Metoclopramide

Biological Activity

Metoclopramide appears to be a promising candidate for the treatment of patients with intractable hiccups, with mild adverse events. Metoclopramide nasal spray offers better symptom control than metoclopramide oral tablet in diabetic patients with symptoms of gastroparesis. Metoclopramide increases peristalsis of the jejunum and duodenum, increases tone and amplitude of gastric contractions, and relaxes the pyloric sphincter and duodenal bulb, while simultaneously increasing lower esophageal sphincter tone.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information

References

Metoclopramide for patients with intractable hiccups: A multi-center, randomized, controlled pilot study.
Wang T, et al. Intern Med J. 2014 Jul 29. PMID: 25069531.

Metoclopramide nasal spray is effective in symptoms of gastroparesis in diabetics compared to conventional oral tablet.
Parkman HP, et al. Neurogastroenterol Motil. 2014 Apr;26(4):521-8. PMID: 24372829.