- Molecular NameCisapride
- Synonymcisapride
- Weight465.953
- Drugbank_IDDB00604
- ACS_NO81098-60-4
- Show 2D model
- LogP (experiment)3.802
- LogP (predicted, AB/LogP v2.0)3.67
- pka7.83
- LogD (pH=7, predicted)3.15
- Solubility (experiment)Insoluble
- LogS (predicted, ACD/Labs)(ph=7)-3.54
- LogSw (predicted, AB/LogsW2.0)0.01
- Sw (mg/ml) (predicted, ACD/Labs)0.03
- No.of HBond Donors3
- No.of HBond Acceptors7
- No.of Rotatable Bonds9
- TPSA86.05
- StatusFDA approved
- Administrationtablets, suspension
- PharmacologyA parasympathomimetic and gastroprokinetic agent that acts as a serotonin 5-HT4 receptor agonist.
- Absorption_value100.0
- Absorption (description)Cisapride is readily absorbed after oral administration, and the presence of food enhances absorption.
- Caco_2N/A
- Bioavailability49.0
- Protein binding98.0
- Volume of distribution (VD)2.4 L/kg
- Blood/Plasma Partitioning ratio (D_blood)N/A
- MetabollsmIt undergoes extensive metabolism in the liver and gut wall mainly via the cytochrome P450 isoenzyme CYP3A4. The main metabolic pathways are oxidative N-dealkylation, producing the major metabolite norcisapride, and aromatic hydroxylation to 3-fluoro-4-hydroxycisapride and 4-fluoro-2-hydroxycisapride.
- Half life7~10 h
- ExcretionMore than 90% of a dose is excreted as metabolites in urine and faeces in approximately equal amounts. 4 to 6% of a dose is recovered as the unchanged drug in faeces and 0.2% in urine. A small amount is distributed into breast milk with approx. 0.1% of a dose being detected (milk:serum ratio, 0.045). It is not removed by haemodialysis.
- Urinary ExcretionN/A
- Clerance100 ml/min
- ToxicityRare cases of cardiac arrhythmia, including ventricular tachycardia, ventricular fibrillation, and torsade de pointes, and QT interval prolongation have been reported.
- LD50 (rat)N/A
- LD50 (mouse)N/A