Nasal decongestants stimulate the alpha adrenegic receptors of the vascular smooth muscles, constricting the dilated arteriolar network within the nasal mucosa and reducing the blood flow in the engorged edematous nasal area. This constriction results in shrinkage of the engorged mucous membranes which promotes drainage, improves nasal ventilation and relieves the feeling of stuffiness
The ideal topical decongestants should have: 1) A prompt and prolonged effect 2) Not produce systemic side effects 3) No irritation to the mucosal with resultant harmful interference on the action of cilia of the respiratory tract 4) No rebound congestion
“An ideal sympathomimetic amine has not yet been found” Topical application of decongestants followed by rebound phenomenon (rhinitis medicamentosa) in which the nasal mucus membranes become even more congested and edematous as the drug’s vasoconstrictor effect subsides. This secondary effect is believed to results from ischemia caused by drug’s intensive local vasoconstriction and local irritation of the topically applied agents it self.
• The use of topical nasal decongestants is restricted to 3-4 days or less, rebound congestion is minimal • With chronic use and/or overuse of these agents, rebound nasal stuffiness may become quite pronounced • Upon questioning the patient, if the pharmacist found that this phenomena is experienced by the patient, the drug should be discontinued and systemic decongestants should be considered • After applying the medication with 3-5 min., the nose should be blown to remove the mucus. If there is still congestion, another dose should be applied that should reach farther into the nasal cavities and to the surface of the turbinates.
Ephedrine • Sympathomimetic drug, increase the release of adrenaline from nerve terminals • Rapid nasal decongestion in 0.5-10 % concentration • Peak effect achieved 1 hour after administration • Products containing this drug should shielded from direct light because of decomposition • Discolored ephedrine solution should not be used • Conc. of 0.5% should be administered as 2 or 3 drops or sprays for adults and 1 or 2 drops or sprays for children 6 to 12 yo • The frequency not more that every 4 hrs • Under 6 yo is not recommended unless prescribed
Phenylphrine • 2 to 3 drops or sprays of 0.25 to 1.0 % solution every 4 hrs • Marked nasal irritation might happen in some individuals, if this happened, the drug must be stopped
Naphazoline • More potent than phenylphrine • It induces CNS depression rather than stimulation when used systemically • Not recommended for use in children under 6 yo • 1 to 2 drops or sprays of 0.05% solution every 6 hrs • Irritating to the mucosal
Oxymetazoline and zylometazoline • Longer acting topical decongestant, their effect may last for 5 to 6 hrs with a gradual decline thereafter • Easier to use because of the duration • Used as 2 to 3 drops or sprays twice daily
Levodesoxyephedrine and propylhexedrine • Volatile and commonly used in inhalants • Not to be used in children less than 6 yo
Oral decongestants
Advantages • Have longer duration than topical decongestants • No rebound congestion because of less vasoconstriction • Lack of local irritation • Does not increase BP except in patients predisposed to hypertension
Disadvantages • Cause less intense vasoconstriction than the topically applied decongestants • Affect other vascular beds • May cause cardiac stimulation and arrhythmia • Increase blood glucose levels • Contraindicated in patients on MAO inhibitors because of hypertension crises
Ephedrine • Effective bronchodilator • Oral dose 12.5 to 25 mg every 4 hrs for adults and children 12 yo and over • Onset; 30 min to 1 hr • CNS stimulant
Phenylpropanolamine • More active as vasoconstrictor • Less active as CNS stimulant and bronchodilator • Peak effect after 3 hrs
Phenylphrine • Hydrolyzed in GI tract, but still has effect
Pseudoephedrine • Less active than ephedrine and less CNS stimulation • 240 mg daily for adults and 120 mg daily for children 6 to 12 yo and 60 mg daily for 2 to 6 yo • Peak effect 4 hrs after administration • Good for nasal stuffiness during sleep • Available as sustained release