Pharmacokinetics of levonorgestrel in the rat.

Levonorgestrel was administered intravenously as a bolus to adult female rats and blood samples were collected at various time intervals. Serum concentrations of levonorgestrel were measured by radioimmunoassay. Analysis of data for two- and three-compartment open models indicated that in the rat, as in the human and the rabbit, a tri-exponential equation provided a better fit of the data. The half-lives for the alpha, beta and gamma phases were 10.1 min, 42.7 min and 23.1 hours, respectively. These values were closer to those reported for women than were the half-lives reported for the rabbit. The alpha and the beta phases appeared to last for 51 min and 1.3 hours, respectively, and the gamma phase was longer than 45 hours.