Clinical and plasma level characteristics of intramuscular and oral loxapine

The intramuscular and oral forms of loxapine succinate were compared in their clinical, side effect, and blood level characteristics in ten hospitalized chronic schizophrenic patients. The first phase of the study determined the single dose that produced moderate sedation (i.e., the sedation threshold), and this dose was essentially the same for the two forms. Continuous administration of the two forms using the individualized sedation threshold dosage also failed to indicate any clinical or side effect differences in the two forms. The blood level characteristics, however, did differ between the two forms. The kinetic studies indicated that there was a larger are under the loxapine curve with the intramuscular form than with the oral form, while the 8-OH loxapine area was larger with the oral form. The steady-state studies also showed that the i.m. form had higher loxapine levels than the oral form. The significance of these findings, both clinically and in terms of the relative activity of loxapine and its metabolites, is discussed.