tetryzoline 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
antihistaminics or local vasoconstrictors, antazoline derivatives 3591 84-22-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tetrahydrozoline nitrate
  • tetrahydrozoline
  • (+/-)-Tetrahydrozoline
  • ocuzolin
  • tetryzolin
  • tetryzoline
  • dl-Tetrahydrozoline
  • tetrahydrozoline hydrochloride
  • tetrahydrozeline hydrochloride
  • tetrahydrozeline nitrate
  • tetrahydrozoline HCl
  • tetrahydrozeline HCl
used as nasal decongestant; Visine is a form of eye drops; RN given refers to parent cpd; structure
  • Molecular weight: 200.29
  • Formula: C13H16N2
  • CLOGP: 3.54
  • LIPINSKI: 0
  • HAC: 2
  • HDO: 1
  • TPSA: 24.39
  • ALOGS: -2.92
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
0.80 mg N

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
azlogd74 LogD at pH 7.4 -0.549 High 1
caco2-efflux Caco-2 efflux ratio (BA/AB) 0.378 High 1
caco2-intrinsic-papp Caco-2 intrinsic apparent permeability 12.162 10^-6 cm/s High 1
dh-clint Dog hepatocyte intrinsic clearance 4.083 uL/min/10^6 cells High 1
dppb Dog plasma protein binding (% unbound) 79.590 % High 1
fcs-ppb Fetal calf serum protein binding (% unbound) 66.670 % High 1
herg hERG pIC50 4.436 pIC50 High 1
hh-clint Human hepatocyte intrinsic clearance 2.128 uL/min/10^6 cells High 1
hlm-clint Human liver microsomal intrinsic clearance 4.571 uL/min/mg protein High 1
hppb Human plasma protein binding (% unbound) 79.810 % High 1
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,EIF2AK3,GRK2,ITK,MAPK10,PDK4,TGFBR1 11
mdck-mdr1-efflux MDCK-MDR1 efflux ratio 0.711 High 1
mh-clint Mouse hepatocyte intrinsic clearance 48.978 High 1
mppb Mouse plasma protein binding (% unbound) 72.180 High 1
nih-mdck-mdr1-efflux NIH MDCK-MDR1 efflux ratio 0.887 High 1
pfas-class PFAS structural alert (1 = True, 0 = False) 0
pppb Pig plasma protein binding (% unbound) 75.810 % High 1
rh-clint Rat hepatocyte intrinsic clearance 57.810 uL/min/10^6 cells High 1
rh-fuinc Rat hepatocyte fraction unbound in incubation 89.590 % High 1
rppb Rat plasma protein binding (% unbound) 74.120 % High 1
solubility-dd Solubility at pH 7.4 in DMSO 887.156 uM High 1

Approvals:

DateAgencyCompanyOrphan
Nov. 30, 1979 FDA FOUGERA PHARMS

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Dry eye 22.13 18.43 11 886 57920 90569630

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Catarrh 211.60 118.14 55 3071 5931 42612278
Burns second degree 210.60 118.14 55 3071 6041 42612168
Steroid dependence 205.27 118.14 55 3071 6667 42611542
Parosmia 197.93 118.14 55 3071 7636 42610573
Hypopnoea 196.60 118.14 55 3071 7827 42610382
Gingival pain 192.53 118.14 55 3071 8439 42609770
Systemic lupus erythematosus 187.46 118.14 55 3071 9269 42608940
Rhinitis 173.88 118.14 55 3071 11922 42606287
Cardiac murmur 170.39 118.14 55 3071 12720 42605489
Alcohol poisoning 162.49 118.14 47 3079 7527 42610682
Impaired work ability 161.02 118.14 52 3074 12039 42606170
Bronchiectasis 155.61 118.14 56 3070 17963 42600246
Frequent bowel movements 149.81 118.14 57 3069 21350 42596859
Swollen tongue 143.06 118.14 55 3071 21176 42597033
Nightmare 134.32 118.14 55 3071 24957 42593252
Migraine 133.47 118.14 55 3071 25359 42592850
Tinnitus 129.87 118.14 56 3070 28882 42589327
Impaired quality of life 129.69 118.14 46 3080 14131 42604078
Colitis ulcerative 121.87 118.14 52 3074 26123 42592086
Accidental overdose 121.16 118.14 53 3073 28277 42589932
Dysgeusia 120.91 118.14 56 3070 34133 42584076

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Catarrh 248.93 37.31 57 4001 7278 110577963
Burns second degree 245.94 37.31 57 4001 7676 110577565
Steroid dependence 240.78 37.31 57 4001 8412 110576829
Hypopnoea 224.05 37.31 57 4001 11323 110573918
Parosmia 215.74 37.31 57 4001 13123 110572118
Gingival pain 205.73 37.31 57 4001 15679 110569562
Alcohol poisoning 191.50 37.31 48 4010 8972 110576269
Rhinitis 185.48 37.31 57 4001 22488 110562753
Cardiac murmur 180.52 37.31 57 4001 24571 110560670
Bronchiectasis 166.10 37.31 59 3999 36434 110548807
Impaired work ability 164.40 37.31 54 4004 26365 110558876
Nightmare 155.03 37.31 57 4001 38806 110546435
Accidental overdose 135.68 37.31 56 4002 51778 110533463
Impaired quality of life 134.55 37.31 48 4010 29969 110555272
Swollen tongue 133.98 37.31 58 4000 60304 110524937
Tinnitus 133.82 37.31 58 4000 60482 110524759
Frequent bowel movements 130.91 37.31 60 3998 71330 110513911
Tubulointerstitial nephritis 129.84 37.31 55 4003 54229 110531012
Dysgeusia 125.75 37.31 58 4000 69927 110515314
Eczema 120.86 37.31 57 4001 72236 110513005
Vertigo 113.83 37.31 58 4000 86812 110498429
Stress 108.79 37.31 60 3998 105288 110479953
Colitis ulcerative 108.23 37.31 54 4004 77309 110507932
Haematochezia 103.62 37.31 60 3998 115464 110469777
Rectal haemorrhage 98.96 37.31 59 3999 119774 110465467
Medication error 97.89 37.31 56 4002 105310 110479931
Loss of personal independence in daily activities 94.03 37.31 62 3996 149958 110435283
Deep vein thrombosis 90.56 37.31 59 3999 139828 110445413
Adverse drug reaction 82.03 37.31 50 4008 105509 110479732
Migraine 77.40 37.31 58 4000 171594 110413647
Palpitations 76.73 37.31 56 4002 159156 110426085
Arthritis 74.16 37.31 56 4002 167530 110417711
Inappropriate schedule of product administration 72.80 37.31 60 3998 203577 110381664
Cerebrovascular accident 72.41 37.31 57 4001 181227 110404014
Pulmonary embolism 70.08 37.31 60 3998 214414 110370827
Intentional product use issue 64.51 37.31 61 3997 247845 110337396
Systemic lupus erythematosus 63.18 37.31 61 3997 254277 110330964
Somnolence 60.47 37.31 64 3994 297385 110287856
COVID-19 59.41 37.31 58 4000 245002 110340239
Depression 48.66 37.31 59 3999 317276 110267965
Abdominal discomfort 45.99 37.31 64 3994 393794 110191447
Weight decreased 41.69 37.31 67 3991 467990 110117251
Confusional state 37.57 37.31 64 3994 468616 110116625

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC R01AA06 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Sympathomimetics, plain
ATC R01AB03 RESPIRATORY SYSTEM
NASAL PREPARATIONS
DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
Sympathomimetics, combinations excl. corticosteroids
ATC S01GA02 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
ATC S01GA52 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
MeSH PA D002317 Cardiovascular Agents
MeSH PA D009883 Ophthalmic Solutions
MeSH PA D013566 Sympathomimetics
MeSH PA D014662 Vasoconstrictor Agents
MeSH PA D014663 Nasal Decongestants
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
MeSH PA D019999 Pharmaceutical Solutions
CHEBI has role CHEBI:35524 sympathomimetic agent
CHEBI has role CHEBI:50514 vasoconstrictor agent
CHEBI has role CHEBI:67079 anti-inflammatory agent
CHEBI has role CHEBI:77715 nasal decongestant
CHEBI has role CHEBI:66981 ophthalmology drug

Related Drugs by ATC class:

R01AA Sympathomimetics, plain 13 drugs
cyclopentamineephedrineepinephrinefenoxazolineindanazolinemetizolinenaphazolineoxymetazolinephenylephrinetramazolinetuaminoheptanetymazoline show all 13 →
R01AB Sympathomimetics, combinations excl. corticosteroids 6 drugs
ephedrinenaphazolineoxymetazolinephenylephrinetuaminoheptanexylometazoline
S01GA Sympathomimetics used as decongestants 6 drugs
brimonidinenaphazolineoxedrineoxymetazolinephenylephrinexylometazoline

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Nasal discharge indication 64531003
Nasal congestion indication 68235000
Red eye indication 75705005
Hyperthyroidism contraindication 34486009 DOID:7998
Disorder of cardiovascular system contraindication 49601007 DOID:1287
Diabetes mellitus contraindication 73211009 DOID:9351




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.93 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Adrenergic receptor alpha GPCR AGONIST CHEMBL CHEMBL
Adrenergic receptor alpha-2 GPCR IC50 7.52 CHEMBL
Adrenergic receptor alpha-1 GPCR IC50 5.80 CHEMBL
Adrenergic receptor alpha GPCR Ki 7.96 CHEMBL

External reference:

IDSource
4022735 VUID
N0000020740 NUI
D00756 KEGG_DRUG
118201-38-0 SECONDARY_CAS_RN
522-48-5 SECONDARY_CAS_RN
4018994 VANDF
4022735 VANDF
C0076286 UMLSCUI
CHEBI:28674 CHEBI
CHEMBL1266 ChEMBL_ID
CHEMBL1200413 ChEMBL_ID
DB06764 DRUGBANK_ID
C005810 MESH_SUPPLEMENTAL_RECORD_UI
5419 PUBCHEM_CID
37935 RXNORM
5562 MMSL
72350 MMSL
7784 MMSL
001803 NDDF
004726 NDDF
2183004 SNOMEDCT_US
372673004 SNOMEDCT_US
50969006 SNOMEDCT_US
519 INN_ID
8P9X484T3F UNII

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Glitch Advanced Relief Eye Drops HUMAN OTC DRUG LABEL 2 0276-0801 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 14 sections
Walgreens Multi-Symptom Relief Eye Drops HUMAN OTC DRUG LABEL 5 0363-1462 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 13 sections
Walgreens Sterile Original Eye Drops HUMAN OTC DRUG LABEL 1 0363-1676 SOLUTION/ DROPS 0.05 mg OPHTHALMIC OTC monograph final 12 sections
Walgreens Sterile Advance Relief Eye Drops HUMAN OTC DRUG LABEL 4 0363-1677 SOLUTION/ DROPS 0.00 mg OPHTHALMIC OTC monograph final 12 sections
Walgreens Eye Drops Seasonal Relief 15mL HUMAN OTC DRUG LABEL 2 0363-4545 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 14 sections
Walgreens Eye Drops Advanced Relief 15mL HUMAN OTC DRUG LABEL 4 0363-4547 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 12 sections
Walgreens Eye Drops Original 15mL and twin pack HUMAN OTC DRUG LABEL 1 0363-4550 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 13 sections
Walgreens Sterile Original Eye HUMAN OTC DRUG LABEL 1 0363-7298 SOLUTION/ DROPS 0.50 mg OPHTHALMIC OTC monograph final 12 sections
Eye Drops HUMAN OTC DRUG LABEL 1 0498-0161 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 14 sections
Industrial Strength Eye Drops HUMAN OTC DRUG LABEL 2 0498-0162 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 15 sections
RohtoAll-In-One HUMAN OTC DRUG LABEL 3 10742-8146 LIQUID 0.50 mg OPHTHALMIC OTC Monograph Drug 11 sections
Rohto Digi-Eye HUMAN OTC DRUG LABEL 2 10742-8175 LIQUID 0.50 mg OPHTHALMIC OTC Monograph Drug 12 sections
Up and Up Ultra Itchy Relief HUMAN OTC DRUG LABEL 2 11673-672 SOLUTION/ DROPS 0.50 mg OPHTHALMIC OTC monograph final 12 sections
GOODSENSE ORIGINAL EYE DROPS HUMAN OTC DRUG LABEL 1 11716-0002 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 12 sections
GOODSENSE IRRITATION RELIEF EYE HUMAN OTC DRUG LABEL 2 11716-0003 SOLUTION/ DROPS 0.50 mg OPHTHALMIC OTC monograph final 12 sections
GOODSENSE ADVANCED RELIEF EYE HUMAN OTC DRUG LABEL 4 11716-0004 SOLUTION/ DROPS 0.50 mg OPHTHALMIC OTC monograph final 12 sections
DG HEALTH ORIGINAL HUMAN OTC DRUG LABEL 1 11716-0053 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
PREMIER VALUE ORIGINAL HUMAN OTC DRUG LABEL 1 11716-0101 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 12 sections
PREMIER VALUE ADVANCED EYE DROPS HUMAN OTC DRUG LABEL 4 11716-0102 SOLUTION 0.00 mL OPHTHALMIC OTC monograph final 11 sections
PREMIER VALUE EYE AC HUMAN OTC DRUG LABEL 2 11716-0103 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
SHOPKO ADVANCED FORMULA EYE DROPS HUMAN OTC DRUG LABEL 4 11716-0458 SOLUTION 0.00 mL OPHTHALMIC OTC monograph final 11 sections
SHOPKO RELIEF HUMAN OTC DRUG LABEL 2 11716-0460 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
LEADER ADVANCED FORMULA EYE DROPS HUMAN OTC DRUG LABEL 4 11716-1104 SOLUTION 0.00 mL OPHTHALMIC OTC monograph final 11 sections
WALGREENS MAXIMUM RELIEF EYE DROPS HUMAN OTC DRUG LABEL 4 11716-1167 SOLUTION 0.00 mL OPHTHALMIC OTC monograph final 11 sections
WALGREENS ORIGINAL EYE DROPS HUMAN OTC DRUG LABEL 1 11716-1168 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
FREDS ORIGINAL EYE DROPS HUMAN OTC DRUG LABEL 1 11716-1187 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
SHOPKO ORIGINAL FORMULA EYE DROPS HUMAN OTC DRUG LABEL 1 11716-1609 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 11 sections
LEADER ORIGINAL FORMULA EYE DROPS HUMAN OTC DRUG LABEL 1 11716-4708 SOLUTION/ DROPS 0.50 mg OPHTHALMIC OTC monograph final 11 sections
LEADER RELIEF HUMAN OTC DRUG LABEL 2 11716-9638 SOLUTION 0.50 mg OPHTHALMIC OTC monograph final 12 sections
Rite Aid Multi-Symptom Relief Eye Drops HUMAN OTC DRUG LABEL 3 11822-0277 SOLUTION/ DROPS 0.05 g OPHTHALMIC OTC Monograph Drug 14 sections