| Customization: | Available |
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| CAS No.: | 57808-66-9 |
| Formula: | C22h24cln5o2 |
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| Product name | Domperidone |
| Cas number | 57808-66-9 |
| Appearance | White powder |
| MF | C22H24ClN5O2 |
| Density | 1.341 |
Pharmacological effects of propiperidone
Propiperone, a derivative of benzimidazole, is a peripheral dopamine receptor antagonist, which can directly block the dopamine D2 receptor in the gastrointestinal tract and promote gastrointestinal motility. Propiperidone can promote peristalsis of upper gastrointestinal tract, normalize its tension, promote gastric emptie, increase the movement of gastric antrum and duodenum, coordinate the contraction of pylorus, inhibit nausea and vomiting, and effectively prevent bile reflux. It can also enhance esophageal peristalsis and lower esophageal sphincter tension to prevent gastro-esophageal reflux. But it has little effect on the colon. Due to the poor permeability of propiperone to the blood-cerebrospinal fluid barrier, it has almost no antagonistic effect on dopamine receptors in the brain, so it can exclude adverse reactions in the mental and central nervous system, which is better than metoclopramide. Propiperidone did not affect gastric secretion. In addition, propiperidone can increase serum prolactin levels, thereby promoting postpartum lactation, but not in patients with prolactin secreting tumors.
Pharmacokinetics of propiperidone
Prophenolone may be administered orally, intramuscularly, intravenously, or rectum. It was absorbed rapidly after oral, intramuscular or rectal administration, and the peak time was 15-30min, 15-30min and 1h, respectively. The peak concentration of 10mg intravenously or orally was 40ng/ml and 23ng/ml, the peak concentration of 60mg intravenously was 20ng/ml, and the peak concentration of 10mg intravenously was 1200ng/ml. Due to the "first pass effect" of liver metabolism and intestinal wall metabolism, the oral bioavailability of propiperidone was low, and the oral bioavailability of propiperidone in fasting patients was only 14%. The bioavailability of piperidol increased linearly in the dose range of 10 ~ 60mg, and the bioavailability also increased significantly in the dose range of 90min after meals, but the time to reach the peak was delayed. The bioavailability of propioperidone given rectum was similar to that given orally at the same dose, while the bioavailability of intramuscular injection was 90%. The protein binding rate of propiperidone was 92% ~ 93%. After intravenous injection of 10mg, the apparent volume of distribution was 5.71L/kg. In addition to the central nervous system, propiperidone is widely distributed in other parts of the body. The concentration of drug was the highest in gastrointestinal area, followed by plasma, and almost none in brain. A small part can be excreted into the milk, and its drug concentration is only 1/4 of the serum concentration. Almost all of propiperidone is metabolized in the liver, and the main metabolites are hydroxyl compounds, 2, 3-dihydro-2-oxo-1H-benzimidazole-propanoic and 5-chloro-4-piperidinyl-1. 3-adihydrobenzimidazol-2-one. Propiperidone has an oral half-life of 7 to 8h and is excreted in feces and urine mainly in the form of inactive metabolites, with an overall clearance of 700ml per minute. Within 24h, 30% of the oral dose was excreted by urine, and the original drug accounted for only 0.4%. About 66% of the dose is excreted in the stool within 4 days, of which 10% is the original drug. Multiple doses have no cumulative effect.
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