Pharmacokinetics of perospirone hydrochloride at an excessive dose and changes in the serum prolactin level

: A 36-year-old female, in whom 8 mg perospirone hydrochloride tablets had been prescribed, took 178 tablets (corresponding to 1,424 mg) as a single dose. After 4.5 hours, she was admitted under a diagnosis of acute drug intoxication. We investigated her clinical course and medical records including the laboratory data, and measured serial changes in the serum levels of perospirone hydrochloride and prolactin by HPLC and ELISA. Concerning the clinical course, the consciousness level on admission was JCS II-10, but normalized 18 hours after dosing. Thereafter, there were no intoxication symptoms or sequelae related to massive administration of this agent, and the patient was discharged 3 days after admission. There were no abnormalities in the laboratory data obtained on admission and 2 days after admission. The serum levels of perospirone hydrochloride were 695 ng/mL 4.5 hours after dosing and approximately 60 ng/mL 18 hours after dosing, when consciousness became clear. The t1/2 beta value was 8 hours, similar to that in healthy adults. Furthermore, the serum level of prolactin 4.5 hours after dosing was 49.5 ng/mL, but returned to the normal range 18 hours after dosing, when consciousness became clear.