Stem definition | Drug id | CAS RN |
---|---|---|
antihistaminics or local vasoconstrictors, antazoline derivatives | 2032 | 1491-59-4 |
Dose | Unit | Route |
---|---|---|
0.40 | mg | N |
Property | Value | Reference |
---|---|---|
BA (Bioavailability) | 11 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Date | Agency | Company | Orphan |
---|---|---|---|
May 30, 1986 | FDA | BAYER HEALTHCARE LLC |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Anosmia | 102.61 | 19.09 | 27 | 2870 | 3904 | 50598323 |
Mydriasis | 54.05 | 19.09 | 21 | 2876 | 10606 | 50591621 |
Trigemino-cardiac reflex | 46.96 | 19.09 | 7 | 2890 | 48 | 50602179 |
Ageusia | 35.64 | 19.09 | 16 | 2881 | 11567 | 50590660 |
Nasal congestion | 31.64 | 19.09 | 25 | 2872 | 51095 | 50551132 |
Nasal discomfort | 28.25 | 19.09 | 10 | 2887 | 3894 | 50598333 |
Eye irritation | 26.92 | 19.09 | 15 | 2882 | 17125 | 50585102 |
Electrocardiogram ST segment depression | 23.97 | 19.09 | 8 | 2889 | 2612 | 50599615 |
Cerebral vasoconstriction | 22.02 | 19.09 | 6 | 2891 | 986 | 50601241 |
Hypervolaemia | 21.44 | 19.09 | 15 | 2882 | 25484 | 50576743 |
Amaurosis | 20.47 | 19.09 | 5 | 2892 | 535 | 50601692 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Anosmia | 61.94 | 20.84 | 16 | 1828 | 1975 | 29570708 |
Epistaxis | 29.56 | 20.84 | 25 | 1819 | 51679 | 29521004 |
Vision blurred | 24.14 | 20.84 | 20 | 1824 | 40156 | 29532527 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Anosmia | 129.13 | 17.74 | 34 | 4112 | 4383 | 64490203 |
Mydriasis | 56.92 | 17.74 | 25 | 4121 | 15287 | 64479299 |
Ageusia | 40.13 | 17.74 | 19 | 4127 | 13794 | 64480792 |
Trigemino-cardiac reflex | 35.73 | 17.74 | 7 | 4139 | 237 | 64494349 |
Epistaxis | 34.88 | 17.74 | 37 | 4109 | 98094 | 64396492 |
Nasal discomfort | 33.47 | 17.74 | 12 | 4134 | 4316 | 64490270 |
Hypervolaemia | 28.70 | 17.74 | 22 | 4124 | 38263 | 64456323 |
Nasal congestion | 27.66 | 17.74 | 26 | 4120 | 59632 | 64434954 |
Hyposmia | 24.61 | 17.74 | 6 | 4140 | 566 | 64494020 |
Eye irritation | 23.72 | 17.74 | 14 | 4132 | 15842 | 64478744 |
Cerebral vasoconstriction | 20.10 | 17.74 | 6 | 4140 | 1216 | 64493370 |
Electrocardiogram ST segment depression | 19.05 | 17.74 | 8 | 4138 | 4381 | 64490205 |
None
Source | Code | Description |
---|---|---|
ATC | D11AX27 | DERMATOLOGICALS OTHER DERMATOLOGICAL PREPARATIONS OTHER DERMATOLOGICAL PREPARATIONS Other dermatologicals |
ATC | R01AA05 | RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Sympathomimetics, plain |
ATC | R01AB07 | RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Sympathomimetics, combinations excl. corticosteroids |
ATC | S01GA04 | SENSORY ORGANS OPHTHALMOLOGICALS DECONGESTANTS AND ANTIALLERGICS Sympathomimetics used as decongestants |
FDA CS | M0461078 | Imidazolines |
FDA PE | N0000009908 | Vasoconstriction |
MeSH PA | D018663 | Adrenergic Agents |
MeSH PA | D000322 | Adrenergic Agonists |
MeSH PA | D000316 | Adrenergic alpha-Agonists |
MeSH PA | D002317 | Cardiovascular Agents |
MeSH PA | D014663 | Nasal Decongestants |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D018373 | Peripheral Nervous System Agents |
MeSH PA | D019141 | Respiratory System Agents |
MeSH PA | D013566 | Sympathomimetics |
MeSH PA | D014662 | Vasoconstrictor Agents |
CHEBI has role | CHEBI:35524 | sympathomimetic |
CHEBI has role | CHEBI:35569 | alpha-adrenergic agonists |
CHEBI has role | CHEBI:77715 | nasal decongestants |
FDA PE | N0000175651 | Increased Sympathetic Activity |
FDA EPC | N0000192562 | Vasoconstrictor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Nasal discharge | indication | 64531003 | |
Nasal congestion | indication | 68235000 | |
Red eye | indication | 75705005 | |
Local anesthesia | indication | 386761002 | |
Persistent erythema of skin | indication | 420356000 | |
Hyperthyroidism | contraindication | 34486009 | DOID:7998 |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Pain in eye | contraindication | 41652007 | |
Heart disease | contraindication | 56265001 | DOID:114 |
Arteriosclerotic vascular disease | contraindication | 72092001 | |
Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
Eye infection | contraindication | 128351009 | |
Benign prostatic hyperplasia | contraindication | 266569009 | |
Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
Visual impairment | contraindication | 397540003 | |
Disorder of coronary artery | contraindication | 414024009 |
None
None
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 11.6 | acidic |
pKa2 | 10.99 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 8815929 | Jan. 22, 2024 | TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS WITH 1% OXYMETAZOLINE HYDROCHLORIDE CREAM |
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 8420688 | Aug. 2, 2024 | TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS WITH 1% OXYMETAZOLINE HYDROCHLORIDE CREAM |
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 7812049 | May 2, 2028 | TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS WITH 1% OXYMETAZOLINE HYDROCHLORIDE CREAM |
0.1MG/SPRAY;6MG/SPRAY | KOVANAZE | ST RENATUS | N208032 | June 29, 2016 | RX | SPRAY, METERED | NASAL | 8580282 | April 2, 2030 | METHOD OF ANESTHETIZING AT LEAST A PORTION OF THE MAXILLARY DENTAL ARCH |
0.1MG/SPRAY;6MG/SPRAY | KOVANAZE | ST RENATUS | N208032 | June 29, 2016 | RX | SPRAY, METERED | NASAL | 9308191 | April 2, 2030 | METHOD OF ANESTHETIZING AT LEAST A PORTION OF THE MAXILLARY DENTAL ARCH |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 10912765 | Aug. 26, 2031 | METHOD OF TREATING BLEPHAROPTOSIS |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 8357714 | Aug. 26, 2031 | METHOD OF TREATING BLEPHAROPTOSIS |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 9867808 | Aug. 26, 2031 | METHOD OF TREATING BLEPHAROPTOSIS |
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 10335391 | June 11, 2035 | ONCE DAILY TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS WITH 1% OXYMETAZOLINE HYDROCHLORIDE CREAM, WHERE THE PATIENT EXPERIENCES NO REBOUND OR WORSENING OF FACIAL ERYTHEMA POST-TREATMENT |
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 10751325 | June 11, 2035 | ONCE DAILY TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS |
1% | RHOFADE | EPI HLTH | N208552 | Jan. 18, 2017 | RX | CREAM | TOPICAL | 9974773 | June 11, 2035 | ONCE DAILY TOPICAL TREATMENT OF PERSISTENT FACIAL ERYTHEMA ASSOCIATED WITH ROSACEA IN ADULTS WITH 1% OXYMETAZOLINE HYDROCHLORIDE CREAM |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 10799481 | Dec. 16, 2039 | METHOD OF TREATING BLEPHAROPTOSIS |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 10940138 | Dec. 16, 2039 | METHOD OF TREATING BLEPHAROPTOSIS |
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | 11324722 | Dec. 16, 2039 | METHOD OF TREATING BLEPHAROPTOSIS |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
---|---|---|---|---|---|---|---|---|---|
0.1% | UPNEEQ | RVL PHARMS | N212520 | July 8, 2020 | RX | SOLUTION/DROPS | OPHTHALMIC | July 8, 2023 | NEW PRODUCT |
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Alpha-1A adrenergic receptor | GPCR | AGONIST | Ki | 8.20 | IUPHAR | SCIENTIFIC LITERATURE | |||
Alpha-2B adrenergic receptor | GPCR | AGONIST | Ki | 6.20 | IUPHAR | SCIENTIFIC LITERATURE | |||
5-hydroxytryptamine receptor 2A | GPCR | Ki | 6.59 | PDSP | |||||
5-hydroxytryptamine receptor 2B | GPCR | Ki | 6.83 | PDSP | |||||
5-hydroxytryptamine receptor 2C | GPCR | AGONIST | Ki | 6.80 | IUPHAR | ||||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 6.11 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.34 | DRUG MATRIX | |||||
Muscarinic acetylcholine receptor M5 | GPCR | Ki | 6.02 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 1B | GPCR | Ki | 9.52 | CHEMBL | |||||
5-hydroxytryptamine receptor 1D | GPCR | Ki | 9.40 | CHEMBL | |||||
Alpha-2C adrenergic receptor | GPCR | AGONIST | Ki | 9 | CHEMBL | ||||
Cytochrome P450 2D6 | Enzyme | IC50 | 6.70 | DRUG MATRIX | |||||
Alpha-1D adrenergic receptor | GPCR | AGONIST | Ki | 6.40 | IUPHAR | ||||
Alpha-1B adrenergic receptor | GPCR | AGONIST | Ki | 6.50 | IUPHAR | ||||
Alpha-2A adrenergic receptor | GPCR | AGONIST | Ki | 9.54 | CHEMBL | ||||
Nischarin | Membrane receptor | Ki | 8.21 | CHEMBL | |||||
5-hydroxytryptamine receptor 1E | GPCR | Ki | 6.38 | PDSP | |||||
5-hydroxytryptamine receptor 1A | GPCR | Ki | 8.49 | DRUG MATRIX | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 6.16 | DRUG MATRIX | |||||
5-hydroxytryptamine receptor 1B | GPCR | Ki | 9.04 | DRUG MATRIX | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 8.19 | CHEMBL | |||||
Alpha-1D adrenergic receptor | GPCR | Ki | 6.48 | CHEMBL | |||||
5-hydroxytryptamine receptor 1A | GPCR | IC50 | 8.25 | CHEMBL | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 7.88 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 7.68 | CHEMBL | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 8.82 | CHEMBL | |||||
Alpha-1B adrenergic receptor | GPCR | Ki | 6.69 | CHEMBL | |||||
Adrenergic receptor alpha-2 | GPCR | Ki | 8.72 | CHEMBL | |||||
Alpha-2 adrenergic receptor | GPCR | Ki | 7.48 | CHEMBL |
ID | Source |
---|---|
4019463 | VUID |
N0000147584 | NUI |
D01022 | KEGG_DRUG |
2315-02-8 | SECONDARY_CAS_RN |
4019462 | VANDF |
4019463 | VANDF |
C0030071 | UMLSCUI |
CHEBI:7862 | CHEBI |
J5C | PDB_CHEM_ID |
CHEMBL762 | ChEMBL_ID |
DB00935 | DRUGBANK_ID |
CHEMBL1200791 | ChEMBL_ID |
D010109 | MESH_DESCRIPTOR_UI |
4636 | PUBCHEM_CID |
124 | IUPHAR_LIGAND_ID |
1400 | INN_ID |
8VLN5B44ZY | UNII |
106101 | RXNORM |
5218 | MMSL |
5411 | MMSL |
5424 | MMSL |
001810 | NDDF |
004728 | NDDF |
29129004 | SNOMEDCT_US |
387158001 | SNOMEDCT_US |
9910008 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
RHOFADE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0023-5300 | CREAM | 10 mg | TOPICAL | NDA | 26 sections |
good sense nasal | HUMAN OTC DRUG LABEL | 1 | 0113-0065 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
Good Sense Nasal | HUMAN OTC DRUG LABEL | 1 | 0113-0304 | SPRAY | 0.50 mg | NASAL | OTC monograph final | 14 sections |
good sense nasal | HUMAN OTC DRUG LABEL | 1 | 0113-0388 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
Good Sense Nasal | HUMAN OTC DRUG LABEL | 1 | 0113-0817 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
Nasal | HUMAN OTC DRUG LABEL | 1 | 0113-2304 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
basic care nasal | HUMAN OTC DRUG LABEL | 1 | 0113-7388 | SPRAY | 0.05 g | NASAL | OTC monograph final | 13 sections |
basic care no drip nasal | HUMAN OTC DRUG LABEL | 1 | 0113-7494 | SPRAY | 0.05 g | NASAL | OTC monograph final | 13 sections |
Anefrin NasalOriginal | HUMAN OTC DRUG LABEL | 1 | 0363-0304 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
Anefrin NasalOriginal | HUMAN OTC DRUG LABEL | 1 | 0363-0304 | SPRAY | 0.05 g | NASAL | OTC monograph final | 14 sections |
Severe Anefrin | HUMAN OTC DRUG LABEL | 1 | 0363-2021 | LIQUID | 0.05 g | NASAL | OTC monograph final | 11 sections |
No Drip Nasal Mist | HUMAN OTC DRUG LABEL | 1 | 0363-2303 | LIQUID | 50 mg | NASAL | OTC monograph final | 13 sections |
Severe Sinus Relief Mist | HUMAN OTC DRUG LABEL | 1 | 0363-2305 | LIQUID | 50 mg | NASAL | OTC monograph final | 13 sections |
No Drip Nasal Mist | HUMAN OTC DRUG LABEL | 1 | 0363-2307 | LIQUID | 50 mg | NASAL | OTC monograph final | 12 sections |
Nasal MistWalgreens | HUMAN OTC DRUG LABEL | 1 | 0363-7000 | LIQUID | 0.05 g | TOPICAL | OTC monograph final | 8 sections |
Severe Congestion Nasal no dripWalgreens | HUMAN OTC DRUG LABEL | 1 | 0363-7001 | LIQUID | 0.05 g | TOPICAL | OTC monograph final | 9 sections |
Maximum Strenth Nasal | HUMAN OTC DRUG LABEL | 1 | 0363-7003 | LIQUID | 0.05 g | TOPICAL | OTC monograph final | 7 sections |
Extra Moisturizing No Drip NasalWalgreens | HUMAN OTC DRUG LABEL | 1 | 0363-7004 | LIQUID | 0.05 g | TOPICAL | OTC monograph final | 7 sections |
Original No Drip NasalWalgreens | HUMAN OTC DRUG LABEL | 1 | 0363-7005 | LIQUID | 0.05 g | TOPICAL | OTC monograph final | 7 sections |
No Drip Anefrin Nasal | HUMAN OTC DRUG LABEL | 1 | 0363-7007 | LIQUID | 0.05 g | NASAL | OTC monograph final | 11 sections |
Severe Sinus Relief Mist | HUMAN OTC DRUG LABEL | 1 | 0363-7009 | LIQUID | 50 mg | NASAL | OTC monograph final | 15 sections |
Walgreen | HUMAN OTC DRUG LABEL | 1 | 0363-7151 | SPRAY | 0.05 g | NASAL | OTC monograph final | 13 sections |
DRISTAN 12 HR | HUMAN OTC DRUG LABEL | 1 | 0573-1191 | SPRAY | 0.50 mg | NASAL | OTC monograph final | 14 sections |
nasal decongestant | HUMAN OTC DRUG LABEL | 1 | 0904-6761 | SPRAY | 0.05 g | NASAL | OTC monograph final | 13 sections |
Major | HUMAN OTC DRUG LABEL | 1 | 0904-7006 | SPRAY | 0.05 g | NASAL | OTC monograph final | 13 sections |
7 Select Original Nasal | HUMAN OTC DRUG LABEL | 1 | 10202-849 | SPRAY | 0.05 g | NASAL | OTC monograph final | 11 sections |
Zicam Extreme Congestion Relief | HUMAN OTC DRUG LABEL | 1 | 10237-464 | SPRAY | 0.50 mg | NASAL | OTC monograph final | 14 sections |
Zicam Intense Sinus Relief | HUMAN OTC DRUG LABEL | 1 | 10237-471 | SPRAY | 0.50 mg | NASAL | OTC monograph final | 15 sections |
Afrin NoDrip Allergy Sinus Night | HUMAN OTC DRUG LABEL | 1 | 11523-0034 | SPRAY | 0.50 mg | NASAL | OTC monograph final | 14 sections |
Afrin Allergy Sinus Nasal | HUMAN OTC DRUG LABEL | 1 | 11523-0073 | SPRAY | 0.50 g | NASAL | OTC monograph final | 14 sections |