timolol ๐Ÿถ Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
beta-adrenoreceptor antagonists 4061 26839-75-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • timolol
  • timolol maleate
  • (-)-Timolol
  • (S)-Timolol
  • arutimol
  • L-Timolol
  • timolol maleate salt
A beta-adrenergic antagonist that is similar in action to PROPRANOLOL; the levo-isomer is more active. Timolol has been proposed as an anti-hypertensive, anti-arrhythmic, anti-angina, and anti-glaucoma agent. It is also used in the treatment of MIGRAINE DISORDERS and tremor.
  • Molecular weight: 316.42
  • Formula: C13H24N4O3S
  • CLOGP: 1.78
  • LIPINSKI: 0
  • HAC: 7
  • HDO: 2
  • TPSA: 79.74
  • ALOGS: -3.07
  • ROTB: 7

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
20 mg O
20 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 1 Benet LZ, Broccatelli F, Oprea TI
S (Water solubility) 2.74 mg/mL Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine) 15 % Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose) 3.16 ยตM/kg/day Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability) 61 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution) 1.50 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 8.50 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.90 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 2.20 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 17, 1978 FDA ATON
March 25, 2020 PMDA Senju Pharmaceutical Co., Ltd

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
Treatment failure 663.43 13.51 500 17079 198543 63272900
Eye irritation 467.48 13.51 189 17390 21782 63449661
Intraocular pressure increased 402.68 13.51 122 17457 5956 63465487
Ocular hyperaemia 299.73 13.51 144 17435 25000 63446443
Eye pain 273.07 13.51 149 17430 33705 63437738
Glaucoma 174.30 13.51 91 17488 18814 63452629
Vision blurred 133.15 13.51 145 17434 91779 63379664
Eye pruritus 122.94 13.51 72 17507 18599 63452844
Visual acuity reduced 122.60 13.51 76 17503 21750 63449693
Product quality issue 99.08 13.51 81 17498 35784 63435659
Product container issue 97.69 13.51 31 17548 1762 63469681
Bradycardia 88.16 13.51 105 17474 73122 63398321
Lacrimation increased 82.22 13.51 58 17521 20573 63450870
Choroidal effusion 80.59 13.51 20 17559 456 63470987
Corneal oedema 77.99 13.51 25 17554 1468 63469975
Foreign body sensation in eyes 71.84 13.51 26 17553 2208 63469235
Product delivery mechanism issue 69.92 13.51 17 17562 355 63471088
Total lung capacity increased 67.30 13.51 25 17554 2285 63469158
Iris adhesions 66.70 13.51 16 17563 315 63471128
Frustration tolerance decreased 65.42 13.51 34 17545 6954 63464489
Eyelid margin crusting 64.52 13.51 20 17559 1052 63470391
Eye discharge 58.20 13.51 30 17549 6033 63465410
Cataract 57.72 13.51 75 17504 56978 63414465
Ulcerative keratitis 56.49 13.51 23 17556 2687 63468756
Choroidal detachment 56.21 13.51 13 17566 217 63471226
Conjunctival hyperaemia 55.86 13.51 22 17557 2357 63469086
Hypotony of eye 55.57 13.51 12 17567 144 63471299
Forced expiratory volume decreased 54.77 13.51 27 17552 4941 63466502
Trabeculectomy 54.52 13.51 9 17570 19 63471424
Pulmonary thrombosis 50.63 13.51 31 17548 8671 63462772
Corneal disorder 50.54 13.51 19 17560 1795 63469648
Eye inflammation 48.88 13.51 26 17553 5573 63465870
Corneal deposits 47.84 13.51 12 17567 286 63471157
Visual impairment 46.91 13.51 84 17495 84362 63387081
Respiration abnormal 45.56 13.51 26 17553 6391 63465052
Iridocyclitis 44.48 13.51 19 17560 2503 63468940
Product packaging quantity issue 44.38 13.51 16 17563 1343 63470100
Peak expiratory flow rate decreased 43.24 13.51 13 17566 616 63470827
Cystoid macular oedema 42.08 13.51 16 17563 1559 63469884
Lung diffusion test decreased 41.91 13.51 13 17566 685 63470758
Punctate keratitis 39.12 13.51 12 17567 609 63470834
Intraocular pressure test abnormal 38.28 13.51 9 17570 162 63471281
Retinal disorder 37.49 13.51 15 17564 1675 63469768
Abdominal discomfort 36.27 13.51 22 17557 320863 63150580
Systemic lupus erythematosus 36.14 13.51 7 17572 208911 63262532
Ocular discomfort 35.11 13.51 19 17560 4214 63467229
Thermal burns of eye 33.62 13.51 8 17571 152 63471291
Abnormal sensation in eye 33.59 13.51 14 17565 1735 63469708
Angle closure glaucoma 33.55 13.51 15 17564 2204 63469239
Procollagen type I C-terminal propeptide increased 33.50 13.51 6 17573 24 63471419
Eye swelling 33.31 13.51 37 17542 23881 63447562
Glossodynia 33.12 13.51 5 17574 178871 63292572
Synovitis 32.89 13.51 6 17573 186912 63284531
Serum procollagen type I N-terminal propeptide increased 32.75 13.51 6 17573 28 63471415
Forced vital capacity decreased 32.62 13.51 12 17567 1067 63470376
Visual field defect 32.23 13.51 21 17558 6540 63464903
Corneal degeneration 32.12 13.51 7 17572 88 63471355
Pain 31.44 13.51 103 17476 740525 62730918
Macular oedema 31.04 13.51 17 17562 3860 63467583
Growth of eyelashes 31.01 13.51 8 17571 214 63471229
Conjunctival ulcer 30.82 13.51 6 17573 41 63471402
Superficial injury of eye 30.10 13.51 8 17571 241 63471202
Incorrect dose administered 29.96 13.51 57 17522 59911 63411532
Flat anterior chamber of eye 29.35 13.51 6 17573 54 63471389
Blindness 29.24 13.51 33 17546 21666 63449777
Obstructive airways disorder 28.79 13.51 32 17547 20667 63450776
Liquid product physical issue 27.99 13.51 11 17568 1171 63470272
Corneal epithelium defect 27.36 13.51 8 17571 344 63471099
Wound 27.13 13.51 6 17573 163257 63308186
Completed suicide 27.13 13.51 4 17575 145669 63325774
Hallucination, visual 27.12 13.51 30 17549 19268 63452175
Chronotropic incompetence 26.93 13.51 6 17573 84 63471359
Erythema of eyelid 26.93 13.51 13 17566 2273 63469170
Glaucoma surgery 26.73 13.51 6 17573 87 63471356
Vitamin B12 decreased 26.59 13.51 15 17564 3605 63467838
Atrioventricular block complete 25.69 13.51 20 17559 8231 63463212
Haemangioma congenital 25.39 13.51 8 17571 444 63470999
Hypopyon 25.35 13.51 9 17570 723 63470720
Vitreous haemorrhage 25.19 13.51 12 17567 2038 63469405
Arthralgia 24.99 13.51 78 17501 569632 62901811
Conjunctival scar 24.56 13.51 5 17574 44 63471399
Retinal detachment 24.28 13.51 17 17562 5952 63465491
Keratitis interstitial 24.06 13.51 4 17575 9 63471434
Foreign body in eye 23.84 13.51 6 17573 145 63471298
Toxic anterior segment syndrome 23.71 13.51 11 17568 1760 63469683
Conjunctivitis 23.66 13.51 29 17550 20767 63450676
Sinoatrial block 23.65 13.51 9 17570 879 63470564
Infusion related reaction 23.58 13.51 20 17559 245501 63225942
Conjunctivitis allergic 23.13 13.51 9 17570 933 63470510
Keratopathy 22.96 13.51 8 17571 608 63470835
Hypersensitivity 22.91 13.51 149 17430 292536 63178907
Fall 22.83 13.51 186 17393 392148 63079295
Vitreous floaters 21.99 13.51 16 17563 5950 63465493
Contraindicated product administered 21.80 13.51 17 17562 217631 63253812
Corneal opacity 21.49 13.51 8 17571 735 63470708
Corneal thickening 21.45 13.51 4 17575 21 63471422
Endophthalmitis 21.41 13.51 13 17566 3579 63467864
Blindness unilateral 21.34 13.51 16 17563 6225 63465218
Drug intolerance 21.14 13.51 33 17546 308628 63162815
Open angle glaucoma 20.30 13.51 6 17573 268 63471175
Swelling 20.26 13.51 28 17551 275350 63196093
Uveitis 20.26 13.51 21 17558 12532 63458911
Eyelid irritation 20.04 13.51 7 17572 536 63470907
Hepatic enzyme increased 20.02 13.51 16 17563 202312 63269131
Discomfort 19.56 13.51 11 17568 167363 63304080
Genital erythema 19.47 13.51 4 17575 37 63471406
Dry eye 19.44 13.51 38 17541 40723 63430720
Sinus bradycardia 19.38 13.51 22 17557 14529 63456914
Blepharitis 19.23 13.51 11 17568 2714 63468729
Dry mouth 19.05 13.51 56 17523 77807 63393636
Product dose omission issue 18.76 13.51 120 17459 234193 63237250
Sinonasal papilloma 18.76 13.51 4 17575 45 63471398
Maternal exposure during pregnancy 18.70 13.51 20 17559 220042 63251401
Eye disorder 18.67 13.51 27 17552 22658 63448785
Intraocular pressure fluctuation 18.52 13.51 4 17575 48 63471395
Lethargy 18.47 13.51 45 17534 55962 63415481
Product physical consistency issue 18.31 13.51 7 17572 692 63470751
Optic nerve cupping 18.28 13.51 3 17576 6 63471437
Bronchopulmonary disease 18.28 13.51 3 17576 6 63471437
Joint swelling 18.04 13.51 40 17539 327626 63143817
No adverse event 17.84 13.51 37 17542 41368 63430075
Nodal rhythm 17.82 13.51 9 17570 1734 63469709
Hypotonia 17.69 13.51 17 17562 9268 63462175
Achromotrichia acquired 17.42 13.51 3 17576 9 63471434
Hypothermia 17.19 13.51 20 17559 13561 63457882
Arthropathy 17.14 13.51 24 17555 234768 63236675
Haemangioma 16.64 13.51 10 17569 2702 63468741
Blood pressure systolic increased 16.62 13.51 39 17540 47358 63424085
Conjunctival follicles 16.38 13.51 3 17576 14 63471429
Symblepharon 16.30 13.51 4 17575 87 63471356
Corneal endothelial cell loss 16.21 13.51 3 17576 15 63471428
Small for dates baby 16.00 13.51 11 17568 3740 63467703
Eye oedema 15.98 13.51 8 17571 1512 63469931
Therapeutic product effect decreased 15.92 13.51 18 17561 193169 63278274
Eye allergy 15.90 13.51 7 17572 992 63470451
Product use issue 15.64 13.51 23 17556 220497 63250946
Dacryocystitis 15.22 13.51 3 17576 22 63471421
Iritis 15.20 13.51 10 17569 3165 63468278
Conjunctival erosion 15.07 13.51 4 17575 120 63471323
Intraocular pressure decreased 15.07 13.51 4 17575 120 63471323
Eyelids pruritus 15.00 13.51 7 17572 1135 63470308
Intraocular lens implant 14.91 13.51 5 17574 338 63471105
Vertigo 14.58 13.51 43 17536 59844 63411599
Photophobia 14.53 13.51 21 17558 17614 63453829
Stag horn calculus 14.26 13.51 4 17575 148 63471295
Iris neovascularisation 14.22 13.51 3 17576 32 63471411
Intentional product use issue 14.10 13.51 9 17570 127883 63343560
Herpes ophthalmic 14.09 13.51 7 17572 1302 63470141
Haematemesis 14.07 13.51 28 17551 30384 63441059
Nasopharyngitis 14.02 13.51 31 17548 254226 63217217
Dizziness 14.00 13.51 181 17398 429744 63041699
Psoriatic arthropathy 13.97 13.51 4 17575 91516 63379927
Retinal vascular occlusion 13.84 13.51 5 17574 422 63471021
Vitrectomy 13.57 13.51 4 17575 177 63471266
Febrile neutropenia 13.53 13.51 8 17571 118441 63353002
Therapeutic product effect incomplete 13.52 13.51 9 17570 125047 63346396

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 735.48 14.58 345 11617 46352 34898617
Intraocular pressure increased 366.95 14.58 116 11846 5267 34939702
Eye irritation 283.17 14.58 104 11858 7457 34937512
Eye pain 179.45 14.58 89 11873 13373 34931596
Visual acuity reduced 164.16 14.58 89 11873 16060 34928909
Ocular hyperaemia 138.79 14.58 71 11891 11381 34933588
Vision blurred 112.32 14.58 106 11856 45857 34899112
Corneal oedema 91.52 14.58 29 11933 1322 34943647
Glaucoma 90.00 14.58 45 11917 6867 34938102
Corneal deposits 80.35 14.58 18 11944 206 34944763
Product delivery mechanism issue 74.13 14.58 16 11946 152 34944817
Bradycardia 71.26 14.58 107 11855 75311 34869658
Lacrimation increased 70.53 14.58 41 11921 8441 34936528
Product quality issue 65.53 14.58 51 11911 16984 34927985
Intraocular pressure test abnormal 61.33 14.58 12 11950 66 34944903
Product container issue 55.26 14.58 17 11945 702 34944267
Cataract 50.25 14.58 53 11909 26133 34918836
Hyphaema 49.91 14.58 15 11947 572 34944397
Anterior chamber disorder 49.42 14.58 10 11952 67 34944902
Blindness 49.41 14.58 41 11921 14945 34930024
Eye pruritus 48.88 14.58 31 11931 7458 34937511
Toxic anterior segment syndrome 43.43 14.58 16 11946 1153 34943816
Eye discharge 41.50 14.58 18 11944 1988 34942981
Visual impairment 41.44 14.58 56 11906 35746 34909223
Choroidal detachment 36.81 14.58 11 11951 411 34944558
Foreign body sensation in eyes 36.38 14.58 12 11950 622 34944347
Corneal disorder 35.50 14.58 13 11949 921 34944048
Floppy iris syndrome 35.35 14.58 10 11952 307 34944662
Ocular discomfort 34.13 14.58 16 11946 2118 34942851
Dry eye 33.25 14.58 27 11935 9548 34935421
Erythema of eyelid 31.70 14.58 12 11950 933 34944036
Iridocyclitis 31.51 14.58 14 11948 1638 34943331
Ocular hypertension 29.33 14.58 11 11951 833 34944136
Visual acuity tests abnormal 28.72 14.58 6 11956 48 34944921
Blindness unilateral 27.66 14.58 18 11944 4524 34940445
Scleral hyperaemia 27.00 14.58 6 11956 66 34944903
Eye infection 25.97 14.58 16 11946 3657 34941312
Off label use 24.99 14.58 68 11894 419456 34525513
Retinal detachment 24.86 14.58 18 11944 5373 34939596
Ulcerative keratitis 24.71 14.58 12 11950 1717 34943252
Eye swelling 24.27 14.58 23 11939 9972 34934997
Eyelid irritation 23.75 14.58 6 11956 118 34944851
Completed suicide 23.38 14.58 3 11959 98165 34846804
Eyelid oedema 23.38 14.58 17 11945 5107 34939862
Conjunctival oedema 23.19 14.58 8 11954 476 34944493
Administration site discomfort 23.12 14.58 5 11957 48 34944921
Intraocular pressure decreased 21.52 14.58 5 11957 68 34944901
Product packaging quantity issue 21.41 14.58 9 11953 920 34944049
Eye disorder 21.39 14.58 21 11941 9507 34935462
Atrioventricular block second degree 20.62 14.58 14 11948 3774 34941195
Scleral disorder 20.60 14.58 4 11958 21 34944948
Trabeculectomy 20.44 14.58 4 11958 22 34944947
Growth of eyelashes 19.81 14.58 5 11957 98 34944871
Abnormal sensation in eye 19.76 14.58 8 11954 744 34944225
Uveitis 19.57 14.58 18 11944 7517 34937452
Accidental exposure to product 19.54 14.58 23 11939 12779 34932190
Hypotony of eye 19.40 14.58 5 11957 107 34944862
Macular degeneration 19.32 14.58 11 11951 2175 34942794
Corneal degeneration 18.83 14.58 4 11958 35 34944934
Anterior chamber inflammation 18.67 14.58 6 11956 286 34944683
Cataract nuclear 18.65 14.58 7 11955 531 34944438
Visual field defect 18.50 14.58 14 11948 4469 34940500
Conjunctival hyperaemia 18.36 14.58 11 11951 2391 34942578
Conjunctival scar 18.32 14.58 5 11957 134 34944835
Blepharitis 17.61 14.58 9 11953 1436 34943533
Corneal epithelium defect 17.14 14.58 6 11956 373 34944596
Eyelids pruritus 17.13 14.58 5 11957 172 34944797
Funguria 17.11 14.58 4 11958 56 34944913
Punctate keratitis 17.08 14.58 6 11956 377 34944592
Photophobia 16.86 14.58 16 11946 6948 34938021
Eye haemorrhage 16.79 14.58 13 11949 4292 34940677
Coronavirus infection 16.78 14.58 13 11949 4294 34940675
Optic nerve cupping 16.73 14.58 4 11958 62 34944907
Cystoid macular oedema 16.72 14.58 7 11955 708 34944261
Electrolyte depletion 16.55 14.58 5 11957 194 34944775
Eye inflammation 16.55 14.58 10 11952 2208 34942761
Cardiovascular insufficiency 16.30 14.58 9 11953 1678 34943291
Dizziness 16.25 14.58 129 11833 218392 34726577
Dermatitis 16.12 14.58 18 11944 9450 34935519
Instillation site irritation 15.92 14.58 3 11959 13 34944956
Madarosis 15.69 14.58 5 11957 232 34944737
Intraocular pressure fluctuation 15.57 14.58 3 11959 15 34944954
Liquid product physical issue 15.49 14.58 6 11956 496 34944473
Hypersensitivity 15.45 14.58 51 11911 60984 34883985
Glaucoma surgery 15.26 14.58 3 11959 17 34944952
Eyelid margin crusting 15.25 14.58 5 11957 254 34944715
Cutis laxa 15.24 14.58 4 11958 92 34944877
Retinal haemorrhage 14.88 14.58 13 11949 5076 34939893
Angle closure glaucoma 14.77 14.58 7 11955 950 34944019
Oversensing 14.71 14.58 3 11959 21 34944948
Corneal opacity 14.59 14.58 6 11956 580 34944389

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 522.42 12.06 164 21870 9041 79713313
Eye irritation 336.55 12.06 147 21887 20534 79701820
Eye pain 234.97 12.06 140 21894 37438 79684916
Visual acuity reduced 224.86 12.06 125 21909 29344 79693010
Ocular hyperaemia 213.45 12.06 119 21915 28087 79694267
Vision blurred 157.07 12.06 169 21865 105729 79616625
Glaucoma 153.94 12.06 85 21949 19676 79702678
Bradycardia 153.27 12.06 188 21846 135369 79586985
Corneal oedema 137.49 12.06 44 21990 2576 79719778
Lacrimation increased 105.86 12.06 70 21964 22407 79699947
Eye pruritus 89.52 12.06 61 21973 20509 79701845
Choroidal detachment 89.30 12.06 23 22011 613 79721741
Corneal deposits 84.73 12.06 21 22013 477 79721877
Corneal disorder 78.76 12.06 28 22006 2263 79720091
Eye discharge 76.30 12.06 36 21998 5998 79716356
Choroidal effusion 73.64 12.06 20 22014 657 79721697
Iris adhesions 73.04 12.06 19 22015 527 79721827
Intraocular pressure test abnormal 68.23 12.06 14 22020 129 79722225
Total lung capacity increased 67.48 12.06 25 22009 2273 79720081
Cataract 65.07 12.06 83 21951 62037 79660317
Trabeculectomy 60.68 12.06 11 22023 48 79722306
Toxic anterior segment syndrome 59.52 12.06 24 22010 2740 79719614
Ulcerative keratitis 59.25 12.06 26 22008 3663 79718691
Conjunctival hyperaemia 57.87 12.06 27 22007 4386 79717968
Frustration tolerance decreased 52.26 12.06 30 22004 7472 79714882
Hyphaema 50.81 12.06 16 22018 888 79721466
Floppy iris syndrome 50.34 12.06 13 22021 350 79722004
Iridocyclitis 49.62 12.06 23 22011 3681 79718673
Anterior chamber disorder 49.60 12.06 11 22023 151 79722203
Hypotony of eye 49.59 12.06 12 22022 246 79722108
Visual field defect 49.58 12.06 31 22003 9014 79713340
Eye inflammation 45.62 12.06 26 22008 6387 79715967
Completed suicide 45.09 12.06 7 22027 245760 79476594
Blindness 45.04 12.06 47 21987 28336 79694018
Angle closure glaucoma 44.66 12.06 20 22014 2956 79719398
Foreign body sensation in eyes 43.95 12.06 18 22016 2139 79720215
Forced expiratory volume decreased 43.38 12.06 27 22007 7787 79714567
Peak expiratory flow rate decreased 42.21 12.06 13 22021 670 79721684
Cystoid macular oedema 41.97 12.06 17 22017 1963 79720391
Retinal detachment 41.61 12.06 28 22006 9219 79713135
Corneal epithelium defect 41.56 12.06 13 22021 706 79721648
Respiration abnormal 40.95 12.06 26 22008 7762 79714592
Ocular discomfort 40.35 12.06 22 22012 4961 79717393
Uveitis 40.32 12.06 35 21999 16795 79705559
Corneal degeneration 40.02 12.06 9 22025 132 79722222
Pulmonary thrombosis 39.03 12.06 30 22004 12141 79710213
Erythema of eyelid 37.70 12.06 17 22017 2553 79719801
Punctate keratitis 37.53 12.06 13 22021 973 79721381
Conjunctival scar 36.16 12.06 9 22025 208 79722146
Ocular hypertension 35.52 12.06 14 22020 1506 79720848
Endophthalmitis 35.15 12.06 22 22012 6406 79715948
Lung diffusion test decreased 33.92 12.06 13 22021 1297 79721057
Procollagen type I C-terminal propeptide increased 33.52 12.06 6 22028 24 79722330
Product quality issue 33.42 12.06 44 21990 33896 79688458
Instillation site irritation 33.42 12.06 7 22027 72 79722282
Sinus bradycardia 33.41 12.06 38 21996 25209 79697145
Serum procollagen type I N-terminal propeptide increased 32.59 12.06 6 22028 29 79722325
Fall 31.82 12.06 237 21797 487392 79234962
Vitreous haemorrhage 31.76 12.06 17 22017 3696 79718658
Blepharitis 31.58 12.06 16 22018 3108 79719246
Forced vital capacity decreased 30.33 12.06 13 22021 1730 79720624
Visual impairment 29.41 12.06 73 21961 92058 79630296
Eyelid margin crusting 29.19 12.06 11 22023 1048 79721306
Flat anterior chamber of eye 28.41 12.06 7 22027 155 79722199
Intraocular pressure fluctuation 28.36 12.06 6 22028 65 79722289
Atrioventricular block complete 27.24 12.06 28 22006 16582 79705772
Product container issue 27.08 12.06 11 22023 1280 79721074
Chronotropic incompetence 26.31 12.06 6 22028 94 79722260
Synovitis 26.08 12.06 5 22029 150729 79571625
Blindness unilateral 25.95 12.06 20 22014 8126 79714228
Abnormal sensation in eye 25.87 12.06 12 22022 1923 79720431
Nodal rhythm 25.83 12.06 14 22020 3121 79719233
Retinal disorder 25.23 12.06 12 22022 2035 79720319
Visual acuity tests abnormal 25.13 12.06 6 22028 116 79722238
Conjunctival oedema 24.74 12.06 10 22024 1148 79721206
Vitamin B12 decreased 24.37 12.06 14 22020 3491 79718863
Eye disorder 24.06 12.06 31 22003 23381 79698973
Conjunctivitis allergic 24.04 12.06 11 22023 1709 79720645
Atrioventricular block 23.62 12.06 24 22010 14017 79708337
Dizziness 23.37 12.06 235 21799 526206 79196148
Optic nerve cupping 23.32 12.06 5 22029 58 79722296
Systemic lupus erythematosus 23.26 12.06 3 22031 121146 79601208
Corneal decompensation 23.09 12.06 5 22029 61 79722293
Product delivery mechanism issue 22.94 12.06 6 22028 170 79722184
Corneal opacity 22.46 12.06 9 22025 1011 79721343
Growth of eyelashes 22.24 12.06 6 22028 192 79722162
Conjunctivitis 21.79 12.06 31 22003 25684 79696670
Arthralgia 21.69 12.06 83 21951 571720 79150634
Ectropion 21.69 12.06 7 22027 421 79721933
Corneal thickening 21.62 12.06 4 22030 20 79722334
Hypopyon 21.47 12.06 9 22025 1133 79721221
Atrioventricular block second degree 21.23 12.06 17 22017 7295 79715059
Keratopathy 21.09 12.06 9 22025 1185 79721169
Iritis 20.59 12.06 13 22021 3842 79718512
Glaucoma surgery 20.37 12.06 5 22029 109 79722245
Thermal burns of eye 20.33 12.06 5 22029 110 79722244
Vertigo 20.24 12.06 53 21981 69029 79653325
Sinoatrial block 20.02 12.06 9 22025 1342 79721012
Hypotonia 19.86 12.06 21 22013 12849 79709505
Anterior chamber inflammation 19.67 12.06 7 22027 567 79721787
Administration site discomfort 19.35 12.06 5 22029 135 79722219
Sinonasal papilloma 18.85 12.06 4 22030 44 79722310
Abdominal discomfort 18.84 12.06 25 22009 250702 79471652
Macular oedema 18.67 12.06 14 22020 5460 79716894
Abdominal pain 18.62 12.06 51 21983 389518 79332836
Hepatic enzyme increased 18.54 12.06 14 22020 182596 79539758
Dry eye 18.36 12.06 35 21999 36896 79685458
Infusion related reaction 18.30 12.06 22 22012 230215 79492139
Hyponatraemia 18.16 12.06 97 21937 177751 79544603
Toxicity to various agents 18.11 12.06 58 21976 421482 79300872
Macular fibrosis 18.10 12.06 7 22027 716 79721638
Photophobia 17.76 12.06 25 22009 20503 79701851
Pain 17.65 12.06 118 21916 703684 79018670
Symblepharon 17.56 12.06 5 22029 196 79722158
Superficial injury of eye 17.53 12.06 5 22029 197 79722157
Retinal haemorrhage 17.52 12.06 16 22018 8201 79714153
Corneal endothelial cell loss 17.43 12.06 3 22031 9 79722345
Loss of consciousness 17.42 12.06 92 21942 167851 79554503
Maternal exposure during pregnancy 17.34 12.06 8 22026 136530 79585824
Eyelid irritation 17.24 12.06 6 22028 455 79721899
Vitreous floaters 17.20 12.06 15 22019 7241 79715113
Arrhythmia 16.93 12.06 46 21988 61226 79661128
Vitreal cells 16.92 12.06 4 22030 74 79722280
Confusional state 16.60 12.06 147 21887 317850 79404504
Bronchopulmonary disease 16.38 12.06 3 22031 14 79722340
Drug intolerance 16.35 12.06 30 22004 264089 79458265
Hallucination, visual 16.25 12.06 31 22003 32698 79689656
Heterochromia iridis 16.05 12.06 3 22031 16 79722338
Off label use 16.01 12.06 167 21867 907048 78815306
Obstructive airways disorder 15.87 12.06 30 22004 31429 79690925
Product complaint 15.84 12.06 19 22015 13330 79709024
Corneal pigmentation 15.75 12.06 3 22031 18 79722336
Conjunctival follicles 15.75 12.06 3 22031 18 79722336
Achromotrichia acquired 15.75 12.06 3 22031 18 79722336
Corneal infection 15.66 12.06 4 22030 103 79722251
Dermatitis 15.61 12.06 24 22010 21297 79701057
Eye swelling 15.59 12.06 27 22007 26441 79695913
Rhinocerebral mucormycosis 15.52 12.06 7 22027 1051 79721303
Therapeutic product effect incomplete 15.51 12.06 10 22024 141635 79580719
Corneal scar 15.45 12.06 5 22029 303 79722051
Scleral hyperaemia 15.36 12.06 5 22029 309 79722045
Eyelid ptosis 15.26 12.06 17 22017 11027 79711327
Product substitution issue 15.11 12.06 23 22011 20233 79702121
Contraindicated product administered 14.84 12.06 13 22021 157525 79564829
Liquid product physical issue 14.83 12.06 7 22027 1167 79721187
Keratitis interstitial 14.78 12.06 3 22031 26 79722328
Metamorphopsia 14.19 12.06 7 22027 1286 79721068
Iris transillumination defect 14.09 12.06 4 22030 155 79722199
Eyelid oedema 13.87 12.06 18 22016 13669 79708685
Electrolyte depletion 13.86 12.06 5 22029 421 79721933
Subretinal fluid 13.80 12.06 6 22028 826 79721528
Chorioretinal disorder 13.78 12.06 4 22030 168 79722186
Oversensing 13.75 12.06 3 22031 38 79722316
Product use issue 13.74 12.06 23 22011 209799 79512555
Choroidal haemorrhage 13.71 12.06 4 22030 171 79722183
Eye oedema 13.70 12.06 8 22026 2055 79720299
Stag horn calculus 13.69 12.06 4 22030 172 79722182
Intraocular pressure decreased 13.56 12.06 4 22030 178 79722176
Cardiovascular insufficiency 13.35 12.06 9 22025 2972 79719382
Corneal thinning 13.32 12.06 4 22030 189 79722165
Herpes ophthalmic 13.17 12.06 7 22027 1500 79720854
Extrasystoles 13.07 12.06 13 22021 7406 79714948
Alkalosis hypochloraemic 13.04 12.06 5 22029 499 79721855
Cataract subcapsular 12.97 12.06 6 22028 955 79721399
Scleral disorder 12.94 12.06 4 22030 209 79722145
Gastrointestinal haemorrhage 12.72 12.06 77 21957 147642 79574712
Seborrhoeic keratosis 12.71 12.06 8 22026 2352 79720002
Intentional product use issue 12.66 12.06 14 22020 152098 79570256
Blood pressure systolic increased 12.63 12.06 44 21990 66942 79655412
Keratitis 12.45 12.06 10 22024 4312 79718042
Pupillary reflex impaired 12.39 12.06 9 22025 3344 79719010
Dacryocystitis 12.28 12.06 3 22031 64 79722290
Myocardial infarction 12.25 12.06 90 21944 184039 79538315
Retinal vascular occlusion 12.14 12.06 5 22029 602 79721752

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C07AA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS
Beta blocking agents, non-selective
ATC C07BA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS AND THIAZIDES
Beta blocking agents, non-selective, and thiazides
ATC C07DA06 CARDIOVASCULAR SYSTEM
BETA BLOCKING AGENTS
BETA BLOCKING AGENTS, THIAZIDES AND OTHER DIURETICS
Beta blocking agents, non-selective, thiazides and other diuretics
ATC S01ED01 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents
ATC S01ED51 SENSORY ORGANS
OPHTHALMOLOGICALS
ANTIGLAUCOMA PREPARATIONS AND MIOTICS
Beta blocking agents
CHEBI has role CHEBI:35530 beta-adrenergic blockers
CHEBI has role CHEBI:35674 antihypertensive drugs
CHEBI has role CHEBI:38070 antiarrhythmic agent
CHEBI has role CHEBI:39456 antiglaucoma agent
MeSH PA D018663 Adrenergic Agents
MeSH PA D018674 Adrenergic Antagonists
MeSH PA D000319 Adrenergic beta-Antagonists
MeSH PA D000889 Anti-Arrhythmia Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D018377 Neurotransmitter Agents

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

DiseaseRelationSNOMED_IDDOID
Ocular hypertension indication 4210003 DOID:9282
Hypertensive disorder indication 38341003 DOID:10763
Open-angle glaucoma indication 84494001 DOID:1067
Myocardial Reinfarction Prevention indication
Migraine Prevention indication
Malignant glaucoma off-label use 10100008
Aphakic glaucoma off-label use 15374009
Secondary glaucoma off-label use 95717004
Angina pectoris off-label use 194828000
Angle-closure glaucoma off-label use 392291006 DOID:13550
Mitral valve prolapse off-label use 409712001
Stalled wound off-label use 789507005
Anuria contraindication 2472002 DOID:2983
Bronchospasm contraindication 4386001
Hypercholesterolemia contraindication 13644009
Secondary angle-closure glaucoma contraindication 21571006
Complete atrioventricular block contraindication 27885002
Hypovolemia contraindication 28560003
Orthostatic hypotension contraindication 28651003
Acute cerebrovascular insufficiency contraindication 29322000
Dehydration contraindication 34095006
Hyperthyroidism contraindication 34486009 DOID:7998
Depressive disorder contraindication 35489007
Hyperuricemia contraindication 35885006 DOID:1920
Anaphylaxis contraindication 39579001
Hypokalemia contraindication 43339004
Sinus bradycardia contraindication 49710005
General anesthesia contraindication 50697003
Thromboangiitis obliterans contraindication 52403007 DOID:12918
Systemic lupus erythematosus contraindication 55464009 DOID:9074
Sympathectomy contraindication 57071006
Acute nephropathy contraindication 58574008
Cerebrovascular disease contraindication 62914000 DOID:6713
Hypercalcemia contraindication 66931009 DOID:12678
Hyperparathyroidism contraindication 66999008 DOID:13543
Hypochloremic alkalosis contraindication 70134007
Hepatic coma contraindication 72836002 DOID:12550
Diabetes mellitus contraindication 73211009 DOID:9351
Pulmonary emphysema contraindication 87433001
Cardiogenic shock contraindication 89138009
Hyponatremia contraindication 89627008
Gout contraindication 90560007 DOID:13189
Kidney disease contraindication 90708001 DOID:557
Myasthenia gravis contraindication 91637004 DOID:437
Acute disease of cardiovascular system contraindication 128487001
Hypomagnesemia contraindication 190855004
Partial atrioventricular block contraindication 195039008
Decompensated cardiac failure contraindication 195111005
Acute pancreatitis contraindication 197456007 DOID:2913
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Raynaud's phenomenon contraindication 266261006
Neonatal hyperbilirubinemia contraindication 281610001
Pregnancy, function contraindication 289908002
Severe chronic obstructive pulmonary disease contraindication 313299006
Right ventricular failure contraindication 367363000
Azotemia contraindication 445009001




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 9.15 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
Beta-1 adrenergic receptor GPCR ANTAGONIST Ki 9 WOMBAT-PK CHEMBL
Beta-2 adrenergic receptor GPCR ANTAGONIST Ki 9.70 WOMBAT-PK CHEMBL
5-hydroxytryptamine receptor 1A GPCR Ki 5.81 DRUG MATRIX
Beta-3 adrenergic receptor GPCR Ki 6.47 DRUG MATRIX
5-hydroxytryptamine receptor 1A GPCR Ki 6.21 CHEMBL
Beta-2 adrenergic receptor GPCR Kd 9.78 CHEMBL
Beta-1 adrenergic receptor GPCR Kd 9.44 CHEMBL

External reference:

IDSource
4019949 VUID
N0000148034 NUI
D00378 KEGG_DRUG
26921-17-5 SECONDARY_CAS_RN
4017930 VANDF
4019949 VANDF
C0040233 UMLSCUI
CHEBI:60787 CHEBI
TIM PDB_CHEM_ID
CHEMBL499 ChEMBL_ID
DB00373 DRUGBANK_ID
CHEMBL1200870 ChEMBL_ID
D013999 MESH_DESCRIPTOR_UI
33624 PUBCHEM_CID
565 IUPHAR_LIGAND_ID
817W3C6175 UNII
10600 RXNORM
24737 MMSL
5585 MMSL
6436 MMSL
d00139 MMSL
001856 NDDF
004741 NDDF
372880004 SNOMEDCT_US
75359005 SNOMEDCT_US
85591001 SNOMEDCT_US
91524-16-2 SECONDARY_CAS_RN

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 0023-9211 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
COMBIGAN HUMAN PRESCRIPTION DRUG LABEL 2 0023-9211 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
Timoptic in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 0187-1496 SOLUTION 6.80 mg OPHTHALMIC NDA 20 sections
Timoptic in Ocudose HUMAN PRESCRIPTION DRUG LABEL 1 0187-1498 SOLUTION 3.40 mg OPHTHALMIC NDA 20 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0055 TABLET 5 mg ORAL ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0221 TABLET 10 mg ORAL ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 0378-0715 TABLET 20 mg ORAL ANDA 22 sections
Dorzolamide Hydrochloride-Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0527-1763 SOLUTION 5 mg OPHTHALMIC ANDA 25 sections
Brimonidine Tartrate/Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0591-2422 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 22 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0781-7186 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0781-7186 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 sections
Brimonidine Tartrate and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 0832-1425 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 27 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-618 TABLET 5 mg ORAL ANDA 14 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-619 TABLET 10 mg ORAL ANDA 14 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 13811-620 TABLET 20 mg ORAL ANDA 14 sections
DORZOLAMIDE HYDROCHLORIDE TIMOLOL MALETAE Human Prescription Drug Label 2 14445-405 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 24 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-189 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 25 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-189 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 25 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-288 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-288 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-289 SOLUTION/ DROPS 2.50 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-289 SOLUTION/ DROPS 2.50 mg OPHTHALMIC ANDA 23 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-365 SOLUTION/ DROPS 2.50 mg OPHTHALMIC ANDA 22 sections
Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 1 17478-366 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 22 sections
Dorzolamide HCl and Timolol Maleate HUMAN PRESCRIPTION DRUG LABEL 2 17478-514 SOLUTION/ DROPS 5 mg OPHTHALMIC ANDA 28 sections
COSOPT PF HUMAN PRESCRIPTION DRUG LABEL 2 17478-604 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
COSOPT PF HUMAN PRESCRIPTION DRUG LABEL 2 17478-604 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 26 sections
COSOPT HUMAN PRESCRIPTION DRUG LABEL 2 17478-605 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 28 sections
COSOPT HUMAN PRESCRIPTION DRUG LABEL 2 17478-605 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 28 sections
Istalol HUMAN PRESCRIPTION DRUG LABEL 1 24208-004 SOLUTION/ DROPS 5 mg OPHTHALMIC NDA 24 sections