Serum Levels of Sulpiride Enantiomers after Oral Treatment with Racemic Sulpiride in Psychiatric Patients: a Pilot Study[1]

Sulpiride (SULP), a substituted benzamide with high selectivity for D₂-like dopamine receptors, has a chiral structure and is used in most countries as the racemate. In an open pilot study, we investigated 26 inpatients (13 female, 13 male) with schizophrenic or depressive disorder treated with SULP (mean daily dosage 64 - 1062 mg) administered orally, either as a monotherapy or as an add-on treatment to a stable and unchanged medication for 3 - 60 days. Serum levels of total SULP and of its enantiomers were measured by high-performance liquid chromatography (HPLC) procedures. Clinically relevant indicators of hepatic and renal function as well as retrospectively assessed clinical outcome parameters were correlated with serum levels of racemic SULP, L-SULP, D-SULP, and the L : D-SULP ratio. A significant correlation between mean daily dosage and serum levels of SULP, L-SULP, and D-SULP emerged (p < 0.05) which was not influenced by age, gender, diagnosis, hepatic, or renal function. The ratio of L : D-SULP serum levels was < 1 (range 0.66 - 0.97) in all patients. A slight negative correlation between CGI improvement and the ratio of L : D-SULP (p < 0.10) and a positive correlation between racemic SULP concentrations and side-effects at endpoint was found (p < 0.05).

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1 Preliminary results of the present paper were presented at the XI. Congress of the World Psychiatric Association, September 1999, Hamburg, Germany