Oxymetazoline

Vasoconstrictor — DERMATOLOGICALS

Key facts

Oxymetazoline is an ofp drug in the Vasoconstrictor class catalogued in DrugCentral. It was first approved by the FDA in 1986. DrugCentral lists 29 molecular targets, including ADRA2A, HTR1B and HTR1D. Recorded indications include Local anesthesia, Nasal congestion, Nasal discharge and Persistent erythema of skin.

• Approval status: ofp (first approved 1986 by the FDA).
• Drug class: Vasoconstrictor.
• Molecular targets: ADRA2A, HTR1B, HTR1D and Htr1b (29 listed in DrugCentral).
• Indications: Local anesthesia, Nasal congestion, Nasal discharge, Persistent erythema of skin and Red eye.
• ATC code: D11AX27 (Other dermatologicals).
• Molecular formula: C16H24N2O; molecular weight 260.38 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (5)

• Local anesthesia
• Nasal congestion
• Nasal discharge
• Persistent erythema of skin
• Red eye

Contraindications (11)

• Angle-closure glaucoma
• Arteriosclerotic vascular disease
• Benign prostatic hyperplasia
• Diabetes mellitus
• Disorder of coronary artery
• Eye infection
• Heart disease
• Hypertensive disorder
• Hyperthyroidism
• Pain in eye
• Visual impairment

Mechanism & targets

• Established pharmacologic class: Vasoconstrictor

Molecular targets (29)

Target	Gene	Action	Activity
Alpha-2A adrenergic receptor	ADRA2A	agonist	Ki 9.54
5-hydroxytryptamine receptor 1B	HTR1B	unknown	Ki 9.52
5-hydroxytryptamine receptor 1D	HTR1D	unknown	Ki 9.40
5-hydroxytryptamine receptor 1B	Htr1b	unknown	Ki 9.04
Alpha-2C adrenergic receptor	ADRA2C	agonist	Ki 9.00
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 8.82
Adrenergic receptor alpha-2	Adra2b|Adra2c|Adra2a	unknown	Ki 8.72
5-hydroxytryptamine receptor 1A	HTR1A	unknown	Ki 8.49
5-hydroxytryptamine receptor 1A	Htr1a	unknown	IC50 8.25
Nischarin	NISCH	unknown	Ki 8.21
Alpha-1A adrenergic receptor	ADRA1A	agonist	Ki 8.20
Alpha-1A adrenergic receptor	Adra1a	unknown	Ki 8.19
Alpha-1A adrenergic receptor	ADRA1A	unknown	Ki 7.88
Alpha-2A adrenergic receptor	ADRA2A	unknown	Ki 7.68
Alpha-2 adrenergic receptor	Adra2b|Adra2c|Adra2a	unknown	Ki 7.48
5-hydroxytryptamine receptor 2B	HTR2B	unknown	Ki 6.83
5-hydroxytryptamine receptor 2C	HTR2C	agonist	Ki 6.80
Cytochrome P450 2D6	CYP2D6	unknown	IC50 6.70
Alpha-1B adrenergic receptor	ADRA1B	unknown	Ki 6.69
5-hydroxytryptamine receptor 2A	HTR2A	unknown	Ki 6.59

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1986-05-30	FDA	—	BAYER HEALTHCARE LLC

ATC classification

ATC code	Therapeutic hierarchy
D11AX27	DERMATOLOGICALS › OTHER DERMATOLOGICAL PREPARATIONS › OTHER DERMATOLOGICAL PREPARATIONS › Other dermatologicals
R01AA05	RESPIRATORY SYSTEM › NASAL PREPARATIONS › DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE › Sympathomimetics, plain
R01AB07	RESPIRATORY SYSTEM › NASAL PREPARATIONS › DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE › Sympathomimetics, combinations excl. corticosteroids
S01GA04	SENSORY ORGANS › OPHTHALMOLOGICALS › DECONGESTANTS AND ANTIALLERGICS › Sympathomimetics used as decongestants

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Mydriasis	95.2
Eye irritation	93.7
Ocular hyperaemia	72.6
Vision blurred	71.5
Swelling of eyelid	53.8
Nasal congestion	51.8
Hypervolaemia	40.9
Cerebral vasoconstriction	40.6
Epistaxis	35.7
Trigemino-cardiac reflex	35.6
Nasal discomfort	30.9
Lacrimation increased	28.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Oxymetazoline is on its molecule page.

• Molecular formula: C₁₆H₂₄N₂O
• Molecular weight: 260.38 g/mol
• CAS number: 1491-59-4
• InChIKey: WYWIFABBXFUGLM-UHFFFAOYSA-N
• PubChem CID: 4636

CC1=CC(=C(O)C(C)=C1CC1=NCCN1)C(C)(C)C

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Oxymetazoline used for?

DrugCentral lists the following indications for Oxymetazoline: Local anesthesia, Nasal congestion, Nasal discharge, Persistent erythema of skin and Red eye.

How does Oxymetazoline work?

Its molecular targets in DrugCentral include ADRA2A (agonist), HTR1B, HTR1D and Htr1b.

When was Oxymetazoline first approved?

Oxymetazoline was first approved by the FDA in 1986.

What drug class does Oxymetazoline belong to?

Oxymetazoline is in the Vasoconstrictor class.

What is the chemical formula of Oxymetazoline?

Oxymetazoline has the molecular formula C16H24N2O and a molecular weight of 260.38 g/mol.

Sources

• DrugCentral drug card 2032 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1200791 — compound record and bioactivity
• PubChem CID 4636 — chemical identifiers
• DrugBank DB00935 — drug record
• FDA UNII 8VLN5B44ZY — substance identity
• DailyMed: FDA labels for Oxymetazoline — current prescribing information (label search)
• UniProt P08913 (ADRA2A) — target protein
• UniProt P28222 (HTR1B) — target protein
• UniProt P28221 (HTR1D) — target protein
• UniProt P18825 (ADRA2C) — target protein
• UniProt P08908 (HTR1A) — target protein
• UniProt Q9Y2I1 (NISCH) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.