ABSTRACT
N-Cyclohexyl-3-methoxyquinoxalin-2-carboxamide (QCM-13), a novel 5-HT3 antagonist identified from a series of compounds with higher pA2 (7.6) and good log P (2.91) value was screened in rodent models of depression such as forced swim test (FST), tail suspension test (TST), interaction studies with standard anti-depressants and confirmatory studies such as reversal of parthenolide induced depression and reserpine induced hypothermia. In FST (2 and 4 mg/kg) and TST (2 and 4 mg/kg), QCM-13 significantly reduced the duration of immobility in mice without affecting the base line locomotion. QCM-13 (2 and 4 mg/kg) was also found to have significant interaction with standard anti-depressants (fluoxetine and bupropion in FST and TST respectively). Further, reversal of parthenolide induced depression in mice and reserpine induced hypothermia in rat models indicate the serotonergic influence of QCM-13 for anti-depressant potential.
ABSTRACT
BACKGROUND: Postoperative nausea and vomiting (PONV) is a distressing adverse effect of anesthesia. This study was designed to evaluate antiemetic effects of metoclopramide, ondansetron and granisetron in middle ear surgery. METHODS: We compared the antiemetic activity of prophylactic administration of metoclopramide, ondansetron and granisetron in 103 patients undergoing middle ear surgery (tympanomastoidectomy and tympanoplasty). All Study drugs were given as a short intravenous infusion 30 minutes before the end of anesthesia. The incidence of PONV were assessed by direct questioning of patients at 6, 12, 24 and 48 hr after recovery from anesthesia. RESULTS: For the first 6 hr recovery period after surgery, the percentages of emesis in patients were 46.7%, 16%, 12% and 16% in the control, metoclopramide, ondansetron and granisetron groups respectively. After 6 hr, the percentage of emesis in patients significantly decreased in the control, ondansetron and granisetron groups when compared with the first 6 hr, but in the metoclopramide group there was no changes after 6 hr. CONCLUSIONS: The antiemetic drugs, metoclopramide, ondansetron and granisetron, were all effective in controling PONV in middle ear surgery.