Radiolabeling and biodistribution of amiodarone and desethylamiodarone.
The antiarrhythmic drug amiodarone and its metabolite desethylamiodarone, were radiolabeled with sodium [123I]-iodide in > 98% yield using the exchange labeling method. Biodistribution studies with 123I-amiodarone in mice showed high liver and lung uptake. Heart uptake of 0.98% of the injected dose (id) peaked at 5 min, with clearance seen over 60 min to 0.44% id. 123I-Desethylamiodarone (123I-DEA) showed heart uptake of 0.58% id peaking at 5 min, with slower clearance seen over 60 min to 0.43% id. These results indicate that both agents have poor selectivity as myocardial imaging tracers. Low 123I-DEA brain uptake at 5 min (0.49% id) and rapid washout after 60 min indicate that 123I-desethylamiodarone has limited application as a brain imaging agent.
Bellen
J C
JC
Royal Adelaide Hospital, Nuclear Medicine Department, North Terrace, Australia.
Penglis
S
S
Tsopelas
C
C
D000638:Amiodarone / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000493:pharmacokinetics*; D000818:Animals; D003300:Copper / Q000737:chemistry; D005260:Female; D007457:Iodine Radioisotopes / Q000737:chemistry*; D007553:Isotope Labeling / Q000379:methods; D051379:Mice; D008807:Mice, Inbred BALB C; D014018:Tissue Distribution
D007457:Iodine Radioisotopes; D003300:Copper; C036116:desethylamiodarone; D000638:Amiodarone