Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1991-04-26
1997-04-01
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514315, 514318, 514646, 514291, A61K 3154, A61K 31445, A61K 31135
Patent
active
056165803
ABSTRACT:
This invention discloses mixtures of NMDA antagonists and anti-cholinergic agents, which can be used to prevent excitotoxic damage in the central nervous system or for anesthetic purposes in human or veterinary medicine. Anti-cholinergic agents such as scopolamine, atropine, benztropine, trihexyphenidyl, biperiden, procyclidine, benactyzine, or diphenhydramine can be used in conjunction with, or subsequent to, administration of an NMDA antagonist such as MK-801. The NMDA antagonist exerts a primary protective effect by preventing or reducing excitotoxic damage due to stroke, perinatal asphyxia, and various other types of injury or disease; however, strong NMDA antagonists such as MK-801 can also cause neurotoxic side effects, including vacuole formation, mitochondrial dissolution, and neuronal death in certain types of neurons such as cingulate/retrosplenial cerebrocortical neurons. The anti-cholinergic agent will reduce or eliminate those damaging side effects, without interfering with the primary protective value of the NMDA antagonist. The anti-cholinergic agents described herein can also reduce the toxic side effects associated with illegal use of drugs such as phencyclidine (also known as PCP or angel dust).
REFERENCES:
Olney et al. "Anti-parkinsonian agents are phencyclidine agonists and N-methyl-asparate antagonists." (1987).
Freedman et al, "Muscarinic M.sub.1, M.sub.2 receptor binding. Relationship with functional efficacy," (1988).
Cintins Marianne M.
Kelly Patrick D.
Weddington K.
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