brimonidine ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definitionDrug idCAS RN
alpha-2 adrenoreceptor agonists 395 59803-98-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • UK 14,304
  • mirvaso
  • brimonidine
  • brimonidine tartrate
  • bromoxidine
A quinoxaline derivative and ADRENERGIC ALHPA-2 RECEPTOR AGONIST that is used to manage INTRAOCULAR PRESSURE associated with OPEN-ANGLE GLAUCOMA and OCULAR HYPERTENSION.
  • Molecular weight: 292.14
  • Formula: C11H10BrN5
  • CLOGP: 1.49
  • LIPINSKI: 0
  • HAC: 5
  • HDO: 2
  • TPSA: 62.20
  • ALOGS: -3.28
  • ROTB: 1
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 1.50 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 10 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 0.01 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ALK,AURKA,AURKB,AXL,BRAF,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,ITK,JAK1,MAP3K21,MAP4K1,MAPK7,MARK4,NTRK2,PDK1,PDK2,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TTK,ULK1 40
kinase-selectivity-class AXL,BRAF,CDK9,PIK3CD 4
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
March 25, 2020 PMDA Senju Pharmaceutical Co., Ltd
Sept. 6, 1996 FDA
Feb. 20, 2014 EMA GALDERMA INTERNATIONAL

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
Ocular hyperaemia 485.28 17.64 181 12456 33617 90582193
Eye irritation 484.34 17.64 181 12456 33797 90582013
Intraocular pressure increased 476.67 17.64 124 12513 6969 90608841
Treatment failure 420.24 17.64 343 12294 303585 90312225
Eye pain 294.83 17.64 137 12500 44031 90571779
Corneal opacity 248.99 17.64 50 12587 861 90614949
Vision blurred 157.00 17.64 127 12510 110166 90505644
Glaucoma 140.31 17.64 65 12572 20690 90595120
Iridocyclitis 135.02 17.64 40 12597 3621 90612189
Dry eye 116.34 17.64 82 12555 57849 90557961
Ocular surface disease 115.43 17.64 18 12619 60 90615750
Visual acuity reduced 115.16 17.64 59 12578 23351 90592459
Eye pruritus 114.12 17.64 63 12574 28964 90586846
Corneal oedema 112.17 17.64 30 12607 1871 90613939
Inappropriate schedule of product administration 104.04 17.64 116 12521 149817 90465993
Choroidal effusion 94.69 17.64 22 12615 767 90615043
Erythema of eyelid 91.80 17.64 29 12608 3254 90612556
Uveitis 80.88 17.64 41 12596 15862 90599948
Conjunctival hyperaemia 80.41 17.64 26 12611 3143 90612667
Foreign body sensation in eyes 79.38 17.64 26 12611 3274 90612536
Erythema 76.40 17.64 124 12513 229122 90386688
Scleral hyperaemia 72.51 17.64 15 12622 301 90615509
Eye inflammation 67.15 17.64 29 12608 7822 90607988
Eye swelling 67.00 17.64 45 12592 29341 90586469
Rebound effect 65.31 17.64 30 12607 9354 90606456
Eye disorder 64.99 17.64 43 12594 27347 90588463
Lacrimation increased 60.64 17.64 41 12596 27021 90588789
Vitreous haemorrhage 60.39 17.64 20 12617 2606 90613204
Blindness unilateral 57.84 17.64 26 12611 7710 90608100
Conjunctivitis 56.38 17.64 39 12598 26667 90589143
Visual impairment 55.94 17.64 80 12557 132285 90483525
Blepharitis 55.89 17.64 21 12616 3955 90611855
Hypotonia 53.88 17.64 28 12609 11398 90604412
Intraocular pressure test abnormal 53.35 17.64 11 12626 217 90615593
Corneal deposits 53.13 17.64 12 12625 368 90615442
Ocular hypertension 51.83 17.64 16 12621 1664 90614146
Iris adhesions 51.74 17.64 12 12625 415 90615395
Conjunctivitis allergic 51.07 17.64 15 12622 1317 90614493
Eye discharge 50.06 17.64 24 12613 8234 90607576
Macular oedema 48.20 17.64 20 12617 4889 90610921
Conjunctival scar 47.19 17.64 8 12629 50 90615760
Vitreous floaters 45.95 17.64 22 12615 7527 90608283
Corneal neovascularisation 45.55 17.64 9 12628 142 90615668
Cataract 45.24 17.64 53 12584 72039 90543771
Product delivery mechanism issue 44.40 17.64 11 12626 505 90615305
Accidental exposure to product by child 42.41 17.64 13 12624 1320 90614490
Ocular vascular disorder 42.22 17.64 11 12626 619 90615191
Meniscus injury 41.19 17.64 21 12616 8216 90607594
Conjunctival follicles 41.02 17.64 6 12631 11 90615799
Visual field defect 40.94 17.64 20 12617 7146 90608664
Corneal disorder 40.83 17.64 14 12623 2028 90613782
Cystoid macular oedema 40.44 17.64 14 12623 2086 90613724
Skin burning sensation 39.90 17.64 28 12609 19583 90596227
Arthropathy 39.66 17.64 3 12634 366239 90249571
Systemic lupus erythematosus 39.08 17.64 3 12634 361893 90253917
Product container issue 36.13 17.64 13 12624 2168 90613642
Hypothermia 35.85 17.64 24 12613 15551 90600259
Photophobia 35.62 17.64 27 12610 21242 90594568
Infusion related reaction 34.35 17.64 8 12629 416772 90199038
Maternal exposure during pregnancy 33.75 17.64 5 12632 360058 90255752
Angle closure glaucoma 33.08 17.64 13 12624 2762 90613048
Bradycardia 32.96 17.64 49 12588 83798 90532012
Hypersensitivity 31.41 17.64 136 12501 454541 90161269
Ocular discomfort 31.16 17.64 16 12621 6354 90609456
Contraindicated product administered 31.06 17.64 4 12633 320135 90295675
Eyelids pruritus 29.90 17.64 11 12626 1953 90613857
Abnormal sensation in eye 29.86 17.64 11 12626 1960 90613850
Hepatic enzyme increased 29.57 17.64 7 12630 360729 90255081
Eyelid oedema 29.54 17.64 19 12618 11515 90604295
Product packaging quantity issue 28.24 17.64 10 12627 1592 90614218
Punctate keratitis 26.34 17.64 8 12629 788 90615022
Intraocular pressure fluctuation 25.73 17.64 5 12632 72 90615738
Fibroadenoma of breast 25.64 17.64 8 12629 861 90614949
Eyelid irritation 24.48 17.64 8 12629 1000 90614810
Endocrine ophthalmopathy 23.98 17.64 8 12629 1066 90614744
Product quality issue 23.81 17.64 41 12596 79284 90536526
Open angle glaucoma 23.64 17.64 6 12631 304 90615506
Anterior chamber fibrin 22.89 17.64 5 12632 131 90615679
Skin irritation 22.19 17.64 17 12620 13586 90602224
Eye colour change 21.98 17.64 6 12631 404 90615406
Dry skin 21.96 17.64 42 12595 88031 90527779
Retinal detachment 21.95 17.64 13 12624 6809 90609001
Eye haemorrhage 21.79 17.64 15 12622 10165 90605645
Corneal infiltrates 21.75 17.64 5 12632 166 90615644
Deep anterior chamber of the eye 21.56 17.64 3 12634 3 90615807
Retinal vascular occlusion 21.55 17.64 6 12631 435 90615375
Vitreous detachment 21.04 17.64 9 12628 2369 90613441
Electric shock sensation 21.01 17.64 8 12629 1562 90614248
Flat anterior chamber of eye 20.69 17.64 4 12633 56 90615754
Joint swelling 20.51 17.64 24 12613 503276 90112534
Giant papillary conjunctivitis 20.34 17.64 3 12634 6 90615804
Dizziness 20.26 17.64 146 12491 589138 90026672
Iritis 20.20 17.64 10 12627 3676 90612134
Short stature 20.09 17.64 7 12630 1063 90614747
Eye operation 19.92 17.64 9 12628 2700 90613110
Pain of skin 19.69 17.64 17 12620 16065 90599745
Keratitis interstitial 19.24 17.64 3 12634 10 90615800
Swelling of eyelid 19.15 17.64 11 12626 5443 90610367
Retinopathy haemorrhagic 19.02 17.64 3 12634 11 90615799
Symblepharon 18.75 17.64 5 12632 308 90615502
Mobility decreased 18.42 17.64 6 12631 250728 90365082
Ocular pemphigoid 18.38 17.64 4 12633 103 90615707
Corneal transplant 18.02 17.64 5 12632 358 90615452
Wound 17.88 17.64 10 12627 302970 90312840
Intraocular pressure decreased 17.83 17.64 4 12633 119 90615691

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
Treatment failure 464.79 17.70 233 8244 62391 42550467
Intraocular pressure increased 463.75 17.70 128 8349 6305 42606553
Ocular hyperaemia 283.82 17.70 110 8367 15853 42597005
Eye irritation 222.68 17.70 84 8393 11234 42601624
Corneal opacity 200.18 17.70 42 8435 623 42612235
Corneal oedema 179.74 17.70 45 8432 1503 42611355
Eye pain 142.62 17.70 69 8408 16961 42595897
Choroidal detachment 127.93 17.70 28 8449 512 42612346
Visual acuity reduced 120.07 17.70 62 8415 17488 42595370
Ocular surface disease 115.52 17.70 20 8457 95 42612763
Hypotony of eye 99.31 17.70 20 8457 239 42612619
Vision blurred 88.04 17.70 78 8399 53621 42559237
Glaucoma 83.14 17.70 38 8439 8210 42604648
Blepharitis 79.79 17.70 25 8452 1908 42610950
Foreign body sensation in eyes 78.03 17.70 21 8456 934 42611924
Conjunctival hyperaemia 75.06 17.70 27 8450 3149 42609709
Eye pruritus 74.26 17.70 39 8438 11373 42601485
Iridocyclitis 68.48 17.70 23 8454 2188 42610670
Conjunctivitis 64.27 17.70 37 8440 12902 42599956
Choroidal effusion 63.55 17.70 14 8463 264 42612594
Corneal neovascularisation 60.95 17.70 11 8466 69 42612789
Corneal infiltrates 58.02 17.70 12 8465 165 42612693
Punctate keratitis 57.12 17.70 14 8463 427 42612431
Hypotony maculopathy 51.43 17.70 9 8468 46 42612812
Cornea verticillata 51.01 17.70 10 8467 103 42612755
Cataract 47.24 17.70 43 8434 30561 42582297
Cystoid macular oedema 45.32 17.70 14 8463 1019 42611839
Eye discharge 43.97 17.70 18 8459 2977 42609881
Infectious crystalline keratopathy 43.20 17.70 8 8469 59 42612799
Scleral hyperaemia 42.40 17.70 8 8469 66 42612792
Intraocular pressure decreased 40.24 17.70 8 8469 89 42612769
Lacrimation increased 38.99 17.70 26 8451 11732 42601126
Erythema of eyelid 36.35 17.70 13 8464 1490 42611368
Hyperaemia 36.16 17.70 13 8464 1513 42611345
Retinal detachment 36.02 17.70 20 8457 6505 42606353
Blindness 35.32 17.70 29 8448 17949 42594909
Dry eye 34.70 17.70 27 8450 15479 42597379
Product container issue 34.32 17.70 11 8466 903 42611955
Visual impairment 33.37 17.70 42 8435 43071 42569787
Corneal deposits 33.02 17.70 8 8469 232 42612626
Product delivery mechanism issue 32.21 17.70 8 8469 258 42612600
Ulcerative keratitis 32.19 17.70 13 8464 2075 42610783
Eye swelling 31.66 17.70 23 8454 11897 42600961
Macular oedema 31.48 17.70 15 8462 3554 42609304
Pyelitis 30.88 17.70 7 8470 151 42612707
Dacryostenosis acquired 30.69 17.70 8 8469 314 42612544
Keratitis interstitial 29.78 17.70 5 8472 19 42612839
Visual field defect 29.65 17.70 16 8461 4922 42607936
Anterior chamber inflammation 28.89 17.70 8 8469 396 42612462
Corneal infection 28.83 17.70 5 8472 24 42612834
Corneal disorder 28.82 17.70 10 8467 1049 42611809
Hyphaema 28.41 17.70 9 8468 711 42612147
Keratic precipitates 27.97 17.70 7 8470 233 42612625
Conjunctival follicles 27.86 17.70 4 8473 3 42612855
Ocular discomfort 27.43 17.70 13 8464 3044 42609814
Thunderclap headache 25.40 17.70 6 8471 156 42612702
Eyelids pruritus 25.35 17.70 7 8470 343 42612515
Eyelid irritation 24.39 17.70 7 8470 395 42612463
Keratitis 23.71 17.70 10 8467 1781 42611077
Visual acuity tests abnormal 22.81 17.70 5 8472 92 42612766
Open angle glaucoma 22.27 17.70 6 8471 268 42612590
Hypersensitivity 21.90 17.70 46 8431 72324 42540534
Meibomian gland dysfunction 21.88 17.70 5 8472 112 42612746
Conjunctivitis allergic 21.87 17.70 14 8463 5897 42606961
Product quality issue 21.67 17.70 22 8455 17860 42594998
Trabeculectomy 21.66 17.70 4 8473 29 42612829
Eyelid margin crusting 21.40 17.70 7 8470 613 42612245
Pneumonia haemophilus 21.27 17.70 8 8469 1056 42611802
Angle closure glaucoma 20.86 17.70 8 8469 1114 42611744
Tendinous contracture 20.84 17.70 5 8472 139 42612719
Keratopathy 20.59 17.70 7 8470 691 42612167
Giant papillary conjunctivitis 20.49 17.70 3 8474 3 42612855
Uveitis 20.45 17.70 16 8461 9242 42603616
Corneal degeneration 20.42 17.70 4 8473 41 42612817
Photophobia 20.06 17.70 15 8462 8104 42604754
Flat anterior chamber of eye 18.77 17.70 4 8473 64 42612794
Reaction to preservatives 18.44 17.70 4 8473 70 42612788
Anterior chamber disorder 17.84 17.70 4 8473 82 42612776

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
Intraocular pressure increased 720.63 15.60 189 15647 10687 110562776
Ocular hyperaemia 422.77 15.60 172 15664 39114 110534349
Eye irritation 331.13 15.60 138 15698 33314 110540149
Corneal oedema 283.22 15.60 70 15766 3103 110570360
Corneal opacity 260.26 15.60 55 15781 1196 110572267
Eye pain 251.37 15.60 129 15707 49970 110523493
Ocular surface disease 216.78 15.60 35 15801 149 110573314
Vision blurred 181.05 15.60 149 15687 128873 110444590
Visual acuity reduced 179.37 15.60 89 15747 32084 110541379
Choroidal effusion 128.55 15.60 29 15807 861 110572602
Conjunctival hyperaemia 127.38 15.60 43 15793 5788 110567675
Glaucoma 124.63 15.60 62 15774 22455 110551008
Blepharitis 117.19 15.60 38 15798 4514 110568949
Choroidal detachment 116.10 15.60 26 15810 746 110572717
Foreign body sensation in eyes 98.88 15.60 31 15805 3303 110570160
Hypotony of eye 93.76 15.60 20 15816 455 110573008
Corneal neovascularisation 90.38 15.60 17 15819 198 110573265
Iridocyclitis 87.89 15.60 32 15804 5376 110568087
Erythema of eyelid 86.02 15.60 29 15807 3886 110569577
Corneal deposits 83.80 15.60 19 15817 577 110572886
Eye pruritus 82.68 15.60 54 15782 32721 110540742
Dry eye 81.46 15.60 66 15770 55727 110517736
Conjunctivitis 78.77 15.60 53 15783 33739 110539724
Uveitis 75.76 15.60 44 15792 21666 110551797
Iris adhesions 71.40 15.60 17 15819 642 110572821
Cystoid macular oedema 70.55 15.60 23 15813 2777 110570686
Punctate keratitis 70.53 15.60 19 15817 1185 110572278
Inappropriate schedule of product administration 69.45 15.60 113 15723 203524 110369939
Eye inflammation 68.35 15.60 31 15805 9140 110564323
Vitreous haemorrhage 66.48 15.60 25 15811 4595 110568868
Scleral hyperaemia 65.86 15.60 14 15822 313 110573150
Erythema 64.32 15.60 134 15702 291313 110282150
Corneal infiltrates 64.29 15.60 14 15822 352 110573111
Corneal disorder 64.09 15.60 21 15815 2576 110570887
Macular oedema 63.07 15.60 27 15809 6939 110566524
Cataract 61.48 15.60 66 15770 79419 110494044
Conjunctival follicles 61.47 15.60 9 15827 16 110573447
Eye discharge 60.25 15.60 28 15808 8726 110564737
Conjunctivitis allergic 59.92 15.60 26 15810 6905 110566558
Hypotony maculopathy 57.95 15.60 9 15827 28 110573435
Visual field defect 53.56 15.60 27 15809 10045 110563418
Lacrimation increased 52.47 15.60 40 15796 30910 110542553
Ocular hypertension 49.62 15.60 17 15819 2391 110571072
Blindness unilateral 48.46 15.60 25 15811 9761 110563702
Retinal detachment 48.27 15.60 26 15810 11074 110562389
Vitreous floaters 47.15 15.60 24 15812 9110 110564353
Visual impairment 46.35 15.60 75 15761 134353 110439110
Eye disorder 46.04 15.60 36 15800 28870 110544593
Anterior chamber inflammation 44.32 15.60 12 15824 763 110572700
Infectious crystalline keratopathy 43.73 15.60 8 15828 79 110573384
Angle closure glaucoma 43.42 15.60 17 15819 3482 110569981
Conjunctival scar 42.96 15.60 10 15826 342 110573121
Eye swelling 41.81 15.60 36 15800 33012 110540451
Ulcerative keratitis 41.60 15.60 18 15818 4748 110568715
Rebound effect 41.31 15.60 26 15810 14780 110558683
Photophobia 40.84 15.60 32 15804 25739 110547724
Hyphaema 40.08 15.60 12 15824 1095 110572368
Hypotonia 39.85 15.60 26 15810 15719 110557744
Ocular vascular disorder 39.58 15.60 11 15825 771 110572692
Cornea verticillata 38.57 15.60 9 15827 311 110573152
Flat anterior chamber of eye 38.34 15.60 8 15828 163 110573300
Eyelids pruritus 38.25 15.60 13 15823 1784 110571679
Intraocular pressure decreased 37.46 15.60 8 15828 183 110573280
Blindness 36.93 15.60 35 15801 36324 110537139
Keratitis interstitial 36.53 15.60 6 15830 29 110573434
Intraocular pressure fluctuation 36.36 15.60 7 15829 93 110573370
Intraocular pressure test abnormal 36.29 15.60 8 15828 213 110573250
Hyperaemia 35.40 15.60 15 15821 3758 110569705
Skin burning sensation 34.36 15.60 27 15809 21798 110551665
Accidental exposure to product by child 34.35 15.60 14 15822 3184 110570279
Keratic precipitates 33.63 15.60 9 15827 547 110572916
Open angle glaucoma 33.35 15.60 9 15827 565 110572898
Corneal scar 32.82 15.60 8 15828 334 110573129
Trabeculectomy 32.73 15.60 6 15830 60 110573403
Anterior chamber disorder 32.62 15.60 7 15829 164 110573299
Floppy iris syndrome 32.54 15.60 8 15828 346 110573117
Bradycardia 32.51 15.60 70 15766 155447 110418016
Skin irritation 31.94 15.60 23 15813 16296 110557167
Dacryostenosis acquired 31.79 15.60 9 15827 675 110572788
Meniscus injury 30.42 15.60 17 15819 7776 110565687
Corneal degeneration 30.14 15.60 7 15829 237 110573226
Keratopathy 29.49 15.60 10 15826 1363 110572100
Reaction to preservatives 29.48 15.60 7 15829 261 110573202
Corneal infection 29.25 15.60 6 15830 112 110573351
Eyelid oedema 28.71 15.60 21 15815 15241 110558222
Abnormal sensation in eye 28.47 15.60 11 15825 2175 110571288
Meibomian gland dysfunction 28.29 15.60 7 15829 311 110573152
Retinal vascular occlusion 28.00 15.60 8 15828 620 110572843
Drug ineffective 27.51 15.60 335 15501 1520205 109053258
Eyelid irritation 27.32 15.60 9 15827 1122 110572341
Fibroadenoma of breast 26.93 15.60 8 15828 711 110572752
Iritis 26.30 15.60 13 15823 4639 110568824
Pyelitis 26.23 15.60 7 15829 421 110573042
Systemic lupus erythematosus 25.97 15.60 3 15833 254335 110319128
Endocrine ophthalmopathy 25.61 15.60 9 15827 1364 110572099
Corneal erosion 25.45 15.60 7 15829 472 110572991
Ocular pemphigoid 25.14 15.60 6 15830 229 110573234
Allergic keratitis 24.08 15.60 4 15832 21 110573442
Giant papillary conjunctivitis 24.08 15.60 4 15832 21 110573442
Dermatitis contact 23.57 15.60 18 15818 13935 110559528
Exfoliation glaucoma 23.56 15.60 3 15833 0 110573463
Dizziness 22.57 15.60 174 15662 698019 109875444
Hepatic enzyme increased 22.32 15.60 9 15827 320883 110252580
Eyelid ptosis 22.09 15.60 17 15819 13310 110560153
Endophthalmitis 21.90 15.60 14 15822 8173 110565290
Arthropathy 21.81 15.60 7 15829 287515 110285948
Maternal exposure during pregnancy 21.59 15.60 5 15831 254878 110318585
Visual acuity tests abnormal 21.39 15.60 5 15831 174 110573289
Ocular discomfort 21.37 15.60 14 15822 8519 110564944
Corneal epithelium defect 21.00 15.60 7 15829 905 110572558
Conjunctival oedema 20.87 15.60 8 15828 1548 110571915
Deep anterior chamber of the eye 20.26 15.60 3 15833 6 110573457
Lower respiratory tract infection 20.14 15.60 5 15831 243101 110330362
Photopsia 20.11 15.60 12 15824 6202 110567261
Malignant glaucoma 19.94 15.60 3 15833 7 110573456
Thunderclap headache 19.79 15.60 6 15830 572 110572891
Anterior chamber fibrin 19.73 15.60 5 15831 245 110573218
Electric shock sensation 19.15 15.60 8 15828 1936 110571527
Infusion related reaction 19.00 15.60 16 15820 381146 110192317
Prostaglandin analogue periorbitopathy 18.94 15.60 3 15833 11 110573452
Eyelid margin crusting 18.87 15.60 8 15828 2008 110571455
Hypothermia 18.86 15.60 21 15815 26281 110547182
Nocturia 18.49 15.60 17 15819 16973 110556490
Impaired healing 18.47 15.60 3 15833 196714 110376749
Mobility decreased 17.62 15.60 6 15830 237416 110336047
Eyelid disorder 17.51 15.60 8 15828 2397 110571066
Eye haemorrhage 17.33 15.60 14 15822 11760 110561703
Corneal transplant 17.13 15.60 5 15831 418 110573045
Keratitis 16.82 15.60 10 15826 5134 110568329
Eye operation 16.72 15.60 8 15828 2659 110570804
Pneumonia haemophilus 16.58 15.60 8 15828 2707 110570756
Brain stem haematoma 16.58 15.60 4 15832 160 110573303
Fall 16.05 15.60 144 15692 603338 109970125
Drug abuse 16.01 15.60 3 15833 177408 110396055

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC D11AX21 DERMATOLOGICALS
OTHER DERMATOLOGICAL PREPARATIONS
OTHER DERMATOLOGICAL PREPARATIONS
Other dermatologicals
ATC S01EA05 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Sympathomimetics in glaucoma therapy
ATC S01EA55 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Sympathomimetics in glaucoma therapy
ATC S01GA07 SENSORY ORGANS
OPHTHALMOLOGICALS
DECONGESTANTS AND ANTIALLERGICS
Sympathomimetics used as decongestants
FDA MoA N0000000209 Adrenergic alpha-Agonists
FDA EPC N0000175552 alpha-Adrenergic Agonist
CHEBI has role CHEBI:35569 ฮฑ-adrenergic agonist
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:37886 adrenergic agonist
CHEBI has role CHEBI:39456 antiglaucoma drug
CHEBI has role CHEBI:66981 ophthalmology drug
MeSH PA D000316 Adrenergic alpha-Agonists
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018663 Adrenergic Agents
MeSH PA D058647 Adrenergic alpha-2 Receptor Agonists

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S01EA Sympathomimetics in glaucoma therapy 5 drugs
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S01GA Sympathomimetics used as decongestants 6 drugs
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Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Open-angle glaucoma indication 84494001 DOID:1067
Rosacea indication 398909004 DOID:8881
Bronchospasm contraindication 4386001
Complete atrioventricular block contraindication 27885002
Orthostatic hypotension contraindication 28651003
Acute cerebrovascular insufficiency contraindication 29322000
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Anaphylaxis contraindication 39579001
Sinus bradycardia contraindication 49710005
General anesthesia contraindication 50697003
Thromboangiitis obliterans contraindication 52403007 DOID:12918
Cerebrovascular disease contraindication 62914000 DOID:6713
Diabetes mellitus contraindication 73211009 DOID:9351
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Myasthenia gravis contraindication 91637004 DOID:437
Acute disease of cardiovascular system contraindication 128487001
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Hypoglycemic disorder contraindication 237630007
Raynaud's phenomenon contraindication 266261006
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006




๐Ÿถ Veterinary Drug Use

None

๐Ÿถ Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 7.64 Basic
pKa2 1.82 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 11596600 July 27, 2029 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 11833245 July 27, 2029 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY PRESERVATIVE FREE BAUSCH AND LOMB INC N218424 April 19, 2024 OTC SOLUTION/DROPS OPHTHALMIC 11596600 July 27, 2029 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 8455494 May 24, 2030 TREATMENT OF PRESBYOPIA
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 8455494 May 24, 2030 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF BRIMONIDINE AND CARBACHOL ONCE DAILY
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 8455494 May 24, 2030 USE OF YUVEZZI FOR THE TREATMENT OF PRESBYOPIA IN ADULTS
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 8293742 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY BAUSCH AND LOMB INC N208144 Dec. 22, 2017 OTC SOLUTION/DROPS OPHTHALMIC 9259425 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY PRESERVATIVE FREE BAUSCH AND LOMB INC N218424 April 19, 2024 OTC SOLUTION/DROPS OPHTHALMIC 8293742 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
0.025% LUMIFY PRESERVATIVE FREE BAUSCH AND LOMB INC N218424 April 19, 2024 OTC SOLUTION/DROPS OPHTHALMIC 9259425 July 14, 2030 RELIEVES REDNESS OF THE EYE DUE TO MINOR EYE IRRITATIONS
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8513247 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8513249 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 9861631 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 9861632 March 25, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
EQ 0.33% BASE MIRVASO GALDERMA LABS LP N204708 Aug. 23, 2013 RX GEL TOPICAL 8053427 June 13, 2031 TOPICAL TREATMENT OF FACIAL ERYTHEMA OF ROSACEA
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 12268662 Nov. 10, 2042 TREATMENT OF PRESBYOPIA
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 12268662 Nov. 10, 2042 TREATMENT OF PRESBYOPIA IN ADULTS BY ADMINISTRATION OF BRIMONIDINE AND CARBACHOL ONCE DAILY
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC 12268662 Nov. 10, 2042 USE OF YUVEZZI FOR THE TREATMENT OF PRESBYOPIA IN ADULTS

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.1%;2.75% YUVEZZI VISUS N220142 Jan. 28, 2026 RX SOLUTION/DROPS OPHTHALMIC Jan. 28, 2029 NEW PRODUCT

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Alpha-2C adrenergic receptor GPCR AGONIST EC50 8.47 WOMBAT-PK CHEMBL
Alpha-2B adrenergic receptor GPCR AGONIST EC50 7.26 WOMBAT-PK CHEMBL
Alpha-2A adrenergic receptor GPCR AGONIST EC50 8.39 WOMBAT-PK CHEMBL
Alpha-1D adrenergic receptor GPCR Ki 6.07 DRUG MATRIX
Alpha-1B adrenergic receptor GPCR Ki 5.27 CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.84 DRUG MATRIX
Alpha-1A adrenergic receptor GPCR Ki 5.55 CHEMBL
Alpha-2B adrenergic receptor GPCR Ki 7.28 CHEMBL
5-hydroxytryptamine receptor 1A GPCR IC50 5.59 CHEMBL
Alpha-1A adrenergic receptor GPCR EC50 5.95 CHEMBL
Adrenergic receptor alpha-2 GPCR Ki 7.52 CHEMBL
Adrenergic receptor alpha-1 GPCR Ki 6.13 CHEMBL
Alpha-1B adrenergic receptor GPCR EC50 6.03 CHEMBL

External reference:

IDSource
E6GNX3HHTE UNII
D02076 KEGG_DRUG
70359-46-5 SECONDARY_CAS_RN
134615 RXNORM
C0525227 UMLSCUI
CHEBI:3175 CHEBI
J59 PDB_CHEM_ID
CHEMBL844 ChEMBL_ID
2435 PUBCHEM_CID
DB00484 DRUGBANK_ID
CHEMBL1200389 ChEMBL_ID
D000068438 MESH_DESCRIPTOR_UI
6863 INN_ID
14807 MMSL
205316 MMSL
240890 MMSL
31659 MMSL
4297 MMSL
44062 MMSL
46686 MMSL
108827001 SNOMEDCT_US
372547000 SNOMEDCT_US
386924004 SNOMEDCT_US
4021002 VANDF
4024043 VANDF
006196 NDDF
006197 NDDF
E6GNX3HHTE INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9177 SOLUTION/ DROPS 1.50 mg OPHTHALMIC NDA 27 sections
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 0023-9211 SOLUTION/ DROPS 2 mg OPHTHALMIC NDA 27 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 0023-9321 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA 27 sections
SIMBRINZA HUMAN PRESCRIPTION DRUG LABEL 2 0065-4147 SUSPENSION/ DROPS 2 mg OPHTHALMIC NDA 25 sections
Mirvaso HUMAN PRESCRIPTION DRUG LABEL 1 0299-5980 GEL 5 mg TOPICAL NDA 26 sections
Brimonidine HUMAN PRESCRIPTION DRUG LABEL 1 0781-7177 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 26 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0781-7186 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 25 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0832-1425 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 27 sections
Brimonidine Tartrate Human Prescription Drug Label 1 14445-400 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 24 sections
BRIMONIDINE TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 16590-883 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 12 sections
Brimonidine HUMAN PRESCRIPTION DRUG LABEL 1 17478-715 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 24208-411 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
LUMIFY Redness Reliever Eye Drops HUMAN OTC DRUG LABEL 1 24208-537 SOLUTION/ DROPS 0.25 mg OPHTHALMIC NDA 13 sections
LUMIFY PRESERVATIVE FREE EYE DROPS HUMAN OTC DRUG LABEL 1 24208-538 SOLUTION/ DROPS 0.25 mg OPHTHALMIC NDA 9 sections
Brimonidine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 42571-419 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 24 sections
brimonidine tartrate HUMAN PRESCRIPTION DRUG LABEL 1 42571-462 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 25 sections
BRIMONIDINE HUMAN PRESCRIPTION DRUG LABEL 1 45802-078 GEL 5 mg TOPICAL ANDA 26 sections
Brimonidine Tartrate ophthalmic solution, 0.15% Human Prescription Drug Label 1 46708-661 SOLUTION/ DROPS 1.50 mg OPHTHALMIC ANDA 24 sections
Brimonidine Tartrate and Timolol Maleate Human Prescription Drug Label 2 46708-706 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 24 sections
Brimonidine Tartrate Human Prescription Drug Label 1 46708-749 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 24 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-1800 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 50090-4224 SOLUTION 2 mg OPHTHALMIC ANDA 24 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 54868-4276 SOLUTION/ DROPS 1 mg OPHTHALMIC NDA 25 sections
ALPHAGAN P HUMAN PRESCRIPTION DRUG LABEL 1 54868-4690 SOLUTION/ DROPS 1.50 mg OPHTHALMIC NDA 25 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 54868-6094 SOLUTION 1.50 mg OPHTHALMIC NDA 10 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 54868-6287 SOLUTION/ DROPS 2 mg OPHTHALMIC ANDA 22 sections
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 54868-6295 SOLUTION/ DROPS 2 mg OPHTHALMIC NDA 23 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 60505-0564 SOLUTION/ DROPS 1.50 mg OPHTHALMIC ANDA 26 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 60505-0564 SOLUTION/ DROPS 1.50 mg OPHTHALMIC ANDA 26 sections
Brimonidine Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 60505-0577 SOLUTION/ DROPS 1 mg OPHTHALMIC ANDA 21 sections