Cisapride

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Danger

• 유해·위험 문구

  H318：눈에 심한 손상을 일으킴

• 예방조치문구

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

  P310：즉시 의료기관(의사)의 진찰을 받으시오. 삼켰다면 즉시 의료기관(의사)의 도움을 받으시오.

Cisapride MSDS

• Cisapride

Cisapride 화학적 특성, 용도, 생산

• 개요

  Cisapride is a gastroprokinetic useful in the treatment of reflux esophagitis, constipation, and a variety of gastro-intestinal motility disorders. Its novel mechanism of action is thought to involve the enhancement of acetylcholine release in the mysenteric plexus of the gut. It is reportedly devoid of CNS and cardiac side-effects.

• 화학적 성질

  White Solid

• 용도

  Cisapride Monohydrate is a cardioactive drug that causes prolongation of cardiac repolarization in human; selective serotonin 5-HT4 receptor agonist.

• Indications

  Cisapride (Propulsid) is serotonin-4 (5-HT4) receptor agonists that stimulate GI motility. Cisapride appears to act by facilitating the release of acetylcholine from the myenteric plexus. It has no antiadrenergic, antidopaminergic, or cholinergic side effects. Following oral administration, peak plasma levels occur in 1.5 to 2 hours; the drug’s half-life is 10 hours.

• 정의

  ChEBI: The amide resulting from formal condensation of 4-amino-5-chloro-2-methoxybenzoic acid with cis-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-amine. It has been used (as its monohydrate or as its tartrate) for the treatment of gastro-oeso hageal reflux disease and for non-ulcer dyspepsia, but its propensity to cause cardiac arrhythmias resulted in its complete withdrawal from many countries, including the U.K., and restrictions on its use elsewhere.

• 생물학적 활성

  5-HT 4 receptor agonist and gastrokinetic agent. Stimulates intestinal acetylcholine release, possibly via 5-HT 4 receptor-dependent and -independent mechanisms, leading to increased intestinal motility.

• Clinical Use

  Cisapride has been successfully used to treat gastroparesis and mild gastroesophageal reflux disease.

• 부작용

  The most frequent side effect has been diarrhea. A few patients had seizure activity that was reversible after medication was discontinued. Cisapride was pulled from the U. S. market after deaths from drug-associated cardiac arrhythmias, including ventricular tachycardia, ventricular fibrillation, torsades de pointes, and QT prolongation.

• 신진 대사 경로

  Cisapride 14C labeled at the carbonyl carbon and 3H labeled at the fluorophenyl moiety or at the piperidine ring is investigated using some animals. N- Dealkylation at the nitrogen of the piperidine ring, resulting in the main urinary metabolite norcisapride, and aromatic hydroxylation of the fluorinated phenyl ring are the major metabolic pathways in dogs and humans. Norcisapride excretion accounts for 14% of the dose in dogs and 41-45% in humans. Minor metabolic pathways are O-dearylation of the 4- fluorophenyl group and oxidation on the piperidine ring (rat, rabbits and dogs: Lavrijsen et al. (1986)15).

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