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

Autor: DeBernardis, John F, Winn, Martin, Kerkman, Daniel J, Kyncl, John J, Buckner, Steven, Horrom, Bruce
Zdroj: Journal of Pharmacy and Pharmacology; September 1987, Vol. 39 Issue: 9 p760-763, 4p
Abstrakt: 2-(4-Amino-3,5-dichlorobenzyl)imidazolin hydrochloride (A-57219), has α1-agonist/α2-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 (1ṁ65 μg, atomized from a 1 μg mL-1solution) 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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