Chapter 3. Sedatives, Hypnotics, Anticonvulsants, Muscle Relaxants, General Anesthetics

Publisher Summary This chapter explores sedatives, hypnotics, anticonvulsants muscle relaxants, and general anesthetics. The hypnotic properties of the theophylline derivative ETTT in mice, rats, rabbits, and dogs are described. Activity was related to the dose but at active doses dogs experienced respiratory stimulation, vomiting, and defecation. The hypnotic efficiency of N -methylbutisol was evaluated in patients against the provocation to awaken to empty the bladder. The compound was inferior to pentobarbital and it was concluded that there were no grounds for recommending the addition of this new agent to the available range of hypnotics. The carbamazepine analog was prepared and found to be equally active as the prototype in reducing the amplitude of trigeminal or thalamic evoked potential in cats following intravenous administration, but with an apparent longer duration of action and more selective effect on the trigeminal sensory system. Among the succinimide derivatives CM-6 was reported to be equipotent with diphenylhydantoin but shorter acting and less toxic in mice challenged with electroshock or pentylenetetrazole. In psychotic patients who received 200–1000 mg of CM-6 per day for a mean of sixteen and a half days, seven often became worse and three remained unchanged. It activated the psychotic syndrome and intensified hallucinatory activity.