Peringatan Keamanan

Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.

Bivalirudin

DB00006

small molecule approved investigational

Deskripsi

Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure.

Struktur Molekul 2D

Berat 2180.2853
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) * Normal renal function: 25 min (in normal conditions) * Creatinine clearance 10-29mL/min: 57min * Dialysis-dependant patients: 3.5h
Volume Distribusi 0.2L/kg
Klirens (Clearance) * 3.4 mL/min/kg [Normal renal function] * 3.4 mL/min/kg [mild renal function] * 2.7 mL/min/kg [moderate renal function] * 2.8 mL/min/kg [severe renal function] * 1 mL/min/kg [Dialysis-dependent patients]

Absorpsi

Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours.

Metabolisme

80% proteolytic cleavage

Rute Eliminasi

Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage.

Interaksi Makanan

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

Interaksi Obat

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

Target Protein

Prothrombin F2

Referensi & Sumber

Synthesis reference: Avi Tovi, Chaim Eidelman, Shimon Shushan, Alon Hagi, Alexander Ivchenko, Gabriel-Marcus Butilca, Leah Bar-Oz, Tehila Gadi, Gil Zaovi, "Process for production of Bivalirudin." U.S. Patent US20070093423, issued April 26, 2007.
Artikel (PubMed)
  • PMID: 16466327
    Seybert AL, Coons JC, Zerumsky K: Treatment of heparin-induced thrombocytopenia: is there a role for bivalirudin? Pharmacotherapy. 2006 Feb;26(2):229-41.
  • PMID: 17381384
    Dager WE, Dougherty JA, Nguyen PH, Militello MA, Smythe MA: Heparin-induced thrombocytopenia: treatment options and special considerations. Pharmacotherapy. 2007 Apr;27(4):564-87.
  • PMID: 16553503
    Dang CH, Durkalski VL, Nappi JM: Evaluation of treatment with direct thrombin inhibitors in patients with heparin-induced thrombocytopenia. Pharmacotherapy. 2006 Apr;26(4):461-8.
  • PMID: 11156732
    Robson R: The use of bivalirudin in patients with renal impairment. J Invasive Cardiol. 2000 Dec;12 Suppl F:33F-6.
  • PMID: 21108549
    Van De Car DA, Rao SV, Ohman EM: Bivalirudin: a review of the pharmacology and clinical application. Expert Rev Cardiovasc Ther. 2010 Dec;8(12):1673-81. doi: 10.1586/erc.10.158.
  • PMID: 16614733
    Shammas NW: Bivalirudin: pharmacology and clinical applications. Cardiovasc Drug Rev. 2005 Winter;23(4):345-60.
  • PMID: 12851152
    Gleason TG, Chengelis CP, Jackson CB, Lindstrom P: A 24-hour continuous infusion study of bivalirudin in the rat. Int J Toxicol. 2003 May-Jun;22(3):195-206.

Contoh Produk & Brand

Produk: 35 • International brands: 2
Produk
  • Angiomax
    Injection, powder, lyophilized, for solution • 250 mg/1 • Intravenous • US • Approved
  • Angiomax
    Injection, powder, lyophilized, for solution • 250 mg/1 • Intravenous • US • Approved
  • Angiomax
    Injection • 250 mg/1 • Intravenous • US • Approved
  • Angiomax
    Powder, for solution • 250 mg / vial • Intravenous • Canada • Approved
  • Angiomax RTU
    Injection, solution • 250 mg/1 • Intravenous • US • Approved
  • Angiox
    - • 250 mg • Intravenous • EU
  • Bivalirudin
    Injection, powder, lyophilized, for solution • 250 mg/5mL • Intravenous • US • Generic • Approved
  • Bivalirudin
    Injection • 250 mg/1 • Intravenous • US • Generic • Approved
Menampilkan 8 dari 35 produk.
International Brands
  • Angiox
  • Hirulog

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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