PRIMPERAN Scored tablet Ref.[115932] Active ingredients: Metoclopramide

Source: Υπουργείο Υγείας (CY)  Revision Year: 2022  Publisher: Sanofi-Aventis groupe, 54, rue La Boetie, F-75008 Paris, France

5.1. Pharmacodynamic properties

STIMULANT OF GASTROINTESTINAL MOTILITY
Code ATC: A03FA01
(A: gastrointestinal system and metabolism)

Metoclopramide – dopamine receptor antagonist (neuroleptic agent), which prevents vomiting by blocking dopaminergic sites.

5.2. Pharmacokinetic properties

Absorption

Metoclopramide is rapidly absorbed from the gastro-intestinal tract. Generally, bioavailability is 80%, but there is inter-individual variability associated with first pass effect of the product in the liver.

Distribution

Metoclopramide is widely distributed in the tissues. The volume of distribution is 2.2 to 3.4 l/kg. It binds little to plasma proteins. It goes through the placenta and in breast milk.

Metabolism

Metoclopramide is little metabolized.

Excretion

Metoclopramide is mainly excreted in the urine in a free or sulfoconjugated form. The elimination half-life is between 5-6 hours. This increases in the event of renal or hepatic insufficiency.

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.

5.3. Preclinical safety data

These data do not indicate the need for any further precautions for use other than those already described above.

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