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Powder: | Yes |
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Name |
Domperidone |
CAS NO |
57808-66-9 |
ENS NO |
260-968-7 |
MF |
C22H24ClN5O2 |
MW |
425.91 |
Type |
Small Molecule |
MP |
242.5 |
Domperidone is a peripherally selective dopamine D2receptor antagonist developed by Janssen Pharmaceutica that is used as an antiemetic, gastroprokinetic agent, and galactogogue.It may be administered orally or rectally, and is available in the form of tablets,orally disintegrating tablets (based on Zydis technology), suspension, and suppositories.The drug is used to relieve nausea and vomiting; to increase the transit of food through the stomach (by increasinggastrointestinal peristalsis); and to promote lactation (breast milk production) by release of prolactin.
Nausea and vomiting
There is some evidence that domperidone has antiemetic activity.It is recommended in the Canadian Headache Society's guidelines for treatment of nausea associated with acute migraine.
Gastroparesis
Gastroparesis is a medical condition characterised by delayed emptying of the stomach when there is no mechanical gastric outlet obstruction. Its cause is most commonly idiopathic, a diabetic complication or a result of abdominal surgery. The condition causes nausea, vomiting, fullness after eating, early satiety (feeling full before the meal is finished), abdominal pain and bloating.
Domperidone may be useful in diabetic and idiopathic gastroparesis.
However, increased rate of gastric emptying induced by drugs like domperidone does not always correlate (equate) well with relief of symptoms.
Parkinson's disease
Parkinson's disease is a chronic neurological condition where a decrease in dopamine in the brain leads to rigidity (stiffness of movement), tremor and other symptoms and signs. Poor gastrointestinal function, nausea and vomiting is a major problem for people with Parkinson's disease because most medications used to treat Parkinson's disease are given by mouth. These medications, such as levodopa can cause nausea as a side effect. Furthermore, anti-nausea drugs, such as metoclopramide, which do cross the blood-brain barrier may worsen theextra-pyramidal symptoms of Parkinson's disease.
Domperidone can be used to relieve gastrointestinal symptoms in Parkinson's disease, because, even though it blocks dopamine receptors (which would be expected to worsen Parkinson's disease), it does not cross theblood-brain barrier (the barrier between the blood circulation of the brain and the rest of the body).In addition to this, domperidone may enhance the bioavailability (effect) of levodopa (one of the main treatments in Parkinson's disease).
Functional dyspepsia
Domperidone may be used in functional dyspepsia in both adults and children.
There is some evidence that domperidone has antiemetic activity. Domperidone is used, together with metoclopramide, cyclizine, and 5HT3 receptor antagonists (such as granisetron) in the treatment of nausea and vomiting.
It can be used in patients with Parkinson's disease because, unlike metoclopramide, domperidone does not cross the blood-brain barrier.
Domperidone has also been found effective in the treatment of gastroparesis, a stomach motility condition, and for paediatric gastroesophageal reflux (infant vomiting).
In Canada, the drug is indicated "for the symptomatic management of upper gastrointestinal motility disorders associated with chronic and subacute gastritis and diabetic gastroparesis." The drug may also be used "to prevent gastrointestinal symptoms associated with the use of dopamine agonist antiparkinsonian agents".
Items |
Requirements |
Results |
Appearance |
White to off white powder |
White powder |
Solubility |
Practically insoluble in water, soluble in dimethylformamide, |
Confirms |
slightly soluble in ethanol(96%) and in methanol |
||
Identification |
A. M.P. 244~248ºC |
244.5~245.5ºC |
B. IR should comply |
Confirms |
|
C. TLC should comply |
Confirms |
|
D. It gives the reaction of non-nitrogen substituted barbiturates. |
Confirms |
|
Clarity of solution |
The solution is clear and not more intensely colored than |
Confirms |
reference solution Y6 |
||
Related substance |
Total impurities≤0.5% |
≤0.29% |
Individual impurity≤0.25% |
≤0.18% |
|
Loss on drying |
≤0.5% |
0.07% |
Sulphated ash |
≤0.1% |
≤0.05% |
Heavy metal |
≤20ppm |
<20ppm |
Assay |
99.0%~101.0% |
99.49% |
Conclusion: This product conforms to the EP7.0 detection. |