EAA antagonists as anti-emetic drugs

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules

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424422, 424 10, 514872, 514922, A61K 948, A61K 4900, A61F 1300

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active

050395289

ABSTRACT:
This invention relates to a method and a class of pharmaceutical agents for suppressing vomiting, nausea, and other emetic symptoms. The method involves administering to a susceptible mammal a glutamate (EAA) receptor antagonist at an anti-emetically effective dose which does not cause undesirable side effects. Preferred EAA antagonists include those that do not readily cross blood-brain barriers (BBB). One suitable formulation comprises a broad-spectrum antagonist such as kynurenic acid or 7-chlorokynurenate. Other formulations include EAA antagonists that preferentially block NMDA receptors (such as D-AP5) or non-NMDA receptors (such as CNQX), or mixtures thereof that can block both classes of EAA receptors. In lab tests, the agents of this invention were shown to reduce or entirely block the effects of several emetic agents, including cisplatin. Treated animals did not vomit or exhibit lethargy or malaise and did not display any adverse side effects, while control animals consistently displayed lethargy, malaise, and vomiting.

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