ABSTRACT
Bizerine-oxalate of hexamethylene-bic-[N-methylcarbamic acid-3-(2-dimethylaminomethyl)pyridyl ether] exhibits the properties of acetylcholine esterase (AChE) inhibitor, being comparable in this respect in in vitro tests to aminostigmine. Bizerine is 2.5 and 6.7 times less active in these tests than proserine and distigmine, respectively, but it forms more stable complex with the enzyme. Bizerine is 10-80 times less toxic for laboratory mammals as compared to prozerine; it is 3-60 times more active on the isolated urinary bladder of rats, but it is 100-500 times less effective on the spinal muscle of leeches and skeletal muscles of mice and rats. Bizerine actively inhibits intestinal cholinesterase (ChE) of guinea pigs. In systematic use, it does not inhibit brain ChE of mice. Bizerine is a prolonged peripheral muscarinic potentiating inhibitor of ChE and activator of intestinal peristalsis.
Subject(s)
Carbamates/pharmacology , Cholinesterase Inhibitors/pharmacology , Gastrointestinal Tract , Pyridines/pharmacology , Animals , Carbamates/adverse effects , Cats , Cholinesterase Inhibitors/adverse effects , Cricetinae , Dogs , Humans , Mice , Neostigmine/adverse effects , Neostigmine/pharmacology , Pyridines/adverse effects , Pyridostigmine Bromide/adverse effects , Pyridostigmine Bromide/analogs & derivatives , Pyridostigmine Bromide/pharmacology , RatsABSTRACT
The pharmacological properties of a new drug approved in the USSR for the treatment of cholinolytics poisonings are described. The drug is as active as physostigmine. However, its action is longer. Aminostigmine exhibits marked central effects, which forms the basis for its use for elimination of brain dysfunctions caused by choline blockers.
