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[Ibopamine--pharmacologic principles].

U Borchard1

  • 1Institut für Pharmakologie, Universität Düsseldorf.

Zeitschrift Fur Kardiologie
|January 1, 1991
PubMed
Summary

Ibopamine, an N-methyl-dopamine ester, converts to active epinine in the body. Epinine activates multiple receptors, primarily promoting renal vasodilation and diuresis.

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Area of Science:

  • Pharmacology
  • Biochemistry

Context:

  • Ibopamine is an orally administered prodrug.
  • It is rapidly metabolized to its active form, epinine, via a first-pass effect.

Purpose:

  • To elucidate the pharmacokinetic and pharmacodynamic properties of ibopamine and its active metabolite, epinine.
  • To characterize the receptor binding affinities and downstream effects of epinine.

Summary:

  • Oral ibopamine is hydrolyzed to epinine, achieving peak plasma concentrations of 60-100 nmol/L.
  • Epinine exhibits varying affinities for dopamine (DA1, DA2), beta (β1, β2), and alpha receptors, with higher affinity for DA receptors.
  • Stimulation of DA1 receptors leads to renal vasodilation and diuresis, while DA2 receptor activation reduces noradrenaline release, contributing to decreased peripheral resistance.

Impact:

  • Understanding ibopamine's metabolism and receptor interactions is crucial for its therapeutic application.
  • Epinine's selective receptor activation profile suggests potential in managing conditions requiring renal vasodilation and reduced sympathetic tone.

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