Nasal absorption of nafarelin acetate, the decapeptide [D-Nal(2)6)]LHRH, in rhesus monkeys. I.

Nafarelin acetate, [D-Nal(2)6]LHRH, a highly potent superagonist of luteinizing hormone-releasing hormone, was given intranasally to six female rhesus monkeys. Absorption was rapid and very reproducible, with peak levels occurring at 15-30 min and a bioavailability of approximately 2% relative to a subcutaneous dose. The nasal dose response was highly nonlinear. The nonlinearity was apparently associated with the absorption phase, since elimination profiles at all doses were similar.