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alpha2-adrenoceptor agonists as nasal decongestants
M R Corboz1, J C Mutter, M A Rivelli
1Pulmonary and Peripheral Neurobiology, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA. michel.corboz@spcorp.com
Pulmonary Pharmacology & Therapeutics
|July 1, 2006
Summary
Selective alpha(2)-adrenoceptor agonists effectively reduce nasal congestion by targeting venous sinusoids. These compounds offer a promising alternative to nonselective decongestants, potentially minimizing side effects like hypertension.
Area of Science:
- Pharmacology
- Otorhinolaryngology
Background:
- Nasal congestion in rhinitis stems from engorged nasal mucosa and obstructed airflow.
- Sympathomimetic alpha-adrenoceptor agonists are the only drugs targeting vascular features of nasal obstruction.
- Nonselective agonists cause side effects like hypertension and nervousness.
Purpose of the Study:
- To evaluate the decongestant effects of selective alpha(2)-adrenoceptor agonists.
- To investigate the mechanism of action on nasal mucosa vasculature.
Main Methods:
- Assessed alpha(2)-adrenoceptor agonists (BHT-920, PGE-6201204) in isolated nasal mucosa contractile bioassays (dog, pig, monkey).
- Utilized a real-time tissue contractility assay with pig nasal explants for BHT-920.
- Evaluated PGE-6201204's in vivo decongestant activity in a cat model.
Main Results:
- Alpha(2)-adrenoceptor agonists contracted nasal mucosa across species.
- Demonstrated preferential vasoconstriction of capacitance vessels (veins, sinusoids).
- Observed significant nasal decongestion effects.
Conclusions:
- Selective alpha(2)-adrenoceptor agonists constrict nasal venous sinusoids and veins.
- These agonists effectively decongest nasal passages.
- Targeting alpha(2)-adrenoceptors offers a potential strategy for nasal congestion treatment with reduced side effects compared to nonselective agents.