Oxymetazoline

R01A - Decongestants and other nasal preparations for topical use ATC R01AA05 Small molecule approved 1986 Topical Natural product

JFDA label: Nasivin Drops

Indications

Approved

Eye Manifestations — eye allergy
Nasal Obstruction — Nasal congestion

Off-label

Erythema
Rhinitis, Allergic, Seasonal
Rosacea

Dosing

Source: openFDA

Directions • adults and children 6 to under 12 years of age (with adult supervision): 2 or 3 sprays in each nostril not more often than every 10 to 12 hours. Do not exceed 2 doses in any 24-hour period. • children under 6 years of age: ask a doctor To Use: Shake well before use. Hold white tabs, SQUEEZE grooved area of cap FIRMLY and turn counter clockwise. Before using the first time, prime metered pump by depressing pump firmly several times. To spray, hold bottle with thumb at base and nozzle between first and second fingers. Without tilting head, insert nozzle into nostril. Fully depress rim with a firm, even stroke and sniff deeply. Wipe nozzle clean after use. Secure cap after use.

Warnings & Precautions

Source: openFDA

Warnings & Precautions

Warnings Ask a doctor before use if you have • heart disease • high blood pressure • thyroid disease • diabetes • trouble urinating due to an enlarged prostate gland When using this product • do not use more than directed • do not use for more than 3 days. Use only as directed. Frequent or prolonged use may cause nasal congestion to recur or worsen. • temporary discomfort such as burning, stinging, sneezing or an increase in nasal discharge may occur • use of this container by more than one person may spread infection Stop use and ask a doctor if symptoms persist If pregnant or breast-feeding, ask a health professional before use. Keep out of reach of children. If swallowed, get medical help or contact a Poison Control Center right away (1-800-222-1222).

Pregnancy & Lactation

Pregnancy

Lactation

Caution Hale L3

It is recommended over oral systemic decongestants such as pseudoephedrine during breastfeeding. Topical use on the face is unlikely to present a risk to the nursing infant.

Chemistry & Properties

Formula	C16H24N2O
Molecular weight	260.38 g/mol
IUPAC name	6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol
CAS	1491-59-4
PubChem CID	4636
InChIKey	`WYWIFABBXFUGLM-UHFFFAOYSA-N`
logP	2.85 (XLogP 2.9)
Polar surface area	44.62 Å²
H-bond acceptors / donors	3 / 2
Drug-likeness (QED)	0.86
Lipinski violations	0

SMILES

Cc1cc(C(C)(C)C)c(O)c(C)c1CC1=NCCN1

Biology & Pharmacokinetics

Pharmacokinetics

BBB penetrant	No

Enzyme interactions

Enzyme	Role	Detail
CYP1A2	Substrate	—
CYP2C19	Substrate	—
CYP2D6	Inhibitor	IC₅₀ 0.20000000000000004 µM
CYP2D6	Substrate	—
CYP3A4	Substrate	—

Receptor binding (top 17)

Target	Action	Affinity
5-HT1B (HTR1B)	Binding	pKi 9.6
5-HT1B receptor (HTR1B)	Agonist	pKi 9.5
5-HT1D receptor (HTR1D)	Agonist	pKi 9.4
adrenergic Alpha2	Binding	pKi 8.9
α2B-adrenoceptor (ADRA2B)	Agonist	pIC50 8.8
adrenergic Alpha2A (ADRA2A)	Binding	pKi 8.4
α2A-adrenoceptor (ADRA2A)	Agonist	pIC50 8.4
α2B-adrenoceptor (ADRA2B)	Agonist	pEC50 7.7
adrenergic Alpha1C	Binding	pKi 7.6
adrenergic Alpha2C (ADRA2C)	Binding	pKi 7.0
5-HT2C (HTR2C)	Binding	pKi 6.9
α2C-adrenoceptor (ADRA2C)	Agonist	pEC50 6.9
5-HT2B (HTR2B)	Binding	pKi 6.8
adrenergic Alpha1	Binding	pKi 6.8
5-HT2A (HTR2A)	Binding	pKi 6.6

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (1)

Brand	Form / strength	Pack	Agent	Citizen (JOD)
Nasivin Drops	Oral Drops 0.05 %	10 ml	Professional Drug Store	0.690