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Metoclopramide (Reglan)

Provides prokinetic and antiemetic activities and is useful in gastroparesis and gastroesophageal reflux disease.

Side effects include fatigue, extrapyramidal problems such as oculogyric crisis, opisthotonos, dystonia, dyskinesias, and akathisia.

Prolonged use can cause movement disorders.

Trade name Reglan

Routes: Oral, intravenous, intramuscular

Bioavailability-80% plus, with hepatic metabolism 70-85%, renal excretion 70-85%, 2% fecal excretion, and half- life 5-6 hours.

An antiemetic and gastroprokinetic agent.

A dopamine-2(D2) receptor antagonist it is now available as a nasal spray formulation for relief of symptoms of acute and recurrent diabetic gastroparesis.

Commonly used to treat nausea and vomiting, anf facilitates gastric emptying in people with gastroparesis,

Frequently used as a treatment for the gastric stasis associated with migraine headaches, to treat chemotherapy associated nausea and vomiting, and postoperative induced nausea.

Can treat nausea and vomiting associated with uremia, radiation, malignancy, labor, infection, migraines, and emetogenic drugs.

Increases peristalsis of the jejunum and duodenum.

Increases tone and amplitude of gastric contractions.

Relaxes the pyloric sphincter and duodenal bulb.

Progastrokinetic effects aid in gastrointestinal radiographic studies by accelerating transit through the gastrointestinal system.

Metoclopramide is a dopamine antagonist that stimulates acetylcholine release in the myenteric plexus, and also acts centrally on chemoreceptor triggers in the floor of the fourth ventricle, providing antiemetic activity.

Commonly used in gastroesophageal reflux disease (GERD).

Inhibits the action of dopamine, and sometimes has been used to stimulate lactation.

Can also help treat migraine headaches.

Common adverse reactions include: restlessness, drowsiness, dizziness, fatigue, and focal dystonia.

Infrequent adverse reactions include: hypertension, hypotension, hyperprolactinaemia with galactorrhea, constipation, depression, headache, and extrapyramidal effects such as oculogyric crisis.

Rare adverse reactions include agranulocytosis, supraventricular tachycardia, hyperaldosteronism, neuroleptic malignant syndrome, akathisia and tardive dyskinesia.

May be the most common cause of drug-induced movement disorders.

The risk of extrapyramidal effects is increased in people under 20 years of age.

Tardive dyskinesia may be persistent and irreversible.

Majority of cases of tardive dyskinesia occur in people who have used metoclopramide for more than three months, and therefore the drug should be used for short term treatment, preferably less than 12 weeks.

The antiemetic action of metoclopramide is due to its antagonist activity at D2 receptors in the chemoreceptor trigger zone (CTZ) in the central nervous system.

At higher doses, 5-HT3 antagonist activity may also contribute to its antiemetic effect.

The gastroprokinetic activity mediated by muscarinic activity, D2 receptor antagonist activity and 5-HT4 receptor agonist activity.

The gastroprokinetic effect imay contribute to the antiemetic effect.

Increases the tone of the lower esophageal sphincter.

Contraindicated in pheochromocytoma, and should be used with caution in Parkinson’s disease since, as a dopamine antagonist, it may worsen symptoms.

It may exacerbate depression.

Contraindicated with a suspected bowel obstruction, and use not recommended in patients taking antipsychotic drugs.

Safe to use in pregnancy.

Not associated with increased risk of major congenital malformations when used in pregnancy.

 

 

 

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