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General pharmacological properties of procyclidine and physostigmine, as a combinational prophylactic regimen for organophosphate poisoning, were investigated in experimental animals and in vitro test system. Procyclidine and physostigmine were administerd by subcutaneous injection or miniosmotic pumps for sustained release. Procyclidine had no effects on general behavior, spontaneous motor activity, pentobarbital sleeping time, motor coordination and normal body temperature at the doses of less than 30 ㎎/㎏ or 1728 ㎍/㎏/hr. Gastric secretion and intestinal motility in rats were not influenced by the sustained release of procyclidine at dose of 1296 ㎍/㎏/hr. Procyclidine up to 40 ㎎/㎏ did not change the mean arterial blood pressure and heart rate in conscious rats. Procyclidine had no effect on the respiratory rate at the same doses when given to anesthetized rats. In in vitro experiments, procyclidine at the concentration of more than 0.1 and 1 ㎎/ℓ showed significant inhibitory action on the acetylcholine-and histamine-induced contractions, respectively, in the isolated ileum of guinea-pig. In the isolated guinea-pig tracheal muscle, procyclidine did not affect the histamine-induced contractions at the dose of 5 ㎎/ℓ, but showed partial inhibition on the acetylcholine-induced contractions at the doses of 3 and 5 ㎎/ℓ. Physostigmine at the concentration of 0.05 ㎎/㎏ or 36 ㎍/㎏/hr neither produced significant change of the normal physiological activity of rats, nor completely recover the inhibitory effect of procyclidine on the gastrointestinal tract. Based on these results, it was concluded that procyclidine and physostigmine did not induce marked adverse effects in experimental animals except the significant inhibitory effect on the gastrointestinal system.

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UCI(KEPA) : I410-ECN-0101-2009-510-016362323