Metoperan Mechanism of Action

Pharmacology: Pharmacodynamics: The action of metoclopramide is closely associated with parasympathetic nervous control of the upper gastrointestinal tract, where it has the effect of encouraging normal peristaltic action. This provides for a fundamental approach to the control of those conditions where disturbed gastrointestinal motility is a common underlying factor. Metoclopramide stimulates activity of the upper gastrointestinal tract and restores normal coordination and tone. Gastric emptying is accelerated and the resting tone of the gastroesophageal sphincter is increased. Metoclopramide is a dopamine-receptor antagonist with a direct anti-emetic effect on the medullary chemoreceptor trigger zone.
Pharmacokinetics: Absorption: Metoclopramide is rapidly absorbed from the gastrointestinal tract and undergoes variable first-pass metabolism in the liver.
Biotransformation and Elimination: Metoclopramide is metabolised in the liver and the predominant route of elimination of metoclopramide and its metabolites is via the kidney. It crosses the placenta and is excreted in breast milk. The elimination half-life is about 6 hours.
Renal impairment: The clearance of metoclopramide is reduced by up to 70% in patients with severe renal impairment, while the plasma elimination half-life is increased (approximately 10 hours for a creatinine clearance of 10-50 mL/minute and 15 hours for a creatinine clearance <10 mL/minute).
Hepatic impairment: In patients with cirrhosis of the liver, accumulation of metoclopramide has been observed, associated with a 50% reduction in plasma clearance.