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外観
白色～わずかにうすい灰色、結晶～結晶性粉末
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溶解性
エタノール及びアセトンに溶け、水にほとんど溶けない。
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用途
合成トロンビン剤です。アン
チトロンビンⅢ非依存的にトロンビンを阻害
し、血液凝固抑制作用を示します。
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使用上の注意
不活性ガス封入
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説明
Argatroban is a new synthetic antithrombotic agent useful in maintenance
anticoagulation them
ischemic stroke and disseminated intravascular coagulation. In patients on hemodialysis, argatroban is su enor to heparin,
generating a more stable antithrombin effect. Other potential uses include progressing ischemic stroke and disseminated intravascular coagulation.
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化学的特性
White to Off-White Crystalline Solid
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薬物動態学
Argatroban is administered subcutaneously because of the low lipophilicity of the drug. The drug is
bound to plasma protein and is metabolized via CYP3A4/5 to the aromatized metabolite and the two
hydroxylated metabolites. The M-1 metabolite retains 20 to 30% of the antithrombotic
activity. Coadministration of argatroban with inhibitors of CYP3A4 does not appear to produce
clinically significant effects. Argatroban is eliminated via biliary secretion into the feces.
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臨床応用
Argatroban has been approved for the prophylaxis and treatment of thrombosis in patients with HIT
(79). Argatroban is a peptidomimetic that binds selectively to the catalytic site of thrombin as a
univalent competitive DTI. Argatroban is available as a mixture of 21-R and 21-S
diastereomers (64:36), with the S-isomer approximately twice as potent as the R-isomer. The
drug is a reversible inhibitor of both free thrombin as well as clot-bound thrombin.
