Comparative clinical evaluation of lofepramine and imipramine. Pharmacological aspects.
A multicentre comparative clinical evaluation of lofepramine, an imipramine analogue, and imipramine has been made with double-blind technique and fixed dosage (lofepramine 70 mg t.i.d., imipramine 50 mg t.i.d.). Plasma was drawn after 3 weeks for determination of noradrenaline-uptake inhibitory capacity of the parent compound and/or its active metabolites. Plasma concentrations of lofepramine and desmethylimipramine (DMI) were determined in the same samples. The concentrations of lofepramine in the whole material were low (5-27 ng/ml) except for one patient who had a level of 53 ng/ml. In both groups of patients there was an almost 40-fold range in the plasma levels of DMI or apparent DMI. The patients were rated for severity of depression before treatment, then once weekly for 3 weeks and finally during the fifth week. For further information concerning the psychiatric aspects, see d'Elia et al. in this issue (1977). A significant correlation was found between the concentrations of DMI and the noradrenaline-uptake inhibitory capacity in the plasma samples. No correlations were found between uptake inhibitory capacity of plasma samples and the amelioration scores.
D000328:Adult; D002849:Chromatography, Gas; D002986:Clinical Trials as Topic; D003863:Depression / Q000097:blood* / Q000188:drug therapy*; D003891:Desipramine / Q000097:blood; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D007099:Imipramine / Q000031:analogs & derivatives* / Q000097:blood / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D009638:Norepinephrine / Q000037:antagonists & inhibitors / Q000097:blood; D011569:Psychiatric Status Rating Scales
D007099:Imipramine; D003891:Desipramine; D009638:Norepinephrine