Domperidone Powder for Antiemetic CAS 57808-66-9

Superiority:

English name: Domperidone

CAS number: 57808-66-9

Molecular formula: C22H24ClN5O2

Molecular weight: 425.91

EINECS Number: 260-968-7

Melting point: 240-244°C

Density: 1.2904 (roughestimate)

Refractive index: 1.5400 (estimate)

Storage condition: Store at RT

Solubility: DMSO:>10mg/mL

Form: solid

Acidity coefficient: (pKa)pKa7.90(Uncertain)

Color: white

Water solubility: Slightly soluble in water.

Domperidone is a commonly used gastric motility drug and antiemetic drug. We are more familiar with its name called morphine, and its other aliases include propperidone, miperidone, chlorperidone, Weideling, Ludolin, duperone, piperimidone, propanediphenone, etc. Appearance is white to slightly yellow powder, bitter taste, almost insoluble in water, slightly soluble in ethanol, easily soluble in lactic acid, soluble in Citric acid. This product is a strong peripheral dopamine receptor antagonist. Domperidone can block the DA1 and DA2 receptors before and after the synapse, and antagonize the inhibitory effect of dopamine on the post-synaptic cholinergic neurons of the intestinal muscular plexus. Stomach contractions. It can promote the peristalsis and tension of the upper gastrointestinal tract to return to normal, promote gastric emptying, increase the movement of the gastric antrum and duodenum, coordinate the contraction of the pylorus, and also enhance the esophageal peristalsis and the tension of the lower esophageal sphincter. Because of its poor permeability to the blood-cerebrospinal fluid barrier, it has almost no antagonistic effect on dopamine receptors in the brain, so the side effects of the mental and central nervous system can be excluded. It is rapidly absorbed after oral administration, and the plasma concentration reaches a peak within 15 to 30 minutes. In addition to the central nervous system, it is widely distributed in other parts of the body. Oral bioavailability is low due to "first pass" hepatic and intestinal metabolism. The half-life of this product is 7h, about 30% is excreted in urine 24h after oral administration, and about 60% is excreted in feces within 4 days. Indication 1, dyspepsia symptoms caused by delayed gastric emptying, gastroesophageal reflux, chronic gastritis, esophagitis, including nausea, vomiting, belching, epigastric distention, abdominal pain, abdominal distension, and oral and Stomach burning. 2. Parkinson's disease and nausea and vomiting caused by various reasons, such as functional, infectious, dietary, radiation therapy or drug therapy, and dopamine receptor agonist (such as levodopa, bromide) therapy, etc. 3. It is suitable for nausea and vomiting caused by migraine, dysmenorrhea, craniocerebral trauma and intracranial lesions, radiation therapy, levodopa, non-steroidal anti-inflammatory drugs, etc. 4. It is also effective for nausea and vomiting caused by various organic or functional gastrointestinal disorders in the elderly. 5. Domperidone is ineffective for vomiting after surgery or due to anesthesia and chemotherapy.

1. A potent peripheral dopamine receptor antagonist, has anti-emesis and gastric kinetic effects, can affect gastrointestinal motility, normalize peristalsis and tension in the upper gastrointestinal tract, promote gastric emptying, and enhance gastric antrum and duodenum Intestinal movement, coordinated contraction of the pylorus. For the treatment of dyspepsia, and functional, organic, infectious, dietary, radiation therapy or drug therapy caused by nausea and vomiting. Since it has little inhibitory effect on dopamine receptors in the brain, it has no psychiatric and neurological side effects. It can also be used for nausea caused by taking dopamine agonists to treat Parkinson's disease.

2. For anticholinergic antispasmodics

3. Domperidone is a benzimidazole compound, which has strong gastric motility and antiemetic effects. It can strengthen the tension of the lower esophageal sphincter, prevent gastroesophageal reflux, enhance gastric peristalsis, promote gastric emptying, and coordinate the stomach and duodenum. Intestinal movement, inhibit nausea, vomiting, and effectively prevent bile reflux without affecting gastric secretion. This product is a peripheral dopamine receptor antagonist, which directly blocks the dopamine receptors in the gastrointestinal tract and exhibits a gastric motility effect. It can enhance the peristalsis of the esophagus and the tension of the lower esophageal sphincter. Due to its poor penetration of the blood-brain barrier and almost no antagonism to dopamine receptors in the brain, side effects of mental and central nervous systems can be excluded.