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PubMed · 10069409

Cilostazol.

Abstract

Cilostazol is an antiplatelet agent with vasodilating properties that has been used in the treatment of patients with peripheral ischaemia such as intermittent claudication. The drug inhibits platelet aggregation induced by ADP, collagen and arachidonic acid. Unlike aspirin (acetylsalicylic acid), cilostazol inhibits both primary and secondary aggregation. It also acts as a vascular vasodilator by inhibiting calcium-induced contractions while having no direct effect on contractile proteins. In double-blind randomised trials, patients with intermittent claudication receiving cilostazol showed significant improvements versus placebo in terms of time to initial pain and maximal walking or absolute claudication distance; these findings were confirmed by cilostazol patients' positive responses on subscales measuring physical functioning and quality of life. In a 24-week randomised double-blind trial in patients with intermittent claudication, cilostazol 100mg twice daily produced significant improvements in pain-free and maximum walking distances, compared with pentoxifylline (oxpentifylline) 400mg 3 times daily and placebo. Cilostazol has been well tolerated, with the most common adverse events being headache, diarrhoea, abnormal stools and dizziness.

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BibTeXRIS

E M Sorkin, A Markham. 1999. Cilostazol.. https://doi.org/10.2165/00002512-199914010-00005

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Polymorphic forms of cilostazol.

Two unique conformational polymorphic forms of the compound 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one (cilostazol), C(20)H(27)N(5)O(2), have been discovered and characterized using single-crystal X-ray structural analysis. A third polymorph also exists, but acceptable crystals could not be obtained. Features of both reported polymorphic structures include a chair conformation of the cyclohexyl ring and puckering in the quinolinone ring. The major feature distinguishing the two polymorphic forms is a rotational twisting of the butoxy chain between the tetrazole and quinolinone rings. This difference in conformation influences the intermolecular forces, and hence the packing of the two molecules during crystallization.

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