Skip to main content
PMC home page
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1978 Nov;6(5):401–407. doi: 10.1111/j.1365-2125.1978.tb04604.x

Pharmacokinetic and concentration-effect studies with intravenous metoclopramide.

D N Bateman, C Kahn, K Mashiter, D S Davies
PMCID: PMC1429552  PMID: 728283

Abstract

1 Pharmacokinetic and concentration-effect studies have been carried out following intravenous injection of 10 mg metoclopramide hydrochloride to seven normal male volunteers. 2 It is proposed that a two-compartment model adequately describes the disposition of the drug which is rapidly distributed (T1/2alpha = 4.9 +/- 1.1 min) and eliminated (T1/2beta = 165.7 +/- 20.2 min). Total body plasma clearance of the drug is high (10.9 +/- 1.5 ml min-1 kg-1) and approximates to liver plasma flow. 3 Metoclopramide i.v. increases gastric emptying as measured by an ethanol absorption test (P less than 0.005). The duration of this effect is at least 3 h. 4 Ethanol given after i.v. metoclopramide administration produces significant sedation during the first hour and at 3 h (P less than 0.001). 5 The effect of metoclopramide on gastric emptying, and the degree of sedation induced by ethanol would appear to be related to plasma metoclopramide concentration. 6 Metoclopramide increases serum prolactin to 59 +/- 5.8 microgram/1 at 30 min after injection. There is a linear relationship (r = 0.809) between serum prolactin increase and plasma metoclopramide concentration.

Full text

PDF
401

Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Ahtee L. Inhibition by apomorphine of the metoclopramide-induced catalepsy and increase in striatal homovanillic acid content. Br J Pharmacol. 1975 Nov;55(3):381–385. doi: 10.1111/j.1476-5381.1975.tb06941.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Bakke O. M., Segura J. The absorption and elimination of metoclopramide in three animal species. J Pharm Pharmacol. 1976 Jan;28(1):32–39. doi: 10.1111/j.2042-7158.1976.tb04019.x. [DOI] [PubMed] [Google Scholar]
  3. Bateman D. N., Leeman S., Metreweli C., Willson K. A non-invasive technique for gastric motility measurement. Br J Radiol. 1977 Jul;50(595):526–527. doi: 10.1259/0007-1285-50-595-526. [DOI] [PubMed] [Google Scholar]
  4. Cowan D. A., Huizing G., Beckett A. H. Identification of four new metabolic products of metoclopramide using mass spectrometry. Xenobiotica. 1976 Oct;6(10):605–616. doi: 10.3109/00498257609151674. [DOI] [PubMed] [Google Scholar]
  5. Davies D. S., Wing A. M., Reid J. L., Neill D. M., Tippett P., Dollery C. T. Pharmacokinetics and concentration-effect relationships of intervenous and oral clonidine. Clin Pharmacol Ther. 1977 May;21(5):593–601. doi: 10.1002/cpt1977215593. [DOI] [PubMed] [Google Scholar]
  6. Donaldson I. M., Jenner P., Marsden C. D., Miller R., Peringer E. Proceedings: Is metoclopramide a directly acting dopamine receptor antagonist? Br J Pharmacol. 1976 Mar;56(3):373P–373P. [PMC free article] [PubMed] [Google Scholar]
  7. Dougan D. F., Mearrick P. T., Wade D. N. Metoclopramide as a dopamine antagonist in the heart and gut of the mollusc Tapes watlingi. Clin Exp Pharmacol Physiol. 1974 Nov-Dec;1(6):473–478. doi: 10.1111/j.1440-1681.1974.tb00568.x. [DOI] [PubMed] [Google Scholar]
  8. Eisner M. Effect of metoclopramide on gastrointestinal motility in man. A manometric study. Am J Dig Dis. 1971 May;16(5):409–419. doi: 10.1007/BF02235085. [DOI] [PubMed] [Google Scholar]
  9. Gibbons D. O., Lant A. F. Effects of intravenous and oral propantheline and metoclopramide on ethanol absorption. Clin Pharmacol Ther. 1975 May;17(5):578–584. doi: 10.1002/cpt1975175578. [DOI] [PubMed] [Google Scholar]
  10. Heading R. C., Nimmo J., Prescott L. F., Tothill P. The dependence of paracetamol absorption on the rate of gastric emptying. Br J Pharmacol. 1973 Feb;47(2):415–421. doi: 10.1111/j.1476-5381.1973.tb08339.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Judd S. J., Lazarus L., Smythe G. Prolactin secretion by metoclopramide in man. J Clin Endocrinol Metab. 1976 Aug;43(2):313–317. doi: 10.1210/jcem-43-2-313. [DOI] [PubMed] [Google Scholar]
  12. Klein R. L., Militello T. E., Ballinger C. M. Antiemetic effect of metoclopramide...evaluation in humans. Anesth Analg. 1968 May-Jun;47(3):259–264. [PubMed] [Google Scholar]
  13. Kreel L., Trott M., Howells T. H. The influence of oral metoclopramide on gastric emptying after a fixed water load. Clin Radiol. 1972 Apr;23(2):213–218. doi: 10.1016/s0009-9260(72)80103-x. [DOI] [PubMed] [Google Scholar]
  14. McCallum R. W., Sowers J. R., Hershman J. M., Sturdevant R. A. Metoclopramide stimulates prolactin secretion in man. J Clin Endocrinol Metab. 1976 Jun;42(6):1148–1152. doi: 10.1210/jcem-42-6-1148. [DOI] [PubMed] [Google Scholar]
  15. McNeilly A. S., Thorner M. O., Volans G., Besser G. M. Letter: Metaclopramide and prolactin. Br Med J. 1974 Jun 29;2(5921):729–729. doi: 10.1136/bmj.2.5921.729. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Ramsbottom N., Hunt J. N. Studies of the effect of metoclopramide and apomorphine on gastric emptying and secretion in man. Gut. 1970 Dec;11(12):989–993. doi: 10.1136/gut.11.12.989. [DOI] [PMC free article] [PubMed] [Google Scholar]
  17. Robinson O. P. Metoclopramide--side effects and safety. Postgrad Med J. 1973 Jul;49 (Suppl 4):suppl 4–4:80. [PubMed] [Google Scholar]
  18. ZIRKLE G. A., KING P. D., McATEE O. B., VAN DYKE R. Effects of chlorpromazine and alcohol on coordination and judgement. J Am Med Assoc. 1959 Nov 14;171:1496–1499. doi: 10.1001/jama.1959.03010290054013. [DOI] [PubMed] [Google Scholar]

Articles from British Journal of Clinical Pharmacology are provided here courtesy of British Pharmacological Society

RESOURCES