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Ethylenediamine, profile of a sensitizing excipient

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Abstract

Ethylenediamine is an excipient with many industrial and pharmaceutical uses. It is included in creams as a stabilizer and in aminophylline as the counter ion of theophylline. Ethylenediamine is one of the most frequent contact sensitizers, producing local and generalized reactions. Besides, many cases of systemically induced dermatitis have also been described both after oral, rectal and intravenous use. Inhalation of ethylenediamine or aminophylline dust may provoke rhinitis and asthmatic reactions. In contrast to these delayed reactions only one immediate reaction of the urticarial type after intravenous use has been described. Ethylenediamine shows cross-reactions with antihistamines of the ethylenediamine derivative group, with edetate, other amines, piperazine and hydroxyzine. Ethylenediamine shows a short half-life of about 0.55 h and a small volume of distribution of 0.133 l/kg. After oral administration its bioavailability is about 0.34, due to a substantial first-pass effect. Renal excretion of the unchanged substance amounts to only about 18% after intravenous and 3% after oral administration. It behaves independently from theophylline after administration of aminophylline. Good alternatives are now available for the pharmaceutical applications of ethylenediamine. Theophylline itself is well absorbed orally; for the intravenous administration theN-methylglucamine salt is sufficiently soluble. Suppositories containing pure theophylline are commercially available in some countries, but the experience with this product is relatively small.

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Zuidema, J. Ethylenediamine, profile of a sensitizing excipient. Pharmaceutisch Weekblad Scientific Edition 7, 134–140 (1985). https://doi.org/10.1007/BF02097249

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