EVALUATION OF CURARIZING DRUGS IN MAN

V. ANTAGONISM TO CURARIZING EFFECTS OF d-TUBOCURARINE BY NEOSTIGMINE, m-HYDROXY PHENYLTRIMETHYLAMMONIIJM AND m-HYDROXY PHENYLETHYLDIMETHYLAMMONIUM

¹ Department of Pharmacology, University of Illinois College of Medicine, Chicago 12, Illinois

The antidotal effect of neostigmine, m-hydroxy phenyltrimethylammonium bromide (Ro 2-2561) and m-hydroxy phenyldimethylethylammonium bromide (Ro 2-3198) has been determined in curarized volunteers.

1. Ro 2-2561 and Ro 2-3198 were more effective in antidoting d-tubocurarine but were of shorter duration of action than neostigmine.

2. Ro 2-2561 appeared to be slightly more effective than Ro 2-3198 in that its immediate anti-curare effect was slightly greater and more rapid in onset. It had a shorter duration of action than Ro 2-3198.

3. In the doses employed, neostigmine had the greatest muscarinic activity; Ro 2-3198 was intermediate, and Ro 2-2561 caused the least muscarinic effects.

4. Ro 2-2561 and 2-3198 were effective in alleviating the muscular weakness of a myasthenic patient.

5. The low anticholinesterase activity of Ro 2-2561 and of Ro 2-3198 indicates that anti-curare action is not dependent on anticholinesterase activity. The implications of these findings have been discussed.

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