Single-dose pharmacokinetics of metoclopramide

Ross-Lee L.M., Eadie M.J., Hooper W.D. and Bochner F. (1981) Single-dose pharmacokinetics of metoclopramide. European Journal of Clinical Pharmacology, 20 6: 465-471. doi:10.1007/BF00542101

Author Ross-Lee L.M.
Eadie M.J.
Hooper W.D.
Bochner F.
Title Single-dose pharmacokinetics of metoclopramide
Journal name European Journal of Clinical Pharmacology   Check publisher's open access policy
ISSN 0031-6970
Publication date 1981-01-01
Sub-type Article (original research)
DOI 10.1007/BF00542101
Open Access Status Not yet assessed
Volume 20
Issue 6
Start page 465
End page 471
Total pages 7
Publisher Springer-Verlag
Subject 3000 Pharmacology, Toxicology and Pharmaceutics
2736 Pharmacology (medical)
Abstract The time courses of plasma metoclopramide concentrations were followed in six subjects after oral and intravenous single dose administration. Plasma concentration-time data following i.v. administration in each subject were found to fit a two compartment model with a mean terminal half-life of 4.55 h±0.80 h and a mean distribution half-time of 0.35 h±0.09 h. Volumes of distribution were high (3.43±1.181 · kg-1), and clearances (0.53±0.191 · kg-1h-1) approached liver plasma flow. This suggests that metoclopramide occurs at higher concentrations in tissues than in plasma, and that its clearance is probably limited by liver blood flow rather than liver metabolic capacity. The post-absorption decline in metoclopramide plasma levels after oral administration was also biexponential in each subject. The terminal half-life was 5.17 h±0.98 h. Mean volume of distribution and mean clearance were similar to intravenous values (after adjustment for bioavailability). Oral absorption was rapid with peak plasma concentrations being reached at a mean time of 0.93 h. A mean bioavailability of 0.77 was calculated for the six subjects, and it was postulated that this incomplete availability is due to a first-pass effect. The inter-individual variation in the degree of 'first-pass' was considerable (0.47-1.14).
Keyword bioavailability
first-pass effect
Q-Index Code C1
Q-Index Status Provisional Code
Institutional Status Unknown

Document type: Journal Article
Sub-type: Article (original research)
Collection: Scopus Import - Archived
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