A new nasal decongestant, A-57219: a comparison with oxymetazoline.
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.
D000316:Adrenergic alpha-Agonists; D000403:Airway Resistance / Q000187:drug effects; D000818:Animals; D004285:Dogs; D005260:Female; D007093:Imidazoles / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D066298:In Vitro Techniques; D008297:Male; D009131:Muscle, Smooth, Vascular / Q000187:drug effects; D014663:Nasal Decongestants / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D010109:Oxymetazoline / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000633:toxicity; D010643:Phenoxybenzamine / Q000494:pharmacology; D011817:Rabbits; D051381:Rats; D011919:Rats, Inbred Strains; D012501:Saphenous Vein / Q000187:drug effects
D000316:Adrenergic alpha-Agonists; D007093:Imidazoles; D014663:Nasal Decongestants; D010643:Phenoxybenzamine; C054140:2-(4-amino-3,5-dichlorobenzyl)imidazoline; D010109:Oxymetazoline