Giachetti A
A Menarini Industrie Farmaceutiche Riunite S.r.l., Firenze, Italy.
Ital J Gastroenterol. 1991 Nov;23(8 Suppl 1):56-9.
Otilonium bromide (OB) is a quaternary ammonium compound characterized by a long aliphatic chain. Its chemical properties are responsible for both a poor penetration in CNS and a prolonged binding to cell membranes. OB is a spasmolytic agent which acts by modifying Ca++ fluxes from extra and intracellular sites. It has been documented that iv administration (10 mg/kg) of OB causes a marked reduction of colonic motility lasting from 2 to 3 hours, whereas an inhibition of upper GI motor activity is present only at higher dosages. In conclusion, OB seems to exert its activity mainly on distal GI tract, and its spasmolytic effect may be due to its ability to inhibit Ca++ fluxes and to a direct action of the drug on the contractile proteins of the smooth muscle.
奥替溴铵（OB）是一种具有长脂肪链的季铵化合物。其化学性质导致其在中枢神经系统中的渗透性较差，且与细胞膜的结合时间延长。OB是一种解痉剂，通过改变细胞外和细胞内位点的钙离子通量发挥作用。据记载，静脉注射（10mg/kg）OB可使结肠运动明显降低，持续2至3小时，而只有在较高剂量时才会出现对上消化道运动活性的抑制。总之，OB似乎主要在胃肠道远端发挥其活性，其解痉作用可能归因于其抑制钙离子通量的能力以及药物对平滑肌收缩蛋白的直接作用。
