Comparison of the neurokinin‐1 antagonist GR205171, alone and in combination with the 5‐HT3 antagonist ondansetron, hyoscine and placebo in the prevention of motion‐induced nausea in man

Aims In man a neurokinin‐1 (NK1) receptor antagonist has previously been shown to be ineffective in the prevention of motion‐induced nausea. The antiemetic efficacy of NK1 receptor antagonists against chemotherapy‐induced emesis is, however, enhanced when combined with a 5‐HT3 receptor antagonist. H...

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Bibliographic Details
Published in:British journal of clinical pharmacology 2000-07, Vol.50 (1), p.61-64
Main Authors: Reid, K., Palmer, J. L., Wright, R. J., Clemes, S. A., Troakes, C., Somal, H. S., House, F., Stott, J. R. R.
Format: Article
Language:English
Subjects:
5‐HT3 receptor antagonist
Adolescent
Adult
Antiemetics - therapeutic use
Biological and medical sciences
Cross-Over Studies
Digestive system
Double-Blind Method
Drug Therapy, Combination
Female
Humans
hyoscine
Male
Medical sciences
Middle Aged
motion sickness
Motion Sickness - prevention & control
Nausea - prevention & control
Neurokinin-1 Receptor Antagonists
NK1 receptor antagonist
Ondansetron - therapeutic use
Pharmacology. Drug treatments
Piperidines - therapeutic use
Scopolamine - therapeutic use
Serotonin Antagonists - therapeutic use
Short Reports
Tetrazoles - therapeutic use
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Summary:Aims In man a neurokinin‐1 (NK1) receptor antagonist has previously been shown to be ineffective in the prevention of motion‐induced nausea. The antiemetic efficacy of NK1 receptor antagonists against chemotherapy‐induced emesis is, however, enhanced when combined with a 5‐HT3 receptor antagonist. Hence the efficacy of the NK1 antagonist GR205171 in combination with the 5‐HT3 antagonist ondansetron (Zofran™) was assessed in motion‐induced nausea. Methods GR205171 25 mg i.v., with and without concomitant administration of ondansetron 8 mg i.v., and hyoscine hydrobromide 0.6 mg orally (positive control) were compared with placebo in a model of motion‐induced nausea. The study was performed to a four‐period, randomized, balanced, double‐blind, crossover design in 16 healthy subjects. The end‐point was the exposure to the motion stimulus required to produce moderate nausea in the subjects. Results The motion stimulus required to produce moderate nausea was significantly greater for the positive control than placebo (P 
ISSN:0306-5251
1365-2125
DOI:10.1046/j.1365-2125.2000.00221.x