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European Journal of Clinical Pharmacology

, Volume 29, Issue 4, pp 417–423 | Cite as

Pharmacokinetics of amiodarone, desethylamiodarone and other iodine-containing amiodarone metabolites

  • M. Stäubli
  • A. Troendle
  • B. Schmid
  • P. Balmer
  • B. Kohler
  • H. Studer
  • J. Bircher
Originals

Summary

In 23 patients treated with the iodine-containing antiarrhythmic drug amiodarone, the plasma concentrations of amiodarone, desethylamiodarone and iodine have been studied. Besides amiodarone and desethylamiodarone, a pool of iodine-containing substances, NANDAI (non-amiodarone-, non-desethylamiodarone-iodine), was present. At steady state the iodine content of NANDAI amounted to 64% and the iodine content of amiodarone plus desethylamiodarone to 36% of total serum iodine. At steady state 26% of the NANDAI fraction was made up of inorganic iodide, the average plasma concentration of which was at least 40 times above the upper limit of the normal range. The serum elimination half-life of NANDAI of 57–160 days exceeded that of amiodarone (35–68 days) and of desethylamiodarone (31–110 days).

At steady state the serum concentration of desethylamiodarone appears to be related to the concentration of amiodarone by a Michaelis-Menten type function, yielding a Km of amiodarone of 2.45 µmol/l and a maximal desethylamiodarone concentration of 3.61 µmol/l.

Key words

amiodarone desethylamiodarone iodine pharmacokinetics thyroid function toxicity 

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Copyright information

© Springer-Verlag 1985

Authors and Affiliations

  • M. Stäubli
    • 1
  • A. Troendle
    • 1
  • B. Schmid
    • 2
  • P. Balmer
    • 3
  • B. Kohler
    • 4
  • H. Studer
    • 1
  • J. Bircher
    • 5
  1. 1.Department of Internal MedicineUniversity of Berne, Practitioners in CardiologySwitzerland
  2. 2.Department of Clinical PharmacologyUniversity of Berne, Practitioners in CardiologySwitzerland
  3. 3.ThunSwitzerland
  4. 4.OltenSwitzerland
  5. 5.Division of Clinical PharmacologyUniversity of GöttingenGöttingenFRG

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