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Crofelemer (USAN, trade name Fulyzaq) is a botanical drug for the treatment of diarrhea associated with anti-HIV drugs such as nucleoside analog reverse transcriptase inhibitors and protease inhibitors. Other possible uses include diarrhea in children, acute infectious diarrhea, and diarrhea in patients with irritable bowel syndrome.〔 It is a purified oligomeric proanthocyanidin from "dragon's blood", the sap of the South American tree ''Croton lechleri''.〔 Fulyzaq treats the symptoms of disease, but it is not used to treat infectious diarrhea (diarrhea caused by infection of the digestive system by a bacteria, virus or parasite). It was initially developed by Napo Pharmaceuticals, which licensed it to Glenmark Pharmaceuticals in 140 emerging markets and to Salix Pharmaceuticals in the US, EU and some other markets. A Phase III clinical trial for diarrhoea in HIV patients was completed in 2012, and the drug was approved by the US Food and Drug Administration (FDA) on 31 December 2012.〔〔〔 ==Mechanism of action== The drug is taken by mouth and works by voltage-independently blocking two structurally unrelated chloride channels in the gut, namely the cystic fibrosis transmembrane conductance regulator (CFTR) with an ''in vitro'' maximum inhibition of about 60%, and the calcium-activated chloride channel anoctamin 1, with a maximum inhibition of over 90%. This is a hitherto undescribed mechanism of action. As a result of the channel inhibition, fewer chloride ions are excreted into the gut, which also decreases the excretion of sodium ions and water, improving stool consistency and reducing duration of the diarrhea.〔 The mechanism seems to be selective as other channels involved in intestinal fluid secretion, namely sodium and potassium channels, are not affected by crofelemer, nor is cAMP or calcium signalling.〔 The substance is hardly, if at all, absorbed from the gut into the bloodstream, and is consequently excreted with the stool.〔 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「crofelemer」の詳細全文を読む スポンサード リンク
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