シロスタゾール 化学特性,用途語,生産方法
外観
白色〜わずかにうすい黄色, 結晶〜粉末
溶解性
メタノール、エタノールに溶けにくく、水にほとんど溶けない。
用途
ホスホジエステラーゼⅢを選 択的に阻害し、血小板凝集抑制作用を示しま す。
用途
ホスホジエステラーゼⅢを選
択的に阻害し、血小板凝集抑制作用を示しま
す。
効能
血管拡張薬, 血小板凝集抑制薬, ホスホジエステラーゼ阻害薬
商品名
プレタール (大塚製薬); プレタール (大塚製薬)
説明
Cilostazol is a platelet aggregation inhibitor with cerebral vasodilating activity, indicated
for use in stroke and myocardial infarction. In patients with cerebral thrombosis, transient
ischemia and cerebral arteriosclerosis, cilostazol significantly inhibits ADP-, collagenand
epinephrine-induced platelet aggregation. Side effects include headache and
tachycardia.
化学的特性
Colourless Needles
使用
A potent phosphodiesterase III A (PDE3A) inhibitor (IC50=0.2uM) and inhibitor of adenosine uptake. Has antimitogeni, antithrombotic, vasodilatory and cardiotonic properties in vivo. Also affects lipid levels in vivo
定義
ChEBI: A lactam that is 3,4-dihydroquinolin-2(1H)-one in which the hydrogen at position 6 is substiuted by a 4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy group.
一般的な説明
Cilostazol is a potent cyclic nucleotide phosphodiesterase inhibitor. It is mainly used as antiplatelet agent.
生物活性
Potent phosphodiesterase III A (PDE3A) inhibitor (IC 50 = 0.2 μ M) and inhibitor of adenosine uptake. Has antimitogenic, antithrombotic, vasodilatory and cardiotonic properties in vivo . Also affects lipid levels in vivo .
作用機序
Cilostazol exhibits greater selectivity than dipyridamole as an inhibitor of
PDE3A. The drug does not affect the other PDEs (PDEs 1, 2, or 4). Cilostazol
reversibly inhibit platelet aggregation induced by a number of stimuli, such as thrombin, ADP,
collagen, or stress from exercise. Additionally, cilostazol inhibits adenosine uptake,
leading to increased activity of adenosine at A1 and A2 receptors.
臨床応用
Cilostazol, a quinolinone derivative, is a potent orally active antiplatelet drug approved for the
treatment of intermittent claudication (a peripheral artery disease resulting from blockage of blood
vessels in the limbs).
代謝
Cilostazol is rapidly absorbed after oral administration, particularly with a high-fat meal, which
greatly increases its bioavailability to approximately 90%. It is extensively metabolized in the liver by
various cytochromes. The most important cytochromes appear to be CYP3A4 and, to lesser extent,
by CYP2C19, with an elimination half-life of approximately 11 to 13 hours. Among the various
metabolites produced (11 metabolites are known), the two major metabolites are
3,4-dehydrocilostazol and 4′-trans-hydroxycliostazol. These two metabolites are
pharmacologically active. Studies indicate that the concomitant administration of cilostazol with
CYP3A inhibitors can greatly increase cilostazol blood concentrations, and a dose reduction may be
required. Similar results are seen when CYP2C19 is inhibited, leading to decreased formation
of 4-trans-hydroxycliostazol and significant increases in cilostazol and 3,4-dehydrocilostazol.
シロスタゾール 上流と下流の製品情報
原材料
準備製品