Stereoselective metabolism of citalopram in plasma and cerebrospinal fluid of depressive patients: relationship with 5-HIAA in CSF and clinical response.

摘要: Plasma and cerebrospinal fluid (CSF) concentrations of the enantiomers citalopram (CIT), its N-demethylated metabolite demethylcitalopram (DCIT) deaminated propionic acid derivative (CIT-PROP) were measured in plasma CSF 22 depressed patients after a 4-week treatment with 40 mg/d citalopram, which was preceded by 1-week washout period. 5-hydroxyindoleacetic (5-HIAA) homovanillic (HVA) at baseline CIT medication Patients assessed clinically, using Hamilton Depression Rating Scale (21-item HAM-D): then weekly intervals. S-CIT R-CIT 10.6 +/- 4.3 20.9 6 ng/mL, respectively, their CSF/plasma ratios 52% 9% 48% 6%, respectively. The resulted significant decrease (28%) 5-HIAA (P or =50% HAM-D score (DeltaHAM-D) treatment. DeltaHAM-D correlated (Spearman) significantly (r = - 0.483, P < 0.05), S-CIT-PROP -0.543, 0.01) (a formed from monoamine oxidase [MAO]) (Delta5-HIAA) 0.572, 0.01). demonstrated correlations between pharmacokinetic parameters clinical outcome as well changes indicate that monitoring S-CIT, may be relevance.