title: A phase 1 study of the cholecystokinin (CCK) B antagonist L-365,260 in human subjects taking morphine for intractable non-cancer pain.
abstract: To investigate the safety and tolerability of L-365,260 in human subjects taking morphine for intractable pain. An open label study of nine adult subjects. Two doses of L-365,260 were administered to all subjects separated by a 4 h interval (three received 10 mg, three 30 mg and three 60 mg). Haemodynamic and respiratory variables were recorded from immediately prior to first drug administration to T + 600 min. In addition, continuous electrocardiogram (ECG) monitoring and serial 12 lead ECGs were recorded along with pain and side effect measurements. No major side effects were observed. L-365,260 was well tolerated. No abnormalities in blood pressure, heart rate, respiratory rate or ECG measurements were recorded. Minor side effects were observed. L-365,260 can be safely administered at the doses investigated to human subjects receiving morphine for intractable pain.
authors.affiliation: Rampark Pain Centre, 2 Rampark, Dromore Road, Lurgan BT66 7JH, Northern Ireland, UK. gary@mccleane.freeserve.co.uk
authors.forename: Gary J
authors.initials: GJ
authors.lastname: McCleane
mesh_terms: D000328:Adult; D000701:Analgesics, Opioid / Q000009:adverse effects / Q000627:therapeutic use*; D001570:Benzodiazepinones / Q000009:adverse effects / Q000627:therapeutic use*; D003692:Delayed-Action Preparations; D004562:Electrocardiography / Q000187:drug effects; D005260:Female; D006439:Hemodynamics / Q000187:drug effects; D006801:Humans; D008297:Male; D009020:Morphine / Q000009:adverse effects / Q000627:therapeutic use*; D010148:Intractable Pain / Q000188:drug therapy*; D010671:Phenylurea Compounds / Q000009:adverse effects / Q000627:therapeutic use*; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin / Q000037:antagonists & inhibitors*; D015656:Respiratory Mechanics
chemical_list: D000701:Analgesics, Opioid; D001570:Benzodiazepinones; D003692:Delayed-Action Preparations; D010671:Phenylurea Compounds; D043887:Receptor, Cholecystokinin B; D011949:Receptors, Cholecystokinin; C058121:L 365260; D009020:Morphine