A clinical evaluation of a piperidine compound alone, and combined with calcium intravenously in antihistamine therapy.

Similar compounds not containing this molecular configuration are devoid of histamine activity. For obvious reasons it is not only impossible but impractical to check histamine formation. Almost a quarter century ago attempts were initiated to make available an antagonist which would either successfully combat formation of histamine or nullify its effects. This presented many difficulties. Naturally, attention was first directed to the sympathomimetic drugs such as epinephrin, but since these substances do not prevent the capillary dilatation induced by histamine, they were discarded. In 1953 Rothlin and Cerletti (1), and Huber (2) evaluated a new antihistaminic drug, designated Sandostene. Chemically this is 1-methyl-4-amino-N'-phenyl-N' (2'-thenyl)-piperidine-tartrate. Rothlin and Cerletti combined this substance with calcium for intravenous administration. The logic of this combination was based on experimental and clinical experience which followed the use of calcium with various other antihistaminic drugs. There was some apparent synergism with benefits not obtainable from either substance alone. While calcium is by no means an antihistaminic it does have a decongestive effect. Calcium also exerts a sedative effect on the cortical sensory centers, the medulla and spinal cord. Combining an antihistaminic with calcium seemed to offer advantages over each substance individually, but the clinical substantiation was still to be demonstrated. Many antihistaminics inhibit acetylcholine; some, however in doses far beyond their therapeutic range. Since acetylcholine seems to play a role in allergic reactions and may even participate in development of vegetative disturbances associated with allergy, some anticholinergic action would be desirable.