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. 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.

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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]

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