A single drop of tritium-labeled 0.1% fluorometholone suspension was administered topically to intact eyes of anesthetized and unanesthetized rabbits. Aqueous humor levels of steroid were monitored as a function of time. The aqueous humor drug concentration-time profile for anesthetized rabbits is considerably different from that for unanesthetized animals. Anesthetized animals show a shift in the time to achieve a maximum aqueous humor steroid concentration, which is ascribed to a change in rate-limiting step from corneal absorption control to dissolution control. In addition, aqueous humor drug levels in the anesthetized rabbits were dependent on position of the animals and level of anesthesia.