Disposition of nebulized pentamidine measured using the direct radiolabel 123I-iodopentamidine

The pulmonary deposition of nebulized pentamidine (300 mg, Respirgard II nebulizer) was measured in seven human immunodeficiency virus (HIV)-positive men using a new radiopharmaceutical, 123I-iodopentamidine. Mean total pulmonary deposition was 15.3 mg or 5.1% of the initial nebulizer dose. Further studies in two of the patients showed that at 24 h, 87% of deposited 123I was retained in the lungs. Small amounts of activity (expressed as a percentage of the initial nebulizer activity) were also detected over the thyroid (0.4%), bladder (1%) and gut (0.7%). The ratio of 123I activity to pentamidine concentration was similar in the nebulizer solution and urine. These results suggest that 123I-pentamidine may be sufficiently stable in vivo to be used to study the biodistribution of inhaled and parenteral pentamidine in humans.