OXYMETAZOLINE

US Approved OTC

First approved in 1964

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H24N2O
Molecular Weight	260.3746
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=C(CC2=NCCN2)C(C)=C(O)C(=C1)C(C)(C)C

InChI

InChIKey=WYWIFABBXFUGLM-UHFFFAOYSA-N

InChI=1S/C16H24N2O/c1-10-8-13(16(3,4)5)15(19)11(2)12(10)9-14-17-6-7-18-14/h8,19H,6-7,9H2,1-5H3,(H,17,18)

HIDE SMILES / InChI

Molecular Formula	C16H24N2O
Molecular Weight	260.3746
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.drugbank.ca/drugs/DB00935
Curator's Comment: Description was created based on several sources, including https://www.drugs.com/monograph/oxymetazoline-hydrochloride.html

Oxymetazoline is an adrenergic alpha-agonist, direct acting sympathomimetic, used as a vasoconstrictor to relieve nasal congestion The sympathomimetic action of oxymetazoline constricts the smaller arterioles of the nasal passages, producing a prolonged (up to 12 hours), gentle and decongesting effect. Oxymetazoline elicits relief of conjunctival hyperemia by causing vasoconstriction of superficial conjunctival blood vessels. The drug's action has been demonstrated in acute allergic conjunctivitis and in chemical (chloride) conjunctivitis. Oxymetazoline is self-medication for temporary relief of nasal congestion associated with the common cold, hay fever, or other upper respiratory allergies. Oxymetazoline is available over-the-counter as a topical decongestant in the form of oxymetazoline hydrochloride in nasal sprays such as Afrin, Operil, Dristan, Dimetapp, oxyspray, Facimin, Nasivin, Nostrilla, Sudafed OM, Vicks Sinex, Zicam, SinuFrin, and Mucinex Full Force. Due to its vasoconstricting properties, oxymetazoline is also used to treat nose bleeds and eye redness.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Adrenergic receptor alpha 65 Target ID: CHEMBL2095203 Sources: https://www.drugbank.ca/drugs/DB00935 \| https://www.ncbi.nlm.nih.gov/pubmed/20030735 \| https://www.ncbi.nlm.nih.gov/pubmed/11844675	Agonist 2752	4.96 null [pEC50]
Alpha-2a adrenergic receptor 70 Target ID: CHEMBL1867 Sources: https://www.drugbank.ca/drugs/DB00935 \| https://www.ncbi.nlm.nih.gov/pubmed/24365159 \| https://www.ncbi.nlm.nih.gov/pubmed/1974694	Partial Agonist 297	0.29 nM [Ki]
Serotonin 1a (5-HT1a) receptor 177 Target ID: CHEMBL214 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1678720	Agonist 2752	7.73 null [pEC50]
Serotonin 1d (5-HT1d) receptor 53 Target ID: CHEMBL1983 Sources: https://www.ncbi.nlm.nih.gov/pubmed/1678720	Agonist 2752	7.35 null [pEC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Nasal congestion 27 Sources: https://www.drugs.com/ppa/oxymetazoline-nasal.html	Palliative		Approved 8583	Oxymetazoline Hydrochloride Approved Use Temporary relief of nasal congestion (due to a cold, hay fever, or other upper respiratory allergies) and sinus congestion/pressure. Launch Date 1989
Eye irritations 2 Sources: https://www.drugs.com/cdi/oxymetazoline-drops.html	Primary		Approved 8583	OCUCLEAR Approved Use Relief of redness of eye due to minor eye irritations Launch Date 1986

C_max

Value	Dose	Co-administered	Analyte	Population
60.5 pg/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf	3 mg single, topical dose: 3 mg route of administration: Topical experiment type: SINGLE co-administered:		OXYMETAZOLINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.78 ng/mL DRUG LABEL https://www.fda.gov/media/98992/download	0.3 mg single, nasal dose: 0.3 mg route of administration: Nasal experiment type: SINGLE co-administered: Tetracaine	Tetracaine	OXYMETAZOLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
895 pg × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf	3 mg single, topical dose: 3 mg route of administration: Topical experiment type: SINGLE co-administered:		OXYMETAZOLINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4.24 ng × h/mL DRUG LABEL https://www.fda.gov/media/98992/download	0.3 mg single, nasal dose: 0.3 mg route of administration: Nasal experiment type: SINGLE co-administered: Tetracaine	Tetracaine	OXYMETAZOLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
5.23 h DRUG LABEL https://www.fda.gov/media/98992/download	0.3 mg single, nasal dose: 0.3 mg route of administration: Nasal experiment type: SINGLE co-administered: Tetracaine	Tetracaine	OXYMETAZOLINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
0.05 % single, intranasal Dose: 0.05 % Route: intranasal Route: single Dose: 0.05 % Sources: https://pubmed.ncbi.nlm.nih.gov/23679077	unhealthy, 4 years Health Status: unhealthy Age Group: 4 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23679077	Other AEs: Hypertensive crisis... Other AEs: Hypertensive crisis (1 patient) Sources: https://pubmed.ncbi.nlm.nih.gov/23679077
1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	Disc. AE: Application site dermatitis, Application site erythema... AEs leading to discontinuation/dose reduction: Application site dermatitis (1.4%) Application site erythema (0.5%) Application site pain (0.5%) Application site dryness (0.2%) Hypoesthesia (0.2%) Paresthesia (0.2%) Rash (0.2%) Urticaria (0.2%) Photosensitivity reaction (0.2%) Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
1.5 % 2 times / day multiple, topical Highest studied dose Dose: 1.5 %, 2 times / day Route: topical Route: multiple Dose: 1.5 %, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29462230	unhealthy, adult Health Status: unhealthy Age Group: adult Sources: https://pubmed.ncbi.nlm.nih.gov/29462230	Sources: https://pubmed.ncbi.nlm.nih.gov/29462230

AEs

AE	Significance	Dose	Population
Hypertensive crisis	1 patient	0.05 % single, intranasal Dose: 0.05 % Route: intranasal Route: single Dose: 0.05 % Sources: https://pubmed.ncbi.nlm.nih.gov/23679077	unhealthy, 4 years Health Status: unhealthy Age Group: 4 years Sex: M Sources: https://pubmed.ncbi.nlm.nih.gov/23679077
Application site dryness	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Hypoesthesia	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Paresthesia	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Photosensitivity reaction	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Rash	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Urticaria	0.2% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Application site erythema	0.5% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Application site pain	0.5% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914
Application site dermatitis	1.4% Disc. AE	1 % 1 times / day multiple, topical Dose: 1 %, 1 times / day Route: topical Route: multiple Dose: 1 %, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/29409914	unhealthy, 53.1 years (range: 19–81 years) Health Status: unhealthy Age Group: 53.1 years (range: 19–81 years) Sex: M+F Sources: https://pubmed.ncbi.nlm.nih.gov/29409914

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 substrate 1946	inhibitor 2438 substrate 1193	inhibitor 2507 substrate 1388	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP3A4/5 296	CYP2C19 1119 CYP1A2 1197 CYP2B6 776 CYP2C8 810 CYP2C18 149 CYP2E1 729 UGT1A9 423 UGT1A1 479 UGT1A3 470 UGT1A4 399 UGT1A6 343 UGT1A8 323 UGT1A10 331 UGT2B4 278 UGT2B7 456 UGT2B15 236 UGT2B17 237	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/208552s000lbl.pdf#page=6 Page: 6.0	no

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2B6 776	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2C18 149	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2C9 1193	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP2E1 729	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/ Page: 7.0	no
UGT1A1 479	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A10 331	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A3 470	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A4 399	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A6 343	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A8 323	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT2B15 236	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT2B17 237	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT2B4 278	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT2B7 456	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	no
UGT1A9 423	substrate 4014 Sources: https://jpharmsci.org/article/S0022-3549(15)32302-9/abstract	yes
CYP2C19 1119	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/; Page: 7.0	yes	no (co-administration study) Comment: concomitant oral moderate CYP2C19 inhibitors (e.g., esomeprazole, fluoxetine, and omeprazole): the results did not indicate an increase in oxymetazoline exposure associated with coadministration of oral moderate CYP2C19 inhibitors Sources: https://pubmed.ncbi.nlm.nih.gov/21177487/; Page: 7.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/208552Orig1s000PharmR.pdf#page=19 Page: 19.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:7862	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:7862
ChemicalBook	CB0371500	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB0371500
eMolecules	902254	https://www.emolecules.com/cgi-bin/more?vid=902254
ZINC	ZINC000000057435	http://zinc15.docking.org/substances/ZINC000000057435

PubMed

Title	Date	PubMed
Vasocontractile effects of alpha 2-adrenergic agonists associated with intracellular calcium release.	2002	12434541
Endothelial inhibitory modulation on the contractile responses to alpha 2-adrenergic agonists.	2002	12434540
[The relationship between ostial patency and medical treatment in acute maxillary sinusitis: an experimental study].	2002 Jul-Aug	12422083
Contractile responses of the rat vas deferens after epithelium removal.	2002 May 3	12269404
Search of antimicrobial activity of selected non-antibiotic drugs.	2002 Nov-Dec	12669766
Topical nasal anesthesia for transnasal fiberoptic laryngoscopy: a prospective, double-blind, cross-over study.	2003 Apr	12707645
Stimulation of interleukin-12 production in mouse macrophages via activation of p38 mitogen-activated protein kinase by alpha2-adrenoceptor agonists.	2003 Apr 25	12706479
Pharmacological characterization of alpha 2-adrenoceptor-mediated responses in pig nasal mucosa.	2003 Aug	15084187
alpha 2B-Adrenoceptor levels govern agonist and inverse agonist responses in PC12 cells.	2003 Aug 15	12890472
Evidence for nonadrenoceptor responses to imidazoline derivatives in the porcine isolated rectal artery.	2003 Dec	15028617
Alpha(2A)-adrenergic versus imidazoline receptor controversy in rilmenidine's action: alpha(2A)-antagonism in humans versus alpha(2A)-agonism in rabbits.	2003 Dec	15028600
Evidence for the role of alpha1D- and alpha1A-adrenoceptors in contraction of the rat mesenteric artery.	2003 Feb	12646397
Transdermal penetration of vasoconstrictors--present understanding and assessment of the human epidermal flux and retention of free bases and ion-pairs.	2003 Feb	12636167
5-HT7 receptor-mediated relaxation of the oviduct in nonpregnant proestrus pigs.	2003 Feb 14	12586216
Contractile actions of imidazoline alpha-adrenoceptor agonists and effects of noncompetitive alpha1-adrenoceptor antagonists in human vas deferens.	2003 Feb 21	12591110
Topical nasal anesthesia and laryngopharyngeal sensory testing: a prospective, double-blind crossover study.	2003 Jan	12537052
Functional characterisation of alpha(1)-adrenoceptors in denervated rat vas deferens.	2003 Jul	12845422
Central serous chorioretinopathy associated with administration of sympathomimetic agents.	2003 Jul	12834690
Stroke associated with sympathomimetics contained in over-the-counter cough and cold drugs.	2003 Jul	12791938
Alpha 2 adrenoceptor-mediated presynaptic inhibition of primary afferent glutamatergic transmission in rat substantia gelatinosa neurons.	2003 Mar	12606912
[The use of oxymetazoline in nasal endoscopic sinus surgery].	2003 May	12916356
[Tolerance and effectiveness of oxymetazoline and xylometazoline in treatment of acute rhinitis].	2003 Oct	14523532
Oligomerization of the alpha 1a- and alpha 1b-adrenergic receptor subtypes. Potential implications in receptor internalization.	2003 Oct 10	12888550
Oxymetazoline nasal spray three times daily for four weeks in normal subjects is not associated with rebound congestion or tachyphylaxis.	2003 Sep	14579657
Alpha 2-adrenoceptors in the basal ganglia have a role in memory consolidation and reinforcement.	2003 Sep	12871653
Sympathomimetic drug allergy: cross-reactivity study by patch test.	2004	15554736
Bulk is a determinant of oxymetazoline affinity for the alpha1A-adrenergic receptor.	2004	15512845
Chronic rhinosinusitis: management for optimal outcomes.	2004	15182211
Intranasal drug delivery: an alternative to intravenous administration in selected emergency cases.	2004 Apr	15039670
Chromatography studies on bio-affinity of nine ligands of alpha1-adrenoceptor to alpha1D subtypes overexpressed in cell membrane.	2004 Aug	15493479
Antimuscarinic action of oxymetazoline on human intraocular muscles.	2004 Aug	15321027
[Ethyl-3H]RS-79948-197 alpha2-adrenoceptor autoradiography validation in alpha2-adrenoceptor knockout mice.	2004 Aug 30	15336948
Behavioral effects of serotonin and serotonin agonists in two crayfish species, Procambarus clarkii and Orconectes rusticus.	2004 Dec	15596395
Construction and analytical applications of plastic membrane electrode for oxymetazoline hydrochloride.	2004 Feb	15055954
Human alpha1D-adrenoceptor phosphorylation and desensitization.	2004 May 15	15130762
The Janus faces of adrenoceptors: factors controlling the coupling of adrenoceptors to multiple signal transduction pathways.	2004 Nov	15566401
Thunderclap headache and reversible segmental cerebral vasoconstriction associated with use of oxymetazoline nasal spray.	2004 Sep 14	15367461
Use of mometasone furoate aqueous nasal spray in the treatment of rhinitis medicamentosa: an experimental study.	2005 Apr	15806055
Pulmonary edema following phenylephrine intranasal spray administration during the induction of general anesthesia in a child.	2005 Apr 30	15861508
Oxymetazoline solutions inhibit middle ear pathogens and are not ototoxic.	2005 Aug	16190099
Oxymetazoline is equivalent to ciprofloxacin in preventing postoperative otorrhea or tympanostomy tube obstruction.	2005 Feb	15689767
Early changes in insulin secretion and action induced by high-fat diet are related to a decreased sympathetic tone.	2005 Jan	15353406
An assessment for the presence of bacterial contamination of Venturi principle atomizers in a clinical setting.	2005 Jan-Feb	15794070
[Investigation of the effect of oxymetazoline on the duration of rhinitis].	2005 Oct 13	16270513
[Investigation of the effect of oxymetazoline on the duration of rhinitis. results of a placebo-controlled double-blind study in patients with acute rhinitis].	2005 Oct 6	16261947
[The observation of the ciliotoxicity of nasal mucosa with nasal decongestant].	2005 Sep	16375111
Pharmacological characterization of postjunctional alpha-adrenoceptors in human nasal mucosa.	2005 Sep-Oct	16270605
Oxymetazoline inhibits proinflammatory reactions: effect on arachidonic acid-derived metabolites.	2006 Feb	16221739
Nasal wall compliance in vasomotor rhinitis.	2006 Jan	16141379
Human breast cell lines exhibit functional alpha2-adrenoceptors.	2006 Jul	16292538

Patents

Sample Use Guides

In Vivo Use Guide

Pediatric Patients Nasal Congestion Intranasal For self-medication in children ≥6 years of age: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily. Conjunctival Congestion Ophthalmic For self-medication in children ≥6 years of age: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed. Adults Nasal Congestion Intranasal For self-medication: 2 or 3 sprays of a 0.05% nasal solution in each nostril every 10–12 hours (usually in the morning and evening), up to 2 times daily. Conjunctival Congestion Ophthalmic For self-medication: 1 or 2 drops of a 0.025% ophthalmic solution in the affected eye(s) every 6 hours as needed.

Route of Administration: Nasal

In Vitro Use Guide

Oxymetazoline had a concentration-dependent inhibitory effect on cultured human nasal CBF from 0.25 to 2.00 g/L.

Substance Class	Chemical Created by `admin` on `Wed Apr 02 08:25:58 GMT 2025` Edited by `admin` on `Wed Apr 02 08:25:58 GMT 2025`
Record UNII	8VLN5B44ZY
Record Status	`Validated (UNII)`
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Name

Type

Language

OXYMETAZOLINE

Official Name

English

OPERIL

Preferred Name

English

NASACON

Brand Name

English

AFRIN

Brand Name

English

OXYMETAZOLINE [VANDF]

Common Name

English

Oxymetazoline [WHO-DD]

Common Name

English

oxymetazoline [INN]

Common Name

English

PHENOL, 3-((4,5-DIHYDRO-1H-IMIDAZOL-2-YL)METHYL)-6-(1,1-DIMETHYLETHYL)-2,4-DIMETHYL-

Systematic Name

English

OXYMETAZOLINE [HSDB]

Common Name

English

6-TERT-BUTYL-3-(2-IMIDAZOLIN-2-YLMETHYL)-2,4-DIMETHYLPHENOL

Systematic Name

English

OXYMETAZOLINE [MI]

Common Name

English

Classification Tree Code System Code

WHO-VATC

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