Because little has been published on early effects of treatment with amiodarone on thyroid function, we studied serum total and free thyroid hormone, reverse T-3, and TSH levels in patients with cardiac arrhythmias during the first 10 days of treatment with a loading dose of amiodarone by iv infusion. Twenty-four patients were enrolled in the study. A standardized loading regimen for the iv infusion of amiodarone was used. The protocol provided the iv infusion of 20 mg/kg per day on day 1, the iv infusion of 10 mg/kg per day on day 2, then 600 mg/day per os for 7-10 days, and finally, in patients chronically treated with the drug, the dose was gradually reduced to 400-200 mg/day per os. Total and free concentrations of T-4 tended to progressively and significantly increase (P < 0.0001 repeated measures ANOVA) starting from the fourth day of therapy, whereas total T-3 decreased from the second day progressively (P < 0.0001) throughout the study; free T-3 did not significantly change. TSH levels early and significantly (P < 0.001, by ANOVA) increased throughout the study, starting from the first day of therapy and reaching at 10 days a value 2.7 times higher than the basal value. Reverse T-3 levels progressively and significantly (after 2 days of treatment) increased and paralleled the TSH values, reaching at the 10th day a value about 2 times higher than basal value. In conclusion, our data suggest that after iv treatment with amiodarone: 1) TSH is the first hormone to change significantly followed by reverse T-3, T-4, and T-3; 2) the progressive fall of T-3 levels reflects an inhibition of the peripheral conversion of T-4 to T-3; 3) the observed later increase of total and free T-4 levels may be explained by a contribution of direct thyroidal stimulation by TSH and/or by a reduction in T-4 clearance.