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Absolute bioavailability of moxonidine.

R Theodor1, H J Weimann, W Weber

  • 1L.A.B. GmbH & Co, Neu-Ulm, Germany.

European Journal of Drug Metabolism and Pharmacokinetics
|April 1, 1991
PubMed
Summary
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This study compared oral tablets and intravenous solutions of moxonidine in healthy males. The oral moxonidine preparation showed good bioavailability and similar pharmacokinetic profiles to the intravenous route.

Area of Science:

  • Pharmacology
  • Clinical Pharmacy
  • Drug Development

Background:

  • Moxonidine is an antihypertensive agent.
  • Understanding moxonidine's bioavailability and pharmacokinetics is crucial for optimizing its therapeutic use.

Purpose of the Study:

  • To investigate the absolute bioavailability and pharmacokinetics of two moxonidine preparations (tablet vs. intravenous solution).
  • To compare the absorption, distribution, metabolism, and excretion of moxonidine administered via different routes.

Main Methods:

  • A randomized 2-way cross-over study was conducted with 18 healthy male volunteers.
  • Single doses of 0.2 mg of moxonidine (tablet and intravenous solution) were administered.
  • Plasma and urine samples were collected over 24 hours to determine moxonidine concentrations using gas chromatography/mass spectrometry.

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Main Results:

  • Oral moxonidine demonstrated good absolute bioavailability.
  • Mean peak plasma concentrations were 1495 pg/ml (oral) and 3965 pg/ml (intravenous).
  • Mean terminal half-lives were approximately 2 hours for both formulations, with 51% of the oral dose excreted unchanged in urine within 24 hours.

Conclusions:

  • Moxonidine tablets provide comparable pharmacokinetic profiles to intravenous administration.
  • The oral formulation is suitable for achieving therapeutic moxonidine levels.
  • Further studies may explore dose-response relationships and efficacy in hypertensive patients.