Literature DB >> 10886120

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.

K Reid1, J L Palmer, R J Wright, S A Clemes, C Troakes, H S Somal, F House, J R Stott.   

Abstract

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 (Zofrantrade mark) 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 < 0. 001). There was no significant difference between either GR205171 or GR205171 plus ondansetron and placebo (P = 0.648 and 0.342, respectively).
CONCLUSIONS: The enhancement of NK1 receptor antagonist antiemetic activity through combination with a 5-HT3 receptor antagonist is not replicated in motion-induced nausea.

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Year:  2000        PMID: 10886120      PMCID: PMC2014963          DOI: 10.1046/j.1365-2125.2000.00221.x

Source DB:  PubMed          Journal:  Br J Clin Pharmacol        ISSN: 0306-5251            Impact factor:   4.335


  8 in total

1.  The effect on motion sickness and oculomotor function of GR 38032F, a 5-HT3-receptor antagonist with anti-emetic properties.

Authors:  J R Stott; G R Barnes; R J Wright; C J Ruddock
Journal:  Br J Clin Pharmacol       Date:  1989-02       Impact factor: 4.335

2.  Comparison of the effects of a selective muscarinic receptor antagonist and hyoscine (scopolamine) on motion sickness, skin conductance and heart rate.

Authors:  J F Golding; J R Stott
Journal:  Br J Clin Pharmacol       Date:  1997-06       Impact factor: 4.335

3.  Randomized phase II study of the neurokinin 1 receptor antagonist CJ-11,974 in the control of cisplatin-induced emesis.

Authors:  P J Hesketh; R J Gralla; R T Webb; W Ueno; S DelPrete; M E Bachinsky; N L Dirlam; C B Stack; S L Silberman
Journal:  J Clin Oncol       Date:  1999-01       Impact factor: 44.544

4.  GR205171: a novel antagonist with high affinity for the tachykinin NK1 receptor, and potent broad-spectrum anti-emetic activity.

Authors:  C J Gardner; D R Armour; D T Beattie; J D Gale; A B Hawcock; G J Kilpatrick; D J Twissell; P Ward
Journal:  Regul Pept       Date:  1996-08-27

5.  Use of an NK1 receptor antagonist to prevent delayed emesis after cisplatin.

Authors:  M G Kris; J E Radford; B A Pizzo; R Inabinet; A Hesketh; P J Hesketh
Journal:  J Natl Cancer Inst       Date:  1997-06-04       Impact factor: 13.506

6.  The effect of CP-99994 on the responses to provocative motion in the cat.

Authors:  J B Lucot; R S Obach; S McLean; J W Watson
Journal:  Br J Pharmacol       Date:  1997-01       Impact factor: 8.739

7.  Anti-emetic profile of a non-peptide neurokinin NK1 receptor antagonist, CP-99,994, in ferrets.

Authors:  C Bountra; K Bunce; T Dale; C Gardner; C Jordan; D Twissell; P Ward
Journal:  Eur J Pharmacol       Date:  1993-11-02       Impact factor: 4.432

8.  Reduction of cisplatin-induced emesis by a selective neurokinin-1-receptor antagonist. L-754,030 Antiemetic Trials Group.

Authors:  R M Navari; R R Reinhardt; R J Gralla; M G Kris; P J Hesketh; A Khojasteh; H Kindler; T H Grote; K Pendergrass; S M Grunberg; A D Carides; B J Gertz
Journal:  N Engl J Med       Date:  1999-01-21       Impact factor: 91.245

  8 in total
  1 in total

Review 1.  Opportunities for the replacement of animals in the study of nausea and vomiting.

Authors:  A M Holmes; J A Rudd; F D Tattersall; Q Aziz; P L R Andrews
Journal:  Br J Pharmacol       Date:  2009-04-09       Impact factor: 8.739

  1 in total

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