The relationship between the pharmacokinetic properties and the analgesic effect of ketorolac was evaluated with the pain-induced functional impairment model in the rat. Female Wistar rats were injected with uric acid in the knee of the right hind limb to produce dysfunction. Then, animals received an oral dose of 0.3, 1, 1.8, 3.2 or 5.6 mg/kg of ketorolac tromethamine and analgesic effect and blood concentration, determined by high-performance liquid chromatography, were evaluated at selected times for a period of 4 hr. Ketorolac produced a dose-dependent analgesic effect, measured as a recovery of the functionality of the injured limb, which reached its maximal effect at doses of 3.2 mg/kg or higher. When functionality index was plotted against ketorolac blood concentration, a direct relationship was observed that was well described by the sigmoidal maximal effect model. The data strongly suggest that ketorolac's analgesic effect depends on the blood concentration of the drug.