A new nasal decongestant, A-57219: a comparison with oxymetazoline

  • J Pharm Pharmacol. 1987 Sep;39(9):760-3. doi: 10.1111/j.2042-7158.1987.tb06989.x.
J F DeBernardis  1 ,  M Winn ,  D J Kerkman ,  J J Kyncl ,  S Buckner ,  B Horrom
Affiliations
  • 1. Division of Cardiovascular Research, Abbott Laboratories, Abbott Park, IL 60065.
PMID: 2445950 DOI: 10.1111/j.2042-7158.1987.tb06989.x
Abstract

2-(4-Amino-3,5-dichlorobenzyl)imidazoline hydrochloride (A-57219), has alpha 1-agonist/alpha 2-antagonist activity and was more effective and long-acting than oxymetazoline on canine nasal mucosa, in-vitro and in-vivo. Upon intranasal administration to dogs, the compound was devoid of systemic effects up to a concentration 1000 times that needed for local decongestant effect (1.65 micrograms, atomized from a 1 microgram mL-1 solution) suggesting limited mucosal absorption. After nasal administration to rats for 15 days at a concentration 1000 times greater than that required for nasal decongestion, no mucosal tissue toxicity or systemic effects were seen.

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