Skip to main content
NCBI home page
Anesthesia Progress logoLink to Anesthesia Progress
. 1987 Jul-Aug;34(4):128–133.

Serum Concentration and Drug Effect After Intravenous and Rectal Administration of Diazepam

Stefan Lundgren
PMCID: PMC2186279  PMID: 3481512

Abstract

In a randomized crossover study on sedation in outpatient oral surgery, the relation between the serum profile and the drug effect profile for intravenously (i.v.) and rectally administered diazepam was studied. Both sedation methods were found to be equally efficient at a mean dose of 0.25 mg/kg (range, 0.14—0.45) for i.v. administration, and 0.53 mg/kg (range, 0.50—0.58) for rectal administration. Both the serum concentration and the effect reached their mean peaks at the same time; however, this was 15 min later after rectal sedation than after i.v. sedation. Intravenous administration yielded a significantly higher serum concentration of diazepam at the clinical endpoint than did rectal administration, but the mean effect levels at the clinical endpoint were equal for both sedation methods. No linear correlation between log-serum concentration and the patient's estimation of effect was found.

Full text

PDF
128

Selected References

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

  1. Agurell S., Berlin A., Ferngren H., Hellström B. Plasma levels of diazepam after parenteral and rectal administration in children. Epilepsia. 1975 Jun;16(2):277–283. doi: 10.1111/j.1528-1157.1975.tb06058.x. [DOI] [PubMed] [Google Scholar]
  2. Arendt R. M., Greenblatt D. J., deJong R. H., Bonin J. D., Abernethy D. R., Ehrenberg B. L., Giles H. G., Sellers E. M., Shader R. I. In vitro correlates of benzodiazepine cerebrospinal fluid uptake, pharmacodynamic action and peripheral distribution. J Pharmacol Exp Ther. 1983 Oct;227(1):98–106. [PubMed] [Google Scholar]
  3. Arnold E. A simple method for determining diazepam and its major metabolites in biological fluids: application in bioavailability studies. Acta Pharmacol Toxicol (Copenh) 1975 Apr;36(4):335–352. doi: 10.1111/j.1600-0773.1975.tb00801.x. [DOI] [PubMed] [Google Scholar]
  4. Bond A. J., Hailey D. M., Lader M. H. Plasma concentrations of benzodiazepines. Br J Clin Pharmacol. 1977 Feb;4(1):51–56. doi: 10.1111/j.1365-2125.1977.tb00666.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  5. Breimer D. D., Jochemsen R., von Albert H. H. Pharmacokinetics of benzodiazepines. Short-acting versus long-acting. Arzneimittelforschung. 1980;30(5A):875–881. [PubMed] [Google Scholar]
  6. Conner J. T. Sedation vs. relief of anxiety. Anesthesiology. 1978 Apr;48(4):300–301. doi: 10.1097/00000542-197804000-00028. [DOI] [PubMed] [Google Scholar]
  7. Dasberg H. H., van der Kleijn E., Guelen J. P., van Praag H. M. Plasma concentrations of diazepam and of its metabolite N-desmethyldiazepam in relation to anxiolytic effect. Clin Pharmacol Ther. 1974 May;15(5):473–483. doi: 10.1002/cpt1974155473. [DOI] [PubMed] [Google Scholar]
  8. Dionne R. A. Differential pharmacology of drugs used for intravenous pre-medication. J Dent Res. 1984 Jun;63(6):842–847. doi: 10.1177/00220345840630060501. [DOI] [PubMed] [Google Scholar]
  9. Greenblatt D. J., Shader R. I., Abernethy D. R. Drug therapy. Current status of benzodiazepines. N Engl J Med. 1983 Aug 11;309(6):354–358. doi: 10.1056/NEJM198308113090607. [DOI] [PubMed] [Google Scholar]
  10. Greenblatt D. J., Shader R. I., Divoll M., Harmatz J. S. Benzodiazepines: a summary of pharmacokinetic properties. Br J Clin Pharmacol. 1981;11 (Suppl 1):11S–16S. doi: 10.1111/j.1365-2125.1981.tb01833.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  11. Harder F., Elsass P., Hvidberg E. F., Hjorting-Hansen E., Hendel J. Clinical and psychological effects of intravenous diazepam related to plasma levels. A controlled, double-blind, cross-over study in oral surgery involving local analgesia. Int J Oral Surg. 1976 Oct;5(5):226–239. doi: 10.1016/s0300-9785(76)80018-x. [DOI] [PubMed] [Google Scholar]
  12. Jack M. L., Colburn W. A. Pharmacokinetic model for diazepam and its major metabolite desmethyldiazepam following diazepam administration. J Pharm Sci. 1983 Nov;72(11):1318–1323. doi: 10.1002/jps.2600721120. [DOI] [PubMed] [Google Scholar]
  13. Lundgren S. Comparison of rectal diazepam and subcutaneous morphine-scopolamine administration for outpatient sedation in minor oral surgery. Acta Anaesthesiol Scand. 1985 Oct;29(7):674–678. doi: 10.1111/j.1399-6576.1985.tb02279.x. [DOI] [PubMed] [Google Scholar]
  14. Lundgren S., Ekman A., Blombäck U. Rectal administration of diazepam in solution. A clinical study on sedation in paediatric dentistry. Swed Dent J. 1978;2(5):161–166. [PubMed] [Google Scholar]
  15. Lundgren S., Rosenquist J. B. Comparison of sedation, amnesia, and patient comfort produced by intravenous and rectal diazepam. J Oral Maxillofac Surg. 1984 Oct;42(10):646–650. doi: 10.1016/0278-2391(84)90206-4. [DOI] [PubMed] [Google Scholar]
  16. Lundgren S., Rosenquist J. B. Intravenous or rectal diazepam for outpatient sedation in minor oral surgery. Int J Oral Maxillofac Surg. 1986 Oct;15(5):541–548. doi: 10.1016/s0300-9785(86)80056-4. [DOI] [PubMed] [Google Scholar]
  17. Tansella M., Zimmermann Tansella C., Ferrario L., Preziati L., Tognoni G., Lader M. Plasma concentrations of diazepam, noradiazepam and amylobarbitone after short-term treatment of anxious patients. Pharmakopsychiatr Neuropsychopharmakol. 1978 Mar;11(2):68–75. doi: 10.1055/s-0028-1094564. [DOI] [PubMed] [Google Scholar]

Articles from Anesthesia Progress are provided here courtesy of American Dental Society of Anesthesiology

RESOURCES