Skip to main content
British Journal of Clinical Pharmacology logoLink to British Journal of Clinical Pharmacology
. 1978 Sep;6(3):227–232. doi: 10.1111/j.1365-2125.1978.tb04589.x

Pharmacokinetics of clonidine and its relation to the hypotensive effect in patients.

M Frisk-Holmberg, P O Edlund, L Paalzow
PMCID: PMC1429456  PMID: 687501

Abstract

1 The kinetics of clonidine and its relation to the blood pressure response after single intravenous doses of 75 micrograms--275 micrograms in hypertensive patients were determined. 2 Clonidine disposition could be described by a two compartment open model and pharmacokinetic parameters show a rapid distribution phase of 20--30 min and a mean plasma clearance of 4.6 ml min-1 kg-1 (75--200 microgram). The half-life of the beta-phase was found to be in the range of 7.4--11.4 h. Indications of dose dependent kinetics were obtained. 3 A dose-dependent decrease in blood pressure was obtained. 4 The maximal reduction in MAP (mean arterial blood pressure) was significantly (P less than 0.01) related to plasma concentrations of clonidine. 5 The reduction in MAP was always related to plasma concentrations of clonidine (r = 0.88, P less than 0.01) when pseudoequilibrium of distribution of the drug was achieved.

Full text

PDF
232

Selected References

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

  1. Brod J., Horbach L., Just H., Rosenthal J., Nicolescu R. Acute effects of clonidine on central and peripheral haemodynamics and plasma renin activity. Eur J Clin Pharmacol. 1972 Mar;4(2):107–114. doi: 10.1007/BF00562506. [DOI] [PubMed] [Google Scholar]
  2. Collste P., Haglund K., Frisk-Holmberg M., Orme M. L., Rawlins M. D., Ostman J. Pharmacokinetics and pharmacodynamics of alprenolol in the treatment of hypertension. II. Relationship to its effect on blood pressure and plasma renin activity. Eur J Clin Pharmacol. 1976 Jun 15;10(2):89–95. doi: 10.1007/BF00609465. [DOI] [PubMed] [Google Scholar]
  3. 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]
  4. Edlumd P. O., Paalzow L. K. Quantitative gas-liquid chromatographic determination of clonidine in plasma. Acta Pharmacol Toxicol (Copenh) 1977 Jan;40(1):145–152. doi: 10.1111/j.1600-0773.1977.tb02062.x. [DOI] [PubMed] [Google Scholar]
  5. Hoobler S. W., Sagastume E. Clonidine hydrochloride in the treatment of hypertension. Am J Cardiol. 1971 Jul;28(1):67–73. doi: 10.1016/0002-9149(71)90036-1. [DOI] [PubMed] [Google Scholar]
  6. Leonetti G., Mayer G., Morganti A., Terzoli L., Zanchetti A., Bianchetti G., Di Salle E., Morselli P. L., Chidsey C. A. Hypotensive and renin-suppressing activities of propranolol in hypertensive patients. Clin Sci Mol Med Suppl. 1975 Jun;48(6):491–499. doi: 10.1042/cs0480491. [DOI] [PubMed] [Google Scholar]
  7. Mroczek W. J., Davidov M., Finnerty F. A., Jr Prolonged treatment with clonidine: comparative antihypertensive effects alone and with a diuretic agent. Am J Cardiol. 1972 Oct;30(5):536–541. doi: 10.1016/0002-9149(72)90045-8. [DOI] [PubMed] [Google Scholar]
  8. Wing L. M., Reid J. L., Davies D. S., Dargie H. J., Dollery C. T. Apparent resistance to hypotensive effect of clonidine. Br Med J. 1977 Jan 15;1(6054):136–138. doi: 10.1136/bmj.1.6054.136. [DOI] [PMC free article] [PubMed] [Google Scholar]

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

RESOURCES