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Argatroban is an anticoagulant that is a small molecule direct thrombin inhibitor.^[1] In 2000, argatroban was licensed by the Food and Drug Administration (FDA) for prophylaxis or treatment of thrombosis in patients with heparin-induced thrombocytopenia (HIT). In 2002, it was approved for use during percutaneous coronary interventions in patients who have HIT or are at risk for developing it. In 2012, it was approved by the MHRA in the UK for anticoagulation in patients with heparin-induced thrombocytopenia Type II (HIT) who require parenteral antithrombotic therapy.^[2]

Argatroban is given intravenously and drug plasma concentrations reach steady state in 1–3 hours.^[3] Argatroban is metabolized in the liver and has a half-life of about 50 minutes. It is monitored by PTT. Because of its hepatic metabolism, it may be used in patients with renal dysfunction. (This is in contrast to lepirudin, a direct thrombin inhibitor that is primarily renally cleared).

Transitioning to warfarin in individuals with heparin induced thrombocytopenia

Argatroban is used as an anticoagulant in individuals with thrombosis and heparin induced thrombocytopenia. Often these individuals require long term anticoagulation. If warfarin is chosen as the long term anticoagulant, this poses particular challenges due to the falsely elevated prothrombin time and INR caused by argatroban. The combination of argatroban and warfarin may raise the INR to greater than 5.0 without a significant increased risk of bleeding complications.^[4] One solution to this problem is to measure the chromogenic factor X level. A level < 40-45% typically indicates that the INR will be therapeutic (2-3) when the argatroban is discontinued.

References

^ Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288
^ http://www.pharmatimes.com/Article/12-07-03/UK_launch_for_Mitsubishi_s_blood_thinner_Exembol.aspx
^ Dhillon S. Argatroban: A Review of its Use in the Management of Heparin-Induced Thrombocytopenia. Am J Cardiovasc Drugs 2009; 9 (4): 261-82. Link text
^ Hursting MJ, Lewis BE, Macfarlane DE (2005). "Transitioning from argatroban to warfarin therapy in patients with heparin-induced thrombocytopenia". Clin Appl Thromb Hemost. 11 (3): 279–87. doi:10.1177/107602960501100306. PMID 16015413.

External links

GlaxoSmithKline's website on argatroban

UpToDate Contents

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1. ヘパリン起因性血小板減少症のマネージメント management of heparin induced thrombocytopenia
2. 直接作用型経口抗凝固薬と直接非経口トロンビン阻害薬：用量および副作用 direct oral anticoagulants and parenteral direct thrombin inhibitors dosing and adverse effects
3. ST上昇型心筋梗塞における抗凝固療法 anticoagulant therapy in acute st elevation myocardial infarction
4. 持続的腎代替療法中の抗凝固療法 anticoagulation for continuous renal replacement therapy
5. 静脈血栓塞栓症：抗凝固療法の開始（開始後10日間） venous thromboembolism initiation of anticoagulation first 10 days

English Journal

Development of a stent capable of the controlled release of basic fibroblast growth factor and argatroban to treat cerebral aneurysms: In vitro experiment and evaluation in a rabbit aneurysm model.

Arai D1,2, Ishii A1, Ikeda H1, Abekura Y1, Nishi H1, Miyamoto S1, Tabata Y2.
Journal of biomedical materials research. Part B, Applied biomaterials.J Biomed Mater Res B Appl Biomater.2019 Jan 17. doi: 10.1002/jbm.b.34314. [Epub ahead of print]
PMID 30653829

[Extracorporeal Membrane Oxygenation in Thoracic Surgery: the Anesthesiologist's Perspective].

Rehers S1, Beiderlinden M2, Ziegeler S1.
Zentralblatt fur Chirurgie.Zentralbl Chir.2019 Jan 8. doi: 10.1055/a-0774-8151. [Epub ahead of print]
PMID 30620971

Attenuation of type-1 diabetes-induced cardiovascular dysfunctions by direct thrombin inhibitor in rats: a mechanistic study.

Bulani Y1, Srinivasan K1, Sharma SS2.
Molecular and cellular biochemistry.Mol Cell Biochem.2019 Jan;451(1-2):69-78. doi: 10.1007/s11010-018-3394-9. Epub 2018 Jul 3.
PMID 29971544

Japanese Journal

肝動注用カテーテル留置術後に肺塞栓を発症したヘパリン起因性血小板減少症の1例

古田陽輝,工藤康一,多田修治,杉原一明,泉和寛,門野義弘,上川健太郎,近澤秀人,今村治男
日本消化器病學會雜誌 = The Japanese journal of gastro-enterology 109(6), 944-951, 2012-06-05
症例は68歳の女性．進行肝細胞癌に対して肝動注化学療法開始後，急性肺塞栓を発症した．血小板数の著明な低下を認め，動注時の使用ヘパリンによるヘパリン起因性血小板減少症を疑った．経過中，抗血小板第4因子・ヘパリン複合体抗体陽性が判明し，確定診断に至った．治療はヘパリン投与中止と，アルガトロバンによる抗血栓療法を施行した．さらに留置したヘパリン化親水性カテーテルの抜去を行い，血小板数の改善を認めた．
NAID 10030651431

抗体陰性化を確認後にもかかわらず,ヘパリン再投与によりヘパリン起因性血小板減少症(heparin-induced thrombocytopenia : HIT)を再発した1例

田中章仁,伊藤祐一,杉山弘高
日本透析医学会雑誌 45(6), 483-486, 2012-06
NAID 40019374456

Related Pictures

Argatroban Intravenous : Uses, Side Effects, Interactions, Pictures, Warnings & Dosing 100 mg/mL Allopathic Argatroban Injection, Intravenous, 100 mg/mL, | ID: 11155667188 Argatroban In Sodium Chloride (Iso-Osmotic) Intravenous : Uses, Side Effects West Ward Pharmaceuticals

★リンクテーブル★

リンク元

「アルガトロバン」

Argatroban
Clinical data
Trade names	Argatroban
AHFS/Drugs.com	Monograph
Routes of; administration	intravenous
ATC code	B01AE03 (WHO);
Pharmacokinetic data
Bioavailability	100% (intravenous)
Protein binding	54%
Metabolism	hepatic
Biological half-life	39 and 51 minutes
Identifiers
	IUPAC name (2R,4R)-1-[(2S)-5-(diaminomethylideneamino)-2-; [[(3R)-3-methyl-1,2,3,4-tetrahydroquinolin-8-yl]; sulfonylamino]pentanoyl]-4-methyl-piperidine-2-; carboxylic acid;
CAS Number	74863-84-6 ;
PubChem CID	440542;
DrugBank	DB00278 ;
ChemSpider	389444 ;
UNII	OCY3U280Y3;
KEGG	C04931 ;
ChEMBL	CHEMBL1166 ;
ECHA InfoCard	100.166.378
Chemical and physical data
Formula	C23H36N6O5S
Molar mass	508.635 g/mol
3D model (JSmol)	Interactive image;
	SMILES O=C(O)[C@@H]3N(C(=O)C(NS(=O)(=O)c1cccc2c1NCC(C2)C)CCC/N=C(\N)N)CC[C@@H](C)C3 ;
	InChI InChI=1S/C23H36N6O5S/c1-14-8-10-29(18(12-14)22(31)32)21(30)17(6-4-9-26-23(24)25)28-35(33,34)19-7-3-5-16-11-15(2)13-27-20(16)19/h3,5,7,14-15,17-18,27-28H,4,6,8-13H2,1-2H3,(H,31,32)(H4,24,25,26)/t14-,15?,17+,18-/m1/s1 ; Key:KXNPVXPOPUZYGB-IOVMHBDKSA-N ;
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英: argatroban
商: アルガロン、ガルトバン、スロンノン、スロンノンＨＩ、ノバスタン、ノバスタンHI
関: その他の循環器官用薬

抗トロンビン薬。トロンビン(第IIa因子)の活性部位に結合して凝固系カスケードの出口？を押さえる。

アテローム血栓性脳梗塞やラクナ梗塞の急性期脳梗塞の際に用いられる。
出血性脳梗塞のリスクが上昇するとされている。　→　脳塞栓症に対して用いない限りこの確率は低いとされている

[1] Di Nisio M, Middeldorp S, Buller HR. Direct thrombin inhibitors. N Engl J Med 2005;353:1028-40. PMID 16148288

[2] ttp://www.pharmatimes.com/Article/12-07-03/UK_launch_for_Mitsubishi_s_blood_thinner_Exembol.aspx

[test-3] Dhillon S. Argatroban: A Review of its Use in the Management of Heparin-Induced Thrombocytopenia. Am J Cardiovasc Drugs 2009; 9 (4): 261-82. Link text

[refname1-4] Hursting MJ, Lewis BE, Macfarlane DE (2005). "Transitioning from argatroban to warfarin therapy in patients with heparin-induced thrombocytopenia". Clin Appl Thromb Hemost. 11 (3): 279–87. doi:10.1177/107602960501100306. PMID 16015413.

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argatroban