaksi Makanan

3 Data
  • 1. Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.
  • 2. Exercise caution with grapefruit products. Grapefruit inhibits CYP3A4 metabolism, which may increase the serum concentration of argatroban; however, the evidence is conflicting.
  • 3. Exercise caution with St. John's Wort.

Interaksi Obat

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

Target Protein

Prothrombin F2

Referensi & Sumber

Synthesis reference: Tomiya Mano, Jin Shiomura, "Argatroban preparations for ophthalmic use." U.S. Patent US5506241, issued October, 1986.
Artikel (PubMed)
  • PMID: 16148288
    Di Nisio M, Middeldorp S, Buller HR: Direct thrombin inhibitors. N Engl J Med. 2005 Sep 8;353(10):1028-40.

Contoh Produk & Brand

Produk: 27 • International brands: 0
Produk
  • Argatroban
    Solution • 125 mg/125mL • Intravenous • US • Generic • Approved
  • Argatroban
    Injection, solution • 100 mg/1mL • Intravenous • US • Approved
  • Argatroban
    Injection, solution • 100 mg/1mL • Intravenous • US • Approved
  • Argatroban
    Injection, solution • 50 mg/50mL • Intravenous • US • Approved
  • Argatroban
    Injection • 250 mg/2.5mL • Intravenous • US • Approved
  • Argatroban
    Injection • 250 mg/2.5mL • Intravenous • US • Generic • Approved
  • Argatroban
    Injection, solution • 100 mg/1mL • Intravenous • US • Generic • Approved
  • Argatroban
    Injection, solution • 100 mg/1mL • Intravenous • US • Generic • Approved
Menampilkan 8 dari 27 produk.

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