Details of the Drug

General Information of Drug (ID: DM8ZXT6)

• Drug Name: Oxymetazoline
• Synonyms: Hazol; Iliadin; Nafrine; Navasin; Navisin; Nezeril; Oximetazolina; Oximetazolinum; Oxylazine; Oxymetazolinum; Oxymethazoline; Oxymetozoline; Rhinofrenol; Rhinolitan; Sinerol; Dristan Long Lasting Mentholated Nasal Spray; Dristan Long Lasting Nasal Mist; Drixoral Nasal Solution; Oxymeta zoline; Oxymetazoline hydrochloride crystalline; Afrin Cherry 12 Hour Nasal Spray; Afrin Extra Moisturizing 12 Hour Nasal Spray; Afrin Original 12 Hour Nasal Spray; Afrin Original 12 Hour Nose Drops; Afrin Original 12 Hour Pump Mist; Afrin Sinus 12 Hour Nasal Spray; Duramist Plus Up To 12 Hour Nasal Decongestant Spray; Genasal Nasal Spray Up to 12 Hour Relief; H 990; Nasal Relief 12 Hour Nasal Spray; Nostrilla 12 Hour Nasal Decongestant; Vicks Sinex 12 Hour Nasal Spray; Vicks Sinex 12 Hour Ultra Fine Mist for Sinus Relief; Decongestant (TN); Neo-Synephrine 12 Hour Spray; Operil (TN); Oximetazolina [INN-Spanish]; Oxymetazoline (INN); Oxymetazoline [INN:BAN]; Oxymetazolinum [INN-Latin]; Visine L.R; Visine L.R.; Phenol, 6-tert-butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethyl-(7CI,8CI); Phenol, 3-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethyl-(9CI); 2-(4-tert-Butyl-2,6-dimethyl-3-hydroxybenzyl)-2-imidazoline; 3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethyl-6-tert-butyl-phenol; 3-[(4,5-Dihydro-1H-imidazol-2-yl)methyl]-6-(1,1-dimethylethyl)-2,4-dimethylphenol; 6-t-Butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol; 6-tert-Butyl-3-(2-imidazolin-2-ylmethyl)-2,4-dimethylphenol; 6-tert-Butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol

Indication

Disease Entry	ICD 11	Status	REF
Eye inflammation	9A02	Approved	[1]
Nasal congestion	MD11.9	Approved	[1]

• Therapeutic Class: Nasal Decongestants
• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 260.37
  Topological Polar Surface Area (xlogp); 2.9
  Rotatable Bond Count (rotbonds); 3
  Hydrogen Bond Donor Count (hbonddonor); 2
  Hydrogen Bond Acceptor Count (hbondacc); 2
• ADMET Property:
  Absorption AUC: The area under the plot of plasma concentration (AUC) of drug is 0.895 +/- 0.798 mcgh/L [2]
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 60.5 +/- 53.9 ng/L [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 8.3 hours [3]
  Metabolism: The drug is metabolized via the human liver enzymes to produce mono-oxygenated and dehydrogenated metabolites [4]
• Chemical Identifiers:
  Formula: C16H24N2O
  IUPAC Name: 6-tert-butyl-3-(4,5-dihydro-1H-imidazol-2-ylmethyl)-2,4-dimethylphenol
  Canonical SMILES: CC1=CC(=C(C(=C1CC2=NCCN2)C)O)C(C)(C)C
  InChI: 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)
  InChIKey: WYWIFABBXFUGLM-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 4636
  ChEBI ID: CHEBI:7862
  CAS Number: 1491-59-4
  DrugBank ID: DB00935
  TTD ID: D09EBS
  INTEDE ID: DR1224
  ACDINA ID: D01309

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Adrenergic receptor Alpha-2 (ADRA2)	TTQ8AFT	NOUNIPROTAC	Agonist	[5]

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
UDP-glucuronosyltransferase 1A1 (UGT1A1) Main DME	DEYGVN4	UD11_HUMAN	Substrate	[6]

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Oxymetazoline (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Methylene blue	DMJAPE7	Moderate	Decreased metabolism of Oxymetazoline caused by Methylene blue mediated inhibition of non-CYP450 enzyme.	Acquired methaemoglobinaemia [3A93]	[26]
Levomilnacipran	DMV26S8	Moderate	Increased risk of rapid heart rate by the combination of Oxymetazoline and Levomilnacipran.	Chronic pain [MG30]	[27]
Selegiline	DM6034S	Moderate	Decreased metabolism of Oxymetazoline caused by Selegiline mediated inhibition of non-CYP450 enzyme.	Depression [6A70-6A7Z]	[26]
Isocarboxazid	DMAF1NB	Moderate	Decreased metabolism of Oxymetazoline caused by Isocarboxazid mediated inhibition of non-CYP450 enzyme.	Depression [6A70-6A7Z]	[26]
Milnacipran	DMBFE74	Moderate	Additive hypertensive effects by the combination of Oxymetazoline and Milnacipran.	Depression [6A70-6A7Z]	[27]
Desvenlafaxine	DMHD4PE	Moderate	Increased risk of rapid heart rate by the combination of Oxymetazoline and Desvenlafaxine.	Depression [6A70-6A7Z]	[27]
Procarbazine	DMIK367	Moderate	Decreased metabolism of Oxymetazoline caused by Procarbazine mediated inhibition of non-CYP450 enzyme.	Hodgkin lymphoma [2B30]	[26]
Ozanimod	DMT6AM2	Moderate	Decreased metabolism of Oxymetazoline caused by Ozanimod mediated inhibition of non-CYP450 enzyme.	Multiple sclerosis [8A40]	[26]
Sibutramine	DMFJTDI	Moderate	Increased risk of rapid heart rate by the combination of Oxymetazoline and Sibutramine.	Obesity [5B80-5B81]	[28]
Safinamide	DM0YWJC	Moderate	Decreased metabolism of Oxymetazoline caused by Safinamide mediated inhibition of non-CYP450 enzyme.	Parkinsonism [8A00]	[26]
Rasagiline	DM3WKQ4	Moderate	Decreased metabolism of Oxymetazoline caused by Rasagiline mediated inhibition of non-CYP450 enzyme.	Parkinsonism [8A00]	[26]
Ergonovine	DM0VEC1	Major	Additive hypertensive effects by the combination of Oxymetazoline and Ergonovine.	Postpartum haemorrhage [JA43]	[29]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Benzyl alcohol	E00010	244	Antimicrobial preservative; Solvent
Butylated hydroxytoluene	E00336	31404	Antioxidant
Hydrochloric acid	E00015	313	Acidulant
Kyselina citronova	E00014	311	Acidulant; Antioxidant; Buffering agent; Complexing agent; Flavoring agent
methylparaben	E00149	7456	Antimicrobial preservative
Potassium chloride	E00074	4873	Tonicity agent
Propylparaben sodium	E00567	23679044	Antimicrobial preservative
Sodium citrate anhydrous	E00102	6224	Alkalizing agent; Buffering agent; Complexing agent; Emulsifying agent
Diisopropyl adipate	E00277	23368	Emollient
Oleyl alcohol	E00475	5284499	Emollient; Emulsifying agent; Penetration agent; Solubilizing agent
Sodium acetate	E00431	517045	Antimicrobial preservative; Buffering agent; Flavoring agent
Calcium chloride	E00474	5284359	Antimicrobial preservative; Desiccant
Cetostearyl alcohol	E00353	62238	Emollient; Emulsifying agent; Viscosity-controlling agent
Edetate disodium	E00186	8759	Complexing agent
Hypromellose	E00634	Not Available	Coating agent
Medium-chain triglyceride	E00640	Not Available	Emollient; Lubricant; Surfactant
Polyethylene glycol 300	E00651	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Sodium chloride	E00077	5234	Diluent; Tonicity agent
Sodium citrate dihydrate	E00369	71474	Alkalizing agent; Buffering agent; Complexing agent; Emulsifying agent
Sodium hydroxide	E00234	14798	Alkalizing agent
Stearyl alcohol	E00172	8221	Emollient; Emulsifying agent; Stiffening agent; Viscosity-controlling agent
Water	E00035	962	Solvent
Ethylene glycol stearate	E00312	24762	Emollient; Emulsion stabilizing agent
Lanolin	E00375	75778	Emollient; Emulsifying agent; Ointment base
Magnesium chloride	E00479	5360315	Viscosity-controlling agent
Phenoxyethanol	E00329	31236	Antimicrobial preservative
Hydroxyethyl cellulose	E00700	Not Available	Coating agent; Suspending agent; Binding agent; Viscosity-controlling agent

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Oxymetazoline 1% cream	1%	Cream	Topical
Oxymetazoline 0.1% solution	0.10%	Solution	Ophthalmic
Oxymetazoline 0.1mg/spray spray	0.1mg/spray	Spray	Nasal
Oxymetazoline 6mg/spray spray	6mg/spray	Spray	Nasal

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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