Skip to main content
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1987 Aug;24(2):185–189. doi: 10.1111/j.1365-2125.1987.tb03160.x

N-monodesmethyldiltiazem is the predominant metabolite of diltiazem in the plasma of young and elderly hypertensives.

S C Montamat, D R Abernethy
PMCID: PMC1387748  PMID: 3620292

Abstract

1 Twelve young (ages 30-39 years) and twelve elderly (ages 65-83 years) hypertensives were administered diltiazem twice daily for 2 weeks at doses up to 240 mg day-1. 2 Plasma was analysed for diltiazem, N-monodesmethyldiltiazem, and desacetyldiltiazem concentrations after a single 10 min intravenous infusion of 21.8 mg diltiazem HCl on day 1 and after the morning oral dose of 120 mg diltiazem base on day 14. 3 N-monodesmethyldiltiazem accumulated to higher plasma concentrations than desacetyldiltiazem at steady state on day 14 in both age groups. 4 Prolongation of plasma diltiazem half-life occurred after 2 weeks of oral diltiazem therapy in both age groups. 5 There were no significant differences between the young and elderly with regard to half-life, area under the curve, and the peak and trough plasma concentrations of diltiazem, N-monodesmethyldiltiazem, and desacetyldiltiazem; systemic clearance and volume of distribution of diltiazem were also similar in both groups.

Full text

PDF
185

Selected References

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

  1. Abernethy D. R., Schwartz J. B., Todd E. L. Diltiazem and desacetyldiltiazem analysis in human plasma using high-performance liquid chromatography: improved sensitivity without derivation. J Chromatogr. 1985 Jul 12;342(1):216–220. doi: 10.1016/s0378-4347(00)84507-7. [DOI] [PubMed] [Google Scholar]
  2. BENDER A. D. THE EFFECT OF INCREASING AGE ON THE DISTRIBUTION OF PERIPHERAL BLOOD FLOW IN MAN. J Am Geriatr Soc. 1965 Mar;13:192–198. doi: 10.1111/j.1532-5415.1965.tb02665.x. [DOI] [PubMed] [Google Scholar]
  3. Carrum G., Egan J. M., Abernethy D. R. Diltiazem treatment impairs hepatic drug oxidation: studies of antipyrine. Clin Pharmacol Ther. 1986 Aug;40(2):140–143. doi: 10.1038/clpt.1986.152. [DOI] [PubMed] [Google Scholar]
  4. Loo J. C., Riegelman S. Assessment of pharmacokinetic constants from postinfusion blood curves obtained after I.V. infusion. J Pharm Sci. 1970 Jan;59(1):53–55. doi: 10.1002/jps.2600590107. [DOI] [PubMed] [Google Scholar]
  5. Meredith P. A., Elliott H. L., Pasanisi F., Kelman A. W., Sumner D. J., Reid J. L. Verapamil pharmacokinetics and apparent hepatic and renal blood flow. Br J Clin Pharmacol. 1985 Aug;20(2):101–106. doi: 10.1111/j.1365-2125.1985.tb05038.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Montamat S. C., Abernethy D. R., Mitchell J. R. High-performance liquid chromatographic determination of diltiazem and its major metabolites, N-monodemethyldiltiazem and desacetyldiltiazem, in plasma. J Chromatogr. 1987 Mar 20;415(1):203–207. doi: 10.1016/s0378-4347(00)83211-9. [DOI] [PubMed] [Google Scholar]
  7. Piepho R. W., Bloedow D. C., Lacz J. P., Runser D. J., Dimmit D. C., Browne R. K. Pharmacokinetics of diltiazem in selected animal species and human beings. Am J Cardiol. 1982 Feb 18;49(3):525–528. doi: 10.1016/s0002-9149(82)80006-4. [DOI] [PubMed] [Google Scholar]
  8. Rovei V., Gomeni R., Mitchard M., Larribaud J., Blatrix C., Thebault J. J., Morselli P. L. Pharmacokinetics and metabolism of diltiazem in man. Acta Cardiol. 1980;35(1):35–45. [PubMed] [Google Scholar]
  9. Schmucker D. L. Aging and drug disposition: an update. Pharmacol Rev. 1985 Jun;37(2):133–148. [PubMed] [Google Scholar]
  10. Smith M. S., Verghese C. P., Shand D. G., Pritchett E. L. Pharmacokinetic and pharmacodynamic effects of diltiazem. Am J Cardiol. 1983 May 1;51(8):1369–1374. doi: 10.1016/0002-9149(83)90314-4. [DOI] [PubMed] [Google Scholar]
  11. Sugihara J., Sugawara Y., Ando H., Harigaya S., Etoh A., Kohno K. Studies on the metabolism of diltiazem in man. J Pharmacobiodyn. 1984 Jan;7(1):24–32. doi: 10.1248/bpb1978.7.24. [DOI] [PubMed] [Google Scholar]
  12. Yabana H., Nagao T., Sato M. Cardiovascular effects of the metabolites of diltiazem in dogs. J Cardiovasc Pharmacol. 1985 Jan-Feb;7(1):152–157. doi: 10.1097/00005344-198501000-00025. [DOI] [PubMed] [Google Scholar]

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

RESOURCES