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Role of Oxymetazoline in Management of Rhinosinusitis
Role of Oxymetazoline in Management of Rhinosinusitis
management of Rhinosinusitis in
daily practice
Meltzer EO, et al. Rhinosinusitis Diagnosis and Management for the Clinician:
Baraniuk JN.
Pathophysiology of nasal
• This reduce the physical congestion. International
as 10- 20%1
Diseases causing NC and Quality of Life (QOL)
1
Stewart M, Ferguson BJ, Fromer L. Epidemiology and burden of nasal congestion. International Journal of General Medicine .
2010; 3:37–45
Adrenergic Receptors
1
Tripathi KD. Essentials of Medical Pharmacology. New Delhi: Jaypee Brothers Medical Publishers;c2013:125-
137
α1, α2 β1, β2, β3
Classification of Nasal Decongestants
Phenylpropanolamin
Oxymetazoline Xylometazoline
e
OXYMETAZOLINE
1
Tripathi KD. Essentials of Medical Pharmacology. New Delhi:
Jaypee Brothers Medical Publishers;c2013:125-137
Overview of Nasal Decongestants
Mechanism of Action 2
• Oxymetazoline is a direct
acting sympathomimetic
amine
• Acts on alpha-adrenergic
receptors in the arterioles
Imidazole derivative with direct acting of the conjunctiva and
1
Oxymetazoline. PubChem.
sympathomimetic activity1 https://pubchem.ncbi.nlm.nih.g
nasal mucosa ov/compound/oxymetazoline#se
Chemical Name - 6-tert-butyl-3-(4,5- • In nasal it produces
ction=Top. Accessed. August
18,2015.
dihydro-1H-imidazol-2-ylmethyl)-2,4- 2
Oxymetazoline. DrugBank.
dimethylphenol constriction, resulting in http://www.drugbank.ca/drugs
/DB00935. Accessed. August
decreased blood flow and 18,2015.
Molecular Formula - C16H24N2O decreased nasal congestion
Molecular weight - 260.37456 g/mol
Common Dosage in Different Age Groups
Strength Dosage
Adults1 0.025% 4 to 6 drops to each nostril twice daily as needed
solution
0.05% 2 to 3 drops to each nostril twice daily as needed
solution
0.05% spray 2-3 sprays per nostril q12hr2
Pediatric1 0.025% >= 2 years to 5 years - 2 to 3 drops to each nostril
1
Oxymetazoline Nasal Dosage.
solution twice daily as needed. Drugs.com.
6 years to 18 years: 4 to 6 drops to each nostril twice http://www.drugs.com/dosage/
oxymetazoline-
daily as needed. nasal.html#Usual_Adult_Dose_fo
r_Nasal_Congestion. Accessed
0.05% >= 6 years to 18 years: 2 to 3 drops to each nostril September 18.09.2015. 2
solution twice daily as needed oxymetazoline (OTC).
Medscape.
0.05% spray >= 6 years to 18 years: 1 to 2 sprays to each nostril http://reference.medscape.co
m/drug/afrin-duramist-plus-
twice daily as needed oxymetazoline-343408.
Accessed September 22, 205.
Pharmacology
Pharmacokinetics- described as what the body does to a drug, refers
to the movement of drug into, through, and out of the body.1
Pharmacodynamics - study of what a drug does to the body
Pharmacokinetics2 Pharmacodynamics6
• Absorption • Used as a vasoconstrictor to relieve nasal
• Occasional systemic absorption may congestion
occur.2 Bioavailability of drug is 11%. 3 • Constricts the (Sympathomimetic action)
The time taken for (Tmax)peak plasma smaller arterioles of the nasal passages.
concentration is 5-10 minutes.4 • Produces a prolonged (up to 12 hours)
• Distribution decongesting effect.
• 80% protein binding.3
• Metabolism
• Half life of drug is 5-6 hours. 3
• Elimination
• Oxymetazoline is eliminated via kidney.5
1
Oxymetazoline Hydrochloride. Drug.com. http://www.drugs.com/monograph/oxymetazoline-hydrochloride.html. 2015. Accessed. August 18,2015.
2
OXYMETAZOLINE.toxnet. http://toxnet.nlm.nih.gov/cgi-bin/sis/search2/r?dbs+hsdb:@term+@rn+@rel+1491-59-4.2007. Accessed August 18, 2015.
Triple Action of Oxymetazoline
Anti-viral
Anti- inflammatory
Vasoconstrictive effect
OMZ has Virucidal Activity Against Human
Pathogenic Viruses
An in-vitro to demonstrate the antiviral activity of Oxymetazoline
on Human Rhinovirus
1
Koelsch S, Tschaikin
M, Sacher F. Anti-
Rhinovirus-specific
Activity of the Alpha-
sympathomimetic
Oxymetazoline.
Arzneimittel-
Forschung (Drug
A direct dose-dependent virucidal Virus titer was less after Research) .
2007;57(7):475–482.
activity of OMZ against HRV-14 treatment with OMZ
1)Sacher et al., 2005 Antiviral Properties of Oxymetazolin, DAZ, No. 5: 111-112 Glatthaar-Saalmueller B et al. 2005. Oxymetazoline exerts antiviral activity against human secretion and (vs. Saline solution)
rhinovirus-14 and downregulates expression of ist receptor ICAM-1 on human umbilical vein endothelial cells. OEGAI Annual Meeting, Graz/Austria, December 01-03: P51.
3)Beck-Speier et al., 2006, Oxymetazoline Inhibits Proinflammatory Reactions: Effects on Arachidonic Acid-Derived Metabolites, JPET 316: 843-851. Westerveld et germs
al,1995, Anti-oxidant actions of oxymethazoline an xylomethazoline, Eur J Clin Pharmacol 291: 27-31 Connell JT., 1969, Effectiveness of topical nasal decongestants.
Annals of Allergy 27: 541-546 Reinecke S. & Tschaikin M., 2005, Investigation of the effect of oxymetazoline on the duration of rhinitis. Results of a placebo-controlled
double-blind study in patients with acute rhinitis. MMW Fortschr Med 147 Suppl 3:113-118
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