Metoclopramide

Metoclopramide- What is the molecule profile and popular brands?

Metoclopramide is an Antiemetic prescribed for nausea and vomiting. Antiemetics treat motion sickness, chemotherapy-induced nausea and vomiting, and the side effects of general anesthetics and opioid analgesics.

Few medicines act on the chemoreceptor trigger zone-CTZ (in the brain) by preventing the stimulation. The chemoreceptor trigger zone is a vomiting center. Some medications act as prokinetic agents by speeding up the rate at which the stomach empties.

Classification of Antiemetics:

  • 5-HT3 receptor antagonists: Ondansetron, Granisetron, Dolasetron, etc.
  • Dopamine D2-receptor antagonists act in the brain:
    Domperidone, Metoclopramide, Mosapride, etc.
  • Antihistamines or H1- histamine receptor antagonists:
    Diphenhydramine, Promethazine, etc.
  • Benzodiazepines: Midazolam, Lorazepam, etc.
  • Anticholinergics: Scopolamine, Hyoscine, Dicyclomine
    etc.
  • Steroids: Dexamethasone etc.
ParametersDescription
Category of DrugDopamine D2-receptor antagonists
Mechanism of ActionMetoclopramide acts by inhibiting dopamine D2 and serotonin 5-HT3 receptors in the chemoreceptor trigger zone (CTZ), and causes antiemetic effects
Chemical structureMetoclopramide.png
Molecular details
Molecular weight- 299.79 g/mol
Molecular formula- C14H22ClN3O2
IUPAC Name4-amino-5-chloro-N-[2-(diethylamino)ethyl]-2-methoxybenzamide
Indications Metoclopramide is used for
1. Nausea and vomiting in gastrointestinal disorders and treatment with cytotoxics or
radiotherapy
2. Gastro-oesophageal reflux
disease
3. Gastroparesis
4. Premedication and postoperatively
5. Aid to gastrointestinal
intubation
Pharmacokinetic Properties1. Rapidly absorbed in the gastrointestinal tract – 84%
2, Bioavailability of the oral preparation-40.7%
3. A 15mg dose reaches a Cmax of 41.0 ng/mL, with a Tmax of 1.25 h, and an AUC of 367 ng*h/mL.4
4. The volume of distribution – 3.5 L/kg
5. Protein binding- 30%
6. Metabolism- first-pass metabolism (metabolized by cytochrome P450 enzymes in the liver.
Well Known
Pharmaceutical Brands
 PERINORM- IPCA
Available dosage forms1. TABLETS
2. INJECTION
3. SYRUP
POM) Metoclopramide 10mg Tablets | Medical Supermarket
Dose 10 mg 3 times daily
Contraindications 1. Gastrointestinal obstruction
2. Haemorrhage or perforation
3. 3-4 days after gastrointestinal
surgery
4. Convulsive disorders
5. Pheochromocytoma
6. Hypersensitivity
Precautions 1. Elderly, children and young adults
2. Hepatic impairment
3. Renal impairment
4. Pregnancy
5. May mask underlying disorders such as cerebral irritation
6. Gastrointestinal surgery
7. Lactation
8. Interactions
9. Parkinson’s disease
10. Epilepsy
11. Hypertension
12. Cirrhosis
13. Congestive heart failure
Adverse Effects1. Extrapyramidal symptoms
2. Tardive dyskinesias on prolonged use
3. Hyperprolactinaemia
4. Drowsiness
5. Restlessness
6. Hypotension and
hypertension reported
7. Neuroleptic malignant syndrome
8. Pruritus
9. Oedema
10. Cardiac conduction abnormalities following intravenous administration
Pregnancy Category B

References

  • National Forumary
  • drug profile 1, 2, 3

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