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Domperidone - Uses, Mechanism Of Action, Pharmacology, Adverse Effects, And Contraindications
Video transcript :-
Domperidone is a dopamine D2 receptor antagonist that belongs to the classes of prokinetic agents and antiemetics.
It is primarily used to enhance gastrointestinal motility and relieve symptoms of nausea and vomiting.
Major Indications of domperidone include the following.
Nausea and vomiting associated with various conditions, including chemotherapy, surgery, and delayed gastric emptying.
In the treatment of gastroesophageal reflux disease, as an adjunct to proton pump inhibitors in refractory cases.
Gastroparesis, which causes delayed gastric emptying, especially in diabetic individuals.
In functional dyspepsia to improve symptoms of bloating and early satiety.
And to enhance lactation, by increasing prolactin levels.
Domperidone blocks dopamine D2 receptors in following areas to exert its pharmacological effects.
The chemoreceptor trigger zone, located outside the blood-brain barrier, reducing nausea and vomiting.
The gastric antrum and duodenum: This enhances gastrointestinal motility by:
Increasing esophageal peristalsis and sphincter tone.
Promoting gastric emptying.
And reducing pyloric sphincter tone.
Domperidone does not cross the blood-brain barrier significantly, resulting in fewer central nervous system side effects.
Domperidone is commonly administered as an oral tablet or a suspension.
In addition, intravenous preparations and suppositories are also available.
The drug has a poor oral bioavailability due to extensive first-pass metabolism in the liver and intestinal wall.
It is metabolized in the liver primarily by cytochrome P450 enzymes.
Domperidone is mainly excreted in feces via biliary excretion.
A smaller fraction is excreted in urine as metabolites.
And the half-life is approximately 7-9 hours.
Domperidone is generally a well-tolerated drug.
However, it might cause the following adverse effects in certain individuals.
Gastrointestinal effects such as dry mouth, diarrhea, or abdominal cramps.
Endocrine effects like elevated prolactin levels, leading to Galactorrhea, Gynecomastia, and Menstrual irregularities.
And cardiovascular effects such as QT interval prolongation, torsades de pointes, and sudden cardiac death, especially in older patients or with higher doses.
Contraindications for the use of domperidone include the following.
Known QT prolongation.
Congestive heart failure or significant bradycardia.
Concurrent use of drugs that prolong the QT interval, such as ketoconazole and erythromycin.
Severe hepatic impairment, as domperidone is extensively metabolized in the liver.
Prolactin-secreting tumors.
And known hypersensitivity to domperidone.
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