Pharmacology of Domperidone (Domdone, motilium) ; Pharmacokinetics, Mechanism of Action, Use, Effect скачать в хорошем качестве

Pharmacology of Domperidone (Domdone, motilium) ; Pharmacokinetics, Mechanism of Action, Use, Effect

Domperidone, also known as Domdone, is a dopamine receptor antagonist primarily used to treat gastrointestinal disorders and nausea. Here's an overview of its pharmacology: Mechanism of Action Dopamine Receptor Antagonism: Domperidone blocks dopamine D2 receptors in the chemoreceptor trigger zone (CTZ) located outside the blood-brain barrier. This prevents nausea and vomiting. Prokinetic Effect: By blocking dopamine receptors in the gastrointestinal tract, it enhances gastric motility and accelerates gastric emptying. Pharmacokinetics Absorption: Oral bioavailability is low (13–17%) due to extensive first-pass metabolism. Metabolism: Metabolized in the liver by cytochrome P450 enzymes (CYP3A4). Excretion: Eliminated via feces (66%) and urine (32%), with a half-life of approximately 7–9 hours. Clinical Uses Nausea and Vomiting: Effective in managing nausea caused by chemotherapy, Parkinson's disease, or gastrointestinal disorders. Gastroparesis: Used to treat delayed gastric emptying. Lactation: Off-label use to stimulate breast milk production by increasing prolactin levels. Adverse Effects Common: Dry mouth, abdominal cramps, diarrhea, and headache. Serious: QT prolongation, which can lead to cardiac arrhythmias or sudden cardiac death in rare cases. Hormonal Effects: Elevated prolactin levels may cause breast changes, menstrual irregularities, or galactorrhea. Precautions Avoid use in patients with QT-prolonging conditions or medications. Not recommended for use in individuals with severe hepatic impairment #Domperidone